Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
  • A61K8/04—Dispersions; Emulsions
  • A61K8/042—Gels
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
  • A61K8/04—Dispersions; Emulsions
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
  • A61K8/11—Encapsulated compositions
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/37—Esters of carboxylic acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
  • A61Q17/04—Topical preparations for affording protection against sunlight or other radiation; Topical sun tanning preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q19/00—Preparations for care of the skin
  • A61Q19/10—Washing or bathing preparations
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
  • A61K2800/41—Particular ingredients further characterized by their size
  • A61K2800/412—Microsized, i.e. having sizes between 0.1 and 100 microns
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
  • A61K2800/80—Process related aspects concerning the preparation of the cosmetic composition or the storage or application thereof
  • A61K2800/88—Two- or multipart kits
  • A61K2800/882—Mixing prior to application
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q5/00—Preparations for care of the hair
  • A61Q5/02—Preparations for cleaning the hair

Definitions

• Exposure to ultraviolet light primarily through exposure to the sun's rays, produces a number of harmful effects including premature skin aging, loss of elasticity, wrinkling, drying, and an increased risk of developing skin cancer.
• sunscreen products are marketed to protect against these harmful effects.
• AU of these products contain agents known to filter out some of the sun's harmful rays incorporated into creams, ointments, lotions, solutions or suspensions. Such products are applied just prior to anticipated sun exposure, provide short term protection, and are removed by bathing, washing or normal desquamation of skin. Soap in the form of bodywash has for years been used to remove oil due to its surfactant composition and associated charges.
• a normal soap contains both charges of a positive and negative nature.
• the invention encompasses bodywashes containing an additive.
• the additive may contain a sunscreen.
• the invention further encompasses methods of making and using bodywashes containing an additive, e.g., an additive containing a sunscreen.
• the invention provides a bodywash containing an additive that comprises a sunscreen, wherein after a single application of the bodywash to skin and rinsing, the skin is protected from sunlight with an average SPF of at least about 15. In some embodiments, the SPF of 15 is maintained for an average of at least about 4 hours after rinsing.
• the sunscreen is encapsulated, e.g., in sol-gel microcapsules.
• the sunscreen is an organic sunscreen that is aminobenzoic acid, avobenzone, cinoxate, dioxybenzone, homosalate, menthyl anthranilate, octocrylene, octyl methoxycinnamate, octyl salicylate, oxybenzone, padimate O, phenylbenzimidazole sulfonic acid, sulisobenzone, or trolamine salicylate.
• the sunscreen is a cinnamate derivative.
• the additive contains 3 organic sunscreens.
• the 3 organic sunscreens are selected from the group consisting of aminobenzoic acid, avobenzone, cinoxate, dioxybenzone, homosalate, menthyl anthranilate, octocrylene, octyl methoxycinnamate, octyl salicylate, oxybenzone, padimate O, phenylbenzimidazole sulfonic acid, sulisobenzone, and trolamine salicylate.
• Embodiments may further contain an inorganic sunscreen.
• the inorganic sunscreen is selected from the group consisting of zinc oxide and titanium dioxide
• the sunscreen is a UVB absorber sunscreen
• the composition also contains a UVA absorber sunscreen and a physical blocker sunscreen
• the UVB-absorber sunscreen is selected from the group consisting of aminobenzoic acid, cinoxate, dioxybenzone, homosalate, octocrylene, octyl methoxycinnamate, octyl salicylate, oxybenzone, padimate O, phenylbenzimidazole sulfonic acid, sulisobenzone, and trolamine salicylate
• the UVA-absorber sunscreen is selected from the group consisting of avobenzone and menthyl anthranilate
• the physical blocker sunscreen is selected from the group consisting of titanium dioxide and zinc oxide.
• Embodiments may further contain a cationic polymer, hi some embodiments, the catioiiic polymer is a polyquaternium. hi some embodiments, the polyquaternium is polyquaternium-4, -7,-11, -22, -27, -44, -51, or -64. In preferred embodiments, the cationic polymer is polyquaternium-4.
• Embodiments may also contain a film former, a preservative, and/or an antioxidant that is stable upon exposure to sunlight.
• the invention provides a bodywash containing an additive that contains a sunscreen, where, after application of the bodywash to skin and rinsing, the sunscreen penetrates an average of no further than 30 microns into the skin after application followed by rinsing, hi some embodiments of this aspect, after application of the bodywash to skin and rinsing, the skin is protected from sunlight with an average SPF of at least about 15.
• the invention provides a bodywash comprising a UVA- absorbing sunscreen, a UVB-absorbing sunscreen, a physical blocker sunscreen, and a cationic polymer
• the UVB-absorber sunscreen is selected from the group consisting of aminobenzoic acid, cinoxate, dioxybenzone, homosalate, octocrylene, octyl methoxycinnamate, octyl salicylate, oxybenzone, padimate O, phenylbenzimidazole sulfonic acid, sulisobenzone, and trolamine salicylate
• the UVA- absorber sunscreen is selected from the group consisting of avobenzone and menthyl anthranilate
• the physical blocker sunscreen is selected from the group consisting of titanium dioxide and zinc oxide
• the cationic polymer is a polyquaternium.
• Some of these embodiments contain octyl methoxycinnamate, octocrylene, avobenzone, titanium dioxide, and a polyquaternium selected from the group consisting of polyquaternium-4, - 7,-11, -22, -27, -44, -51, or -64.
• a preferred polyquaternium is ⁇ olyquaternium-4.
• the octylmethoxy cinnamate maybe encapsulated, e.g., in sol-gel microcapsules.
• the octyl methoxycinnamate can present at about 4.5-9%, the octocrylene can present at about 0.5-
• the avobenzone can present at about 2-4%, and the titanium dioxide can present at about 3-9%. Additionally, in embodiments containing polyquaternium-4, the polyquaternium-4 can be present at about 0.5-3%. In some embodiments, the octyl methoxycinnamate is present at about 7.6%, the octocrylene is present at about 11.3%, the avobenzone is present at about 2.8%, and the titanium dioxide is present at about
• the polyquaternium-4 can be present at about 2.8%.
• a film former can also be present, e.g., at about 1.5%.
• the bodywash of claim can further contain a non-sunscreen active.
• the non-sunscreen active is selected from the group consisting of steroidal anti-inflammatory actives, analgesic actives, antifungals, antibacterials, and antiparasitics, anti-allergenics, medicinal actives, skin rash, skin disease and dermatitis medications, insect repellant actives, antioxidants, hair growth promoter, hair bleaching agents, deodorant compounds, and mixtures and combinations thereof, hi some embodiments, at least one of the sunscreens is encapsulated, e.g., in sol- gel microcapsules, hi some embodiments, the cationic polymer is a polyquaternium.
• the polyquaternium is polyquaternium-4, -7,-11, -22, -27, -44, -51, or -64.
• the cationic polymer is polyquaternium-4.
• Embodiments may also contain a film former, a preservative, and/or an antioxidant that is stable upon exposure to sunlight.
• the present invention encompasses compositions containing one or more active ingredients (also referred to herein as "actives”) that may be added to a bodywash composition to provide an active/bodywash combination.
• actives also referred to herein as "actives”
• bodywash encompasses all cleansing vehicles applied to the body. Exemplary forms of cleansing vehicles include, but are not limited to, liquid, bar, gel, foam, aerosol or pump spray, cream, lotion, stick, powder, or incorporated into a patch or a towelette.
• soapless cleansers may be used as well.
• bodywash includes, but is not limited to, a soap including liquid and bar soap; a shampoo; a hair conditioner; a shower gel; including an exfoliating shower gel; a foaming bath product (e.g. gel, soap or lotion); a milk bath; a soapless cleanser, including a gel cleanser, a liquid cleanser and a cleansing bar; moist towelletes; a body lotion; a body spray, mist or gel; bath effervescent tablets (e.g., bubble bath); a hand and nail cream; a bath/shower gel; a shower cream; a depilatory cream; a shaving product e.g.
• a shaving cream, gel, foam or soap an after-shave, after-shave moisturizer; and combinations thereof, and any other composition used for cleansing or post-cleansing application to the body, including the skin and hair.
• bodywashes in the invention are soaps, e.g., liquid soaps and bar soaps, and shampoos.
• the invention provides additives containing active ingredients, where the additive is designed to be added to a bodywash (e.g., soap or shampoo).
• a bodywash e.g., soap or shampoo
• sunscreen compositions that may be added to a bodywash preparation to impart sun protection.
• the invention provides a combination of a sunscreen additive and a bodywash preparation ("sunscreen/bodywash").
• a sunscreen additive of the invention may be mixed with a conventional bodywash; alternatively, the invention provides pre-mixed sunscreen/bodywash.
• the sunscreen/bodywash composition is generally applied in the same manner as the bodywash alone and, typically, rinsed, with additive, e.g., sunscreen protection, being left on the skin after rinsing.
• additive e.g., sunscreen protection
• the bodywash is applied without rinsing.
• the sunscreen protection after application and, typically, rinsing is, on average, greater than an SPF of 1, up to about SPF 50.
• average SPF is the SPF, determined as described herein, for about 5 to about 50 subjects, or about 5 to about 20 subjects, or about 5 to about 10 subjects, where the subjects preferably have Type II skin.
• the average SPF provided by the sunscreen/bodywash after rinsing is about 1 to about 50, or about 2 to about 50, or about 2 to about 40, or about 2 to about 30, or about 2 to about 20, or about 2 to about 10, or about 2 to about 5, or about 5 to about 25, or about 5 to about 20, or about 5 to about 15, or about 5 to about 10.
• the average SPF provided by the sunscreen/bodywash, after rinsing is above about 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, or 20.
• the average SPF after rinsing is above about 2. In some preferred embodiments, the average SPF after rinsing is above about 5.
• the average SPF after rinsing is above about 10. In some preferred embodiments, the average SPF after rinsing is above about 15. In some embodiments, the average SPF provided by the sunscreen/bodywash of the invention remains above about 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, or 20, for an average of at least about 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, or more than about 10 hours after rinsing, hi some embodiments the average SPF provided by the sunscreen/bodywash of the invention increases with each additional washing after a first wash, so that after a second, third, fourth, or fifth wash, the SPF provided can be above about 2, 4, 6, 8, 10, 15,, 20, 25, 30, 40, 45, or more than about 45.
• SPF is a commonly used measure of photo protection of a sunscreen against erythema. This number is derived from another parameter, the minimal erythemal dose (MED). MED is defined as the "least exposure dose at a specified wavelength that will elicit a delayed erythema response.” The MED indicates the amount of energy irradiating the skin and the responsiveness of the skin to the radiation.
• the SPF of a particular photo protector is obtained by dividing the MED of protected skin by the MED of unprotected skin. The higher the SPF, the more effective the agent in preventing sunburn. The SPF value tells how many times longer a person can stay in the sun before the person will experience 1 MED.
• utilizing a sunscreen with an SPF of 6 will allow an individual to stay in the sun six times longer before receiving 1 MED.
• SPF value of a sunscreen increases, the less chance exists for development of tanning of the skin.
• commercially available sunscreening products have SPF values ranging from about 2 to 45. [00 ⁇ 2] ' Methods for measuring SPF are described in, e.g., FDA monograph C.F.R. 21.
• a method for applying the sunscreen prior to measurement is as follows: Wet 50 cm square area of testing site with 10 ml of water delivered with a syringe. Apply test sample as per FDA monograph to area. Work lather on the subject for 3 minutes to allow the product to absorb into the skin. Rinse area after 2 additional minutes with 20ml of water. Pat dry and allow 15 minutes before exposure to radiation as per FDA monograph.
• the additive e.g., sunscreen
• the additive e.g., sunscreen
• the additive penetrates to an average of at least about 5 microns beneath the skin surface.
