WO2009067095A1 - Compositions cosmétiques topiques d'éclaircissement de la peau et leurs procédés d'utilisation - Google Patents
Compositions cosmétiques topiques d'éclaircissement de la peau et leurs procédés d'utilisation Download PDFInfo
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- WO2009067095A1 WO2009067095A1 PCT/US2007/024109 US2007024109W WO2009067095A1 WO 2009067095 A1 WO2009067095 A1 WO 2009067095A1 US 2007024109 W US2007024109 W US 2007024109W WO 2009067095 A1 WO2009067095 A1 WO 2009067095A1
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- topical cosmetic
- cosmetic composition
- skin
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- 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
- A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
- A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
- A61K8/9783—Angiosperms [Magnoliophyta]
- A61K8/9789—Magnoliopsida [dicotyledons]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/28—Asteraceae or Compositae (Aster or Sunflower family), e.g. chamomile, feverfew, yarrow or echinacea
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/47—Euphorbiaceae (Spurge family), e.g. Ricinus (castorbean)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/48—Fabaceae or Leguminosae (Pea or Legume family); Caesalpiniaceae; Mimosaceae; Papilionaceae
- A61K36/484—Glycyrrhiza (licorice)
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/16—Emollients or protectives, e.g. against radiation
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
Definitions
- compositions comprising plant extracts. These compositions are used for topical cosmetic applications, particularly to treat undesired skin pigmentation.
- Melanocytes which are found in the lowest layer of the epidermis, the stratum basale, next to the basal cells, are pigment-forming cells which occur either singly or in clusters, depending on the skin type. Melanocytes contain melanosomes that form melanin at higher rates when stimulated by UV radiation. The melanin is transported into the keratinocytes and leads to a more or less pronounced tan or brown skin color.
- Melanin is the end product of an oxidative process in which tyrosine is converted with the aid of the enzyme tyrosinase via 3,4-dihydroxyphenylalanine (dopa), dopaquinone, leucodopachrome, dopachrome, 5,6-dihydroxyindole and indole-5,6- quinone to give, finally, melanin.
- Topical cosmetic skin lightening compositions that are safe and effective are particularly desirable for treating undesirable skin pigmentation, including for example, regional hyperpigmentation caused by melanocyte hyperactivity such as idiopathic melasma occurring during pregnancy (mask of pregnancy or chloasma) or secondary to estrogen-progesterone contraception; local hyperpigmentation caused by benign melanocyte hyperactivity and proliferation such as lentigo senilis, known as liver spots; accidental hyperpigmentation such as post-lesional photosensitization and scarring; skin ageing (for example lentigines seniles); and certain forms of leukoderma such as vitiligo where, if the injured skin cannot be repigmented, the residual zones of normal skin are lightened or depigmented to impart a homogeneous color to the entire skin.
- melanocyte hyperactivity such as idiopathic melasma occurring during pregnancy (mask of pregnancy or chloasma) or secondary to estrogen-progesterone
- U.S. Published Patent Application No. 2006/0018867 describes a cosmetic composition having improved preservative and/or antibacterial effects comprising one or a combination of two or more of polyorganosiloxane-containing epsilon-polylysine compounds obtained by reacting epsilon-polylysine with polyorganosiloxane or a physiologically acceptable salt thereof, and polyhydric alcohol, where the composition can be a skin whitening composition.
- compositions for skin lightening that comprise bis-pantoyl-cystamine.
- U.S. Published Patent Application No. 2004/0028642 describes a cosmetic composition comprising an extract of Embilica officinalis and methods of using same.
- U.S. Published Patent Application No. 2005/0271608 describes skin whitening compositions based on hydroxyaryl alkyl ketones and their isosteric derivatives.
- the present subject matter relates generally to topical cosmetic compositions useful for treating various skin disorders or conditions associated with undesired skin pigmentation. Further, the present subject matter relates to topical cosmetic compositions useful for cosmetic lightening of skin areas whose pigmentation is adequate for the individual skin type. [0013] In an embodiment, the present subject matter relates to a topical cosmetic composition, comprising or consisting of a Phyllanthus extract; a BeIHs extract; and a licorice extract.
- the present subject matter relates to a topical cosmetic composition, comprising or consisting of a Phyllanthus embilica extract; a BeIHs perennis extract; and a licorice extract.
- the present subject matter relates to a topical cosmetic composition, comprising or consisting of a skin-lightening active component comprising or consisting of a Phyllanthus extract, a BeIHs extract, and a licorice extract; at least one sunscreen; and a cosmetically acceptable carrier.
- the present subject matter relates to a topical cosmetic composition, comprising or consisting of a skin-lightening active component comprising or consisting of a Phyllanthus embilica extract, a BeIHs perennis extract, and a licorice extract; at least one sunscreen; and a cosmetically acceptable carrier.
- a topical cosmetic composition comprising or consisting of a skin-lightening active component comprising or consisting of a Phyllanthus extract, a BeIHs extract, and a licorice extract; and a non- skin lightening component comprising at least one sunscreen.
- the present subject matter relates to a topical cosmetic composition, comprising or consisting of a skin-lightening active component comprising or consisting of a Phyllanthus embilica extract, a BeIHs perennis extract, and a licorice extract; and a non-skin lightening component comprising at least one sunscreen.
- the present subject matter relates to a method of lightening skin pigmentation in a subject, comprising topically administering to skin of a subject in need thereof, a therapeutically effective amount of a topical cosmetic composition in accordance with the presently described subject matter.
- the present subject matter relates to a method of treating a skin disorder or condition in a subject, comprising topically administering to skin of a subject in need thereof a therapeutically effective amount of a topical cosmetic composition in accordance with the presently described subject matter.
- Figure 1 illustrates progressive lightening over time that becomes statistically significant after 21 days for Site B treated with 2 % hydroquinone.
- Figure 2 illustrates progressive lightening over time that becomes statistically significant after 14 days for Site E treated with the present topical cosmetic composition.
- Figure 3 illustrates progressive lightening (natural degradation of the synthesized melanin), without any significance over the experimental times for the control location (Site F) which was not treated.
- Figure 4 illustrates the comparison between the averages of the colorimetric values in treatments 1 (Site B) and 2 (Site E) and the control (Site F) over the evaluation times DETAILED DESCRIPTION Definitions
- administering refers to any method which, in sound medical or cosmetic practice, delivers the composition to a subject in such a manner as to provide a positive effect on a dermatological disorder, condition, or appearance.
- the compositions can be administered such that they cover the entire area to be treated.
- Direct administration refers to any method which, in sound medical or cosmetic practice, delivers the composition to a subject without the use of another composition, delivery agent, or device.
- Indirect administration refers to any method which, in sound medical or cosmetic practice, delivers the composition to a subject with the use of at least another composition, delivery agent, or device.
- aqueous solvent refers to a solvent such as water or containing water.
- Other dissolved components may be present in small amounts, such as, for example, salts, buffers, and other components understood by one of ordinary skill in the art to be optionally present in an aqueous solution.
- Anhydrous formulation refers to any formulation of the present topical cosmetic composition that does not contain water.
- Cosmetically acceptable refers to a non-toxic, inert, and/or physiologically compatible composition.
- an "effective amount” or a "therapeutically effective amount” of an active agent or ingredient refer to an amount of the active agent sufficient enough to have a positive effect on the area of application. Accordingly, these amounts are sufficient to modify the skin disorder, condition, or appearance to be treated but low enough to avoid serious side effects, within the scope of sound medical or dermatological advice.
- a therapeutically effective amount of the active agent will cause a substantial relief of symptoms when applied repeatedly over time. Effective amounts of the active agent will vary with the particular condition or conditions being treated, the severity of the condition, the duration of the treatment, the specific components of the composition being used, and like factors.
- effecting refers to the process of producing an effect on biological activity, function, health, or condition of an organism in which such activity is maintained, enhanced, diminished, or treated in a manner consistent with the general health and well-being of the organism.
- enhancing the biological activity, function, health, or condition of an organism refers to the process of augmenting, fortifying, strengthening, or improving the biological activity, function, health, or condition.
- epithelium or “epithelial” refers to the layer of cells forming the epidermis of the skin and the surface layer of mucous and serous membranes. Epithelial cells have the general functions of protection, absorption, and secretion. Epithelial cells are often in close proximity to blood vessels, although generally lacking in a direct blood supply.
- extract refers to one or more components isolated from a plant source in a fluid or powder form.
- the plant source can comprise or consist of the entire plant or one or more parts of the plant, for example, the plant fruit, flower, root, leaves, stems, and/or bark.
- a fluid or liquid extract can be dried, for example, spray dried or desiccated, to form a powder.
- the extract can be a mixture of one or more components from a plant in a fluid and/or powder form.
- non-skin lightening any compound, substance or composition; or agent; or component comprising or consisting of one or more agents, substances, compounds and compositions, which upon topical application to skin does not depigment or lighten the skin.
- Such agents can include, for example, one or more active agents, for example, a sunscreen, an anti-acne agent, an anti-microbial agent, an anti-wrinkle agent, an anti-atrophy agent, an anti-inflammatory agent, and an optical brightener; and/or one or more cosmetically acceptable excipients, for example, a thickener, a chelating agent, a moisturizer, an emollient, a humectant, a gelling agent, a pH adjuster, a surfactant, a stabilizer, a vitamin, a penetration enhancer, a perfume, a coloring agent, and a solvent; and/or combinations thereof; as described herein.
- active agents for example, a sunscreen, an anti-acne agent, an anti-microbial agent, an anti-wrinkle agent, an anti-atrophy agent, an anti-inflammatory agent, and an optical brightener
- cosmetically acceptable excipients for example, a thickener, a chelating agent, a
- a “penetration enhancer” refers to a compound, substance or composition that reversibly reduces the barrier resistance of the horny layer of the skin, allowing an active agent to reach the living tissues at a greater rate.
- a “pH adjuster” or “pH modifier” refers to a specific pH adjusting agent added to a composition to convey a certain designated pH to the composition.
- salts, esters, or solvates refers to free bases, salts, esters, or solvates of subject compound(s) which possesses the same pharmacological activity as the subject compound(s) and which are neither biologically nor otherwise undesirable.
- a salt, ester, or solvate can be formed with, for example, organic or inorganic acids.
- Non-limiting examples of suitable acids include acetic acid, acetylsalicylic acid, adipic acid, alginic acid, ascorbic acid, aspartic acid, benzoic acid, benzenesulfonic acid, bisulfic acid, boric acid, butyric acid, camphoric acid, camphorsulfonic acid, carbonic acid, citric acid, cyclopentanepropionic acid, digluconic acid, dodecylsulfic acid, ethanesulfonic acid, formic acid, fumaric acid, glyceric acid, glycerophosphoric acid, glycine, glucoheptanoic acid, gluconic acid, glutamic acid, glutaric acid, glycolic acid, hemisulfic acid, heptanoic acid, hexanoic acid, hippuric acid, hydrobromic acid, hydrochloric acid, hydroiodic acid, hydroxyethanesulfonic acid, lactic acid, maleic
- Non-limiting examples of base salts, esters, or solvates include ammonium salts; alkali metal salts, such as sodium and potassium salts; alkaline earth metal salts, such as calcium and magnesium salts; salts with organic bases, such as dicyclohexylamine salts; methyl-D-glucamine; and salts with amino acids, such as arginine, lysine, and so forth.
