NZ729134A - Methods and compositions for enhancing hair quality using blackberry extract - Google Patents
Methods and compositions for enhancing hair quality using blackberry extractInfo
- Publication number
- NZ729134A NZ729134A NZ729134A NZ72913414A NZ729134A NZ 729134 A NZ729134 A NZ 729134A NZ 729134 A NZ729134 A NZ 729134A NZ 72913414 A NZ72913414 A NZ 72913414A NZ 729134 A NZ729134 A NZ 729134A
- Authority
- NZ
- New Zealand
- Prior art keywords
- extract
- hair
- blackberry
- composition
- compositions
- Prior art date
Links
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Landscapes
- Cosmetics (AREA)
Abstract
Disclosed is a method of enhancing hair growth by applying to the scalp, the skin, the eyelashes, eyebrows, moustache region or beard region of a patient a topical composition comprising a concentration of at least 90 mg extract/ml of solution but less than 300 mg/ml of a Rubus fruticosus leaf extract; and additionally comprising at least 1 weight percent of carbomer by weight of the composition.
Description
METHODS AND COMPOSITIONS FOR ENHANCING HAIR QUALITY USING BLACKBERRY EXTRACT FIELD OF THE INVENTION This disclosure relates to topical compositions and methods for inducing hair growth and improving hair y utilizing extracts from the Blackberry plant (Rubus fruticosus).
BACKGROUND OF THE INVENTION Genetic disposition as well as the natural aging process and/or disease contribute to hair loss and slower hair growth in both males and females.
Approximately 50% of the population ys this trait to some degree by the age of 50, and ng of the hair can begin between 12 and 40 years of age independent of gender. Thus, agents able to stimulate hair growth as well as prevent and slow down or reduce hair loss could be beneficial not only to cure alopecia but to affect positively the psychosocial events ated with hair disorders. s reveal psychosocial impact with hair loss to include body image dissatisfaction associated with negative stereotypes, such as feeling older, weaker and less attractive.
Drugs, including Minoxidil (Rogaine), Finasteride (Propecia) and Dutasteride (Avodart) are approved treatments for hair loss. However, they may e medical prescription, and are active only on a certain percent of the tion. Moreover, some of these drugs are not permitted to be used by females due to hormonal effects. For example, premenopausal women should not take Finesteride due to the risk of male pseudo-hermaphroditism to the fetus. Finasteride has been found to lower cially the results of the prostate-specific antigen (PSA) test, the standard screening test for prostate cancer which can delay the detection and the treatment of the disease.
Minoxidil is a topically applied drug that is effective in inducing hair growth for a subset of patients and will re-grow hair only on top of the scalp.
Further, it has limited effect on older people.
Minoxidil may slow the rate of hair loss in five out of ten male patients.
Other medical treatments available to treat hair loss include drastic surgical ques such as scalp reduction, scalp flaps or ular unit transplantation. These surgeries carry the risk of complications such as elevation of hairline associated with donor region, ility of necrosis and unnatural appearance of hair growth ion, anesthesia and post-op care, not to mention high costs.
Herbal preparations that claim to induce hair growth (e.g. Hair Prime) are available at low cost but their effectiveness is very limited.
M. nn et al. have described that a hydroalcoholic blackberry leaf extract (SymMatrix), exhibits the MMP-1, MMP-2, and MMP-9 inhibitory activity. (See, for example, US2008/0095719 SUMMARY OF THE ION Surprisingly, we have found that a concentrated, aqueous Rubus fruticosus extract can effectively induce hair growth by applying a ition comprising, consisting ially and consisting of such t to the scalp, the skin, the eyelashes, eyebrows, mustache region or beard region of a patient a topically active composition comprising a concentration of at least 90 mg extract/ml of solution but less than 300 mg/ml of a Rubus fruticosus extract, which may start to increase hair coverage to the area of interest after daily application for at least five (5) to seven (7) days.We observed a potent increase in hair growth in vivo in all animals treated with a concentrated Rubus fruticosus extract. Even more surprisingly, the compositions of our invention containing Rubus fruticosus extract initially induced a visible telogen phase (i.e., ng of club hairs) prior to rapid entry into the anagen phase (i.e., active growth phase of hair follicles). The compositions of our invention induced anagen in 100% of animals treated over a period of at least eight days.
In a first embodiment the present invention provides a method of enhancing hair growth by applying to the scalp, the skin, the eyelashes, eyebrows, mustache region or beard region of a patient a topical composition comprising a concentration of at least 90 mg extract/ml of solution but less than 300 mg/ml of a Rubus fruticosus leaf extract; and onally comprising at least 1 weight percent of carbomer by weight of the composition, wherein the extract is produced by a method having the following steps: a. addition to blackberry leaves of an tant containing water and ethanol, wherein the extractant contains ethanol and water in a ratio of 2:8 to 8:2 by weight; and b. tion of the blackberry leaves with the extractant for up to 72 hours at an extraction temperature in the range of from 80oC to 100oC.
DETAILED PTION OF THE PREFERRED EMBODIMENTS As used herein, "blackberry extract" means the extract of a plant of the genus Rubus. Preferably, the species utilized in the compositions described herein is Rubus fruticosus. Blackberry extract may be a blend of compounds ed from the plant of the genus Rubus.
In one ment, the compounds are isolated from the flowers of the plant. In another embodiment, the compounds may be isolated from dried flowers of the plant. They may also be isolated from one or more parts of the plant, including the whole plant, flower, seed, root, rhizome, stem, fruit and/or leaf of the plant.
Preferably, erry extract useful in the itions described herein is isolated from the leaf of the blackberry plant.