• the additive penetrates to an average of at least about 10, 15, 20, 25, 30, 40, 50, 60, 70, 80, 90, 100,120, or 150 microns beneath the skin surface.
• the additive e.g., sunscreen
• the additive penetrates to an average of no more than about 30 microns beneath the skin surface.
• the additive penetrates to an average of no more than about 50, 40, 30, 25, 20, 15, 10, or 5 microns beneath the skin surface.
• the additive e.g., sunscreen
• the additive penetrates to an average of about 5 to about 50, or about 5 to about 40, or about 5 to about 30, or about 10 to about 40, or about 15 to about 40, or about 20 to about 40, or about 5, 10, 15,
• Depth of penetration may be tested by tape stripping methods, as are well-known in the art.
• the sunscreen additives and sunscreen/bodywashes of the invention contain at least one sunscreen.
• the sunscreen additives of the invention contain one, two, three, four, or more than four sunscreens.
• the sunscreen additives of the invention include three sunscreens.
• the sunscreen additives of the invention include four sunscreens.
• the sunscreens may be organic or inorganic.
• the sunscreens may be a UVA absorber, a UVB absorber, a physical blocker, or any combination thereof.
• one or more of the sunscreens is encapsulated. A number of types of encapsulation may be employed as described herein.
• compositions of the invention may include one or more actives that are not sunscreens, where the composition is designed to be an additive to a bodywash.
• the actives are provided in combination with one or more sunscreens.
• the actives are provided without sunscreen.
• the additives, e.g., sunscreen additives, and additive/bodywashes, e.g., sunscreen/bodywashes, of the invention may further include one or more components to provide a positive charge to the system to assist with attachment to protein and other charged components of skin and/or hair, e.g., cationic polymeric agents.
• the cationic polymer may be, for example, a quaternium, e.g., polyquaternium.
• the additives e.g., sunscreen additives, and additive/bodywashes, e.g., sunscreen/bodywashes, of the invention may further include a film former.
• Other optional ingredients of the additives, e.g., sunscreen additives, and additive/bodywashes, e.g., sunscreen/bodywashes, of the invention include preservatives, antioxidants, chelating agents, liquid hydrocarbon (e.g., similar to pentane), foaming agents (e.g., a cationic foaming agent), skin nourishing components, antibacterials, medicinals, and the like, as described below.
• the additives, e.g., sunscreen additives, of the invention may be combined with any conventional bodywash.
• the bodywash composition with which the additive, e.g., sunscreen additive is combined may be any bodywash known in the art or apparent to one of skill in the art, as described above.
• the additive may be combined with any composition intended for topical application.
• the additive is often encapsulated, e.g., in sol- gel microcapsules.
• the invention provides an additive, e.g., sunscreen additive, in combination with a bodywash composition to provide an additive/bodywash, e.g. sunscreen/bodywash, composition.
• the additive e.g., sunscreen additives
• the additive are provided in combination with one or more surfactants.
• the surfactant(s) may be cationic, anionic, nonionic, zwitterionic, amphoteric, or any combination thereof.
• the sunscreen/bodywash compositions of the invention include at least one cationic surfactant.
• the sunscreen additives and sunscreen/bodywashes of the invention contain at least one sunscreen.
• the sunscreen may be organic or inorganic, or a combination of both may be used.
• Sunscreens of use in the invention include UV absorbers or blockers (e.g., many inorganic sunscreens are UV blockers). UV absorbers may be a UVB or UVA absorber (e.g., UVA I or UVA II absorber).
• the sunscreen additives or sunscreen/bodywashes of the invention include an organic and an inorganic sunscreen. Ih some embodiments, the sunscreen additives or sunscreen/bodywashes of the invention include more man one organic sunscreen (e.g., at least one UVB absorber and at least one UVA absorber) and at least one inorganic sunscreen.
• the sunscreen additives of the invention include only a physical blocker sunscreen, e.g., titanium dioxide. These embodiments may further contain a cationic polymer and/or a film former, as well as any other components described herein for sunscreen additives.
• Additional ingredients may include film formers, cationic polymers, antioxidants, preservatives, and the like, as described herein.
• the sunscreen additives or sunscreen/bodywashes of the invention include an organic and an inorganic sunscreen.
• the sunscreen additives or sunscreen/bodywashes of the invention include more than one organic sunscreen (e.g., at least one UVB absorber and at least one UVA absorber) and at least one inorganic sunscreen.
• sunscreens used in the invention are encapsulated.
• Any sunscreen known in the art or apparent to the skilled artisan may be used in the invention.
• the term "sunscreen” or “sunscreen agent” as used herein defines ultraviolet ray-blocking compounds exhibiting absorption or blockage within the wavelength region between about 290 and 420 nm. Sunscreens may be classified into five groups based upon their chemical structure: para-amino benzoates; salicylates; cinnamates; benzophenones; and miscellaneous chemicals including menthyl anthralinate and digalloyl trioleate.
• Inorganic sunscreens may also be used including titanium dioxide, zinc oxide, iron oxide and polymer particles such as those of polyethylene and polyamides.
• Specific suitable sunscreens include, for example: p-aminobenzoic acid, its salts and its derivatives (ethyl, isobutyl, glyceryl esters; p-dimethylaminobenzoic acid);
• Anthranilates i.e., o-aminobenzoates; methyl, menthyl, phenyl, benzyl, phenylethyl, linalyl, terpinyl, and cyclohexenyl esters
• Salicylates amyl, phenyl, benzyl, menthyl, glyceryl, and dipropylene glycol esters
• Cinnamic acid derivatives methyl and benzyl esters, alpha-phenyl cinnamonitrile; butyl cinnamoyl pyruvate
• Dihydroxycinnamic acid derivatives umbelliferone, methylumbelliferone, methylaceto-urnbelliferone
• Trihydroxycinnamic acid derivatives (esculetin, methylesculetin, daphnetin, and the glucosides, esculin and daphnin); Hydrocarbons (diphenylbutadiene, stilbene); Dibenzalacetone and benzalacetophenone; Naphtholsulfonates (sodium salts of 2- naphthol-3,3-disulfonic and of 2-naphthol-6,8-disulfonic acids); Dihydroxynaphthoic acid and its salts; o- and p-Hydroxybiphenyidisulfonates; Coumarin derivatives (J- hydroxy, 7-methyl, 3-phenlyll); Diazoles (2-acetyl-3-bromoindazole, phenyl benzoxazole, methyl naphthoxalole, various aryl benzothiazoles); Quinine salts (bisulfate, sulfate, chloride,
• compositions include diethanolamine methoxycinnamate (10% or less), ethyl-[bis(hydroxypropyl)]aminobenzoate (5% or less), glyceryl aminobenzoate (3% or less), 4-isopropyl dibenzoylmethane (5% or less), 4- methylbenzylidene camphor (6% or less), terephthalylidene dicamphor sulfonic acid
• sunscreens are FDA-approved or approved for use in the European Union.
• FDA-approved sunscreens may be used, singly or, preferably, in combination. See, e.g., U.S. Patent Nos. 5,169,624; 5, 543,136; 5,849,273; 5,904,917; 6,224,852; 6,217,852; and Segarin et al., chapter ViI, pages 189 of Cosmetics
• preferred cosmetically- acceptable sunscreens and concentrations include: aminobenzoic acid (also called para- aminobenzoic acid and PABA; 15% or less; a UVB absorbing organic sunscreen), avobenzone (also called butyl methoxy dibenzoylmethane; 3% or less, a UVA I absorbing organic sunscreen), cinoxate (also called 2-ethoxyethyl p-methoxycinnamate;
• a UVB absorbing organic sunscreen dioxybenzone (also called benzophenone-8; 3% or less, a UVB and UVA II absorbing organic sunscreen), homosalate (15% or less, a UVB absorbing organic sunscreen), menthyl anthranilate (also called menthyl 2-aminobenzoate; 5% or less, a UVA II absorbing organic sunscreen), octocrylene (also called 2-ethylhexyl-2-cyano-3,3 diphenylacrylate; 10% or less, a UVB absorbing organic sunscreen), octyl methoxycinnamate (7.5% or less, a UVB absorbing organic sunscreen), octyl salicylate (also called 2-ethylhexyl salicylate; 5% or less, a UVB absorbing organic sunscreen), oxybenzone (also called benzophenone-3; 6% or less, a UVB and UVA II absorbing organic sunscreen), padimate O (also called o
• preferred cosmetically-acceptable photoactive compounds and concentrations include: PABA (5% or less), camphor benzalkonium methosulfate (6% or less), homosalate (10% or less), benzophenone-3 (10% or less), phenylbenzimidazole sulfonic acid (8% or less, expressed as acid), terephthalidene dicamphor sulfonic acid (10% or less, expressed as acid), butyl niethoxydibenzoylmethane (5% or less), benzylidene camphor sulfonic acid (6% or less, expressed as acid), octocrylene (10% or less, expressed as acid), polyacrylamidomethyl benzylidene camphor (6% or less), octyl methoxycinnamate (10% or less), PEG-25
• the sunscreen additives or sunscreen/bodywashes of the invention include a silicone long-chain molecule with chromophores, e.g., PARASOL SLX (DSM Nutritional Products), which contains benzyl malonate chromophores attached to specific points on a polysiloxane chain.
• the invention provides a sunscreen additive or sunscreen/bodywash composition that contains sunscreen that comprises a silicone long-chain molecule with chromophores.
• compositions of the invention include a composition containing octyl methoxycinnamate, octocrylene, avobenzone, titanium dioxide, and a silicone long-chain molecule with chromophores.
• the silicon long-chain molecule may be used in sunscreen additives at about 0.5 to about 5%, or in sunscreen/bodywashes at about 0.2 to about 2%.
• Inorganic physical blockers of UVA and UVB useful in the invention further include iron oxide and polymer particles such as those of polyethylene and polyamides.
• the sunscreen additives and sunscreen/bodywashes contain at least one sunscreen active that is cinnamate (e.g., Octylmethoxycinnamate (ethyl hexyl methoxycinnamate), (available under the tradename PARSOL MCX), oxybenzone (e.g., benzophenone-3 (2-Hydroxy4-Methoxybenzophenone), avobenzone (4-tert-Butyl-4'- methoxydibenzoylmethane or PARSOL 1789), octyl salicylate (2-Ethylhexyl Salicylate), octocrylene (2-Ethylhexyl 2-Cyano-3,3-Diphenylacrylate), methyl anthranilate, and/or titanium dioxide, or combinations thereof.
• cinnamate e.g., Octylmethoxycinnamate (ethyl hexyl methoxycinnamate),
• Sunscreen additives and sunscreen/bodywashes of the invention may, in some embodiments, contain as a sunscreen component only titanium dioxide.
• titanium dioxide When titanium dioxide is used in compositions of the invention, either alone or in combination with other sunscreens, the titanium dioxide can have an anatase, rutile, or amorphous structure.
• the titanium dioxide particles can be uncoated or can be coated with a variety of materials including, but not limited to, aluminum compounds such as aluminum oxide, aluminum stearate, aluminum laurate and the like; phospholipids such as lecithin; silicone compounds; and mixtures thereof.
• Various grades and forms of titanium dioxide are described in CTFA Cosmetic Ingredient Dictionary, Third Edition (1982), pp. 318- 319; U.S. Pat. No. 4,820,508 to Wortzman, issued Apr.l 1, 1989; and World Patent No.
• Suitable grades of titanium dioxide for use in the compositions of the present invention are available commercially such as the MT micronized series from Tri-K Industries (Emerson, NJ). These micronized titanium dioxides generally have a mean primary particle size ranging from about 10 nm to about
• titanium dioxide having a mean primary particle size of about 15 nm is available under the trade designations MT-15OW (uncoated) and MT-100T (coated with stearic acid and aluminum compounds).
• Uncoated titanium dioxides having mean primary particle sizes of around 35 nm and around 50 nm are available under the trade designations MT-500B and MT-600B, respectively.
