Anti-gray hair care composition
By combining taurine glucoside, N-acetyltyrosine, and PPAR[α] activator in the hair care composition, the problems of hair pigmentation and aging are addressed, resulting in significant improvements in hair health and a reduction in oxidative stress.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- UNILEVER IP HLDG BV
- Filing Date
- 2024-12-20
- Publication Date
- 2026-07-14
AI Technical Summary
Existing technologies are insufficient to effectively reduce age-related functional changes in hair pigmentation while providing improvements in age-related hair characteristics, and chemical hair dyes lead to increased hair damage.
Taxiardin glucoside is combined with N-acetyltyrosine and lipid peroxidase proliferator-activated receptor (PPAR) [α] activator in hair care compositions to enhance antioxidant activity, protect melanocytes, reduce oxidative stress, and improve hair health.
It significantly reduces gray hair formation, restores hair pigmentation, enhances hair growth, increases hair volume and thickness, reduces hair loss, improves scalp health, reduces oxidative stress, and synergistically improves various age-related hair characteristics.
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Abstract
Description
Technical Field
[0001] This invention relates to hair care compositions, particularly anti-gray hair care compositions. Background Technology
[0002] As people age, the appearance of their hair may become less desirable. Graying and whitening of hair are common signs of aging. Hair also loses its elasticity, becoming thinner and more fragile. In addition, the diameter of hair follicles and the number of hairs may decrease, resulting in a sparse appearance of the scalp.
[0003] For many consumers, maintaining hair color and good thickness, fullness, and hair count is a way to mitigate signs of aging. Many people choose to dye their hair to cover up age-related graying or whitening. However, hair coloring does not help mask other age-related changes in hair quality. On the contrary, chemical hair dyes are known to cause increased hair damage over time.
[0004] Therefore, EP3873483A1 describes a hair care active agent containing taxifolin glucoside and N-acetyltyrosine, which can provide some reduction in the appearance of gray and white hair in individuals. In EP3873483A1, the hair care active agent was found to reduce the average number of white hairs by 17% after 4 months.
[0005] However, despite the existence of such existing technologies, there has long been a need to provide consumers with compositions that effectively reduce age-related functional changes in hair pigmentation. There is also a need for compositions that can also reduce or prevent other harmful changes in age-related hair.
[0006] Surprisingly, it was found that when the taurine glucoside and N-acetyltyrosine of the present invention are combined with lipid peroxidase proliferator-activated receptor (PPAR) [α] activators, an effective reduction in age-related functional changes in hair pigmentation can be achieved, while also providing beneficial improvements in further age-related hair characteristics.
[0007] In particular, it was surprisingly found that when the taurine glucoside and N-acetyltyrosine of the present invention are combined with lipid PPAR[α] activators, the antioxidant activity of the hair care composition can be increased and the oxidative stress of melanocytes in the scalp / hair follicles can be reduced.
[0008] Increased antioxidant activity in melanocytes is associated with reduced and / or delayed gray hair formation. Oxidative stress is known to damage melanocytes, leading to graying of hair. Enhanced antioxidant activity helps neutralize reactive oxygen species (ROS), thereby reducing oxidative damage to melanocytes and gray hair formation. Furthermore, enhanced antioxidant defense better protects melanocytes and their precursor cells in the hair follicles of the scalp from oxidative stress. This protection helps maintain melanocyte function, lifespan, and melanin production for a longer period. Increased antioxidant activity is also known to be associated with restoration of pigmentation in gray hair due to reduced ROS levels, protection of melanocyte reservoirs, and reactivation of melanin production.
[0009] In addition, reducing oxidative stress in the scalp / hair follicles is also associated with improving other age-related hair characteristics, such as reducing hair loss and / or enhancing the growth of stronger hair. Summary of the Invention
[0010] In a first aspect, the present invention relates to a hair care composition comprising: (i) Taxonitrile glucoside; (ii) N-acetyltyrosine; and (iii) At least one lipid peroxisome proliferator-activated receptor (PPAR) [α] activator, selected from: C10-C18 saturated fatty acids, preferably branched, or, if straight-chain, preferably hydroxylated; C10-C20 monounsaturated fatty acids; and C10-C22 polyunsaturated fatty acids.