The extraction process may include physically removing a piece of the blackberry plant and grinding it. Organic solvent extraction processes known to those of skill in the art may also be used to obtain the blackberry ts useful in the compositions bed herein. Solvents such as lower C1-C8 alcohols, C1-C8 alkyl polyols, C1-C8 alkyl ketones, C1-C8 alkyl ethers, acetic acid C1-C8 alkyl esters, and chloroform, and/or inorganic solvents such as water, inorganic acids such as hydrochloric acid, and inorganic bases such as sodium hydroxide may be used to extract active compounds from the blackberry plant.
A erry leaf extract may also be prepared by an extraction produced with water, using alcohols such as ethanol or combination thereof as the extractant.
However, an t produced with an extractant including both ethanol and water extractant.
Blackberry leaves are preferably dried prior to extraction. It is also preferable to use only the leaves of the blackberry plant for the extraction and not also other plant parts such as the fruit (berries) of the blackberry, its branches, flowers or roots.
In one embodiment, the process of the extraction for the production of a blackberry leaf t may have the following steps: a) addition to blackberry leaves of an extractant containing an alcohol ed from the group consisting of methanol, ethanol, n-propanol, isopropanol, and b) extraction of the blackberry leaves with the tant for up to 72 hours.
The ratio of the mass of extractant to leaf solids is preferably established such that at least a 10-fold mass of extractant relative to the leaf solids and preferably no more than a 50-fold mass of extractant relative to the leaf solids is obtained, ably a 10-to 20-fold mass. A 14-to d mass of extractant relative to the leaf solids is particularly preferably used for extraction. Good results were achieved with a 16-fold mass of an ethanol-containing solvent (relative once again to the leaf solids).
The extraction time for performing step (b) is at most 72 hours but can also be shorter. With particularly short extraction times, a relatively dilute extract is obtained in step (b). It is therefore preferable to extract the blackberry leaves in step (b) for at least one (1) hour, and more preferably, for at least two (2) hours. The preferred extraction time is chosen on the basis of the y of the blackberry leaves to be extracted, particularly their age of the leaves and of the other tion conditions, particularly the extraction temperature.
At elevated extraction temperatures, for example, at an extraction ature in the range from about 60 to about 100°C, preferably in the range from about 80 to about 100°C, the extraction time is preferably about one hour to about six hours and more preferably about two to about four hours.
In addition, it is most preferable to perform the extraction in step (b) by refluxing the extractant, particularly at extraction temperatures in the range from about 60°C to about 100°C, and more preferably in the range from about 80 to about 100°C. When using the refluxing process, the extraction time is preferably no more than about 24 hours.
The tion temperature is established on the basis of the extractant that is used. If an ethanolcontaining solvent is used, an extraction temperature in the range from about 60°C to about 100°C, in particular an extraction temperature in the range from about 80°C to about 100°C, is preferred, ularly if a mixture of ethanol and water is used as the extractant.
Preferably, the extractant contains a lower alkyl alcohol solvent, more preferably ethanol, in a proportion of at least about 20 wt.%, relative to the total extractant. Preferably, the extractant should also contain water in a tion of at least 15 wt.%, relative to the total extractant. It is more preferable for the tant simultaneously contains both at least wt.%, relative to the total extractant, of an alcohol (preferably ethanol) and water in a proportion of at least 15 wt.%, relative to the total extractant.
Blackberry leaf ts that are particularly effective in the compositions and s described herein are obtained with an extract containing ethanol and water in the ratio of about 2:8 (2 parts by weight of ethanol mixed with 8 parts by weight of water) to about 8:2, more preferably in the ratio of about 3:7 to about 7:3 and most preferably in the ratio of about 3:7 to about 1:1. ingly, in one preferred embodiment, the blackberry extract is a blackberry leaf extract, i.e., the extract is ed from the leaves of the blackberry plant. In a particularly preferred embodiment, the blackberry extract is produced from the leaves of Rubus fruticosus. In a r particularly preferred embodiment, the blackberry extract is produced by extracting the leaves of Rubus fruticosus with a mixture of water and a lower alcohol such as ethanol as set forth above.
One particularly suitable blackberry extract is produced by extracting the leaves of Rubus fruticosus with a mixture of water and ethanol is commercially available as compounded to an activity of about 5% to about 10%, with a maltodextrin matrix, from Symrise Inc. of Teterboro, NJ, and is sold under the name, "SymMatrix." Detailed procedures for preparing a suitable blackberry leaf extract are set forth in U.S. Patent Publication No. 2008/0095719, which is herein orated in its entirety.
As used herein, "topical ation" means directly laying on or spreading on outer skin using, e.g., by use of the hands or an applicator such as a wipe, puff, roller, or spray.
As used herein, "cosmetically-acceptable" means that the product(s) or compound(s) which the term describes are suitable for use in contact with tissues (e.g., the skin) without undue toxicity, incompatibility, ility, irritation, allergic response, and the like. This term is not intended to limit the ient/product, which it bes to use solely as a cosmetic (e.g., the ingredient/product may be used as a pharmaceutical).
As used herein, "topical carrier" means one or more compatible solid or liquid filler diluents that are suitable for topical administration to a mammal.
Examples of topical carriers include, but are not limited to, water, waxes, oils, emollients, emulsifiers, thickening agents, g agents, and mixtures thereof.
As used herein, "hair" means scalp, head, facial and/or body hair, including but not limited to the scalp, eye lashes, brows, mustache, beard, ear, nasal, chest, pubic, auxiliary and the like.
As used herein, "inducing hair growth" means the r induction of growth of a new hair cycle, and/or prolonging the active growth phase (anagen) of the hair cycle and/or increasing the growth rate of the hair and/or sing the width of hair shaft, including, but not limited to, the induction of the growth of hair and making it more visible to the eye.