• Other coated titanium dioxides having a mean primary particle size around 15 nm include MT-100F (modified with stearic acid and iron hydroxide) and MT-100S (treated with lauric acid and aluminum hydroxide). Mixtures of two or more types and particle size variations of titanium dioxide can be used in the present invention.
• a particularly preferred form of titanium dioxide is silica-coated TiO 2 .
• silica-coated TiO 2 is available under the tradename T-AVO (Eusolex).
• T-AVO Tin-AVO
• some zinc-based compositions e.g., Z-CoteTM HPl [registered trademark, SkinCeuticals]
• Z-CoteTM HPl registered trademark, SkinCeuticals
• the dimethicone coating transforms the frequently granular and pasty particles of zinc oxide to a smooth formulation which is transparent. The micronizing of these particles achieves the important advantage of providing effective sunscreening without giving the appearance of skin coated with white paint.
• Tioveil and Spectraveil both of the Tioxide Group.
• Tioveil include products which are 40% dispersions of surface-treated titanium dioxide in a range of cosmetic vehicles.
• Spectraveil include products which are 60% dispersions of zinc oxide in a range of cosmetic vehicles. In certain variations, these products may be film-formers and may have advantageous uses here.
• sunscreen additives the total sunscreens comprise about 0.1-50%, or about 1-
• the total sunscreens can comprise 0.05-30%, or about 0.5-15%, or about 0.5-12%, or about 1.5-12%, or about 2.5-12%, or about 5-12% or about 7-12%, or about 2.5, 5, 7.5, 10, 12.5, 15, 20, 25, 30, 33, 35, 40, 45, 50, or more than 50% of the composition.
• a sunscreen additive of the invention includes octyl methoxycinnamate at about 4.5-9% , Octocrylene at about 0.5-15%, Avobenzone (e.g., PARSOL 1789) at about 2-4%, and titanium dioxide at about 3-9%.
• the octyl methoxy ciniiamate is encapsulated, e.g., in amorphous silica.
• Such encapsulated octyl methoxy cinnamate is commercially available under the trade name UV PEARLS; about 20-40% UV PEARLS supplies about 4.5-9% octyl methoxy cinnamate.
• a sunscreen additive of the invention includes octyl methoxycinnamate at about 7.6% (in some embodiments, encapsulated as described, e.g., in UV PEARLS wherein the UV PEARLS are provided at about 33.3%), Octocrylene at about 11.3 %, Avobenzone (PARSOL 1789) at about 2.8%, and titanium dioxide at about 6.4%.
• the sunscreen additives may further include a polyquatemium, e.g., polyquaternium-4. In some embodiments, the polyquaternium-4 is present at about 0.5% to about 5%, in some embodiments, the polyquaternium-4 is present at about 2.8%.
• the sunscreen additives may further include a film-former, which may comprise dimethicone and/or petrolatum, and/or a preservative, such as BHT.
• This sunscreen additive may be added to a conventional bodywash formulation (e.g., SUAVE Bodywash) in a ratio of about one part sunscreen additive to two parts bodywash (w/w).
• bodywash formulation e.g., SUAVE Bodywash
• Other ratios are encompassed by the invention, e.g., about one part sunscreen additive to about 0.2, 0.5,
• the sunscreen additive comprises at least two components.
• the first component may comprise all the ingredients except an inorganic or physical blocker sunscreen
• the second component may comprise the inorganic or physical blocker sunscreen.
• the first component is added to the bodywash with thorough mixing, then the second component is added.
• all ingredients except the titanium dioxide are mixed, then added to the bodywash, and then the titanium dioxide is added (see Examples).
• the sunscreen additives of the invention include about 0.1 to 7.5 weight percent of octylmethoxy cinnamate, about 0.1 to 6 parts weight percent of octyl salicylate, about 0.1 to 5 parts weight percent of oxybenzone, about 1 to 10 weight percent of cationic surfactant, and about 0.01 to 1 weight percent of a quaternized compound.
• These composition may further include a film former.
• These compositions may further include 0.01 to 1 weight percent of a preservative.
• Encapsulation Sunscreens and other actives used in the invention may be encapsulated.
• One or more of the sunscreens used in a composition may be encapsulated; preferably, all sunscreens used are encapsulated.
• Sunscreen actives may be encapsulated together, or may be encapsulated separately, in any combination, in the same or in different types of encapsulations.
• encapsulation involves trapping the sunscreen in, e.g., a vesicle.
• the vesicle may break open when applied, without being limited by theory, it is thought that the vesicle breaks open in various types of encapsulation due to friction, temperature, or pH from the skin or hair, or some combination of these.
• the stability, durability, and/or SPF provided by the sunscreen additives and sunscreen/bodywashes of the invention can be increased.
• any means of encapsulation known in the art including but not limited to liposomes, maltodextrin capsules, silica gels, siloxanes, and the like, may be used in the compositions of the invention.
• a cationic or catanionic in dry powder form may also be used to encapsulate sunscreen.
• Commercial embodiments of encapsulated sunscreens or vehicles suitable for encapsulating sunscreens include CATEZOMES (Engelhard Corp.),
• EUSOLEX UV PEARLS EMD Biosciences
• Methods of encapsulation suitable for delivering benefit agents that are mixed with a bodywash composition are well-known in the art. See, e.g., U.S. Patent Nos. 6,825,161; 6,436,375; 6,238,650; 6,468,509, 6,362,146; 6,074,630; 5,455,048; 5,770,556; 5,955,409; 5,876,755; 4,803,195; 5,508,259; 4,749,501 ; 6,248,703 ; 5,476,660; and 4,904,524 and EP Pat. Nos.
• a particularly preferred method of encapsulation is sol-gel encapsulation.
• This technique is described in, e.g., U.S. Patent Nos. 6,238,650; 6,436,375, 6,303,149; and 6,468,509. Any or all of the sunscreens and/or other active ingredients of the compositions of the invention may be encapsulated by such sol-gel encapsulation.
• the sol-gel capsules maybe prepared so as to have a surface charge, e.g., a cationic charge. This is advantageous in that otherwise water-insoluble components may be encapsulated within the microcapsules, which are then freely miscible in water, e.g., without the need for an emulsifying agent.
• a UVA absorber, a UVB absorber (e.g., octyl methoxycinnamate) and/or a physical blocker, e.g., titanium dioxide is provided as a silica sol-gel encapsulate, optionally with further ingredients including PVP, Chlorphenesin, and an antioxidant such as BHT.
• a commercial embodiment of such an encapsulation containing octyl methoxycinnamate, PVP, chlorphenesin, and BHT is available under the trade name EUSOLEX UV PEARLS (EMD Biosciences).
• Such a silica sol-gel encapsulated UVB absorber e.g., octyl methoxycinnamate
• a sunscreen additive may be used in a sunscreen additive at a concentration that results in a final concentration of the UVB absorber of about 1% to about 40%, or about 2% to about 20%, or about 2% to about 10%, or about 5% to about 10%, or about 6%, 7%, 7.4%, 7.5%, 7.6%, 8%, or 9%.
• the preferred final concentration is about 7.6%.
• more than one sunscreen is encapsulated as silica sol-gel encapsulate.
• the final concentration of each of the sunscreens, independently, in the final sunscreen additive is about 1% to about 40%, or about 2% to about 20%, or about 2% to about 10%, or about 1%, 2%, 3%, 4%, 5%, 6%, 7%, 7.5%, 8%, 9%, or 10%.
• the sunscreens may be encapsulated together or separately, or any combination thereof.
• the invention provides an additive for addition to a bodywash that includes a sunscreen encapsulated in a sol-gel microcapsule and a cationic polymer (described below).
• compositions of the microcapsule e.g., sol-gel microcapsule
• the composition of the microcapsule may be varied so as to allow for varying amounts of the active, e.g., sunscreen, within the microcapsule to be released.
• the microcapsules, e.g., sol-gel microcapsules can be prepared so as to experience no or minimal breakage when applied to the skin and when left on the skin.
• the microcapsules can be prepared so as to experience various degrees of breakage, on average, when applied to the skin and when left on the skin.
• the microcapsules e.g., sol-gel microcapsules
• microcapsules may be formulated so as to break open in response to conditions that occur on the skin, so that after application the microcapsules act to release their contents in a time-release or controlled manner.
• Non- limiting exemplary skin or hair conditions that can vary with the user's environment, the variation of which can trigger breakage of microcapsules, include pH, temperature, friction, exposure to light or air, pressure, and the like.
• compositions of the invention may employ an organic sunscreen such as octyl methoxycinnamate trapped within a matrix.
• an organic sunscreen such as octyl methoxycinnamate trapped within a matrix.
• SunCapsTM trademark, SkinCeuticals
• the invention provides additives containing non-sunscreen active ingredients, where the additive is designed to be added to a composition for topical application, e.g., a bodywash.
• a composition for topical application e.g., a bodywash.
• these actives may be used in combination with the sunscreens described above in a sunscreen additive or sunscreen/bodywash, or may be used in separate, non-sunscreen compositions.
• at least one of the actives is encapsulated.
• the invention provides a composition for topical application, e.g., a bodywash, containing one or more such actives. These actives may be used in combination with the sunscreens described above in a sunscreen additive or sunscreen/bodywash, or may be used in separate, non-sunscreen compositions.
• Non-limiting examples of non-sunscreen actives useful in compositions of the invention include sunless tanning actives, skin lightening actives, anti-acne actives, anti- skin wrinkling and anti-skin aging actives, vitamins, anti-inflammatory actives, anesthetic actives, analgesic actives, anti-pruritic actives, anti-microbial actives (e.g.
• antifungals e.g., skin rash, skin disease and dermatitis medications
• anti-cellulite additives e.g., insect repellant actives, antioxidants, hair growth promoters, hair growth inhibitors, hair bleaching agents, deodorant compounds, and mixtures and combinations thereof.
• Sunless tanning actives include dihydroxyacetone (DHA); glyceryl aldehyde; tyrosine and tyrosine derivatives such as malyltyrosine, tyrosine glucosinate, and ethyl tyrosine; phospho-DOPA, indoles and derivatives; and mixtures thereof
• DHA dihydroxyacetone
• glyceryl aldehyde tyrosine and tyrosine derivatives such as malyltyrosine, tyrosine glucosinate, and ethyl tyrosine
• phospho-DOPA indoles and derivatives
• Non-limiting examples of skin lightening actives include EMBLICA (also an antioxidant), monobenzone (a depigmenting agent), kojic acid, arbutin, ascorbic acid and derivatives thereof (e.g., magnesium ascorbyl phosphate or sodium ascorbyl phosphate), and extracts (e.g.,
• Non-limiting examples of skin lightening agents suitable for use herein also include those described in WO 95/34280, WO 95/07432, and WO 95/23780.
• Vitamins may be included in the compositions of the present invention. Examples include Vitamin A and derivatives thereof (including, for example, retinol, see anti- wrinkling actives), ascorbic acid (Vitamin C and derivatives), Vitamin B (e.g., riboflavin, vitamin B 2 ), biotin, Vitamin D (all forms), Vitamin E and derivatives thereof such as tocopheryl acetate, beta-carotene, pantothenic acid and mixtures thereof.
• Anti-acne actives include benzoyl peroxide, erythromycin, clindamycin phosphate, 5,7-dichloro-8-hydroxyquinoline, resorcinol, resorcinol acetate, salicylic acid, azaleic acid, long chain dicarboxylic acids, sulfur, zinc, various natural agents such as tnose derived, irom green tree, and mixtures thereof.
• suitable anti-acne actives for use herein are described in U.S. Pat. No. 5,607,980, which description is incorporated herein by reference.