- the basic nitrogen- containing groups can be quatemized with such agents as lower alkyl halides, such as methyl, ethyl, propyl, and butyl chlorides, bromides, and iodides; dialkyl sulfates, such as dimethyl, diethyl, dibutyl, and diamyl sulfates; long chain halides, such as decyl, lauryl, myristyl, and stearyl chlorides, bromides, and iodides; asthma halides, such as benzyl and phenethyl bromides; and others. Water or oil-soluble or dispersible products are thereby obtained.
- lower alkyl halides such as methyl, ethyl, propyl, and butyl chlorides, bromides, and iodides
- dialkyl sulfates such as dimethyl, diethyl, dibutyl, and diamyl sulfates
- serum refers to a hydrophilic liquid formulation.
- a serum may optionally be free from one or more of an emollient, a wax and a silicone.
- skin lightening agent refers to any compound, substance, or composition which upon topical application to skin lightens or depigments the skin. Such skin lightening agents can include, but are not limited to, pigmentation inhibitors, tyrosinase inhibitors, and melanocyte melanogenesis inhibitors.
- subject or “individual” or “animal” or “patient” or
- mammal refers to any subject, particularly a mammalian subject, for whom diagnosis, prognosis, or therapy is desired, for example, a human.
- “synergistic skin lightening system” or “synergistic skin lightening component” refers to a skin lightening active component comprising or consisting of a Phyllanthus embilica extract, a BeIHs perennis extract, and a licorice extract, that exhibits synergistic skin lightening efficacy as compared to the skin lightening efficacy of each individual skin lightening active agent.
- the combination of these ingredients provides a greater than additive skin lightening effect.
- a “treatment” or “treating” of a skin disease, disorder, or condition encompasses alleviation of at least one symptom thereof, a reduction in the severity thereof, or the delay, prevention, or inhibition of the progression thereof. Treatment need not mean that the disease, disorder, or condition is totally cured.
- a useful composition herein needs only to reduce the severity of a skin disease, disorder, or condition, reduce the severity of symptoms associated therewith, provide improvement to a patient's quality of life, or delay, prevent, or inhibit the onset of a skin disease, disorder, or condition.
- the present subject matter relates to a topical cosmetic composition, comprising or consisting of a Phyllanthus extract; a BeIHs extract; and a licorice extract.
- a topical cosmetic composition comprising or consisting of a Phyllanthus extract; a BeIHs extract; and a licorice extract.
- the present topical cosmetic compositions can comprise or consist of a Phyllanthus extract, i.e., Phyllanthus embilica extract; a BeIHs extract, i.e., a BeIHs perennis extract; and a licorice extract.
- “Phyllanthus extract” means an extract obtained from the fruit of a member of the Phyllanthus genus, including for example, of Phyllanthus embilica, Phyllanthus niruri L, Phyllanthus elegans Wall, Phyllanthus iniruri, Phyllanthus reticulatus, Phyllanthus urinaria L, Phyllanthus reticulatus Poir, Phyllanthus conami Sw, Phyllanthus lathyroides H. B. K., Phyllanthus casticum Soy-Will, and Phyllanthus madagascariensis. Phyllanthus extract is a safe and effective natural antioxidant.
- “Phyllanthus embilica extract” means a standardized extract of
- Phyllanthus embilica including for example, EMBLICA® (Merck KGaA, Darmstadt, Germany and EM industries, Inc., USA, an affiliate of Merck KGaA).
- Phyllanth ⁇ s embilica is also commonly known as "Emblica officinalis Gaertn" and is a member of the family “Euphorbiaceae.”
- Phyllanthus embilica is a very rich source of vitamin C, having an ascorbic acid content in the range from 1000 to 1800 mg per 100 grams of fruit.
- Phyllanthus embilica extract is a safe and effective natural antioxidant that has no pro- oxidation activity and can exhibit dual functionality, i.e., chelation and antioxidant.
- Phyllanthus embilica extract can exhibit a cascading effect that provides long-lasting and stable antioxidant activity.
- Phyllanthus embilica extract can be produced by extracting premium quality fruits using a water-based process as described in U.S. Patent No. 6,124,268, incorporated herein by reference in its entirety.
- Phyllanthus embilica extract typically contains low-molecular weight tannins, namely Emblicanin A and Emblicanin B, along with Pedunculagin and Punigluconin, Rutin and Gallo-ellagitannoids.
- BeIHs extract means an extract obtained from a member of the BeIHs genus, including for example, the extract obtained from the flowers of a member of the BeIHs genus, for example, from BeIHs perennis flowers and/or from BeIHs rotundifolia L. flowers.
- the BeIHs extract can comprise or consist of one or more bioactive molecules including saponins (triterpene glycosides), polyphenols (phenolic acid), flavonoid glycosides, polysaccharides and inulin.
- BeIHs perennis extract means the extract obtained from BeIHs perennis flowers that can comprise or consist of one or more bioactive molecules including saponins (triterpene glycosides), polyphenols (phenolic acid), flavonoid glycosides, polysaccharides and inulin.
- Suitable BeIHs perennis extracts can include BELIDES® available from CLR Chemisches Laboratorium, Berlin, Germany. BeIHs perennis is also commonly known as BeIHs alpina Hegetschw., BeIHs hortensis Mill., BeIHs hybrida Ten., BeIHs integrifolia DC, and BeIHs scaposa Gilib.
- “Licorice extract” means an extract obtained from a member of the
- Glycyrrhiza genus for example obtained from the root of a member of the Glycyrrhiza genus.
- the genus "Glycyrrhiza” is a member of the family "Fabaceae.”
- Suitable Glycyrrhiza extracts can include the oil soluble licorice extract available from Bioland, Korea.
- Other suitable Glycyrrhiza extracts can be obtained from one or more of the following members of the Glycyrrhiza genus including Glycyrrhiza echinata L. (Chinese licorice), Glycyrrhiza glabra L.
- the present topical cosmetic composition can comprise or consist of a skin lightening active component that can comprise or consist of a Phyllanthus extract, a BeIHs extract, and a licorice extract.
- the present topical cosmetic composition can comprise or consist of a skin lightening active component that can comprise or consist of a Phyllanthus embilica extract, a BeIHs perennis extract, and a licorice extract.
- the present subject matter relates to a topical cosmetic composition wherein the total skin lightening active component is present in the topical cosmetic composition in an amount of from about 0.5% to about 43% by weight, from about 1 % to about 30% by weight, from about 1.5% to about 23% by weight, from about 1.5% to about 15% by weight, from about 3% to about 10% by weight, from about 6% to about 8% by weight, or about 7.05% by weight, based on the total weight of the composition.
- the present subject matter relates to a topical cosmetic composition wherein the Phyllanthus extract, for example, the Phyllanthus embilica extract, is present in the topical cosmetic composition in an amount of from about 0.1% to about 8% by weight, from about 0.25% to about 4% by weight, from about 0.5% to about 3% by weight, from about 0.5% to about 2% by weight, from about 1% to about 2% by weight, or about 2% by weight, based on the total weight of the composition.
- the Phyllanthus extract for example, the Phyllanthus embilica extract
- the present subject matter relates to a topical cosmetic composition wherein the BeIHs extract, for example, the BeIHs perennis extract, is present in the topical cosmetic composition in an amount of from about 0.5% to about 30% by weight, from about 1% to about 20% by weight, from about 2% to about 10% by weight, from about 3% to about 7% by weight, from about 4% to about 6% by weight, or about 5.0% by weight, based on the total weight of the composition.
- the BeIHs extract for example, the BeIHs perennis extract
- the present subject matter relates to a topical cosmetic composition wherein the licorice extract is present in the topical cosmetic composition in an amount of from about 0.005% to about 5% by weight, from about 0.01 % to about 2% by weight, from about 0.01% to about 1% by weight, from about
- the present subject matter relates to a topical cosmetic composition
- the Phyllanthus extract for example, the Phyllanth ⁇ s embilica extract
- the BeIHs extract for example, the BeIHs perennis extract
- the licorice extract is present in the topical cosmetic composition in an amount of from about 0.01 wt% to about 1 wt%.
- the present subject matter relates to a topical cosmetic composition, wherein the Phyllanthus embilica extract is present in the topical cosmetic composition in an amount of about 2 wt%; the BeIHs perennis extract is present in an amount of about 5 wt%; and the licorice extract is present in the topical cosmetic composition in an amount of about 0.05 wt%.
- the present subject matter relates to a topical cosmetic composition, comprising or consisting of a skin-lightening active component comprising or consisting of a Phyllanthus extract, for example, a Phyllanthus embilica extract; a
- BeIHs extract for example, a BeIHs perennis extract; and a licorice extract; at least one sunscreen; and a cosmetically acceptable carrier.
- the cosmetically acceptable carrier can comprise or consist of one or more cosmetically acceptable excipients.
- the present subject matter relates to a topical cosmetic composition, comprising or consisting of a skin-lightening active component comprising or consisting of a Phyllanthus extract, for example, a Phyllanthus embilica extract; a BeIHs extract, for example, a BeIHs perennis extract; and a licorice extract; and a non-skin lightening component.
- the non-skin lightening component can comprise or consist of one or more of an active agent, for example, a sunscreen; a cosmetically acceptable carrier; and/or a cosmetically acceptable excipient, as described herein.
- the present subject matter relates to a topical cosmetic composition in accordance with the subject matter described herein that can comprise one or more non-skin lightening active agents.
- the topical cosmetic composition and/or the cosmetically acceptable carrier and/or one or more cosmetically acceptable excipients can be free from any skin lightening agents other than a Phyllanthus extract, for example a Phyllanthus embilica extract; a BeIHs extract, for example, a BeIHs perennis extract; and licorice extract.
- a Phyllanthus extract for example a Phyllanthus embilica extract
- a BeIHs extract for example, a BeIHs perennis extract
- licorice extract licorice extract
- the topical cosmetic composition and/or the cosmetically acceptable carrier and/or one or more cosmetically acceptable excipients can be free from any plant derived skin lightening agents other than a Phyllanthus extract, for example a Phyllanthus embilica extract; a BeIHs extract, for example, a BeIHs perennis extract; and licorice extract.
- the topical cosmetic composition and/or the cosmetically acceptable carrier and/or one or more cosmetically acceptable excipients can be free from any non-plant derived skin lightening agents.
- the present subject matter relates to a topical cosmetic composition, wherein the composition and/or a skin lightening active component and/or a non-skin lightening component, does not comprise hydroquinone or a derivative thereof, and/or does not comprise a polyorganosiloxane-containing epsilon-polylysine compound, and/or does not comprise a flavan.