As used herein, "improving hair quality" means increasing the diameter of the hair shaft and/or enhancing the visual attributes of the hair like hair volume, hair shine and hair thickness, and/or affecting the teristics of the hair shaft and/or hair cuticles, including, but not limited to, creating a smoother look or feel, and/or increase in shine.
As used herein, "safe and effective amount" means an amount of a physiologically active nd or composition sufficient to induce a positive modification in the condition to be ted or treated, (e.g. hair growth) but low enough to avoid serious side effects.
The safe and effective amount of the compound or composition will vary with the particular condition being treated, the age and physical condition of the end user, the severity of the condition being treated/prevented, the duration of the treatment, the nature of other treatments, the ic compound or product/composition employed, the particular cosmetically-acceptable carrier utilized, and like factors.
Topical Compositions The topical compositions useful herein contain formulations suitable for topical application to the hair and scalp. In one ment, the composition contains a blackberry extract and a cosmeticallyacceptable topical r. In one embodiment, the cosmetically-acceptable topical carrier constitutes from about 75% to about 95%, by weight, of the composition more preferably from about 75% to about 85%, by weight, of the composition.
The compositions described herein may be made into a wide variety of product types that include but are not limited to solid and liquid compositions such as lotions, creams, gels, sticks, sprays, nts, ing liquid washes and solid bars, shampoos, pastes, powders, foams, mousses, and wipes. These product types may n several types of cosmetically acceptable topical carriers including, but not d to solutions, emulsions (e.g., microemulsions and nanoemulsions), gels, solids and liposomes. Non-limiting es of such carriers are set forth herein. Other carriers may be formulated by those of ordinary skill in the art.
The topical compositions useful herein can be formulated as solutions. Solutions should preferably include an aqueous solvent (e.g., from about 75% to about 95% or from about 75% to about 85% of a cosmetically acceptable aqueous solvent). More preferably, such compositions should contain about 30% solvent, although this may vary dependent upon the formulation. Such solvents may include ethanol, propylene glycol, polyethylene glycol, mixtures thereof and the like which are good carriers for successful delivery to the hair follicles.
Topical compositions useful in the methods described herein may be formulated as a solution ning an emollient. Such compositions preferably contain from about 2% to about 50% of an emollient(s).
As used herein, "emollients" refer to materials used for the tion or relief of s, as well as for the tion of the skin. A wide variety of suitable ents are known and may be used herein. The International Cosmetic Ingredient Dictionary and Handbook, Fourteenth Edition, 1012 Volume 3, eds.
Gottschlack and Breslawec, pp. 3868-80, published by Personal Care Products Council (hereinafter, "INCI Handbook"), which is hereby incorporated herein by A lotion may be made from a on. Lotions typically contain from about 1% to about 20% (more preferably, from about 5% to about 10%) of an emollient(s) and from about 50% to about 90% (more preferably, from about 60% to about 80%) of water.
Another type of product may be a solution that is a cream. A cream typically comprises from about 5% to about 50% (more preferably, from about 10% to about 20%) of an emollient(s) and from about 45% to about 85% (more preferably, from about 50% to about 75%) of water.
Yet another type of product that may be formulated from a solution is an ointment. An ointment may be constituted of a simple base of animal or vegetable oils or semi-solid arbons. An ointment may contain from about 2% to about 100% of an ent(s), and from about 0.1% to about 2% of a thickening s). The INCI Handbook ns a list of acceptable thickening agents or viscosity increasing agents useful in the compositions and methods described herein at pages 1693 through 1697.
The topical compositions useful in the methods described herein may also be preferably formulated as emulsions. If the carrier is an emulsion, from about 1% to about 10% (preferably from about 2% to about 5%) of the carrier should be made up one or more fiers.
Emulsifiers may be nonionic, anionic or cationic.
Suitable emulsifiers may be found in, for example, the INCI Handbook, pp. 3816-191 and 7.
Lotions and creams may also be formulated as emulsions. Typically such lotions preferably contain from 0.5% to about 5% of an emulsifier(s). Such creams would typically comprise from about 1% to about 20% (preferably from about 5% to about 10%) of an ent(s); from about 20% to about 80% (preferably, from 30% to about 70%) of water; and from about 1% to about 10% (preferably, from about 2% to about 5%) of an emulsifier(s).
Single emulsion skin care preparations, such as lotions and creams, of the oil-in-water type and waterin-oil type are well-known in the cosmetic art and are useful in the methods described herein. Multiphase emulsion itions, such as the water-in-oil-in-water type are also useful in the methods described herein. In general, such single or multiphase emulsions contain water, emollients, and emulsifiers as essential ingredients.
Compositions bed herein may also be in the form of shampoo, hair conditioning products, leave-on hair masks, mousse, sprays, in combination with dyes and other hair care ts for ng, treating, conditioning and coloring the hair aneous with topical application of the novel compositions bed herein.
The topical compositions described herein may be formulated as a gel (e.g., an aqueous gel using a suitable gelling agent(s)). Suitable gelling agents for aqueous gels include, but are not limited to, natural gums, acrylic acid and acrylate polymers and copolymers, and cellulose derivatives (e.g., hydroxymethyl cellulose and hydroxypropyl cellulose). Suitable gelling agents for oils (such as mineral oil) include, but are not limited to, hydrogenated ne/ethylene/styrene copolymer and hydrogenated ethylene/propylene/styrene copolymer. Such gels typically comprises between about 0.1% and 5%, by weight, of such gelling .
Microgels may be used to enhance follicular delivery of the formulations.
The topical compositions bed herein may also be formulated into a solid formulation (e.g., a waxbased stick, mascara, soap bar composition, powder, or a wipe containing powder.