• Anti-skin wrinkling actives include a variety of agents, often in combination, that prevent or treat wrinkling through a variety of actions. Many approaches are taken to reduce the appearance of facial wrinkles based on the understanding of the molecular basis of wrinkle formation. Such treatments include cosmetic products, drug therapy and surgical procedures. For example, many cosmetic products contain hydroxy acids, which may stimulate collagen synthesis. Another common treatment utilizes retinol, retinoic, retinol palmitate, a derivative of vitamin A, (or its stronger, prescribed version Retin-A and Renova) which helps collagen production. Bicyclic aromatic compounds with retinoid-type activity, which are useful in particular in preventing or treating various keratinization disorders, are described in EP 679 630. These compounds are particularly active for repairing or combating chronological or actinic ageing of the skin, for example such as in anti-wrinkle products. Antioxidants such as vitamin C and E and coenzyme Q-
• non- sunscreen actives of the invention that are anti-skin aging or anti-wrinkling actives may contain, alone or in combination, the bicyclic aromatic compounds defined above, other compounds which have retinoid-type activity, free-radical scavengers, hydroxy or keto acids or derivatives thereof.
• free-radical scavenger refers to, for example, a- tocopherol, superoxide dismutase, ubiquinol or certain metal-chelating agents.
• Hydroxy acids include, e.g., alpha-hydroxy acids such as lactic acid and glycolic acid or beta- hydroxy acids such as salicylic acid and salicylic acid derivatives such as the octanoyl derivative; other hydroxy acids and keto acids include malic, citric, mandelic, tartaric or glyceric acids or the salts, amides or esters thereof.
• Other anti-wrinkling agents and anti-skin aging agents useful in the invention include sulfur-containing D and L amino acids and their derivatives and salts, particularly the N-acetyl derivatives, a preferred example of which is N-acetyl-L-cysteine; thiols, e.g.
• ethane thiol fat-soluble vitamins, ascorbyl palmitate, ceramides, pseudoceramides (e.g., pseudoceramides described in U.S. Pat. Nos. 5,198,210; 4,778,823; 4,985,547; 5,175,321, all of which are incorporated by reference herein), phospholipids (e.g., distearoyl lecithin phospholipid), fatty acids, fatty alcohols, cholesterol, plant sterols, phytic acid, lipoic acid; lysophosphatidic acid, and skin peel agents (e.g., phenol and the like), and mixtures thereoi.
• phospholipids e.g., distearoyl lecithin phospholipid
• fatty acids or alcohols are those that have straight or branched alkyl chains containing 12-20 carbon atoms.
• a particularly preferred fatty acid is linoleic acid since linoleic acid assists in the absorption of ultraviolet light and furthermore is a vital component of the natural skin lipids.
• suitable anti-wrinkle actives for use herein are described in U.S. Pat. No. 6,217,888, which description is incorporated herein by reference.
• Anti-inflammatory actives include steroidal, non-steroidal, and other compounds.
• Non-limiting examples of steroidal anti-inflammatory agents suitable for use herein include corticosteroids such as hydrocortisone, hydroxyltriamcinolone, alpha- methyl dexamethasone, dexamethasone-phosphate, beclomethasone dipropionates, clobetasol valerate, desonide, desoxymethasone, desoxycorticosterone acetate, dexamethasone, dichlorisone, diflorasone diacetate, diflucortolone valerate, fluadrenolone, fluclorolone acetonide, fludrocortisone, flumethasone pivalate, fluosinolone acetonide, fluocinonide, flucortine butylesters, fluocortolone, fluprednidene (fluprednylidene) acetate, flurandrenolone, halcinonide, hydrocortisone acetate, hydrocorticoster
• Nonsteroidal anti-inflammatory agents are also suitable for use herein as skin active agents in the compositions of the invention.
• Non-limiting examples of nonsteroidal anti-inflammatory agents suitable for use herein include oxicams (e.g., piroxicam, isoxicam, tenoxicam, sudoxicam, CP-14,304); salicylates (e.g., aspirin, disalcid, benorylate, trilisate, safapryn, solprin, diflunisal, fendosal); acetic acid derivatives (e.g., diclofenac, fenclofenac, indomethacin, sulindac, tolmetin, isoxepac, furofenac, tiopinac, zidometacin, acematacin, fentiazac, zomepirac, clindanac, oxepinac, felbinac, ketorolac); fenamates (e.
• Valdecoxib PARMACIA Corp. (4-(5-methyl-3- ⁇ henyl-4-isox-azolyl) benzenesulfonamide
• Etodolac WYETH Ayerst Laboratories ((.+-.) 1,8-diethyl- l,3,4,9-tetrahydropyrano-[3,4-b]acid).
• Suitable anti-inflammatory or similar other skin active agents include candelilla wax, bisabolol (e.g., alpha bisabolol), aloe vera, plant sterols (e.g., phytosterol), Manjistha (extracted from plants in the genus Rubia, particularly Rubia Cordifolia), and Guggal (extracted from plants in the genus Commiphora, particularly Commiphora Mukul), kola extract, chamomile, red clover extract, sea whip extract, anise oil, garlic oil, ginger extract, vasoconstrictors such as phenylephrine hydrochloride, and combinations thereof.
• bisabolol e.g., alpha bisabolol
• aloe vera e.g., plant sterols (e.g., phytosterol)
• Manjistha extracted from plants in the genus Rubia, particularly Rubia Cordifolia
• Guggal extended from plants in the
• suitable anti-inflammatory or similar other skin active agents include compounds of the Licorice (the plant genus/species Glycyrrhiza glabra) family, including glycyrrhetic acid, glycyrrhizic acid, and derivatives thereof (e.g., salts and esters).
• Suitable salts of the foregoing compounds include metal and ammonium salts.
• Suitable esters include C 2 -C 24 saturated or unsaturated esters of the acids, preferably C 10 -C 24 , more preferably C 16 -C 24 .
• oil soluble licorice extract examples include oil soluble licorice extract, the glycyrrhizic and glycyrrhetic acids themselves, monoammonium glycyrrhizinate, monopotassium glycyrrhizinate, dipotassium glycyrrhizinate, 1 -beta- glycyrrhetic acid, stearyl glycyrrhetinate, and 3- stearyloxy-glycyrrhetinic acid, disodium S-succinyloxy-beta-glycyrrhetinate, and combinations thereof.
• Anesthetic actives include butamben picrate, lidocaine, xylocaine, benzocaine, bupivacaine, chlorprocaine, dibucaine, etidocaine, mepivacaine, tetracaine, dyclom ' ne, hexylcaine, procaine, ***e, ketamine, pramoxine, phenol, and pharmaceutically acceptable salts thereof.
• Analgesic actives include dyclonine hydrochloride, aloe vera, fentanyl, capsaicin, and the like.
• Anti-pruritic actives include alclometasone dipropionate, betamethasone valerate, and isopropyl myristate MSD.
• Anti-microbial actives include antifungal, antibacterial, and antiseptic compounds.
• Antifungal compounds include, but are not limited to, compounds such as imidazole antifungals. Specific antifungals include butocouazole nitrate, miconazole, econazole, ketoconazole, oxiconizole, haloprogin, clotrimazole, and butenafine HCl, naftifme, terbinafine, ciclopirox, and tolnaftate.
• Antibacterial and antiseptic compounds include phenol-TEA complex, mupirocin, triclosan, chlorocresol, chlorbutol, iodine, clindamycin, CAE (Anjinomoto Co., Inc., containing DL-pyrrolidone Carboxylic acid salt of L-Cocoyl Arginine Ethyl Ester), povidone-iodine, polymyxin b sulfate-bacitracin, zinc-neomycin sulfate-hydrocortisone, chloramphenicol, rnethylbenzethonium chloride, and erythromycin and antiseptics (e.g., benzalkonium chloride, benzethonium chloride, chlorhexidine gluconate, mafenide acetate, nitrofurazone, nitromersol and the like may be included in compositions of the invention.
• antimicrobial and antifungal actives useful in the compositions of the present invention include, but are not limited to, /3-lactam drugs, quinolone drugs, ciprofloxacin, norfloxacin, tetracycline, amikacin, 2,4,4'-trichloro-2'- hydroxy diphenyl ether, 3,4,4'-trichlorocarbanilide, phenoxyethanol, phenoxy propanol, phenoxyisopropanol, doxycycline, capreomycin, chlorhexidine, chlortetracycline, oxytetracycline, ethambutol, hexamidine isethionate, metronidazole, pentamidine, gentamicin, kanamycin, lineomycin, methacycline, methenamine, minocycline, n
• Suitable anti-viral agents include, but are not limited to, metal salts (e.g., silver nitrate, copper sulfate, iron chloride, etc.) and organic acids (e.g., malic acid, salicylic acid, succinic acid, benzoic acid, etc.).
• metal salts e.g., silver nitrate, copper sulfate, iron chloride, etc.
• organic acids e.g., malic acid, salicylic acid, succinic acid, benzoic acid, etc.
• compositions which contain additional suitable anti-viral agents include those described in copending U.S. patent applications Ser. Nos. 09/421,084
• Anti-allergenics include antihistamines.
• Antihistamines can be OfH 1 or H 2 antagonists or other types of histamine release inhibitors.
• the H 1 antagonists can be sedating or non-sedating.
• Examples OfH 1 -sedating antihistamines include diphenhydramine (Benadryl), chlorpheniramine, tripelennamine, promethazine, clemastine, doxylamine, benadryl etc.
• Examples of Hi -non-sedating antihistamines include astemizole, terfenadine, loratadine etc.
• H 2 antagonists include cimetadine, famotidine, nizatidine, and ranitidine.
• Examples of histamine-release- inhibitors include cromolyn.
• a further active useful in the invention may be a medicinal for treatment of dermatological conditions such as psoriasis, acne, eczema, and other skin conditions due to disease, pathology, accident, and the like.
• Medicinals include burn relief ointments, such as o-amino-p-toluenesulfonamide monoacetate; dermatitis relief agents, such as the active steroid amcinonide, diflorasone diacetate, and hydrocortisone; diaper rash relief agents, such as methylbenzethonium chloride and the like; herpes treatment drugs, such as O-[(2-hydroxyethoxy)methyl]guanine; psoriasis, seborrhea and scabicide agents, such as shale oil and derivatives thereof, elubiol, ketoconazole, coal tar and petroleum distillates, salicylic acid, zinc pyrithione, selenium sulfide, hydrocortis
• Anticellulite actives include isobutylmethylxanthine, caffeine, theophylline, theobromine, aminophylline,yohinibine, and mixtures thereof.
• actives suitable for treating hair loss include, but are not limited to potassium channel openers or peripheral vasodilators such as minoxidil, diazoxide, and compounds such as N*-cyano-N-(tert-pentyl)-N'-3-pyridmyl-guanidine ("P- 1075") as disclosed in U.S. Pat.
• vitamins such as vitamin E and vitamin C, and derivatives thereof such as vitamin E acetate and vitamin C palmitate; hormones, such as erythropoietin, prostaglandins, such as prostaglandin EI and prostaglandin F2-alpha; fatty acids, such as oleic acid; diruretics such as spironolactone; heat shock proteins ("HSP"), such as HSP 27 and HSP 72; calcium channel blockers, such as verapamil HCL, nifedipine, and diltiazemamiloride; immunosuppressant drugs, such as cyclosporin and Fk-506; 5 alpha-reductase inhibitors such as finasteride; growth factors such as, EGF, IGF and FGF; transforming growth factor beta; tumor necrosis factor; non-steroidal anti-inflammatory agents such as benoxaprofen; retinoids such as tretinoin; cytochromase inhibitors, and others.
• Joborandi DI genes for cytokines, growth factors, and male-pattered baldness; antifungals such as ketoconazole and elubiol; antibiotics such as streptomycin; proteins inhibitors such as cycloheximide; acetazolamide; benoxaprofen; cortisone; diltiazem; hexachlorobenzene; hydantoin; nifedipine; penicillamine; phenothaiazines; pinacidil; psoralens, verapamil; zidovudine; alpha-glucosylated rutin having at least one of the following rutins: quercetin, isoquercitrin, hespeddin, naringin, and methylhesperidin, and flavonoids and transglycosidated derivatives thereof which are all disclosed in JP 7002677, which is incorporated by reference in its entirety herein; and mixtures thereof.