- the present subject matter relates to a topical cosmetic composition that can comprise or consist of a synergistic skin lightening active component comprising or consisting of a Phyllanthus extract, for example a Phyllanthus embilica extract; a BeIHs extract, for example, a BeIHs perennis extract; and licorice extract, wherein the synergistic skin lightening active component exhibits synergistic skin lightening efficacy as compared to the skin lightening efficacy of each individual skin lightening active agent.
- a synergistic skin lightening active component comprising or consisting of a Phyllanthus extract, for example a Phyllanthus embilica extract
- BeIHs extract for example, a BeIHs perennis extract
- licorice extract wherein the synergistic skin lightening active component exhibits synergistic skin lightening efficacy as compared to the skin lightening efficacy of each individual skin lightening active
- the present subject matter relates to a synergistic skin lightening component for use in a topical cosmetic composition
- a synergistic skin lightening component for use in a topical cosmetic composition
- a Phyllanthus extract for example a Phyllanthus embilica extract
- a Bellis extract for example, a Bellis perennis extract
- licorice extract for use in a topical cosmetic composition
- the present subject matter relates to a synergistic skin lightening component for use in a topical cosmetic composition
- a synergistic skin lightening component for use in a topical cosmetic composition
- a Phyllanthus extract for example a Phyllanthus embilica extract
- a Bellis extract for example, a Bellis perennis extract
- licorice extract wherein the synergistic skin lightening component demonstrates enhanced skin lightening efficacy.
- the synergistic skin lightening component can be free from hydroquinone.
- the topical cosmetic composition in accordance with the presently described subject matter can comprise or consist of a skin lightening active component that exhibits synergistic skin lightening efficacy.
- the topical cosmetic composition in accordance with the presently described subject matter can comprise or consist of a skin lightening active component that exhibits synergistic skin lightening efficacy, wherein the topical cosmetic composition is free from hydroquinone.
- the topical cosmetic composition or the synergistic skin lightening system in accordance with the presently described subject matter, can comprise or consist of a skin lightening active component that exhibits synergistic skin lightening efficacy, wherein the topical cosmetic composition is free from hydroquinone and/or a flavan and/or a polyorganosiloxane-containing epsilon-polylysine compound.
- Cosmetically acceptable carrier
- any non-toxic, inert, and effective topical cosmetically acceptable carrier may be used to formulate the compositions described herein.
- Well-known carriers used to formulate other topical therapeutic compositions for administration to humans are useful in these compositions. Examples of these components that are well known to those of skill in the art are described in The Merck Index, Thirteenth Edition, Budavari et al., Eds., Merck & Co., Inc., Rahway, N.J. (2001 ); the CTFA (Cosmetic, Toiletry, and Fragrance Association) International Cosmetic Ingredient Dictionary and Handbook, Tenth Edition (2004); and the "Inactive Ingredient Guide", U.S.
- the present subject matter relates to a topical cosmetic composition that can comprise at least one sunscreen.
- the at least one sunscreen can be present in an amount of from about 0.5% to about 30% by weight based on the total weight of the topical cosmetic composition, from about 1% by weight to about 20% by weight, or from about 1 % by weight to about 10% by weight based on the total weight of the composition.
- Suitable sunscreens can include broad-spectrum sunscreens that protect against both UVA and UVB radiation, or sunscreen agents that protect against UVA or
- sunscreens include sunscreen agents that can comprise or consist of one or more of 2-ethylhexyl p-methoxycinnamate, 2- ethylhexyl N,N-dimethyl-p-aminobenzoate, p-aminobenzoic acid, 2- phenylbenzimidazole-5-sulfonic acid, octocrylene, oxybenzone, homomenthyl salicylate, octyl salicylate, 4,4'-methoxy-t-butyldibenzoylmethane, 4-isopropy dibenzoylmethane, 3- benzylidene camphor, 3-(4-methylbenzylidene) camphor, titanium dioxide, zinc oxide, silica, iron oxide, 4-N,N-(2-ethylhexyl)methylaminobenzoic acid ester of 2,4- dihydroxybenzophenone, 4-N,N-(2-ethyl
- the present topical cosmetic compositions can comprise a sunscreen comprising or consisting of one or more of methylene bis- benzotriazolyl tetramethylphenol, diethylamino hydroxybenzoyl hexyl benzoate, coated zinc oxide, ethylhexyl methoxycinnamate, isoamyl methoxycinnamate, homosalate ethyl hexyl salicilate, octocrylene, polysilicone-15, butyl methoxydibenzoylmethane, menthyl anthranilate, and ethylhexyl dimethyl PABA.
- a sunscreen comprising or consisting of one or more of methylene bis- benzotriazolyl tetramethylphenol, diethylamino hydroxybenzoyl hexyl benzoate, coated zinc oxide, ethylhexyl methoxycinnamate, isoamyl methoxycinnam
- the present topical cosmetic compositions can comprise a sunscreen comprising one or more of methylene bis-benzotriazolyl tetramethylphenol (TINOSORB M available from CIBA), diethylamino hydroxybenzoyl hexyl benzoate, and coated zinc oxide, in an amount of from about 1% to about 20% by weight, from about 2% to about 10% by weight, or of about 5% by weight, based on the total weight of the composition.
- a sunscreen comprising one or more of methylene bis-benzotriazolyl tetramethylphenol (TINOSORB M available from CIBA), diethylamino hydroxybenzoyl hexyl benzoate, and coated zinc oxide, in an amount of from about 1% to about 20% by weight, from about 2% to about 10% by weight, or of about 5% by weight, based on the total weight of the composition.
- the present topical cosmetic compositions can comprise a sunscreen comprising methylene bis-benzotriazolyl tetramethylphenol in an amount of from about 1 % to about 20% by weight, from about 2% to about 10% by weight, or of about 5% by weight, based on the total weight of the composition.
- the present topical cosmetic compositions can comprise a sunscreen comprising or consisting of one or more of ethylhexyl methoxycinnamate (available from BASF), isoamyl methoxycinnamate, homosalate ethyl hexyl salicilate, octocrylene, polysilicone-15, butyl methoxydibenzoylmethane, menthyl anthranilate, and ethylhexyl dimethyl PABA, in an amount of from about 1% to about 10%, from about 5% to about 9%, or of about 7.5% by weight, based on the total weight of the composition.
- ethylhexyl methoxycinnamate available from BASF
- isoamyl methoxycinnamate homosalate ethyl hexyl salicilate
- octocrylene polysilicone-15
- butyl methoxydibenzoylmethane men
- the present topical cosmetic compositions can comprise one or more sunscreens in an amount of from about 0.5% by weight to about 30% by weight, from about 1% by weight to about 20% by weight, or from about 1% by weight to about 10% by weight based on the total weight of the composition.
- the at least one sunscreen can comprise or consist of a first sunscreen selected from the group consisting of methylene bis-benzotriazolyl tetramethylphenol, diethylamino hydroxybenzoyl hexyl benzoate, and coated zinc oxide; and a second sunscreen selected from the group consisting of ethylhexyl methoxycinnamate, isoamyl methoxycinnamate, homosalate ethyl hexyl salicilate, octocrylene, polysilicone-15, butyl methoxydibenzoylmethane, menthyl anthranilate, and ethylhexyl dimethyl PABA.
- a first sunscreen selected from the group consisting of methylene bis-benzotriazolyl tetramethylphenol, diethylamino hydroxybenzoyl hexyl benzoate, and coated zinc oxide
- a second sunscreen selected from the group consisting of ethyl
- the first sunscreen can be present in an amount of from about 1 % to about 20% by weight, and the second sunscreen can be present in an amount of from about 1 % to about 10% by weight, based on the total weight of the topical cosmetic composition.
- the first sunscreen can comprise or consist of methylene bis-benzotriazolyl tetramethylphenol, and the second sunscreen can comprise or consist of ethylhexyl methoxycinnamate.
- the present subject matter relates to a topical cosmetic composition that has an SPF of greater than about 10, has an SPF of greater than about 15, an SPF of at least about 15, an SPF of about 15, an SPF of from about 10 to about 45, an SPF of from about 15 to about 45, or an SPF of from about 15 to about 25.
- Aqueous Solvent is aqueous Solvent that has an SPF of greater than about 10, has an SPF of greater than about 15, an SPF of at least about 15, an SPF of about 15, an SPF of from about 10 to about 45, an SPF of from about 15 to about 45, or an SPF of from about 15 to about 25.
- the present topical cosmetic compositions can additionally comprise an aqueous solvent.
- the present compositions comprise an aqueous solvent, for example, water, in an amount of from about 5% to about 95% by weight, from about 10% to about 90% by weight, from about 25% to about 80% by weight, from about 55% to about 75% by weight, from about 60% to about 70% by weight, or about
- the present subject matter relates to a topical cosmetic composition that can comprise water and at least one cosmetically acceptable excipient.
- Suitable cosmetically acceptable excipients include those commonly known to one of ordinary skill in the art as useful in topical compositions.
- the at least one cosmetically acceptable excipient can comprise or consist of one or more members selected from the group consisting of an antioxidant, a chelating agent, a pH adjuster, an emollient, a thickening agent, gelling agent, free radical scavenger, a preservative, an emulsifier, a humectant, a moisturizer, a suspending agent, a surfactant, a stabilizer, a vitamin, a penetration enhancer, a perfume or fragrance, a coloring agent, fluid alkyl alcohols, polysiloxanes, modified polysiloxanes, and combinations thereof.
- the topical cosmetic compositions may optionally further comprise one or more anti-oxidants.
- Suitable anti-oxidants that can optionally be included in these compositions can comprise or consist of one or more of ascorbic acid, ascorbyl esters of fatty acids, magnesium ascorbyl phosphate, sodium ascorbyl phosphate, ascorbyl sorbate, tocopherol, tocopherol sorbate, tocopherol acetate, butylated hydroxy benzoic acid, thioglycolates, persulfate salts, ⁇ -hydroxy ⁇ . ⁇ j. ⁇ -tetramethylchroman ⁇ -carboxylic acid, lipoic acid, gallic acid, propyl gallate, uric acid, sorbic acid, lipoic acid, amines, N,N-diethylhydroxylamine, N-acetyl-L-cysteine, amino-guanidine, sulfhydryl compounds, glutathione, dihydroxy fumaric acid, lycine pider
- the present topical cosmetic composition can include a suitable antioxidant that can comprise or consist of one or more of butylated hydroxytoluene, sodium metabissulfite, butylated hydroxyl anisol, ascorbic acid and derivatives thereof, a sulfite and derivatives thereof, an ester, and tocopherol acetate, for example, in an amount of from about 0.01 % to about 0.5% by weight, of from about 0.01% to about 0.2% by weight, from about 0.02% to about 0.1% by weight, from about 0.03% to about 0.07% by weight, or about 0.05% by weight, based on the total weight of the composition.