The topical compositions useful in the methods described herein may contain, in addition to the aforementioned components, a wide variety of onal oil-soluble, organic solvent-soluble, and/or watersoluble materials conventionally used in compositions for use on skin and hair, at their art-established levels. For example, a formulation of 70% ethanol and 30% propylene glycol or variable amounts of these two agents may be used for ed delivery of the actives.
Surfactants In one ment, the composition described herein contains one or more tants. In one embodiment, the composition contains a lathering surfactant. What is meant by a "lathering surfactant" is a surfactant that generates lather when combined with water and mechanically agitated. In one embodiment, the lathering surfactant has an initial foam height reading of at least 20 mm, such as at least 50 mm, in the Standard Test Method for Foaming Properties of Surface-Active Agents D1173-53 Set forth in the ASTM Annual Book of ASTM Standards 1001 Section 15 Volume 15.04 (using a concentration of 5 grams per liter, temperature of 49° C., and water ss of 8 grains per gallon). Examples of lathering surfactants include, but are not limited to, anionic, nonionic, ic, and amphoteric lathering surfactants. miting examples of anionic lathering surfactants include those selected from the group consisting of inates, sulfates, isethionates, taurates, phosphates, lactylates, and glutamates.
Specific es include, but are not limited to, those selected from the group consisting of sodium lauryl sulfate, ammonium lauryl sulfate, ammonium laureth sulfate, sodium laureth sulfate, sodium trideceth sulfate, ammonium cetyl sulfate, sodium cetyl sulfate, ammonium cocoyl isethionate, sodium lauroyl onate, sodium lauroyl lactylate, anolamine l lactylate, sodium caproyl lactylate, sodium lauroyl sarcosinate, sodium myristoyl sarcosinate, sodium cocoyl sarcosinate, sodium lauroyl methyl taurate, sodium cocoyl methyl taurate, sodium lauroyl glutamate, sodium myristoyl glutamate, and sodium cocoyl glutamate and mixtures thereof.
Non-limiting es of nonionic lathering surfactants include those selected from the group consisting of alkyl glucosides, alkyl polyglucosides, polyhydroxy fatty acid amides, alkoxylated fatty acid esters, ing sucrose esters, amine oxides, and es thereof. ic examples include, but are not limited to, nonionic surfactants to those selected form the group consisting of C8-C14 glucose amides, C8-C14 alkyl polyglucosides, sucrose cocoate, sucrose laurate, lauramine oxide, cocoamine oxide, and mixtures thereof.
Non-limiting examples of amphoteric lathering surfactants (which also es zwitterionic lathering surfactants are those selected from the group consisting of es, sultaines, hydroxysultaines, alkyliminoacetates, iminodialkanoates, aminoalkanoates, and mixtures thereof.
Non-limiting examples of amphoteric surfactants described herein include disodium lauroamphodiacetate, sodium lauroamphoacetate, cetyl dimethyl betaine, cocoamidopropyl betaine, cocoamidopropyl hydroxy sultaine, and mixtures thereof.
Additional ically Active Agents In one embodiment, the compositions described herein may r contain one or more additional cosmetically active agent(s) as well as the abovementioned components. What is meant by a "cosmetically active agent" is a compound, which may be a synthetic compound or a compound isolated, purified or concentrated from a natural source, or a natural extract ning a mixture of compounds, that has a cosmetic or eutic effect on the tissue, including, but not limited to: icrobial agents such as anti-yeast agents, anti-fungal, and anti-bacterial agents, antiinflammatory agents, anti-aging agents, anti-parasite agents, external analgesics, sunscreens, photoprotectors, antioxidants, keratolytic agents, detergents/surfactants, moisturizers, nts, vitamins, ls, energy enhancers, anti-perspiration agents, astringents, hair growth enhancing agents, hair coloring agents, pigments, firming agents, agents for skin conditioning, and odor-control agents such as odor masking or pH-changing agents.
In one embodiment, the cosmetically active agent may be selected from, but not limited to, the group consisting of hydroxy acids, benzoyl peroxide, D- panthenol, octyl methoxycinnimate, titanium dioxide, octyl salicylate, homosalate, avobenzone, carotenoids, free radical scavengers, spin traps, retinoids such as retinoic acid (tretinoin) and id precursors such as retinol and retinyl palmitate, vitamins such as n E (alpha, beta or delta tocopherols and/or their mixtures) des, polyunsaturated fatty acids, ial fatty acids, enzymes, enzyme inhibitors, minerals, hormones such as progesterones, steroids such as hydrocortisone, 2-dimethylaminoethanol, metal (including but not limited to iron or zinc) salts such as copper chloride, peptides containing copper such as Cu:Gly-His-Lys, coenzyme Q10, amino acids, vitamins, acetyl-coenzyme A, niacin, riboflavin, thiamin, ribose, electron transporters such as NADH and FADH2, botanical extracts such as aloe vera, feverfew, and soy, and derivatives and mixtures thereof. The cosmetically active agent will preferably be present in the composition bed herein in an amount of from about 0.001% to about 20% by weight of the composition, more preferably, from about 0.005% to about 10% and most preferably, from about 0.01% to about 5%.
Also expected to be particularly effective in the compositions and methods described herein are the presence of synthetic or l 5-alpha reductase inhibitors, or other anti-sebum ingredients ing, but not limited to, Sepicontrol (Capryloyl Glycine, ine and Cinamomum Zeylanicum Bark Extract), licorice powder or extract, and the like. MC5 receptor antagonists may also be utilized in the compositions described herein. Examples of MC5-R antagonists may be found in U.S. Pat. 49,331.
The compositions bed herein may also be utilized in combination with compounds known to promote hair growth that are available as drugs, such as finasteride (Propecia), a type 2 5-alpha-reductase inhibitor, and dutasteride, a type 1- and 2alphareductase tor, as well as flutamide, bicalutamide, pregnane derivatives, terone derivatives, mental agents such as FCE 28260 and the like.