• Preferred hair loss treatment agents include minoxidil, 6-(I-piperdinyl)-2,4- pyrimidinediamme-3-oxide, N'-cyano-N-Ctert-penty ⁇ -N'-S-pyridinyl-guanidine, finasteride, retinoids and derivatives thereof, ketoconazole, elubiol or mixtures thereof.
• Examples of actives suitable for use in inhibiting hair growth include: serine proteases such as trypsin; vitamins such as alpha-tocophenol (vitamin E) and derivatives thereof such as tocophenol acetate and tocophenol palmitate; antineoplastic agents, such as doxorubicin, cyclophosphamide, chlormethine, methotrexate, fluorouracil, vincristine, daunorubicin, bleomycin and hydroxycarbamide; anticoagulants, such as heparin, heparinoids, coumaerins, detran and indandiones; antithyroid drugs, such as iodine, thiouracils and carbimazole; lithium and lithium carbonate; interferons, such as interferon alpha, interferon alpha-2a and interferon alpha-2b; retinoids, such as retinol (vitamin A), isotretinoin: glucocorticoids such as betamethasone
• hair bleaching agents include perborate or persulfate salts.
• Deodorant compounds include astringent salts and bioactive compounds.
• the astringent salts include organic and inorganic salts of aluminum, zirconium, zinc, and mixtures thereof.
• the anion of the astringent salt can be, for example, sulfate, chloride, chlorohydroxide, alum, formate, lactate, benzyl sulfonate or phenyl sulfonate.
• Exemplary classes of antiperspirant astringent salts include aluminum halides, aluminum hydroxyhalides, zirconyl oxyhalides, zirconyl hydroxyhalides, and mixtures thereof.
• Exemplary aluminum salts include aluminum chloride and the aluminum hydroxyhalides having the general formula Al 2 (OH) x Q y XH 2 ⁇ , wherein Q is chlorine, bromine or iodine; x is about 2 to about 5; x+y is about 6, wherein x and y are not necessarily integers; and X is about 1 to about 6.
• Exemplary zirconium compounds include zirconium oxy salts and zirconium hydroxy salts, also referred to as zirconyl salts and zirconyl hydroxy salts, and represented by the general empirical formula ZrO(OH) 2 -nz L z , wherein z varies from about U.y to about L ana is not necessarily an integer; n is the valence of L; 2-nz is greater than or equal to 0; and L is selected from the group consisting of halides, nitrate, sulfamate, sulfate, and mixtures thereof.
• Exemplary deodorant compounds therefore include, but are not limited to, aluminum bromohydrate, potassium alum, sodium aluminum chlorohydroxy lactate, aluminum sulfate, aluminum chlorohydrate, aluminum-zirconium tetrachlorohydrate, an aluminum-zirconium polychlorohydrate complexed with glycine, aluminum-zirconium trichlorohydrate, aluminum-zirconium octachlorohydrate, aluminum sesquichlorohydrate, aluminum sesquichlorohydrex PG 3 aluminum chlorohydrex PEG, aluminum zirconium octachlorohydrex glycine complex, aluminum zirconium pentachlorohydrex glycine complex, aluminum zirconium tetrachlorohydrex glycine complex, aluminum zirconium trichlorohydrex glycine complex, aluminum chlorohydrex PG, zirconium chlorohydrate, aluminum dichlorohydrate, aluminum dichlorohydrex PEG, aluminum dichlorohydrex PEG, aluminum
• the deodorant compound can be a bacteriostatic quaternary ammonium compound, such as, for example, cetyl trimethyl ammonium bromide, cetyl pyridinium chloride, benzethonium chloride, diisobutylbenzoxyethoxyethyldimethylbenzyl ammonium chloride, sodium N-lauryl sarcosine, sodium N-polymethyl sarcosine, lauroyl sarcosine, N-myristolyl glycine, potassium N-lauroyl sarcosine, and stearyl trimethyl ammonium chloride; or a bioactive compound; or a carbonate or bicarbonate salt, such as, for example, the alkali metal carbonates and bicarbonates, and the ammonium and tetralkylammonium carbonates and bicarbonates.
• a bioactive compound such as, for example, the alkali metal carbonates and bicarbonates, and the ammonium and te
• antioxidants include propyl, octyl and dodecyl esters of gallic acid, butylated hydroxyanisole (BHA, usually purchased as a mixture of ortho and meta isomers), butylated hydroxytoluene (BHT), nordihydroguaiaretic acid, Vitamin A, ascorbic acid and its salts, ascorbyl esters of fatty acids, ascorbic acid derivatives (e.g., magnesium ascorbyl phosphate, sodium ascorbyl phosphate, ascorbyl sorbate), tocopherol, tocopherol acetate, other esters of tocopherol, tocotrienols and their esters, and 6- hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid
• antioxidants include uric acid and its salts and alkyl esters, sorbic acid and its salts, lipoic acid, amines (e.g., N,N-diethylhydroxylamine, amino-guanidine), sulfhydryl compounds (e.g., glutathione, N-acetyl cysteine), dihydroxy fumaric acid and its salts, lycine pidolate, arginine pilolate, nordihydroguaiaretic acid, bioflavonoids, curcumin, lysine, methionine, proline, superoxide dismutase, silymarin, tea extracts, grape skin/seed extracts, melanin, and rosemary extracts may be used.
• amines e.g., N,N-diethylhydroxylamine, amino-guanidine
• sulfhydryl compounds e.g., glutathione, N-acetyl cysteine
• Preferred antioxidants are photostable antioxidants.
• An exemplary photostable antioxidant is marketed under the tradename EMBLICA by EMD Chemicals. See, e.g., U.S. Patent No. 6,831,191.
• Insect repellants include the most widely used active agent for personal care products, N,N-Diethyl-m-toluamide, frequently called "DEET" and available in the form of a concentrate containing at least about 95 percent DEET.
• Other synthetic chemical repellents include dimethyl phthalate, ethyl hexanediol, indalone, di-n- propylisocinchoronat- e, bicycloheptene, dicarboximide and tetrahydrofuraldehyde.
• Certain plant-derived materials also have insect repellent activity, including citronella oil and other sources of citronella (including lemon grass oil), limonene, rosemary oil and eucalyptus oil.
• Choice of an insect repellent for incorporation into compositions of the invention will frequently be influenced by the odor of the repellent.
• the amount of repellent agent used will depend upon the choice of agent; DEET is useful at high concentrations, such as up to about 15 percent or more, while some of the plant-derived substances are typically used in much lower amounts, such as 0.1 percent or less
• compositions of the present invention may contain a wide range of additional active components.
• CTFA Cosmetic Ingredient Handbook Seventh Edition, 1997 and the Eighth Edition, 2000, which are incorporated by reference herein in its entirety, describes a wide variety of active ingredients commonly used in skin care compositions, which are suitable for use in the compositions of the present invention.
• Other topically- active compounds are listed in Remington's Pharmaceutical Sciences, 20th Ed., Lippincott Williams & Witkins, Baltimore, MD (2000) (hereinafter Remington's), U.S. Pharmacopeia and National Formulary, The United States Pharmacopeial Convention, Inc., Rockville, Md. and Physician's Desk Reference, Medical Economics Co., Inc., Oradell, N J.incorporated herein by reference.
• the non-sunscreen active may be provided as is or in encapsulated form.
• an additive or composition for topical application containing the active further includes a cationic polymer, as described herein, as well as, optionally, a film former, a preservative, and/or an antioxidant that is stable upon exposure to sunlight.
• a film former as described herein
• the additive or composition for topical application may comprise two, three, four, five, six, seven, eight, nine, ten, or more than ten actives, each of which may be encapsulated or non-encapsulated, in any combination.
• the active is encapsulated sol-gel microcapsules, such as silica sol-gel microcapsules.
• the invention provides an additive for addition to a composition for topical application, where the additive comprises an encapsulated non-sunscreen active, and optionally further comprises a cationic polymer
• the invention provides a composition for topical application that contains an additive, where the additive comprises an encapsulated non-sunscreen active, and optionally further comprises a cationic polymer.
• Further ingredients include film formers, antioxidants, preservatives, and other ingredients as listed herein.
• the composition for topical application may be, e.g., a bodywash.
• the invention provides microcapsules, e.g., sol-gel microcapsules (e.g., as described in U.S. Patents No. 6,238,650; 6,436,375, 6,303,149; and 6,468,509) that act as a protective barrier on the skin when used either alone, or as an additive in a bodywash.
• the sol-gel microcapsules may be used without any additional active ingredients (i.e., empty) , providing a physical barrier, or they may be used with additional encapsulated active ingredients that enhance their barrier function.
• the microcapsules may contain substances that act to screen toxic agents (e.g., biological or chemical warfare agents) or radiation (e.g., alpha, beta, or gamma radiation) partially or completely from penetrating the user's skin, hi some embodiments, the microcapsules may contain one or more agents that absorb radiation, such as graphite, lead, tungsten, and others known in the art, or agents that reflect radiation such as ceramic beads.
• toxic agents e.g., biological or chemical warfare agents
• radiation e.g., alpha, beta, or gamma radiation
• the microcapsules may contain one or more agents that absorb radiation, such as graphite, lead, tungsten, and others known in the art, or agents that reflect radiation such as ceramic beads.
• microcapsules maybe designed so as to experience minimal or no breakage when applied to the skin, as well as to experience minimal penetration of the skin, it is possible to use even toxic substances (e.g., lead) that provide a screening effect, since these substances will not be released or will be released m only minimal amounts, l He microcapsules are eventually removed from the skin through repeated washing and/or normal sloughing of the external skin cell layers.
• toxic substances e.g., lead
• the invention provides a means to deliver a last line of defense on the skin of personnel where the active used in the microcapsules may be one that is not appropriate for long- term use, but that is appropriate for a limited number of applications in order to protect the wearer from a greater risk (e.g., microcapsules encapsulating lead to protect against a radiation attack).
• the microcapsules e.g., sol-gel microcapsules, can be prepared so as to experience no or minimal breakage when applied to the skin, either as is or in the form of a bodywash.
• the microcapsules e.g., sol-gel microcapsules
• the microcapsules can be prepared so as to experience various degrees of breakage, on average, when applied as is or in a bodywash.
• the microcapsules e.g., sol-gel microcapsules
• microcapsules may be formulated so as to break open in response to conditions that occur on the skin, so that after application the microcapsules act to release their contents in a time-release or controlled manner.
• Non- limiting exemplary skin or hair conditions that can vary with the user's environment, the variation of which can trigger breakage of microcapsules, include pH, temperature, friction, exposure to light or air, pressure, and the like.
• the additives e.g., sunscreen additives and sunscreen/bodywashes of the invention further include a cationic component.
• a cationic component serves as a protein binder, to provide a positive charge to promote attachment of the composition to proteins of the skin and hair, thus increasing retention of the components, e.g., sunscreen, after rinse and during normal activities. This positive charge creates a strong affinity for the protein in the hair or skin. Any means of imparting a positive charge may be used.
• Preferred means are by including one or more cationic polymers in the composition. Various cationic polymers may be used. Examples of cationic polymers are described in U.S. Pat. Nos.
• Cationic polymers are available commercially, e.g., from Union Carbide Corp. under the trademark POLYMER JR., from Celanese- Stein Hall under the trademark JAGUAR, from GAF Corporation under the tradename Gafquatm and from Merck & Co., Inc under the trademark MERQUAT by.