- a suitable antioxidant can comprise or consist of one or more of butylated hydroxytoluene, sodium metabissulfite, butylated hydroxyl anisol, ascorbic acid and derivatives thereof, a sulfite and derivatives thereof, an ester, and tocopherol acetate, for example, in an amount of from about 0.01 %
- the present topical cosmetic composition can comprise sodium metabissulfite, for example, in an amount of from about 0.1% to about 0.5% by weight, from about 0.2% to about 0.4% by weight, or about 0.3% by weight, based on the total weight of the composition.
- the present topical cosmetic composition can comprise butylated hydroxytoluene, for example, in an amount of from about 0.01% to about 0.2% by weight, from about 0.02% to about 0.1% by weight, from about 0.03% to about 0.07% by weight, or about 0.05% by weight, based on the total weight of the composition.
- the present topical cosmetic composition can comprise an antioxidant that can comprise or consist of butylated hydroxytoluene and sodium metabissulfite, for example, in a combined amount of from about 0.01 % to about 0.6% by weight, from about 0.2% to about 0.5% by weight, or about 0.35% by weight, based on the total weight of the composition.
- an antioxidant can comprise or consist of butylated hydroxytoluene and sodium metabissulfite, for example, in a combined amount of from about 0.01 % to about 0.6% by weight, from about 0.2% to about 0.5% by weight, or about 0.35% by weight, based on the total weight of the composition.
- the one or more antioxidants can be present in the topical cosmetic composition, for example, in an amount of from about 0.01% to about 0.6% by weight, from about 0.1% to about 0.5% by weight, or from about 0.2% to about 0.5% by weight, based on the total weight of the composition.
- the present topical cosmetic compositions may optionally further comprise one or more chelating agents.
- Suitable chelating agents that can optionally be included in these compositions can comprise or consist of one or more of citric acid, isopropyl (mono) citrate, stearyl citrate, lecithin citrate, gluconic acid, tartaric acid, oxalic acid, phosphoric acid, sodium tetrapyrophosphate, potassium monophosphate, sodium hexametaphosphate, calcium hexametaphosphate, sorbitol, glycine (aminoacetic acid), methyl glucamine, triethanolamine (trolamine), EDTA, DEG (dihydroxyethylglycine), DPTA (diethylene triamine pentaacetic acid), NTA (Nitrilotriacetic Acid), HEDTA (N- (hydroxyethyl)-ethylenetriaminetriacetic acid), aminocarboxylates, dimercaperol (BAL),
- the present topical cosmetic composition can include one or more chelating agents present in an amount of from about 0.05% to about 1% by weight, from about 0.1 % to about 0.5% by weight, or about 0.2% by weight, based on the total weight of the composition.
- the present topical cosmetic composition can include a chelating agent that can comprise or consist of one or more of disodium edetate, EDTA, disodium EDTA, trisodium EDTA, and tetrasodium EDTA, for example, in an amount of from about 0.2% to about 0.4% by weight, based on the total weight of the composition.
- a chelating agent that can comprise or consist of one or more of disodium edetate, EDTA, disodium EDTA, trisodium EDTA, and tetrasodium EDTA, for example, in an amount of from about 0.2% to about 0.4% by weight, based on the total weight of the composition.
- the present topical cosmetic compositions may optionally further comprise one or more pH adjusters.
- Suitable neutralizing pH adjusters that can optionally be included in these compositions can comprise or consist of one or more of inorganic hydroxides, inorganic oxides, inorganic salts of weak acids, derivatives thereof, and mixtures thereof.
- Suitable inorganic hydroxides useful in this regard can comprise or consist of one or more of ammonium hydroxide, alkali metal hydroxide, alkaline earth metal hydroxides, derivatives thereof, and mixtures thereof.
- Suitable inorganic hydroxides useful in this regard can comprise or consist of one or more of ammonium hydroxide, monovalent alkali metal hydroxides such as sodium hydroxide and potassium hydroxide, divalent alkali earth metal hydroxides such as calcium hydroxide and magnesium hydroxide, derivatives thereof, and mixtures thereof.
- Suitable inorganic oxides useful in this regard can comprise or consist of one or more of magnesium oxide, calcium oxide, derivatives thereof, and mixtures thereof.
- Suitable inorganic salts of weak acids useful in this regard can comprise or consist of one or more of ammonium phosphate (dibasic), alkali metal salts of weak acids such as sodium acetate, sodium borate, sodium metaborate, sodium carbonate, sodium bicarbonate, sodium phosphate (tribasic), sodium phosphate (dibasic), potassium carbonate, potassium bicarbonate, potassium citrate, potassium acetate, potassium phosphate (dibasic), potassium phosphate (tribasic), alkaline earth metal salts of weak acids such as magnesium phosphate and calcium phosphate, derivatives thereof, and mixtures thereof.
- ammonium phosphate dibasic
- alkali metal salts of weak acids such as sodium acetate, sodium borate, sodium metaborate, sodium carbonate, sodium bicarbonate, sodium phosphate (tribasic), sodium phosphate (dibasic), potassium carbonate, potassium bicarbonate, potassium citrate, potassium acetate, potassium phosphate (dibasic), potassium phosphate
- the present topical cosmetic composition can include a pH adjuster that can comprise or consist of one or more of triethanolamine, aminomethylpropanol, and sodium hydroxide.
- the pH adjuster can be present in the composition, for example, in an amount of from about 0.1% to about 1% by weight, from about 0.2% to about 0.9% by weight, or about 0.6% by weight, based on the total weight of the composition.
- the present topical cosmetic composition can comprise a pH in the range of from about 2.5 to about 8, or from about 3 to about 7.
- the present topical cosmetic compositions may further comprise an emollient.
- emollients useful in the present compositions include one or more of myristyl lactate, isopropyl palmitate, light liquid paraffin, cetearyl alcohol, lanolin, lanolin derivatives, mineral oil, petrolatum, cetyl esters wax, cholesterol, glycerol, glycerol monostearate, isopropyl myristate, a glycol, lecithin, and mixtures thereof.
- a suitable emollient can comprise or consist of one or more of glycerin; a glycol, for example, propylene glycol, butyleneglycol, and pentyleneglycol; cyclopentasiloxane dimethicone crosspolymer (DC9040 available from Dow Corning); cyclopentasiloxane PEG/PPG-18/18 dimethicone (DC5225C available from Dow Corning); and a silicon derivate.
- the emollient may be present in an amount of from about 1 % to about 20% by weight, from about 2% to about 10% by weight, from about 3% to about 8% by weight, or about 4% by weight. Thickening/Gelling Agents
- the present topical cosmetic composition may optionally further comprise one or more thickening agents.
- Suitable thickening agents that can optionally be included in these compositions can comprise or consist of, but are not limited to, one or more of a cellulosic polymer, such as gum arabic, gum tragacanth, locust bean gum, guar gum, xanthan gum, cellulose gum, methylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, and hydroxypropylmethylcellulose; sodium carbomer; carbomer; a polyacrylic polymer; an aqueous gelling agent, such as neutral, anionic, and cationic polymers; polymers, such as carboxy vinyl polymers, such as carboxypolymethylene; an acrylate copolymer; a polysorbate; a fatty alcohol, for example, cetyl alcohol and stearyl alcohol; glyceryl stearate; an alkyl derivate; and mixtures thereof.
- Suitable acrylate copolymers
- a suitable thickening agent can comprise or consist of one or more of a fatty alcohol, for example, cetyl alcohol and stearyl alcohol; glyceryl stearate; an alkyl derivate; and combinations thereof; for example, present in an amount of from about 0.25% to about 4% by weight, from about 0.5% to about 3% by weight, from about 1 % to about 2% by weight, or about 2% by weight, based on the total weight of the composition.
- a fatty alcohol for example, cetyl alcohol and stearyl alcohol
- glyceryl stearate for example, present in an amount of from about 0.25% to about 4% by weight, from about 0.5% to about 3% by weight, from about 1 % to about 2% by weight, or about 2% by weight, based on the total weight of the composition.
- a suitable thickening agent can comprise or consist of one or more of hydroxyethyl acrylate, sodium acryloyldimethyltaurate copolymer, squalane, polysorbate 60, a carbomer derivative, an acrylate, an acrylamide, xanthan gum, carrageenan gum, aluminium silicate, magnesium silicate, and a cellulose derivate, for example, present in an amount of from about 1% to about 10% by weight, from about 2% to about 8% by weight, from about 3% to about 7% by weight, or about 5% by weight, based on the total weight of the composition.
- a suitable thickening agent can comprise or consist of hydroxyethyl acrylate, sodium acryloyldimethyltaurate copolymer, squalane, and polysorbate 60, for example, in an amount of from about 1 % to about 10% by weight, or about 5% by weight, based on the total weight of the composition, which is available as SIMUGEL NS® from SEPPIC, Fairfield, NJ.
- This thickening agent can be used in the presently described topical cosmetic composition in combination with a further thickening agent, for example, cetyl alcohol, in an amount of from about 0.5% to about 2% by weight, or about 2% by weight, based on the total weight of the composition.
- the one or more thickening agents can be present in the topical cosmetic composition in an amount of from about 0.25% to about 15% by weight, from about 1% to about 12% by weight, from about 4% to about 10% by weight, from about 5% to about 9% by weight or about 7% by weight, based on the total weight of the composition.
- the described topical cosmetic compositions may optionally further comprise an effective amount of a free radical scavenger.
- effective amount is meant an amount sufficient to provide protection when the composition is properly applied, but not so much as to cause any side effects or adverse skin reactions; generally from about 0.1% to about 20%, or from about 1% to about 5%, of the composition.
- free radical scavengers include but are not limited to, ascorbic acid (Vitamin C) and its salts and derivatives (e.g., magnesium ascorbyl phosphate, sodium ascorbyl phosphate, Ascorbyl palmitate, etc.), tocopherol (Vitamin E), tocopherol esters (e.g., tocopheryl acetate, tocopheryl succinate, tocopheryl sorbate), butylated hydroxy benzoic acids and their salts, 6-hydroxy-2, 5,7,8- tetramethylchroman- 2-carboxylic acid (commercially available under the tradename TROLOX R®), gallic acid and its alkyl esters (propyl gallate), uric acid and its salts and alkyl esters, sorbic acid and its salts, the ascorbyl esters of fatty acids, amines (e.g., N,N-diethylhydroxylamine, aminoguanidine), sulfhydryl
- catechins and polyphenols e.g., those found in green tea extract
- flavonoids e.g., isoflavones such as genistein, and daidxein which are found in soy extracts, flavones, chalcones, flavanones, coumarins, etc.
- catechins and polyphenols e.g., those found in green tea extract
- flavonoids e.g., isoflavones such as genistein, and daidxein which are found in soy extracts, flavones, chalcones, flavanones, coumarins, etc.
- the described topical cosmetic compositions may optionally further comprise one or more preservatives.