Spironolactone and other diuretics may also be utilized as it is indicated for women in some cases (also known as Aldactone: an aldosterone receptor antagonist).
Potassium channel openers, such as Minoxidil (Rogaine), which are known to promote hair growth, are also believed to be especially promising combinations.
Herbal remedies that may have 5-alpha reductase inhibitory action may include: Saw Palmetto and Pygeum africanum. Other agents that may have such activity are Beta-sisterol, Sepicontrol and Licorice, gamma-linolenic acid and other unsaturated fatty acids (Tehming LIANG and Shutsung LIAO) m. J. (1992) 285, 557-562, Inhibition of steroid 5-alpha-reductase by specific aliphatic unsaturated fatty acids), Zinc and Zinc salts, green tea catechin (−)-epigallocatechin gallate (EGCG) and other polyphenols, and the like. Grape seed, apple seed, apple juice and barley extracts may also be potential agents that may induce hair growth, although they are not thought to be very (s) or satisfactory in achieving satisfactory results (Takahashi et al., Procyanidin Oligomers Selectively and Intensively Promote Proliferation of Mouse Hair Epithelial Cells In Vitro and Activate Hair Follicle Growth In Vivo, J Invest Dermatol 112:310-316).
Additional ations may e other known ators of hair growth, such as, zinc, calcineurin inhibitors such as FK506 (Tacrolimus, Fujimycin), a ide antibiotic produced by Streptomyces tsukubaensis, and its derivatives, or Cyclosporin A, a cyclic endecapeptide and a T cell-specific suppressant, and the like.
Active ingredients in Provillus, a product suggested to block DHT (Vitamin B6, Biotin, Magnesium, Zinc, Saw Palmetto, Nettle, Gotu Kola, Pumpkin, Eleuthero Root, Uva-Ursi, Muria Puama) may also be included in the compositions described .
Examples of vitamins that may be constituents of the compositions described herein include, but are not limited to, vitamin A, vitamin Bs such as vitamin B3, vitamin B5, and vitamin B12, vitamin C, vitamin K, n E such as alpha, gamma or delta-tocopherol, and derivatives (such as salts and esters) and es thereof.
Examples of hydroxy acids include, but are not limited, to glycolic acid, lactic acid, malic acid, salicylic acid, citric acid, and tartaric acid. Such hydroxy acids, it is believed, serve to support the regeneration of the us layer of the scalp. We also believe that such hydroxy acids assist in normalizing the pH of the compositions described herein and may, as with lactic acid, add a conditioning effect to the hair.
Examples of antioxidants which may be utilized in the compositions and methods described herein include, but are not limited to, water-soluble antioxidants such as sulfhydryl compounds and their derivatives (e.g., sodium sulfite and N-acetyl-cysteine), lipoic acid and dihydrolipoic acid, resveratrol, lactoferrin, and ascorbic acid and ascorbic acid derivatives (e.g., ascorbyl palmitate and ascorbyl polypeptide). Oilsoluble antioxidants le for use in the compositions described herein include, but are not limited to, butylated hydroxytoluene, retinoids (e.g., retinol and retinyl palmitate), different types of tocopherols (e.g., alpha-, gamma-, and delta-tocopherols and their esters such as acetate) and their mixtures, tocotrienols, and ubiquinone. Natural ts ning antioxidants le for use in the compositions described herein, include, but not limited to, extracts containing flavonoids, isoflavonoids, and their derivatives such as genistein and daidzein (e.g., such as soy and clover extracts, extracts containing resveratrol and the like. Examples of such natural extracts include grape seed, green tea, pine bark, and propolis. terones, and naturally-derived ingredients with progesterone-like activity, on the other hand, may be useful, as well as astringents such as witch hazel, triclosan, cerulenin, alpha-methylene-gamma- butyralactone, glycine derivatives such as capryloylglycine and glycine, salicylic acid, or l peroxide.
Fabao 101, which has the following active ingredients, may also be included in the compositions described herein: Aralia Quinquetolia, Astragalus hyllos, Angelica Arhangelica Root, Salvia Officinalis, Capsicum, Carya Alba, Corthamis rius, Cortex dictamni radicis, Flos Chrysanthemum, Heshouwu, ist Ginseng, Miltiorrhizae, nseng, Paorulca Glandulosa, Peach Kernel Oil, Rhizome of an Lovage, Radix astragali, Radix Ginseng, Radix Polygoni Multiflori, Red-rooted Salvia, Rhizhoma gastroidia ginseng, Seu radix notopterygii, Sophera flavescens.
Other Materials Various other materials may also be present in the compositions useful in the methods bed herein.
These include humectants, proteins and polypeptides, preservatives and an alkaline agent. Examples of such agents are disclosed in the INCI Handbook, pp. 1650- 1667. The compositions described herein may also comprise chelating agents (e.g., EDTA) and preservatives (e.g., parabens). Examples of suitable preservatives and chelating agents are listed in pp. 1626 and 1654-55 of the INCI Handbook. In addition, the topical itions useful herein can contain conventional cosmetic adjuvants, such as dyes, opacifiers (e.g., titanium dioxide), pigments, and nces.
Darkening Agents In one embodiment, the compositions described herein further contain darkening agents such as melanin or tic melanin derivatives, or melanin-like molecules, vanillin polymers, natural extracts such as, but not limited to Coleus Forskoli extract, e-P extract, extracts from natural sources containing pigments (e.g., brown pigments from plants from the Hedychium genus or Bearberry genus or yellow, orange and red pigments, from plants containing carotenoids or canthaxanthins); or synthetic chemicals such as nds containing copper (e.g., copper salts such as CuCl2) or synthetic carotenoids or canthaxantins. es of synthetic melanin derivatives are set forth in U.S. Pat. Nos. 5,618,519, 5,384,116, and 5,227,459.