• Merquat 100 a highly charged cationic dimethyldiallylammonium chloride homopolymer
• MerquatTM 550 a highly charged cationic copolymer prepared with dimethyidiallylammonium chloride and acrylamide.
• These materials are designated in the CTFA dictionary as Quaternium40 and Quaternium-41, respectively.
• polyquaterniums Quaternized material in powder form, not limited to the polyquaterniums, may also be used.
• Exemplary polyquaterniums of use in the invention include polyquaternium-4, -7, -11, -22, -37, -44, -51, and -64.
• Poryquaternium compounds are available commercially, e.g., CELQUAT L-200 for polyquaternium-4.
• Further exemplary polyquaterniums can be quaternized copolymers of vinylpyrrolidone, methacrylamide, vinylimidiazole, and quaternized vinylimidiazole and or with vinyl caprolactum. They all range with different charge densities. We are mainly concerned with those of gretaer cationic charges.
• a dry cationic component such as sold under the tradename CAE (Anjinomoto Co., Inc.), containing DL-pyrrolidone Carboxylic acid salt of L-Cocoyl Arginine Ethyl Ester, which is a cationic agent useful for binding to proteins and providing an antimicrobial effect.
• CAE Anjinomoto Co., Inc.
• the cationic component (e.g., cationic polymer) comprises about 0.1 to about 20%, or about 0.1 to about 10%, or about 0.5 to about 10%, or about 1 to about 10%, or about 0.5 to about 5%, or about 0.5 to about 3%or about 1 to about 5%, or about 1 to about 3%, or about 1% of the total composition.
• the cationic component is polyquaternium-
• the cationic component (e.g., cationic polymer) comprises about 0.03 to about 7%, or about 0.03 to about 4%, or about 0.2 to about 4%, or about 0.3 to about 4%, or about 0.2 to about 2%, or about 0.3 to about 4%, or about 0.3 to about 1%,, or about 0.3 or 0.4% of the total composition, in some embodiments, the cationic component is polyquaternium- 4; in some embodiments the polyquaternium-4 is present at about 0.33%.
• compositions of the invention further include a component that provide a film barrier system, typically a hydrophobic layer that serves to maintain the residual sunscreen after rinse.
• Film barrier systems are well-known in the art and include, without limitation, petrolatum, silicon derivatives, and combinations thereof. Also useful are polymers with carboxylic ends which render themselves insoluble until neutralized. After being neutralized they can act as film formers. Film formers also include emollient esters, lanolin derivatives (e.g., acetylated lanolins), and superfatted oils.
• Film formers are available commercially, e.g., a preferred film former is MOISTUREGUARDTM, which contains petrolatum, dimethicone, stearamidopropyl dimethylamine stearate, and tocopheryl acetate, available from Engelhard. [0088] It may also be desirable to add acrylic co-polymers to the formulations of the invention as film formers.
• An exemplary liquid acrylic copolymer formulation is DERMACRYL, marketed by National Starch and Chemical.
• Acrylic co-polymers may be included in sunscreen additives at about 0.1 to about 5%, or about 0.2 to about 3%, or about 0.2%, 0.3%, 0.4%, or 0.5%, or in sunscreen/bodywashes at about 0.05 to about 2%, or about 0.1 to about 1%, or about 0.05%, 0.1%, 0.2%, 0.3%, 0.4%, or 0.5%.
• a secondary film former may also be used, e.g., keratin or other protein derivative in an amino acid complex such as cysteine.
• the film former may be present in the sunscreen additive in the range of about
• the film former MoistureGuard is used at a concentration of about
• Equivalent film formers at equivalent concentrations, may also be used.
• some preparations may perform more than one function, for example, inorganic blockers such as Tioveil and Spectraveil (both of the Tioxide Group), in certain variations, may be film-formers and may have advantageous uses here.
• inorganic blockers such as Tioveil and Spectraveil (both of the Tioxide Group)
• Spectraveil both of the Tioxide Group
• many emollients may also perform a film former function in that they provide a barrier on the skin.
• compositions of the invention may include water- insoluble emollients that include fatty acids such as oleic and stearic; fatty alcohols such as cetyl, and hexadecyl (ENJAY); esters such as diisopropyl adipate, benzoic acid esters of C 9 -C 15 alcohols, and isononyl iso-nonanoate; alkanes such as mineral oil; silicones; such as dimethyl polysiloxane and ethers such as polyoxypropylene butyl ethers and polyoxypropylene cetyl ethers. If a water-insoluble emollient is used it may be in an amount from about 2% to about 15% by weight, and most preferably from about 4% to about 10%.
• film formers include polythylenes, such as those available from New Phase Technologies as PERFORMALENE 400, a polyethylene having a molecular weight of 400.
• Another suitable water-proofing agent is polyethylene 2000 (molecular weight of 2000), which is available from New Phase Technologies as PERFORMALENE 2000.
• Yet another suitable film former/waterproofing agent is synthetic wax, also available from New Phase Technologies as PERFORMA V-825.
• Still yet another suitable film former/waterproofing agent is octadecene/MA copolymer
• Additional film formers which also may be used within the framework of the invention include any film former chemistry known in the art.
• suitable additional film formers include acacia gum, cellulose derivatives, guar derivatives and all those set forth on pages 68-69 of the C.T.F.A. Cosmetic Ingredient Handbook, First Edition, 1988, which is hereby incorporated by reference.
• film formers include acrylamides copolymer, acrylamide/sodium aciylate copolymer, acrylate/acrylamide copolymer, acrylate/ammonium methacrylate copolymer, acrylates copolymer, acrylates/diacetoneacrylamide copolymer, acrylic/acrylate copolymer, adipic acid/dimethylaminohydroxypropyl diethlenetnamine copolymer, adipic acid/epoxypropyl/diethlenetriarnine copolymer, albumen, allyl stearate/VA copolymer, aminoethylacrylate phosphate/acrylate copolymer, ammonium acrylates copolymer, ammonium alg
• compositions of the present invention A wide variety of additional components may be added to the compositions of the present invention, as long as the components are selected so as to avoid any undesirable reaction with the primary components (e.g., one or more of the sunscreen agents) of the composition.
• additional components include one or more of the following: Absorbents, abrasives, anticaking agents, antifoaming agents, binders, biological additives, buffering agents, bulking agents, chelating agents/sequestrants (e.g., disodium EDTA), chemical additives, colorants, cosmetic astringents, cosmetic biocides, denaturants, drug astringents, emollients (including glycerin alovera, and Vitamins A, C, and D [hydrating agents and skin protectants]), foam boosters, fragrance components, gums, humectants/moisturizers (including urea, guanidine, glycolic acid, polyhydroxy alcohols such as sorbitol, glycerin, hexanetriol, propylene glycol, hexylene glycol and the like, polyethylene glycol
• the additives and bodywashes of the invention include a preservative.
• exemplary preservatives useful in the invention include citric acid, tartaric acid, phosphoric acid, iminodiacetic acid, nitrilotriacetic acid, hydroxyethyleneaminodiacetic acid and ethylenediaminetetraacetic acid and salts thereof; parahydroxybenzoates such as butyl paraben, methyl paraben and propyl paraben; imidazolines (e.g., imidiazolinylurea), triclosan, hydantoins (e.g., dimethyloldimethylhydantoin), isothiazolidinone compounds and mixtures thereof.
• preservatives useful in the invention include citric acid, tartaric acid, phosphoric acid, iminodiacetic acid, nitrilotriacetic acid, hydroxyethyleneaminodiacetic acid and ethylenediaminetetraacetic acid and salts thereof; parahydroxybenzoates such as but
• preservatives include KATHON CG and KATHON CGII, which contain methylchloroisothiazolinone and methylisothiazolinone (Rohm and Haas). When present, the quantity of preservative is in the range from 0.001 to 2%, preferably from 0.01 to 0.2%.
• the compositions of the invention include a chelating agent. Chelating agents are substances used to chelate or bind metallic ions, such as with a heterocyclic ring structure so that the ion is held by chemical bonds from each of the participating rings.
• Suitable chelating agents include ethylene diaminetetraacetic acid (EDTA), EDTA disodium, calcium disodium edetate, EDTA trisodium, EDTA tetrasodium and EDTA dipotassium.
• One or more chelating agents can optionally be included in the additives or additive/bodywashes in amounts ranging from about 0.001 to about 0.2 weight percent, or about 0.01% weight percent.
• Thickening agents or gellants may be added as desired to adjust the texture and viscosity of the composition.
• Exemplary agents or gellants maybe selected from CarbopolTM resins [e.g., 934, 971, 974, 980, 981] and PemulenTM [TR-I and TR-2][both Carbopol TMand PemulenTM are registered trademarks of BF Goodrich], Noveon AA-I, ETD resins, and UltrezTM resins [registered trademark, BF Goodrich], hi addition, carbomers might be useful for this purpose.
• non-polar wax examples include ester waxes, diester waxes, hydrocarbon waxes, silicone waxes and triglyceride waxes and mixtures thereof.
• Other components may include a liquid hydrocarbon (similar to pentane), and/or a cationic foaming agent derived from arginine and or cysteine.
• compositions include fragrance, dyes, antimicrobial materials such as triclocarban, triclosaii, iodophors, iodine formulations, phenolic compounds, e.g. hexachlorophene, and bisbiguanides, e.g. chlorhexidene gluconate, and the like. See, e.g., U.S. Patent Nos. 6,827,795; 6,517,854; 6,010,817; 5,173,216; 5,719,113; 5,259,984; 5,562,912; 5,629,006; 5,728,662; 5,767,163;
• the components of the composition are generally mixed in water.
• compositions of the invention may be formulated as products for washing the skin, for example, bath or shower gels, hand washing compositions or facial washing liquids; pre- and post-shaving products; rinse-off, wipe-off and leave-on skin care products; products for washing the hair and for dental use.
• shower gels are particularly preferred product forms.
• the sunscreen additives of the invention may be combined with other ingredients to produce a bodywash (e.g., a liquid or solid formulation).
• the sunscreen/bodywash may include one or more surfactants. The use of surfactants in bodywashes is well-known in the art.
• any surfactant known in the art and appropriate for a bodywash composition may be used. See, McCutcheon's Detergents & Emulsifiers, M.C. Publishing Co. (North American edition 1989); Schwartz, et al., Surface Active Agents, Their Chemistry and Technology, New York, Interscience Publishers, 1949, and U.S. Patent Nos.
• the surfactant(s) maybe cationic, anionic, nonionic, zwitterionic, amphoteric, or any combination thereof.
• anionic surfactants include those selected from the group consisting of alkyl and alkyl ether sulfates, sulfated monoglycerides, sulfonated olefins, alkyl aryl sulfonates, primary or secondary alkane sulfonates, alkyl sulfosuccinates, acyl taurates, acyl isethionates, alkyl glycerylether sulfonate, sulfonated methyl esters, sulfonated fatty acids, alkyl phosphates, ethoxylated alkyl phosphates, acyl glutamates, acyl sarcosinates, alkyl sulfoacetates, acylated peptides, alkyl ether carboxylates, acyl lactylates, anionic fluorosurfactants, and combinations thereof.
• alkyl sulfates that may be used are sodium, ammonium, potassium, magnesium, or TEA salts of lauryl or myristyl sulfate.
• alkyl ether sulfates that maybe used include ammonium, sodium, magnesium, or TEA laureth-3 sulfate.
• Another suitable class of anionic surfactants are the sulfated monoglycerides of the form R1CO-O ⁇ CH 2 -C(OH)H ⁇ CH 2 -O—SO 3 M, wherein Rl is a saturated or unsaturated, branched or unbranched alkyl group from about 8 to about 24 carbon atoms, and M is a water-soluble cation such as ammonium, sodium, potassium, magnesium, triethanolamine, diethanolamine and monoethanolamine.
• An example of a sulfated monoglyceride is sodium cocomonoglyceride sulfate.