- Suitable preservatives that can optionally be included in these compositions can comprise or consist of, but are not limited to, one or more of propylene glycol, glycerol, butylene glycol, pentylene glycol, hexylene glycol, sorbitol, benzyl alcohol, derivatives thereof, and mixtures thereof.
- a suitable preservative can comprise or consist of one or more of phenoxyethanol, methylisothiazolinone, phenoxyethanol, a paraben, imidazolynidyl urea, and combinations thereof. Additionally, the preservative can be present in an amount of from about 0.05% to about 1.5% by weight, from about 0.1% to about 1% by weight, from about 0.1% to about 0.6% by weight, or of about 0.6% by weight, based on the total weight of the composition.
- a suitable preservative can comprise or consist of phenoxyethanol and methylisothiazolinone, for example, NEOLONE PE® which is a formaldehyde-free broad-spectrum bactericide based on methylisothiazolinone and phenoxyethanol Rohm
- the topical cosmetic compositions may optionally further comprise one or more emulsifiers.
- Suitable emulsifiers that can optionally be included in these compositions can comprise or consist of any of a wide variety of nonionic, cationic, anionic, zwitterionic and amphoteric emulsifiers.
- emulsifiers useful in this regard can include emulsifiers that can comprise or consist of one or more of glycol esters, fatty acids, fatty alcohols, fatty acid glycol esters, fatty esters, fatty ethers, esters of glycerin, esters of propylene glycol, fatty acid esters of polyethylene glycol, fatty acid esters of polypropylene glycol, esters of sorbitol, esters of sorbitan anhydrides, carboxylic acid copolymers, esters and ethers of glucose, ethoxylated ethers, ethoxylated alcohols, alkyl phosphates, polyoxyethylene fatty ether phosphates, fatty acid amides, acyl lactylates, soaps, polyethylene glycol 20 sorbitan monolaurate (polysorbate 20), polyethylene glycol 5 soya sterol, steareth-2, steareth-20,
- the present topical cosmetic composition can include an emulsifier that can comprise or consist of one or more of a Ci 4- 22 alcohol and a C-i2-2o alkyglucoside, for example, MONTANOV L® which is a combination of fatty alcohols and alkyl glucosides available fro SEPPIC, Fairfield, NJ.
- Suitable emulsifiers can include one or more of potassium cetyl phosphate, an alkyl phosphate, PEG 100- glyceryl stearate and blends thereof, an ethoxylated fatty alcohol in combination with one or more fatty alcohols and/ or glyceryl stearates, and an alkyl sulphate.
- the present topical cosmetic skin-lightening compositions can comprise of from about 0.5% to about 10% by weight of an emulsifier, from about 1% to about 5% by weight, from about 1.5% to about 3.5% by weight, or about 2% by weight emulsifier, based on the total weight of the composition.
- an emulsifier from about 1% to about 5% by weight, from about 1.5% to about 3.5% by weight, or about 2% by weight emulsifier, based on the total weight of the composition.
- the present topical cosmetic compositions may further comprise a humectant.
- humectants useful in the present compositions include glycerin, butylene glycol, propylene glycol, sorbitol, and triacetin.
- the topical cosmetic compositions may optionally further comprise one or more moisturizers.
- Suitable moisturizers can comprise or consist of, but are not limited to, one or more of glycerin, pentylene glycol, butylene glycol, polyethylene glycol, sodium pyrrolidone carboxylate, alpha-hydroxy acids, beta-hydroxy acids, polyhydric alcohols, ethoxylated and propoxylated polyols, polyols, polysaccharides, panthenol, hexylene glycol, propylene glycol, dipropylene glycol, sorbitol, derivatives thereof, and mixtures thereof.
- Suspending Agents can comprise or consist of, but are not limited to, one or more of glycerin, pentylene glycol, butylene glycol, polyethylene glycol, sodium pyrrolidone carboxylate, alpha-hydroxy acids, beta-hydroxy acids, polyhydric alcohols, ethoxylated and propoxylated polyols, poly
- the present topical cosmetic compositions may further comprise a suspending agent.
- suitable suspending agents useful in the present compositions include one or more of alginic acid, bentonite, carbomer, carboxymethylcellulose and salts thereof, hydroxyethylcellulose, hydroxypropylcellulose, microcrystalline cellulose, colloidal silicon dioxide, dextrin, gelatin, guar gum, xanthan gum, kaolin, magnesium aluminum silicate, maltitol, triglycerides, methylcellulose, polyoxyethylene fatty acid esters, polyvinylpyrrolidone, propylene glycol alginate, sodium alginate, sorbitan fatty acid esters, tragacanth, and mixtures thereof.
- Surfactants include one or more of alginic acid, bentonite, carbomer, carboxymethylcellulose and salts thereof, hydroxyethylcellulose, hydroxypropylcellulose, microcrystalline cellulose, colloidal silicon dioxide, dextrin, gelatin, guar gum,
- the topical cosmetic compositions may optionally further comprise one or more surfactants.
- Suitable surfactants that can optionally be included in these compositions can comprise or consist of one or more of zwitterionic, amphoteric, anionic, cationic, and nonionic surfactants, and mixtures thereof.
- Suitable zwitterionic, amphoteric, anionic, cationic, and nonionic surfactants include those disclosed in
- Non-limiting examples of surfactants useful in the present compositions include nonionic surfactants, anionic surfactants, amphoteric surfactants, cationic surfactants, and mixtures thereof.
- Non-limiting examples of amphoteric surfactants useful in the present compositions are those selected from the group consisting of alkyl betaines, alkylamidobetaines, aminopropionates, iminodipropionates, aminoglycinates, imidazolinium betaines, sulfobetaines, and mixtures thereof.
- amphoteric surfactants useful in the present compositions are those selected from the group consisting of sodium 3-dodecyl- aminopropionate, sodium 3-dodecylaminopropane sulfonate, sodium lauroamphoacetate, coco dimethyl carboxymethyl betaine, cocoamidopropyl betaine, cocobetaine, lauryl amidopropyl betaine, oleyl betaine, lauryl dimethyl carboxymethyl betaine, lauryl dimethyl alphacarboxyethyl betaine, cetyl dimethyl carboxymethyl betaine, lauryl bis-(2-hydroxyethyl) carboxymethyl betaine, stearyl bis-(2-hydroxypropyl) carboxymethyl betaine, oleyl dimethyl gamma-carboxypropyl betaine, lauryl bis-(2- hydroxypropyl)alpha-carboxyethyl betaine, oleamidopropyl betaine, coco dimethyl
- anionic surfactants useful in the present compositions are those selected from the group consisting of alkyl sulfates, alkyl ethoxylated sulfates, beta-alkyloxy alkane sulfonates, alkyl ether sulfates, alkyl glyceryl ether sulfonates, alkyl ether carboxylates, acyl isethionates, acyl sarcosinates, acyl taurines, succinates, alkali metal, ammonium, or alkanolammonium salts thereof, and mixtures thereof.
- anionic surfactants useful in the present compositions are those selected from the group consisting of ammonium lauryl sulfate, sodium lauryl sulfate, ammonium laureth sulfate, sodium laureth sulfate, alkyl glyceryl ether sulfonate, triethylamine lauryl sulfate, triethylamine laureth sulfate, triethanolamine lauryl sulfate, triethanolamine laureth sulfate, monoethanolamine lauryl sulfate, monoethanolamine laureth sulfate, diethanolamine lauryl sulfate, diethanolamine laureth sulfate, lauric monoglyceride sodium sulfate, potassium lauryl sulfate, potassium laureth sulfate, sodium lauryl sarcosinate, sodium lauroyl sarcosinate, lauryl
- cationic surfactants useful in the present compositions include those selected from the group consisting of behenyl trimethyl ammonium chloride, bis(acyloxyethyl) hydroxyethyl methyl ammonium methosulfate, cetrimonium bromide, cetrimonium chloride, cetyl trimethyl ammonium chloride, cocamido propylamine oxide, distearyl dimethyl ammonium chloride, ditallowdimonium chloride, guar hydroxypropyltrimonium chloride, lauralkonium chloride, lauryl dimethylamine oxide, lauryl dimethylbenzyl ammonium chloride, lauryl polyoxyethylene dimethylamine oxide, lauryl trimethyl ammonium chloride, lautrimonium chloride, methyl-1-oleyl amide ethyl-2-oleyl imidazolinium methyl sulfate, picolin benzyl ammonium chloride, polyquaternium, stearal
- nonionic surfactants useful in the present compositions include those selected from the group consisting of polyoxyethylene fatty acid esters, sorbitan esters, cetyl octanoate, cocamide DEA, cocamide MEA, cocamido propyl dimethyl amine oxide, coconut fatty acid diethanol amide, coconut fatty acid monoethanol amide, diglycery!
- the present topical cosmetic compositions may optionally further comprise one or more vitamins or derivatives thereof.
- the present topical cosmetic compositions in accordance with the subject matter described herein can comprise vitamin C and/or vitamin E.
- vitamin C and/or vitamin E can be present in an amount effective to function as an antioxidant, either alone or in combination with other antioxidants, in the present topical cosmetic composition.
- the present topical cosmetic compositions may optionally further comprise one or more penetration enhancers.
- suitable penetration enhancers can include penetration enhancers that comprise or consist of one or more of a hydrophilic solvent, for example, DMSO, DMF, DMA, glycerol, polyethylene glycol, pyrrolidone derivatives, N-Decyl-methylsulfoxide (Brij 36T), lower alcohol's, fatty acids, and /or esters; a lipophilic enhancer, for example, dedecylazacycloheptane-2-one (azone), ethyl acetate, ethylpropionate, liquid paraffin, lamonin, lard, hexadecyl alcohol, oleyl alcohol, hydro ethyl lactamide, solketal, glycofural, tetrahydro-furfuryl alcohol, oleic acid, isopropyl myristate, lauryl alcohol, miglyo
- the present topical cosmetic compositions may optionally further comprise a fragrance.
- Suitable non-limiting examples of fragrances can include essential oils and blends, for example, Perfume FAV22000 (BOUQUET® available from BOUQUET®.
- the present topical cosmetic compositions may optionally further comprise a coloring agent, including but not limited to, one or more of a dye, a colorant, a pigment, a nanopigment, and/or combinations thereof.
- a coloring agent including but not limited to, one or more of a dye, a colorant, a pigment, a nanopigment, and/or combinations thereof.
- Pigments can be present in the composition in an amount ranging from
- the final composition for example, from 3 to 10 wt. %.
- They can be white or colored, inorganic or organic.
- Non-limiting examples include the titanium, zirconium or cerium oxides, as well as the zinc, iron or chromium oxides, ferric blue, chromium hydroxide, carbon black, ultramarines (polysulphides of aluminosilicates), manganese pyrophosphate and certain metal powders such as those of silver or of aluminium.