Examples of soluble melanin tives are set forth in 125, 435, 5,218,079, and 5,216,116. Examples of commercially available soluble n derivatives include Melasyn-100™ from San-mar laboratories, Inc.
(Elmsford, N.Y.) and MelanZe™ from Zylepsis (Ashford, Kent, United Kingdom).
These agents will preferably be present in the composition in an amount from about 0.001% to about 10% by weight, in particular in an amount from about 0.01% to about 5% by weight.
In another embodiment, the composition may include a peptide. Examples of darkening peptides are set forth in U.S. Pat. No. 7,025,951. The peptide described herein set forth therein may be provided in the form of cosmetically acceptable salts. Examples of preferred salts are those with therapeutically acceptable organic acids, e.g., , palmitic, oleic, stearic, lactic, , , malic, ascorbic, succinic, benzoic, salicylic, methanesulfonic, or Palmoic acid, as well as polymeric acids such as tannic acid or carboxymethyl cellulose, and salts with inorganic acids such as the hydrohalic acids (e.g., hydrochloric acid), sulfuric acid or phosphoric acid.
The amount of peptide present in the composition depends on the peptide used. The peptide should be present in the composition in an amount from about 0.001% to about 10% by weight, in particular in an amount from about 0.005% to about 5% by weight.
Mineral Water The itions described herein may be prepared using a mineral water, for example mineral water that has been naturally mineralized such as Evian® Mineral Water (Evian, France). In one ment, the mineral water has a mineralization of at least about 200 mg/L (e.g., from about 300 mg/L to about 1000 mg/L). In one embodiment, the mineral water comprises at least about mg/L of calcium and/or at least about 5 mg/L of magnesium.
Methods of Use The compositions described herein may be utilized to induce hair growth by topical application of said compositions to the area of the body on which hair growth is desired. Preferably, the compositions described herein are applied topically to the d area of the body at least once per day for at least five (5) days and more preferably on a daily basis for at least six weeks and most preferably, indefinitely. For ement to hair quality, said compositions should be d at least once per day for at least twelve weeks.
After about two weeks, the user may begin to observe increased hair growth and may be able to observe sed hair shaft diameter and/or enhanced visual attributes of the hair, such as hair volume, hair shine and hair thickness.
Examples Example 1 A gel base formula A1 was ed according to Table 1 below: The following ingredients were combined in a mixing vessel: DI water, Disodium EDTA, Glycerin, Dimethicone and Butylated Hydroxytoluene (BHT) and heated to 40-45°C while using prop mixing at medium to high speed (sweep blade) and mixed until uniform. Once a temperature below 40°C was achieved the following ingredients were added one at a time with prop mixing (sweep blade, medium speed): Sepigel 305, Phenonip XB. The pH was adjusted to .0 with Sodium Hydroxide.
Table 1 INCI Name gms Water 364.5 Disodium EDTA 10.00 in 30.00 Dimethicone 20.00 Butylated Hydroxytoluene Polyacrylamide & Laureth 7 & C13 - 14 65.00 Isoparafin Phenoxyethanol & Methylparaben & .00 Propylparaben & Ethylparaben NaOH, 20% w/w in water Example 2 A composition ning blackberry extract (A2) and a composition containing only butylene glycol and water (A3) were prepared in accordance with the procedure set forth in Example 1 with the following formulas set forth in Table 2.
Table 2 A2 A3 INCI Name %w/w %w/w Rubus fruticosus 50.00 0.00 Butylene Glycol 25.00 25.00 Water 25.00 75.00 Total 100 100.00 Example 3 Compositions E1 and C were ed according to the following formula in Table 3. Inventive example E1 was prepared by combining the gel base A1 of Example 1 and the Blackberry extract composition A2 of Example 2 to yield a concentration of 25% blackberry extract (a 1:1 ratio of A1 and A2) by mixing until uniformity was ed. Additionally, comparative example C1 was prepared by combining gel base A1 and A3 of Example 2.
Table 3 E1 C1 %w/w %w/w 50.00 50.00 A2 50.00 0 A3 0.00 50.00 Total 100 .00 100.00 Example 4 Hair growth induction in C3H mice with Blackberry (Rubus fruticosus) extract Hair growth induction in C3H mice was measured as a percentage of mice entering the anagen phase as a function of time (days of study).
C3H female mice age 6-7 weeks was purchased from Taconic Farms (Germantown, NY). Mice were housed in appropriately sized cages in an nmentally lled room with a 12-hour lighthour dark eriod and supplied with food and water ad libitum.
Animal care was based on the "Guide for the Care and Use of Laboratory Animals", NIH Publication No. 85-23.
Animals were acclimated for a week before study starts.
Once all mice have entered their prolonged telogen/resting phase (about 50-60 days long) of the hair cycle, they were clipped over the dorsal area about 1.5 x 5cm (Wahl Clippers 8900 Series, Blade # 1086).
Four female mice per group were clipped while sedated with 2% induction and maintenance isoflurane and 0.5L . In addition to E1 (250mg/ml Rubus fruticosus formulation), the treatment groups included a placebo (C1) and an untreated group (n=4) to serve as control for natural hair growth tion and to observe placebo effects and 200µl of test materials were applied topically to the area daily, five days a week (Monday through ). Images were taken at the first signs of anagen/active growth phase and when needed based on visual observation. A study log documenting -day observations of mice entering anagen (grey skin) was recorded. Treatments continued for up to about 8 weeks.