• Suitable anionic surfactants include olefin sulfonates of the form RlSO 3 M, wherein Rl is a mono-olefm having from about 12 to about 24 carbon atoms, and M is a water-soluble cation such as ammonium, sodium, potassium, magnesium, triethanolamine, diethanolamine and monoethanolamine.
• Rl is a mono-olefm having from about 12 to about 24 carbon atoms
• M is a water-soluble cation such as ammonium, sodium, potassium, magnesium, triethanolamine, diethanolamine and monoethanolamine.
• An example of a sulfonated olefin is sodium C 14/Cl 6 alpha olefin sulfonate.
• Suitable anionic surfactants are the linear alkylbenzene sulfonates of the form Rl-C 6 H 4 -SO 3 M, wherein Rl is a saturated or unsaturated, branched or unbranched alkyl group from about 8 to about 24 carbon atoms, and M is a water-soluble cation such as ammonium, sodium, potassium, magnesium, triethanolamine, diethanolamine and monoethanolamine.
• Rl is a saturated or unsaturated, branched or unbranched alkyl group from about 8 to about 24 carbon atoms
• M is a water-soluble cation such as ammonium, sodium, potassium, magnesium, triethanolamine, diethanolamine and monoethanolamine.
• An example of this anionic surfactant is sodium dodecylbenzene sulfonate.
• Still other anionic surfactants suitable for the compositions of the present invention include the primary or secondary alkane sulfonates of the form Rl SO 3 M, wherein Rl is a saturated or unsaturated, branched or unbranched alkyl chain from about 8 to about 24 carbon atoms, and M is a water-soluble cation such as ammonium, sodium, potassium, magnesium, triethanolamine, diethanolamine and monoethanolamine.
• Rl is a saturated or unsaturated, branched or unbranched alkyl chain from about 8 to about 24 carbon atoms
• M is a water-soluble cation such as ammonium, sodium, potassium, magnesium, triethanolamine, diethanolamine and monoethanolamine.
• An example of an alkane sulfonate useful herein is alkali metal or ammonium C 13-Cl 7 paraffin sulfonates.
• alkyl sulfosuccinates which include disodium N-octadecylsulfosuccinamate; diammonium lauryl sulfosuccinate; tetrasodium N-(l,2-dicarboxyethyl)-N-octadecylsulfosuccinate; diamyl ester of sodium sulfosuccinic acid; dihexyl ester of sodium sulfosuccinic acid; and dioctyl esters of sodium sulfosuccinic acid.
• taurates that are based on taurine.
• taurates include
• N-alkyltaurines such as the one prepared by reacting dodecylamine with sodium isethionate as detailed in U.S. Pat. No. 2,658,072.
• Another class of suitable anionic surfactants is the acyl isethionates.
• Nonlimiting examples of these acyl isethionates include ammonium cocoyl isethionate, sodium cocoyl isethionate, sodium lauroyl isethionate, and mixtures thereof.
• alkylglyceryl ether sulfonates of the form Rl-OCH 2 -C(OH)H-CH 2 -SO 3 M, wherein Rl is a saturated or unsaturated, branched or unbranched alkyl group from about 8 to about 24 carbon atoms, and M is a water- soluble cation such as ammonium, sodium, potassium, magnesium, triethanolamine, diethanolamine and monoethanolamine.
• Rl is a saturated or unsaturated, branched or unbranched alkyl group from about 8 to about 24 carbon atoms
• M is a water- soluble cation such as ammonium, sodium, potassium, magnesium, triethanolamine, diethanolamine and monoethanolamine.
• sodium cocoglyceryl ether sulfonate is sodium cocoglyceryl ether sulfonate.
• Suitable anionic surfactants include: Sulfonated fatty acids of the form Rl- CH(SO 4 )-COOH and sulfonated methyl esters of the from R1-CH(SO 4 )-CO-O— CH 3 , where Rl is a saturated or unsaturated, branched or unbranched alkyl group from about 8 to about 24 carbon atoms (e.g., alpha sulphonated coconut fatty acid and lauryl methyl ester); phosphates such as monoalkyl, dialkyl, and trialkylphosphate salts formed by the reaction of phosphorous pentoxide with monohydric branched or unbranched alcohols having from about 8 to about 24 carbon atoms (e.g., sodium mono or dilaurylphosphate, ethoxylated monoalkyl phosphates, etc.); acyl glutamates corresponding to the formula RICO-N(COOH)-CH 2 CH 2 -CO 2 M wherein Rl is
• x 8 to about 24 carbon atoms
• M is a water-soluble cation (e.g., sodium laureth carboxylate); acyl lactylates corresponding to the formula RlCO-[O-CH(CH 3 )- CO]X-CO 2 M wherein Rl is a saturated or unsaturated, branched or unbranched alkyl or alkenyl group of about 8 to about 24 carbon atoms, x is 3, and M is a water-soluble cation ( e -g- 5 sodium cocoyl lactylate); carboxylates, nonlimiting examples of which include sodium lauroyl carboxylate, sodium cocoyl carboxylate, and ammonium lauroyl carboxylate; anionic fiourosurfactants; and natural soaps derived from the saponification of vegetable and/or animal fats & oils examples of which include sodium laurate, sodium myristate, palmitate, stearate, tallowate, cocoate.
• any counter cation, M can be used on the anionic surfactant.
• the counter cation is selected from the group consisting of sodium, potassium, ammonium, monoethanolamine, diethanolamine, and triethanolamine.
• Nonlimiting examples of nonionic surfactants that may be included in the compositions of the present invention include those selected from the group consisting of alkyl glucosides, alkyl polyglucosides, polyhydroxy fatty acid amides, alkoxylated fatty acid esters, sucrose esters, amine oxides, and mixtures thereof.
• Alkyl glucosides and alkyl polyglucosides are useful herein, and can be broadly defined as condensation products of long chain alcohols, e.g., C8-30 alcohols, with sugars or starches or sugar or starch polymers, i.e., glycosides or polyglyco sides.
• These compounds can be represented by the formula (S) n — O--R wherein S is a sugar moiety such as glucose, fructose, mannose, and galactose; n is an integer of from about 1 to about 1000, and R is a C8-30 alkyl group.
• long chain alcohols from which the alkyl group can be derived include decyl alcohol, cetyl alcohol, stearyl alcohol, lauryl alcohol, myristyl alcohol, oleyl alcohol, and the like.
• Preferred examples of these surfactants include those wherein S is a glucose moiety, R is a C8-20 alkyl group, and n is an integer of trom about 1 to about 9.
• Commercially available examples of these surfactants include decyl polyglucoside (available as APG 325 CS from Henkel) and ⁇ lauryl polyglucoside (available as APG 600CS and 625 CS from Henkel).
• sucrose ester surfactants such as sucrose cocoate and sucrose laurate.
• Nonionic surfactants include polyhydroxy fatty acid amide surfactants, more specific examples of which include glucosarm ' des Processes for making compositions containing polyhydroxy fatty acid amides are disclosed, for example, in GB. Pat. Specification 809,060, published Feb. 18, 1959, by Thomas Hedley & Co., Ltd.; U.S. Pat. No. 2,965,576, to E. R. Wilson, issued Dec. 20, 1960; U.S. Pat. No. 2,703,798, to A. M. Schwartz, issued Mar. 8, 1955; and U.S. Pat. No. 1,985,424, to
• Nonionic surfactants include amine oxides.
• Amine oxides correspond to the general formula R 1 R 2 R 3 N ⁇ O, wherein R 1 contains an alkyl, alkenyl or monohydroxy alkyl radical of from about 8 to about 18 carbon atoms, from 0 to about 10 ethylene oxide moieties, and from 0 to about 1 glyceryl moiety, and R 2 and R 3 contain from about 1 to about 3 carbon atoms and from 0 to about 1 hydroxy group, e.g., methyl, ethyl, propyl, hydroxyethyl, or hydroxypropyl radicals.
• the arrow in the formula is a conventional representation of a semipolar bond.
• amine oxides suitable for use in this invention include dimethyl-dodecylamine oxide, oleyldi(2-hydroxyethyl) amine oxide, dimethyloctylamine oxide, dimethyl-decylamine oxide, dimethyl- tetradecylamine oxide, 3,6,9-trioxaheptadecyldiethylamine oxide, di(2-hydroxyethyl)- tetradecylamine oxide, 2-dodecoxyethyldimethylarnine oxide, 3-dodecoxy-2- hydroxypropyldi(3-hydroxypropyl)amine oxide, dimethylhexadecylamine oxide.
• amphoteric surfactant is also intended to encompass zwitterionic surfactants, which are well known to formulators skilled in the art as a subset of amphoteric surfactants.
• amphoteric lathering surfactants can be used in the compositions of the present invention.
• Particularly useful are those which are broadly described as derivatives of aliphatic secondary and tertiary amines, preferably wherein the nitrogen is in a cationic state, in which the aliphatic radicals can be straight or branched chain and wherein one of the radicals contains an ionizable water solubilizing group, e.g., carboxy, sulfonate, sulfate, phosphate, or phosphonate.
• an ionizable water solubilizing group e.g., carboxy, sulfonate, sulfate, phosphate, or phosphonate.
• Nonlimiting examples of amphoteric or zwitterionic surfactants are those selected from the group consisting of betaines, sultaines, hydroxysultaines, alkyliminoacetates, iminodialkanoates, aminoalkanoates, and mixtures thereof.
• betaines include the higher alkyl betaines, such as coco dimethyl carboxymethyl betaine, lauryl dimethyl carboxymethyl betaine, lauryl dimethyl alphacarboxyethyl betaine, cetyl dimethyl carboxymethyl betaine, cetyl dimethyl betaine (available as Lonzaine 16SP from Lonza Corp.), lauryl bis-(2-hydroxyethyl) carboxymethyl betaine, oleyl dimethyl gamma-carboxypropyl betaine, lauryl bis-(2- hydroxypropyl)alpha-carboxyethyl betaine, coco dimethyl sulfopropyl betaine, lauryl dimethyl sulfoethyl betaine, lauryl bis-(2-hydroxyethyl) sulfopropyl betaine, amidobetaines and amidosulfobetaines (wherein the RCONH(CH.sub.2).sub.3 radical is attached to the nitrogen atom of the betaine),
• Examples of sultaines and hydroxysultaines include materials such as cocamidopropyl hydroxysultaine (available as Mirataine CBS from Rhone-Poulenc).
• Examples of amphoteric surfactants of the present invention include the following compounds: Cetyl dimethyl betaine (this material also has the CTFA designation cetyl betaine); Cocamidopropylbetaine; Cocamidopropyl hydroxy sultaine.
• Examples of other useful amphoteric surfactants are alkyliminoacetates, and iminodialkanoates and aminoalkanoates of the formulas RNC(CH 2 ) CO 2 M] 2 and RNH(CH 2 ).
• m CO 2 M wherein m is from 1 to 4, R is a C 8 -C 22 alkyl or alkenyl, and M is H, alkali metal, alkaline earth metal ammonium, or alkanolammonium.
• imidazolmium and ammonium derivatives include sodium 3-dodecyl-aminopropionate, sodium 3-dodecylaminopropane sulfonate, N-higher alkyl aspartic acids such as those produced according to the teaching of U.S. Pat. 2,438,091; and the products sold under the trade name "Miranol" and described in U.S. Pat. 2,528,378.
• amphoterics include amphoteric phosphates, such as coamidopropyl PG-dimonium chloride phosphate (commercially available as Monaquat PTC, from Mona Corp.). Also useful are amphoacetates such as disodium lauroamphodiacetate, sodium lauroamphoacetate, and mixtures thereof.
• the sunscreen/bodywashes of the invention include at least one cationic surfactant. Many cationic surfactants are known to the art.
• Suitable cationic surfactants include, but are not limited to, fatty amines, di-fatty quaternary amines, tri-fatty quaternary amines, imidazolmium quaternary amines, and combinations thereof.