- Further non-limiting examples include the D&C pigments and the lakes commonly employed for imparting a make-up effect to the lips and to the skin, which include salts of calcium, of barium, of aluminium, of strontium or of zirconium.
- fat-soluble or water-soluble dyes that can be present in the composition, alone or as a mixture, in an amount ranging from 0.001 to 15 wt. %, for example from 0.01 to 5 wt. % or from 0.1 to 2 wt. %, relative to the total weight of the composition.
- Non-limiting examples include the disodium salt of ponceau, the disodium salt of alizarin green, quinoline yellow, amaranth trisodium salt, tartrazine disodium salt, rhodamine monosodium salt, fuchsin disodium salt, xanthophyll, methylene blue, carmine, halo-acid, azo and anthraquinone dyes, copper or iron sulphate, Sudan brown, Sudan red and annatto, as well as beetroot juice and carotene, and/or combinations thereof.
- the described topical cosmetic compositions can optionally further comprise at least one cosmetically acceptable excipient that can comprise or consist of at least one of an antioxidant that can comprise or consist of one or more members selected from the group consisting of butylated hydroxytoluene, sodium metabissulfite, butylated hydroxyl anisol, ascorbic acid and derivatives thereof, a sulfite and derivatives thereof, an ester, tocoferyl acetate, and combinations thereof; a chelating agent that can comprise or consist of one or more members selected from the group consisting of disodium edetate, EDTA, disodium EDTA, trisodium EDTA, tetrasodium EDTA, and combinations thereof; an emollient that can comprise or consist of one or more members selected from the group consisting of a glycol, a silicon- containing emollient, and combinations thereof; a thickening agent that can comprise or consist of one or more members selected from the group
- the present subject matter relates to a topical cosmetic composition
- the emollient can comprise or consist of one or more members selected from the group consisting of propylene glycol, glycerin, butyleneglycol, pentyleneglycol, cyclopentasiloxane dimethicone crosspolymer, cyclopentasiloxane PEG/PPG-18/18 dimethicone, and combinations thereof
- the thickening agent can comprise or consist of one or more members selected from the group consisting of hydroxyethyl acrylate, sodium acryloyldimethyltaurate copolymer, squalane, polysorbate 60, a carbomer derivative, xanthan gum, carrageenan gum, aluminium silicate, magnesium silicate, a cellulose derivate, cetyl alcohol, stearyl alcohol, cetyl and stearyl alcohol, glyceryl stearate, and combinations thereof.
- the present topical cosmetic compositions are formulated in a serum, a gel cream, a lotion, a cream, an ointment, a gel, an aerosol, a foam, a foamable liquid, a solution (solubilized system), a paste, a suspension, a dispersion, an emulsion, a skin cleanser, a milk, a mask, a solid stick, a bar (such as a soap bar), an encapsulated formulation, a microencapsulated formulation, microspheres or nanospheres or vesicular dispersions, or other cosmetically acceptable topical dosage form.
- the lipids of which the vesicles are made can be of the ionic or nonionic type, or a mixture thereof.
- the formulation can comprise one or more of an aqueous formulation and/or an anhydrous formulation.
- the present topical cosmetic composition in accordance with the subject matter described herein can comprise or consist of an anhydrous formulation, an aqueous formulation, or an emulsion.
- the present topical cosmetic compositions in accordance with the subject matter described herein are formulated in a serum or a gel cream.
- the presently described topical cosmetic compositions can optionally further comprise one or more cosmetic active agents or dermatological active agents in addition to the described skin-lightening active agents.
- Such agents can include, for example, additional skin lightening active agents including plant derived and non-plant derived skin lightening agents, including for example, pigmentation inhibitors, tyrosinase inhibitors, and/or melanocyte melanogenesis inhibitors; and/or non-skin lightening active agents, including for example, optical brightening agents, sunscreen agents, antiinflammatory agents, anti-microbial agents, anti-fungal agents, anti-wrinkle agents, anti- atrophy agents, anti-acne agents, free-radical scavengers, keratolytic agents, vitamins, anti-elastase and/or anti-collagenase agents, peptides, fatty acid derivatives, steroids, trace elements, extracts of algae and/or of planktons, enzymes and/or coenzymes, flavonoids and/or ceramide
- the topical cosmetic compositions may optionally further contain one or more additional skin lightening agents.
- Suitable additional skin lightening agents can comprise or consist of, but are not limited to, one or more of gingko extract, carob extract, rose fruit extract, geranium herb extract, Perilla extract, cinnamon extract, sweet marjoram extract, Arnica extract, Concha Blanca extract, cola ed Caballo, Piri-Piri, Pinon Negro, Pinon Blanco, extracts of clove, alfalfa, Basospermum montanum, Melia azadirachta, Convolvulus arvensis, Gaiyo, Sansonin, Syuroyo, Seimkko, Soukyo, Taiso, Hakusempi, Woodfordia fructosa, Lagerstroemia speciosa, passiflorine, tepezcohite, amoule, Hobiyu, Baffalo uri, Achote, Guayule, Adhatoda, Cy
- Yet other skin lightening agents can comprise or consist of, but are not limited to, one or more of teprenone, dihydroxy-isoquinoline, indomethacin, 3- hydroxymanule, vitamin K (such as vitamin K1-K7, its homologues, salts, and derivatives), thiazolidinone derivatives, and kynurenine and its derivatives and salts, retinol and its derivatives (e.g., Tretinoin, retinoic acid), resorcinol and its derivatives (e.g., 4-alkyl resorcinols, etc.), reservatol, placenta extracts, ellagic acid, linoleic acid and ⁇ -lipoic acid, and aminophenols e.g., such as those described in U.S. Pat. No. 6,203,781 (formula I). Amounts of additional skin lightening agents generally range from about 0.01% to about 20%, based
- the cosmetic composition according to the present subject matter may optionally comprise a pigmentation inhibitor.
- the pigmentation inhibitor include, but are not limited to, p-aminobenzoic acid derivatives, salicylic acid derivatives, benzenesulfonamide derivatives, imidazole derivatives, naphthalene derivatives, hydroxyanthranilic acid or salts thereof and their derivatives, anthranilic acid derivatives, coumarin derivatives, amino acid derivatives (e.g., 2-amino-3-[1-carboxyl-2- (1H-imidazol-4-yl)ethyl]aminobutanoic acid, 2-amino-3-[1-carboxyl-2-(1 H-imidazol-4- yl)ethyl]aminobutanoic acid hydrochloride, 2-amino-3-[1-carboxyl-2-(1 H-imidazol-4- yl)ethyl]aminobutanoic acid hydro
- Vitex trifolia (MAN JING Zl) extract Vitex trifolia (MAN JING Zl) extract, Hamamelis virginiana extract, palm extract, Parietaria extract, Carthamus tinctorius (HONG HUA) extract, Moms alba L. (SANG BAI Pl) extract, Sophora flavescens (KU SHEN) extract, Iris germanica L. extract, Iris florentina L. extract, Artemisia mongolia extract, Alnus firma fruit extract, Hong Kong extract, Sanguisorba officinalis (Dl YU) extract, Daphniphyllum macropodum extract, Polygonum multiflorum extract, and Fatsia japonica extract.
- the cosmetic composition according to the present subject matter may contain a tyrosinase inhibitor.
- the tyrosinase inhibitor include ascorbic acid or salts thereof and their derivatives (e.g., magnesium-L-ascorbic acid phosphate, ascorbyl palmitate, ascorbyl dipalmitate, ascorbic acid hydroxyproline phosphate ester, 5-o-alpha-D-glucopyranosyl-L-ascorbic acid, L-ascorbic acid phosphate ester sodium salt, L-ascorbic acid phosphate ester potassium salt, L- ascorbic acid phosphate ester magnesium salt, L-ascorbic acid phosphate ester calcium salt, L-ascorbic acid phosphate ester aluminum salt, L-ascorbic acid sulfate ester sodium salt, L-ascorbic acid sulfate ester potassium salt, L-ascorbic acid sulfate ester magnesium salt, L-ascorbic acid
- the cosmetic composition according to the present subject matter may contain a melanocyte melanogenesis inhibitor.
- the melanocyte melanogenesis inhibitor include lobeline or lobeline derivatives, liquiritin derivatives (e.g., liquiritin-alpha-glucoside, and liquiritin-alpha-maltoside), phenylchroman derivatives, chromone derivatives (e.g., 2-butylchromone, 2-pentylchromone, 2- heptylchromone, 2-nonylchromone, 2-hexadecylchromone, 2-(1-ethylpentyl)chromone, 2-butyl-7-methoxychromone, 2-pentyl-7-methoxychromone, 2-heptyl-7- methoxychromone, 2-nonyl-7-methoxychromone, 2-pentadecyl-7-methoxychromone, 2- (1-
- hachidyoensis extract Tribulus terrestris extract, Pyrrosia lingua (SHI WEI) extract, Typha angustifolia L. (XIANG PU) extract, Angelica dahurica extract, Buddleja Americana L.
- Tortuosa extract Salix Reinii extract, Salix sieboldiana extract, Toisusu urbaniana extract, Salix schwemii extract, Salix vulpina extract, Populus maximowiczii extract, Myrica rubra (YANG MEI Pl) extract, Agave americana extract, Agave americana var.
- the topical cosmetic compositions may optionally further comprise one or more optical brighteners.
- Optical brighteners are described in Fluorescent Whitening Agent, Encyclopedia of Chemical Technology, Kirk-Othmer, Vol. 11 , pp. 227-241 , 4th edition, 1994, Wiley, which is hereby incorporated by reference herein in its entirety.
- Optical brighteners can be defined more particularly as compounds which absorb in the UVA range between 300 and 390 nm and re-emit essentially between 400 and 525 nm.
- Suitable optical brighteners can comprise or consist of, but are not limited to, one or more of stilbene derivatives (e.g., sodium 4,4 l -bis[(4,6-dianilino-1 ,3,5-triazin-2- yl)amino]stilbene-2,2'-disulphonate), coumarin derivatives, oxazole and benzoxazole derivatives (e.g., 2,5-thiophenediylbis(5-tert-butyl-1 ,3-benzoxazole)) and imidazole- derivatives.
- Amounts of optical brighteners generally range from about 0.1% to about 5.0%, based on total weight of the composition.
- a suitable optical brightener is oxazole.
- the topical cosmetic compositions may optionally further comprise one or more anti-inflammatory agents.