Table 4 HAIR GROWTH INDUCTION IN C3H MICE REPRESENTING % OF MICE ENTERING ANAGEN AS A FUNCTION OF TIME (DAYS OF STUDY) Groups/Day % mice entering anagen 7 8 9 10 14 20 22 23 24 29 31 35 42 43 44 45 46 50 Untreated (n=4 animals) 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 0 % Symmatrix (n=4 animals) (E1) 50 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 100 rix Placebo (n=4 animals)(C1) 0 0 0 0 0 0 0 0 0 0 0 0 0 25 50 50 75 100 Most effective of % Minoxidil (N=4 studies) 0 0 20 40 80 80 80 80 75 100 100 100 100 100 100 NA NA NA Minoxidil (N=4 studies) 0 0 7 18 31 32 41 38 36 36 45 48 63 87 93 NA NA NA Number of animals per group for Minoxidil reference: Day 7-22 (N=7), Day 23-26 (N=6), Day 27-44(N=5) NA=Not Assessed Surprisingly the Rubus osus topical treatment (E1) induced hair growth in all the C3H mice by day 8.
When evaluations are compared against a commercially available hair growth t (5% Generic Minoxidil Solution for Men purchased from Eckerd Pharmacy) using the same test model, the induction with E1 topical application occurred faster and at a higher incidence/responder rate. On average about 63% of mice d with 5% marketed Minoxidil entered anagen by week 6 (N=4 studies) with 100% by week 4 (Day 29) where Minoxidil performed the best as a positive control.
Hence, we conclude that the hair growth induction occurred faster and at a higher incidence when treated with E1 resulting in a 100% responder rate at eight (8) days ed with 5% marketed Minoxidil where on average about 63% of mice (n=4 studies) entered anagen by week 6 and with 100% by week 4 (Day 29) where Minoxidil performed the best as a positive control.
Example 5 Medium consisting of ms E medium (minus glutamine), L-glutamine, Fungizone, penicillin and streptomycin (supplied by Gibco) was prepared. A stock solution of Blackberry extract and medium was prepared. 1:10 serial dilutions of the stock solution were prepared until the appropriate concentration was achieved.
Human terminal hair follicles are ed from fresh facial cosmetic surgery samples. Individual follicles are placed into 12 well Falcon insert cell culture plates in a 0.4um insert filled with 0.5ml of medium. ents are added to the medium using a w/v calculation. Medium is d every other day. Images are taken on Day 0, 1, 3, 5, 7 & 9. Image analysis is done by measuring the length of the hair shaft. Means of each group and percent increases are calculated.
Table 5 Treatment N % change over untreated Untreated 9 0 erry Ext. 0.01% 10 -4.278326281 Blackberry Ext. 0.001% 7 63.6577339 Blackberry extract (Rubus fruticosus) at 0.001% (w/v) was able to increase hair shaft elongation by 63.65% compared to follicles grown medium without the blackberry extract.
Example 6 Human hair follicles were isolated from fresh facial ic surgery samples. Individual follicles were placed into 6 well Falcon insert cell culture plates onto 0.4 µm inserts filled with 2.0 mL of medium.
The medium and a stock solution as in Example 5 were prepared. ents were added to the medium using a w/v calculation. Medium was changed every other day.
Images were taken on Day 0, 1, 3, 5, 7, and 9. Image analysis was done by measuring the length of the hair shaft. Means of each group and percent increases were calculated.
Table 6 ent N % Change over untreated Untreated 12 0 Blackberry Ext. 0.001% 5 51.936 Blackberry Ext. 0.001% 4 44.412 Blackberry Ext. 0.0001% 4 15.466 erry Ext. 0.05% 5 -27.4437 Blackberry extract (Rubus fruticosus) at concentration ranges between 0.0001% to 0.001% (w/v) was able to increase hair shaft elongation by more than 15% compared to follicles grown medium without the blackberry extract. It should be noted that, unexpectedly, blackberry extract at the higher concentration range of 0.05% did not increase hair shaft elongation.
The following embodiments were made using the formulations set forth in Table 7: INCI Name C2 C3 C4 C5 C6 C7 C8 C9 E2 E3 E4 E5 Water DI 88.97 88.9 64.9 64.67 63.4 75.97 74.97 73.97 79.4 79.17 60.3 69.8 7 7 7 7 Carbomer- 0.5 0.8 1 1.5 2 2.5 Acrylic Acid, Cyclohexan Sodium 2 Polyacryla te (and) Hydrogenat Polydecene Methulcell 5 ulose and Hydroxypro Methylcell ulose Lithium 2 3 4 Magnesium Sodium Silicate Dehydroxan 0.5 0.5 0.5 0.5 than Gum Butylene 2 2 2 Glycol Sodium q.s. q.s. q.s. q.s. q.s. q.s. q.s. q.s. q.s. q.s. q.s. q.s.
Hydroxide % Soln.