• Suitable fatty amines include monalkyl quaternary amines such as cetyltrimethylammonium bromide.
• a suitable quaternary amine is dialklamidoethyl hydroxyethylmonium methosulfate.
• stearyldimenthylbenzyl ammonium chloride dodecyltrimethylammonium chloride; nonylbenzylethyldimethyl ammonium nitrate; tetradecylpyridinium bromide; laurylpyridinium chloride; cetylpyridinium chloride; laurylpyridinium chloride; laurylisoquinolium bromide; ditallow(Hydrogenated)dimethyl ammonium chloride; dilauryldimethyl ammonium chloride; and stearalkonium chloride.
• Additional cationic surfactants are disclosed in U.S. Pat. No.
• the total surfactants may be present in the sunscreen/bodywash at about 0.1 to about 20%, or about 0.1 to about 10%, or about 0.1 to about 5%, or about 0.5 to about 5%, or about 1 to about 10%, or about 1 to about 5%, or about 0.1 to about 2%, or about 1 to about 2%.
• a sunscreen/bodywash composition of the invention contains a surfactant, e.g., a cationic surfactant, at about 1%.
• soapless cleansers may be used in addition to, or instead of, soaps/surfactants.
• OilatumTM AD registered trademark, Stiefel Laboratories
• Aquanil registered trademark, Person & Covey, Inc.
• Cetaphil trademark, Galderma Laboratories, Inc.
• SpectroDermTM registered trademark, Draxis Pharmaceutical Inc.
• the sunscreen additives of the invention may also be combined with conventional bodywash compositions, as well as with shampoos for hair, and post- wash skincare compositions. Proportions for addition and mixing are given above as well as in more detail hereafter.
• An exemplary bodywash that may be used with additives of the invention is exemplified by SUAVE Body Wash. Ingredients of a typical
• SUAVE bodywash include: Water, Ammonium Lauryl Sulfate, Ammonium Laureth Sulfate, Cocamidopropyl Betaine, Fragrance, Glycerin, Hydrolyzed Milk Protein & Honey Extract, PEG-10 Sunflower Glycerides, Cocamide MEA, Guar Hydroxypropylrimonium Chloride, Acrylates Copolymer, PEG-5 Cocamide, Helianthus Annuus (Sunflower) Seed Oil or Glycine Soja (Soybean) Oil, Tetrasoidum EDTA, Propylene Glycol, Ammonium Chloride, Sodium Hydroxide, Methylchloroisothiazolinone, Methylisothiazolinone, Titanium Dioxide (CI 77891)
• compositions of the invention may be prepared by any suitable method.
• a “Phase I” which is a "water phase” is prepared by mixing the more water-soluble components of the composition.
• Polyquaternium-4, a film former (e.g., in MOISTUREGUARD), and encapsulated sunscreen (e.g., in UV PEARLS) may be mixed until uniform.
• a “Phase II,” which is an “oil phase,” is prepared by mixing the more hydrophobic components of the composition.
• Avobenzone e.g., PARSOL 1789
• Octocrylene with heating, until dissolved.
• Phase III Phase III may be further combined with a bodywash composition (e.g., SUAVE bodywash) and mixed until uniform.
• a further sunscreen such as titanium dioxide, may be added to the Phase III/bodywash composition and mixed until uniform.
• the sunscreen may be added before addition to the bodywash or soap to provide an additive ready for formulation with a bodywash or soap.
• Additives e.g., sunscreen additives of the invention are generally designed to be used in combination with a bodywash.
• the compositions of the invention are typically designed to be applied while washing. This characteristic facilitates ease of use and may have the added benefit of being cumulative.
• Compositions of the present invention are readily applied during washing in a suitable or effective amount and may be generally applied all over the body. Shampoos may be applied specifically to the hair.
• a selected amount of a composition may be applied directly to the skin or may be used through intermediate application to a washcloth, pad, sponge, or other applicator.
• methods of the invention include methods for protection of skin from sunlight, comprising applying a bodywash comprising a sunscreen to the skin, wherein after application of the bodywash to skin and rinsing, the skin is protected from sunlight with an average SPF of at least about 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, or more than 20.
• the skin is protected from sunlight with an average SPF of at least about 2. In some preferred embodiments, the skin is protected from sunlight with an average SPF of at least about 5. In some preferred embodiments, the skin is protected from sunlight with an average SPF of at least about
• the skin is protected from sunlight with an average SPF of at least about 15.
• the bodywash is applied more than once; in these cases, the SPF may be cumulative and can increase with the second wash to, e.g., an average ofmore than 2, 5, 6, 7, 8, 9, 10, 11, 12, 13, 15, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 30, 35, 40, 45, or more than about 45.
• the bodywash is applied once per day.
• the bodywash is applied more than once per day, for example, 2, 3, 4, or more than 4 times per day.
• the bodywash is applied about every other day.
• the body wash is applied about 10, 8, 7, 6, 5, 4, 3, 2 or 1 time per week.
• the active additive e.g., sunscreen
• the active additive often does not penetrate beyond a certain level in the skin, typically due to encapsulation.
• the active additive e.g., sunscreen
• the active additive does not penetrate more than about 10, 20, 25, 30, 35, 40, 45, or 50 microns into the skin with one washing with a bodywash containing the additive.
• the active additive e.g., sunscreen
• the sunscreen or other additive is designed to penetrate into the skin, thus, in these embodiments, the active additive, e.g., sunscreen, penetrates to at least about 10, 20, 25, 30, 35, 40, 45, or 50 microns into the skin with one washing with a bodywash containing the additive. In some embodiments, the active additive, e.g., sunscreen, penetrates more than about 10, 20, 25, 30, 35, 40, 45, 50, 60, 70, 80, 90, 100, 120, or 150 microns into the skin. In some embodiments this penetration occurs with a single washing and rinsing.
• any additive described herein e.g., sunscreen additives, generally as a component of a bodywash, may be used in the methods of the invention.
• the additive is a non-sunscreen additive and is encapsulated, e.g., in the form of sol-gel microcapsules.
• the additive may be used in combination with a non- bodywash vehicle, such as a skin lotion, gel, cream, and the like, as are well-known in the art.
• compositions of the present invention in a manner similar to ordinary soap (i.e., wetting, application of composition, rinsing), it is also anticipated that the composition may be used by application without wetting followed by removal through, for example, wiping. This is the case for soapless cleansers.
• the invention also encompasses methods of doing business in the field of topical delivery of cosmeceuticals and the transdermal delivery of pharmaceuticals using lathering products, including everyday soap and shampoo, as the delivery agents.
• Business methods of the invention encompass a method of doing business comprising marketing an additive for use with an existing bodywash, wherein the additive, when combined with the bodywash, causes an additional effect to the normal effect of the soap or the bodywash.
• the business methods include methods involving any of the additives described herein, including sunscreens, insect repellants, anti-acne medications, anti-wrinkling agents, deodorants, and all others described herein
• the methods include marketing a sunscreen benefit agent (additive) for use with a bodywash, e.g., bar and liquid soaps, and shampoos, to add the benefit of a sunscreen.
• the sunscreen may be any one of the sunscreen additives described herein.
• the sunscreen or other benefit agent may be licensed as an additive, in both liquid and bar soap forms, to personal care product makers of all sizes, to enhance and differentiate their branded product offerings.
• the license may be exclusive or, preferably, non-exclusive. If exclusive, it may be exclusive in a defined geographical territory, for a defined time period (often with an option to renew or right of first refusal at the expiration of the time period), for a defined type of skin care product, or any combination of these.
• the methods also include supplying one or more customers with an option to license or buy the additive, generally for a defined period of time.
• an option may be exclusive or non-exclusive.
• the sunscreen or other benefit agent may be manufactured and supplied to personal care product makers.
• a further alternative is to manufacture a stand-alone brand of soap/bodywash that includes the additive.
• a further component of the business methods of the invention typically includes receiving payment for supplying the additive, license, or the like, to the customer.
• "payment" may be any form of consideration, included monetary consideration.
• license payments take the form of an up-front payment, royalties, license maintenance fees or some combination thereof.
• equity in the company receiving the additive or the license to the additive are also included in payment options.
• any other form of consideration may also constitute payment in the business methods of the invention.
• the business methods of the invention may further include manufacturing the additive and/or the additive/bodywash. In some embodiments, different entities perform different aspects; for example, a first entity may manufacture the additive and a second entity may market and/or distribute it.
• a single entity performs both manufacturing and marketing.
• Business methods of the invention further include a method including the steps of: a) designing an additive for use in a personal care product; b) testing the additive for safety and effectiveness in humans; c) arranging for distribution and marketing of the additive.
• steps a) and c) are performed by a first entity, typically a business entity, and step b) is performed by a second entity, such as a business entity or an academic entity.
• step b) is performed as a joint venture between the two entities.
• a sunscreen additive for addition to a bodywash was prepared as follows: To
• Phase III a sunscreen additive.
• the sunscreen additive of Phase III was added to 64.5 g of SUAVE Bodywash and stirred until uniform. Finally, 2.3 g of titanium dioxide were added with stirring.
• the final composition was a sunscreen/bodywash.
• test sample 50 cm 2 of testing site was wetted with 10ml of water delivered with a syringe.
• the test sample was applied as per FDA monograph C.F.R. 21 to the area.
• Lather was worked into the subject for 3 minutes to allow the product to absorb into the skin.
• the area was rinsed after 2 additional minutes with 20ml of water, then the area was patted dry and allowed 15 minutes before exposure to radiation as per FDA monograph.
• the skin was exposed to UV radiation and the MED was noted and compared to the MED for skin without treatment. Results are shown in the Table below.
• This Example demonstrates that the sunscreen/bodywash enhanced the sun protection as measured by this protocol, as compared to untreated skin, by an average SPF of over 18.
• a sunscreen/bodywash is prepared by mixing the following ingredients: 0.1 to 7.5 parts by weight of octylmethoxy cinnamate, 0.1 to 6 parts by weight of octyl salicylate, 0.1 to 5 parts by weight of oxybenzone, 1 to 10 parts by weight of cationic surfactant, 0.01 to 1 part by weight of a quaternized compound and 0.01 to 1 part by weight of a preservative.
• a sunscreen/bodywash is prepared by mixing the following ingredients:
• Titanium Dioxide .01-20%
• Generic type soap bases for shampoos, body washes, facial cleansers or specialty washes can consist of base such as;
• This base shows an example of adding a polyquat to enhance the benefits of SPF added at the mixtures mentioned in the art. Ranges of polyquats in the base can vary from .001%- 10% to the base to enhance the system. The addition of additional film formers can also enhance the additive, an example being the Acrylate Copolymer, Dermacryl AQFtm . Acrylates especially carboxylated added at a .001%- 20% level, being hydrophobic offer substantial water resistance allowing the final product to be water resistant to a greater degree. These components can all be added in the soap base formulation to create a synergistic effect with the additive.
• EXAMPLE 6 50 subjects were tested with the sunscreen/bodywash of Example 1 of the invention for skin irritation. Subjects bathed or washed as usual, then 0.2ml or 0.2g of test material was dispensed on a designated area of the subject's back and allowed to air dry. The procedure was completed nine consecutive times (Monday, Wednesday, and Friday for three consecutive weeks). Areas of application were monitored for erythema and edema. Subjects were then given a 10-14 day rest followed by reapplication at another test site, equivalent to any one of the original nine exposures. [00159] No adverse reactions of any kind were noted during the course of this study.
• a water resistance test was performed using the sunscreen/bodywash of Example 1. Per the FDA Monograph for Water Resistant and Very Water Resistant claims, the product sample was applied to dry skin of subjects, then submersed in a whirlpool bath tor 40 or 80 minutes prior to measurement. The average SPF after the 40 minute immersion was 12.45 and after the 80 minute immersion was 10.35.

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