- Suitable anti-inflammatory agents useful in this regard can comprise or consist of, but are not limited to, one or more of propionic acid derivatives, acetic acid derivatives, fenamic acid derivatives, biphenylcarboxylic acid derivatives, oxicams, acetyl salicylic acid, ibuprofen, naproxen, benoxaprofen, flurbiprofen, fenoprofen, fenbufen, ketoprofen, indoprofen, pirprofen, carprofen, oxaprozin, pranoprofen, microprofen, tioxaprofen, suprofen, alminoprofen, tiaprofenic acid, fluprofen, bucloxic acid, apazone, bromfenac, celecoxib, diclofenac, difenpiramide, diflunis
- Non-limiting examples of suitable anti-microbial and anti-fungal agents useful in this regard include, but are not limited to, beta-lactam drugs, quinolone drugs, ciprofloxacin, norfloxacin, tetracycline, erythromycin, amikacin, 2,4,4'-trichloro-2'- hydroxy diphenyl ether, 3,4,4'-trichlorobanilide, phenoxyethanol, phenoxy propanol, phenoxyisopropanol, doxycycline, capreomycin, chlorhexidine, chlortetracycline, oxytetracycline, clindamycin, ethambutol, hexamidine isethionate, metronidazole, pentamidine, gentamicin, kanamycin, lineomycin, methacycline, methenamine, minocycline, neomycin, netilmicin, paromomycin, streptomycin, tobramycin
- the topical cosmetic compositions may optionally further comprise one or more anti-wrinkle and/or anti-atrophy agents.
- Suitable non-limiting examples of anti- wrinkle and/or anti-atrophy agents useful in this regard can include anti-wrinkle and/or anti-atrophy agents that can comprise or consist of one or more of cis and trans retinoic acid, retinol, retinyl esters, salicylic acid, sulfur-containing D and L amino acids, N-acetyl derivatives sulfur-containing D and L amino acids, N-acetyl-L-cystein, thiols, ethane thiol, alpha-hydroxy acids, glycolic acid, lactic acid, phytic acid, lipoic acid, lysophosphatidic acid, skin peel agents, phenol, pharmaceutically or cosmetically acceptable salts thereof, and mixtures thereof.
- Anti-acne agents can comprise or consist of one or more of cis and trans retinoic acid, retinol, retin
- the topical cosmetic compositions may optionally further comprise one or more anti-acne agents.
- anti-acne agents useful in this regard can include anti-acne agents that can comprise or consist of one or more of keratolyses, salicylic acid (o-hydroxybenzoic acid), 5-octanoyl salicylic acid, resorcinol, retinoids, cis and trans retinoic acid, sulfur-containing D and L amino acids, N-acetyl sulfur-containing D and L amino acids, N-acetyl-L-cysteine, lipoic acid, sebostats, flavonoids, bile salts, scymnol sulfate, deoxycholate, cholate, adapalene, azelaic acid, benzoyl peroxide, clindamycin, clindamycin phosphate, doxycycline, erythromycin, norgestimate, organic
- the present subject matter relates to a method of treating skin in a subject, comprising topically administering to skin of a subject in need thereof, a therapeutically effective amount of the topical cosmetic composition in accordance with the subject matter described herein.
- the present subject matter relates to a method of lightening skin pigmentation in a subject, comprising topically administering to skin of a subject in need thereof, a therapeutically effective amount of the topical cosmetic composition in accordance with the subject matter described herein.
- the present subject matter relates to a method of treating a skin disorder or condition in a subject, comprising topically administering to skin of a subject in need thereof, a therapeutically effective amount of the topical cosmetic composition in accordance with the subject matter described herein.
- the skin disorder or condition can be a disorder or condition associated with undesirable skin pigmentation.
- the present subject matter relates to a method of lightening skin pigmentation in a subject or treating a skin disorder or condition in a subject, comprising topically administering for at least once per day for at least three days, for at least five days, or for at least seven days, to skin of a subject in need thereof, a therapeutically effective amount of the topical cosmetic composition in accordance with the subject matter described herein.
- a therapeutically effective amount of the topical cosmetic composition in accordance with the subject matter described herein.
- the skin is visibly altered.
- the present subject matter relates to a method of lightening skin pigmentation in a subject or treating a skin disorder or condition in a subject, comprising topically administering for at least once per day for at least three weeks to skin of a subject in need thereof, a therapeutically effective amount of the topical cosmetic composition in accordance with the subject matter described herein, wherein after three weeks the skin is visibly lightened.
- the present topical cosmetic compositions are effective in treating a variety of skin disorders or conditions characterized by undesirable skin pigmentation.
- disorders and/or conditions can include regional hyperpigmentation caused by melanocyte hyperactivity such as idiopathic melasma occurring during pregnancy (mask of pregnancy or chloasma) or secondary to estrogen- progesterone contraception; local hyperpigmentation caused by benign melanocyte hyperactivity and proliferation such as lentigo senilis, known as liver spots; accidental hyperpigmentation such as post-lesional photosensitization and scarring; freckles; malpigmentation; and certain forms of leukoderma such as vitiligo where, if the injured skin cannot be repigmented, the residual zones of normal skin are lightened or depigmented to impart a homogeneous color to the entire skin.
- Skin can be treated according to the presently described methods for purely cosmetic lightening of areas, for example, large areas, of skin whose pigmentation, although undesired, is adequate for the individual skin type.
- the skin disorder or condition to be treated according to the present methods is undesired skin pigmentation.
- Suitable skin areas for treatment and/or lightening in accordance with the subject matter described herein can include thin skin areas including for example areas of skin on the face, neck, and/or hands.
- the present compositions and methods as described herein are suitable for use in both men and women, and are suitable for use on all skin types including dry skin types, normal skin types, and greasy skin types.
- the present subject matter relates to a method of treating a skin disorder or condition in a subject, or to a method of lightening skin pigmentation in a subject, wherein topically administering to skin comprises administering at least once per day or at least twice per day for a period of at least two weeks, wherein skin pigmentation is lightened.
- Topically administering can comprise administering at least once per day or at least twice per day for a period of at least three weeks, wherein skin pigmentation is lightened. Topically administering can comprise administering at least once per day or at least twice per day for a period of at least four weeks, wherein skin pigmentation is lightened. Administering at least once per day can comprise administering once in the morning or in the evening. Administering at least twice per day can comprise administering once in the morning and once in the evening.
- compositions of the present topical cosmetic compositions in accordance with the presently described subject matter can be readily produced by the skilled artisan according to known methods of producing such formulations including for example, a cream, a gel, a serum, a lotion, or other formulation described herein, without undue experimentation.
- a process for producing a cream or emulsion formulation can comprise separately producing an aqueous phase and an oil phase, adding the oil phase to the aqueous phase, for example with mixing and/or homogenization (with high shear), to an emulsion.
- one or more of the following components can be optionally added thereto, for example, in the following order, to produce the final emulsion or cream: one or more skin lightening actives; one or more pH adjusters; one or more emollients; one or more skin lightening actives; one or more sunscreen actives; one or more thickening agents; one or more antioxidants; and one or more fragrances.
- the aqueous phase and the oil phase Prior to forming the emulsion, can be separately heated to a temperature of from about 7O 0 C to about 99 0 C; from about 75 0 C to about 95°C; from about 8O 0 C to about 9O 0 C; or about 85°C. After heating the oil phase can be slowly added to the aqueous phase, for example, with mixing and high shear homogenization. The resultant emulsion can then be cooled while maintaining mixing and high shear homogenization, for example, to a temperature of from about 47°C to about 27°C; from about 42 0 C to about 3O 0 C; from about 39°C to about 35 0 C; or about 37°C.
- compositions produced according to the above-described processes. If produced according to these processes, these compositions exhibit chemical and physical stability suitable for topical administration.
- the topical cosmetic compositions produced according to these processes can be placed in a suitable containment vessel comprising a product contact surface composed of a material selected from the group consisting of glass, plastic, steel, stainless steel, aluminum, Teflon, polymeric structure, ceramic structure, alloys, and mixtures thereof.
- a suitable containment vessel comprising a product contact surface composed of a material selected from the group consisting of glass, plastic, steel, stainless steel, aluminum, Teflon, polymeric structure, ceramic structure, alloys, and mixtures thereof.
- These containment vessels are used to facilitate manufacturing, handling, processing, packaging, storage, and administration of said topical cosmetic composition.
- Suitable containment vessels in this regard can be selected from the group consisting of plastic tubes, bottles, metal tubes, and any combination thereof.
- Appropriate dosage levels for the active agents contemplated in the present topical cosmetic compositions and methods are well known to those of ordinary skill in the art and are selected to maximize the treatment of the above skin conditions. Dosage levels on the order of about 0.001 mg to about 5,000 mg per kilogram body weight of the skin lightening active components are known to be useful in the treatment of the diseases, disorders, and conditions contemplated herein. Typically, this effective amount of the skin lightening active components will generally comprise from about 0.001 mg to about 100 mg per kilogram of patient body weight per day. Moreover, it will be understood that this dosage of ingredients can be administered in a single or multiple dosage units to provide the desired therapeutic effect.
- compositions can be combined with other therapeutic agents in conjunction with those provided in the above-described compositions.
- amount of active ingredients that may be combined with the carrier materials to produce a single dosage form will vary depending upon the host treated, the nature of the disease, disorder, or condition, and the nature of the active ingredients.
- the present compositions may be given in a single dose or multiple doses daily.
- the present topical cosmetic compositions are given from one to four times daily. Starting with a low dose once or twice daily and slowly working up to higher doses if needed is a strategy.
- the amount of active ingredients that may be combined with the carrier materials to produce a single dosage form will vary depending upon the host treated, the nature of the disease, disorder, or condition, and the nature of the active ingredients.
- the topical cosmetic compositions may be topically applied once or multiple times per day.
- the present topical cosmetic compositions are topically applied from one to four times daily. For example, starting with once daily and progressing to more frequent applications, if needed, is one strategy.
- the present topical cosmetic compositions are topically applied from one to four times daily, for example, in the morning, at noon, in the afternoon, and/or in the evening.
- the topical composition can be topically applied once a day in the morning, at noon, in the afternoon, or in the evening.
- the topical composition can be topically applied twice a day, for example, in the morning and in the evening, at noon and in the evening, in the morning and at noon, in the morning and in the afternoon, in the afternoon and in the evening.
- the topical composition can be topically applied three times a day, for example, in the morning, at noon or afternoon, and in the evening.
- the topical composition can be topically applied four times a day, for example, in the morning, at noon, in the afternoon, and in the evening.
- the topical cosmetic compositions as described herein can be administered once or multiple times per day for a period of time of at least one week, for a period of at least two weeks, for a period of at least four weeks, or for a period of at least eight weeks.
- the topical cosmetic compositions can be administered once or multiple times per day for a period of time of up to one year, of up to six months, of up to three months, or of up to two months.
- the topical cosmetic compositions can be administered once or multiple times per day for a period of time of from at least one week to one year, for a period of from at least one week to six months, for a period of from at least one week to four months, for a period of from at least one week to three months, for a period of from at least one week to two months, for a period of from at least two weeks to two months, for a period of from at least three weeks to two months, for a period of from at least one week to one month, for a period of from at least one week to three weeks, or for a period of from at least four weeks to two months.
- a specific dose level for any particular patient will vary depending upon a variety of factors, including the activity of the specific active agent; the age, body weight, general health, sex and diet of the patient; the time of administration; the rate of excretion; possible drug combinations; the severity of the particular condition being treated; and the form of administration.