Glycerin 1 Glyceryl 24 24 24 10 10 10 10 10 20 10 Polymethac rylate extr 8.33 8.33 8.33 8.33 8.33 8.33 8.33 8.33 8.33 8.33 16.7 16.7 in (40%) Rubus Fruticosus (Blackberr y) Leaf (60%) Phenoxyeth 0.7 0.7 0.7 0.7 0.7 0.7 0.7 0.7 0.7 Sodium 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 Benzoate Phenoxyeth 1 1 1 enol (and) Caprylyl Glycol (and) Sorbic Polyacryla 1 1 1 mide (and) C13-14 Isoparaffi n (and) 100 100 100 100 100 100 100 100 100 100 100 100 Result Too too did insuf panc thin paste thick GEL Stabl Thin Gel thin thin not ficie ake grit e Gel Gel thic ntly mix ken thick with o clum form ps Each of the embodiment compositions set forth in Table 7 was independently prepared as follows: E2- E5: Water was measured into a main vessel and stirring with vortex initiated. Carbomer- Acrylic Acid, Cyclohexane was slowly added by screen sifting. The mixture was heated until the temperature reached 55- 60°C. A 20% Sodium Hydroxide solution was made. The pH was adjusted with a 20% Solution Sodium Hydroxide to pH 5.5-6 to neutralize the Carbomer. The heat was turned off and the mixture was cooled down to 45°C. The Maltodextrin (40%) Rubus Fruticosus (Blackberry) Leaf t (60%) was pre-mixed in Glyceryl Polymethacrylate. The Maltodextrin (40%) Rubus Fruticosus berry) Leaf Extract (60%), Glyceryl Polymethacrylate paste was added to the vessel with ng. The viscosity continued to decrease as it was added. The pH was adjusted with a 20% solution of Sodium Hydroxide to pH 5.5-6.0. The Phenoxyethanol (and) Caprylyl Glycol (and) Sorbic Acid were added to the beaker (Formulation C12 had Phenoxyethanol and Sodium Benzoate) with stirring. The pH was adjusted with a 20% Solution of Sodium Hydroxide to pH 5.5-6. QS with Water was performed. A gel was formed.
E-2 - A stable gel was formed and the formula passed 13 weeks stability. Stability was tested using a T spindle at 20 RPM for two weeks and four weeks. The s were kept at room ature, 4°C, 40°C and 50°C. The sample kept at 50°C was taken out of the test at six weeks and the other samples (room temperature, 4°C and 40°C) were read at eight weeks and 13 weeks. A freeze/thaw test was med on three cycles. As more (40%) Rubus Fruticosus (Blackberry) Leaf Extract (60%) is added, more Carbomer must be added.
C2 - For C2, the same ure was followed with the exception that Dehydroxanthan Gum was pre-wet with glycerin and slowly added to the vessel with stirring. The Maltodextrin (40%) Rubus Fruticosus (Blackberry) Leaf Extract (60%) was not pre-wet with Glyceryl Polymethacrylate. The preservative added was Phenoxyethanol and Sodium Benzoate.
C3 - For C3 the same procedure was followed with the exception of after the water was added to the vessel, it was heated until the temperature reached 55-60°C.
Methylcellulose and Hydroxy Propyl cellulose were slowly added with stirring for 30 minutes. The Maltodextrin (40%) Rubus Fruticosus (Blackberry) Leaf t (60%) was not pre-wet with Glyceryl Polymethacrylate. It was sprinkled in directly to the vessel.
C4 and C5- For C4 and C5, the same procedure was followed with the exception that rylamide (and) C13- 14 Isoparaffin (and) Laureth-7 was post added to the composition.
C6 - For C6, the same procedure was followed with the exception that Sodium Polyacrylate (and) Hydrogenated Polydecene was sprinkled in the water. Polyacrylamide (and) C13-14 Isoparaffin (and) Laureth-7 was post added to the formula.
C7, C8 and C9 - For C7, C8 and C9, the same procedure was followed with the addition of oxanthan Gum pre- wet in Butylene Glycol. Continued mixing and slowly added Lithium Magnesium Sodium Silicate. It was noted that as more Laponite was added to the composition, the consistency became more of a paste as opposed to becoming a gel).
The term "comprising" as used in this specification and claims means "consisting at least in part of". When interpreting statements in this specification, and claims which include the term "comprising", it is to be understood that other es that are additional to the features prefaced by this term in each statement or claim may also be present. Related terms such as "comprise" and "comprised" are to be interpreted in similar .
In this ication where nce has been made to patent specifications, other external documents, or other sources of information, this is generally for the purpose of providing a context for discussing the features of the ion. Unless spepcifically stated otherwise, reference to such external documents is not to be construed as an admission that such documents, or such sources of information, in any jurisdiction, are prior art, or form part of the common general knowledge in the art.
In the description in this specification reference may be made to subject matter that is not within the scope of the claims of the current application. That subject matter should be y identifiable by a person d in the art and may assist in putting into practice the invention as defined in the claims of this application.
Claims (5)
1. A method of enhancing hair growth by applying to the scalp, the skin, the eyelashes, eyebrows, mustache 5 region or beard region of a patient a topical composition comprising a tration of at least 90 mg extract/ml of solution but less than 300 mg/ml of a Rubus fruticosus leaf extract; and additionally comprising at least 1 weight percent of carbomer by 10 weight of the composition, wherein the extract is produced by a method having the following steps: a. addition to erry leaves of an extractant containing water and l, wherein the extractant contains ethanol and water in a ratio 15 of 2:8 to 8:2 by weight; and b. extraction of the blackberry leaves with the extractant for up to 72 hours at an extraction temperature in the range of from 80oC to 100oC.
2. A method according to claim 1 wherein said 20 composition ses a concentration of at least 120 mg/ml but less than 300 mg/ml of a Rubus fruticosus leaf extract.
3. A method according to claim 1 or 2 n said composition comprises a concentration of at least 25 250 mg/ml but less than 300 mg/ml of a Rubus fruticosus leaf extract.
4. A method according to any one of claims 1-3 n said composition further comprises skin care agents consisting of vitamins, minerals, proteins, 30 peptides, fatty acids, antioxidants, anti- inflammatory agents, darkening agents, botanical ts and mixtures thereof.
5. A method as claimed in claim 1 substantially as herein described or exemplified.
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US13/765,498 US8962041B2 (en) | 2013-02-12 | 2013-02-12 | Methods and compositions for enhancing hair quality using blackberry extract |
NZ71098514 | 2014-02-10 |
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NZ729134A true NZ729134A (en) | 2021-12-24 |
NZ729134B2 NZ729134B2 (en) | 2022-03-25 |
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