- One of ordinary skill in the art would appreciate the variability of such factors and would be able to establish specific dose levels using no more than routine experimentation.
- Pharmacokinetic parameters such as bioavailability, absorption rate constant, apparent volume of distribution, unbound fraction, total clearance, fraction excreted unchanged, first-pass metabolism, elimination rate constant, half-life, and mean residence time are well known in the art.
- the optimal cosmetic formulations can be determined by one skilled in the art depending upon considerations such as the particular ingredients and the desired dosage. See, for example, Remington's Pharmaceutical Sciences, 18th ed. (1990, Mack Publishing Co., Easton, PA 18042), pp. 1435-1712, and "Harry's Cosmeticology", 8th ed. (2000, Chemical Publishing Co., Inc., New York, N.Y. 10016), the disclosure of each of which is hereby incorporated by reference herein in its entirety. Such formulations may influence the physical state, stability, rate of in vivo release, and rate of in vivo clearance.
- the present topical cosmetic composition in accordance with the subject matter described herein may be a gel cream packaged in, for example, a tube, or a serum packaged in, for example, a non-aerosol non-foaming pump container or bottle, wherein the amount of the composition contained in the container can be in the range of from about 10 gm to about 60 gm, between about 20 gm and about 50 gm, or about 30 gm, or about 40 gm.
- Single dosage kits and packages containing once per day amount of composition may be prepared.
- Single dose, unit dose, and once-daily disposable containers of the present compositions are contemplated as within the scope of the present subject matter.
- compositions in accordance with the subject matter described herein may be formulated for storage in a substantially non-reactive laminated package to enhance stability of the package. This method of storage provides enhanced package stability in comparison with other, paper-based packages.
- amount of composition per single packet may range be from about
- compositions capable of long term storage are also contemplated.
- present compositions remain unexpectedly stable in storage for periods including between about 3 months and about 3 years, about 3 months and about 2.5 years, between about 3 months and about 2 years, between about 3 months and about 20 months, and alternately any time period between about 6 months and about 18 months.
- the presently described topical cosmetic formulation in accordance with the subject matter described herein remains stable for at least three years at a temperature of less than 30 0 C.
- the presently described topical cosmetic formulation remains stable for at least two years at a temperature of less than or equal to 30 0 C.
- the presently described topical cosmetic formulation remains stable for at least two years at a temperature of less than or equal to 25 0 C.
- the color is expressed by a system of three-dimensional coordinates where the L * axis corresponds to skin luminosity, the a* axis corresponds to green and red colors, and the b * axis corresponds to blue and yellow colors.
- This equipment provides continuous light emission in the UVB and UVA spectrum, ranging between 290 and 400nm.
- the device includes a set of lenses and filters that absorb or disperse irradiation lower than 320nm or higher than 400nm.
- the irradiation occurs through a set of 6 branches of optic fiber called "ports", programmed to apply pre-established individual doses of irradiation. Irradiation monitoring was performed using a Dose Controlling System (DCS), which includes a UVB irradiation detector and an electronic monitor. In this study, only three "ports" were used for each application site of the tested compositions.
- DCS Dose Controlling System
- Hydroquinone 2% (positive control): Component Function % W/W Citric acid pH adjuster 0.08 Purified water vehicle 67.08 Benzophenone-3 sunscreen active 1.5 Octyl methoxycinnamate sunscreen active 6 Hydroquinone lightening agent 2 Lanette emulsifier 13
- Phenoxyethanol and methylisothiazolinone preservative 0.6
- Age level 18 to 60 years old
- Photo-induced pathologies such as sun hives, lupus erythematosus, polyform rash at light, recurring herpes simplex;
- Presence of active inflammatory dermatoses at test site Presence of nevus lesions at the test site;
- MED minimum erythematose dose
- each volunteer was released and instructed to return within 24 hours, whereby the exposure site was read with the volunteer in a vertical position at a predetermined distance and illumination which was kept constant for each volunteer. The MED was then determined for each volunteer.
- iMED Minimum Erythematose Dose
- UV ultraviolet
- each test site located on the back, between the pelvic and scapular waist, laterally to the medial line of the spine, was marked with the volunteer in a horizontal position and using a marker.
- Three sites indicated for the application of the products were delimited, i.e., Site B, Site E, and Site F. Each site was 35 cm 2 (07 x 05cm).
- irradiation equivalent to 1.5 times the minimum erythematose dose, previously calculated for each volunteer was applied. This application was repeated twice whereby each site was irradiated a total of three times.
- Site E The present topical cosmetic composition
- Figure 2 illustrates the results obtained for Site E, i.e., the application location of the evaluated present topical cosmetic composition. Figure 2 illustrates that there is progressive lightening over time that becomes statistically significant after 14 days.
- Table V illustrates the results of the comparison test between the L * of TO averages and the other experimental times for area 2 (Site E).
- Table Vl shows the raw data for the individual results for area 2 (Site E) for each volunteer in term of L* , a * , and b * for each of TO, T07, T14, and T21.
- Figure 3 illustrates, for the control location Site F, i.e., where there was no treatment for the irradiation, progressive lightening (natural degradation of the synthesized melanin), without any significance over the experimental times.
- Table VII shows the results of the comparison test between the L* of TO averages and the other experimental times for the control area (Site F).
- Table VIII shows the raw data for the individual results for the control area (Site F) for each volunteer in term of L * , a * , and b * for each of TO, T07, T14, and T21.
- Figure 4 illustrates the comparison between the averages of the colorimetric values in treatments 1 and 2 and the control over the evaluation times.
- Table IX illustrates that only the present topical cosmetic formulation exhibited statistically significant reduction in pigmentation as compared to the spontaneous reduction in pigmentation observed in the control group.
- the colorimeter was used as a complementary instrumental evaluation, enabling the detection of differences which the human eye cannot detect.
- the L* parameter provided by the colorimetric measurement is the index directly related to the skin's luminosity. The higher the value of L* the lighter the evaluated region.
- Phenoxyethanol and methylisothiazolinone preservative .6
- composition is prepared as in Example 1. More specifically, after
- Neolone PE Phenoxiethanol and Methylisothiazolinone
- cyclomethicone are added under high shearing homogenization and mixing for about 15 minutes.
- the thickening agents including xanthan gum are added in the oil phase.
- a topical cosmetic composition is administered topically to the skin of a subject being treated by conventional means. This is preferably done through the use of a serum or cream gel formulation. A topical preparation may thus be applied to the desired skin surface area with, for example, the use of the fingertips.
- the subject should be told to first clean the affected area gently and to pat it dry. The topical cosmetic composition may then be applied directly to the affected skin area or dispensed into the palm of the hand or suitable vessel from which material may be taken and manually applied to the skin area to be treated.
- a subject is suffering from undesired skin pigmentation.
- a topical cosmetic composition as described herein is topically administered to undesirably pigmented areas of the skin of the subject. It would be expected that the undesirably pigmented areas of the skin of the subject would be lightened.
- a subject is suffering from vitiligo.
- a topical cosmetic composition as described herein is topically administered to the residual areas of normal skin of the subject. It would be expected that the residual areas of normal skin of the subject would be lightened to impart a homogeneous color to the entire skin.
- a subject is suffering from age spots.
- a topical cosmetic composition as described herein is topically administered to the affected skin areas of the subject. It would be expected that the age spots would be lightened.
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Abstract
Priority Applications (13)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CN2007801022167A CN101917965B (zh) | 2007-11-19 | 2007-11-19 | 局部化妆用皮肤增亮组合物及其使用方法 |
EP07867501A EP2219600A4 (fr) | 2007-11-19 | 2007-11-19 | Compositions cosmétiques topiques d'éclaircissement de la peau et leurs procédés d'utilisation |
BRPI0722043A BRPI0722043A2 (pt) | 2007-11-19 | 2007-11-19 | composições de clareamento de pele cosmética tópicas e métodos de uso das mesmas. |
CA2706797A CA2706797A1 (fr) | 2007-11-19 | 2007-11-19 | Compositions cosmetiques topiques d'eclaircissement de la peau et leurs procedes d'utilisation |
AU2007361455A AU2007361455A1 (en) | 2007-11-19 | 2007-11-19 | Topical cosmetic skin lightening compositions and methods of use thereof |
MX2010005548A MX299318B (es) | 2007-11-19 | 2007-11-19 | Composiciones cosmeticas topicas para aclarar la piel, y metodos de uso de las mismas. |
JP2010534920A JP2011504498A (ja) | 2007-11-19 | 2007-11-19 | 局所美白化粧品組成物およびその使用方法 |
PCT/US2007/024109 WO2009067095A1 (fr) | 2007-11-19 | 2007-11-19 | Compositions cosmétiques topiques d'éclaircissement de la peau et leurs procédés d'utilisation |
CA 2706992 CA2706992C (fr) | 2007-11-19 | 2008-11-19 | Compositions cosmetiques topiques d'eclaircissement de la peau et leurs procedes d'utilisation |
US12/743,353 US9241893B2 (en) | 2007-11-19 | 2008-11-19 | Topical cosmetic skin lightening compositions and methods of use thereof |
AU2008364312A AU2008364312B2 (en) | 2007-11-19 | 2008-11-19 | Topical cosmetic skin lightening compositions |
US14/950,395 US9364424B2 (en) | 2007-11-19 | 2015-11-24 | Topical cosmetic skin lightening compositions and methods of use thereof |
US14/950,451 US20160074316A1 (en) | 2007-11-19 | 2015-11-24 | Topical cosmetic skin lightening compositions and methods of use thereof |
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PCT/US2008/012952 Continuation-In-Part WO2010059140A1 (fr) | 2007-11-19 | 2008-11-19 | Compositions cosmétiques topiques d'éclaircissement de la peau et leurs procédés d'utilisation |
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AU (1) | AU2007361455A1 (fr) |
BR (1) | BRPI0722043A2 (fr) |
CA (1) | CA2706797A1 (fr) |
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WO (1) | WO2009067095A1 (fr) |
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CN114869820A (zh) * | 2022-05-24 | 2022-08-09 | 安科化妆品(浙江)有限公司 | 一种含有北沙参叶提取物的防晒乳 |
WO2024065609A1 (fr) * | 2022-09-30 | 2024-04-04 | L'oreal | Composition pour le soin des matières kératiniques et masque la contenant |
Also Published As
Publication number | Publication date |
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CN101917965B (zh) | 2013-01-02 |
CA2706797A1 (fr) | 2009-05-28 |
CN101917965A (zh) | 2010-12-15 |
MX2010005548A (es) | 2010-08-06 |
BRPI0722043A2 (pt) | 2016-10-18 |
EP2219600A1 (fr) | 2010-08-25 |
AU2007361455A1 (en) | 2009-05-28 |
MX299318B (es) | 2012-05-18 |
JP2011504498A (ja) | 2011-02-10 |
EP2219600A4 (fr) | 2012-09-12 |
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