[0011] In a further aspect, the present invention relates to the non-therapeutic uses of the hair care compositions of the present invention for reducing the appearance of gray or white hair in an individual, for reducing age-related functional changes in hair pigmentation, for increasing melanin production in gray hair, for increasing cell proliferation, for increasing melanocyte proliferation, for increasing melanosome transfer, for increasing tyrosinase levels and / or activity, for increasing gene and / or protein expression in hair-related pigmentation pathways, for increasing hair volume, for increasing hair thickness, for increasing hair count, for increasing hair strength, for reducing hair loss and / or for hair fiber repair, for improving scalp health, for reducing scalp inflammation, for reducing scalp itching, for reducing oxidative stress in the scalp / hair follicles, for reducing oxidized lipid substances in the scalp / hair follicles, for improving sebum control, for improving the scalp barrier and / or for improving the microbiome balance of the scalp.
[0012] In a further aspect, the present invention relates to a method for reducing the presence of gray or white hair in an individual, reducing age-related functional changes in hair pigmentation, increasing melanin production in gray hair, increasing cell proliferation, increasing melanocyte proliferation, increasing melanosome transfer, increasing tyrosinase levels and / or activity, and / or increasing gene and / or protein expression in hair-related pigmentation pathways, increasing hair volume, increasing hair thickness, increasing hair count, increasing hair strength, reducing hair loss, providing hair fiber repair, improving scalp health, reducing scalp inflammation, reducing scalp itching, reducing oxidative stress in the scalp / hair follicles, reducing oxidized lipid substances in the scalp / hair follicles, improving sebum control, improving the scalp barrier, and / or improving the scalp microbiome balance, said method comprising applying the hair care composition of the present invention to the scalp or hair.
[0013] Preferably, the present invention provides a non-therapeutic use of the hair care composition of the present invention for reducing oxidative stress in melanocytes, preferably in hair follicles and / or scalp. Preferably, the present invention provides a non-therapeutic use of the hair care composition of the present invention for reducing oxidized lipid substances on the scalp.
[0014] Preferably, the present invention provides a method for reducing oxidative stress in melanocytes, preferably in hair follicles and / or scalp, the method comprising applying the hair care composition of the present invention to the scalp or hair. Preferably, the present invention provides a method for reducing oxidized lipid substances on the scalp, the method comprising applying the hair care composition of the present invention to the scalp or hair.
[0015] Surprisingly, the combination of components in the hair care composition of the present invention provides a reduction in the appearance of gray or white hair in an individual. In some embodiments, the components of the hair care composition provide a synergistic reduction in gray or white hair in an individual. In some embodiments, the combination of components in the hair care composition of the present invention provides a reduction in age-related functional changes in hair pigmentation. In some embodiments, the components of the hair care composition provide a synergistic reduction in age-related functional changes in hair pigmentation. For example, advantageously, the hair care composition of the present invention can provide increased melanin production, such as a synergistic increase in melanin production. The hair care composition of the present invention advantageously provides an increase in cell proliferation, such as an increase in melanocyte proliferation, such as a synergistic increase in melanocyte proliferation. The hair care composition of the present invention advantageously provides enhanced melanosome transfer from melanocytes to keratinocytes, such as a synergistic enhancement in melanosome transfer from melanocytes to keratinocytes. The hair care composition of the present invention advantageously provides enhanced tyrosinase levels and / or activity, such as a synergistic enhancement in tyrosinase levels and / or activity. Furthermore, the hair care compositions of the present invention can advantageously provide increased gene and / or protein expression (e.g., MITF, QYR, TYRP1, MSH, MC1R) in the pigmentation pathway, such as a synergistic increase in gene and / or protein expression in the pigmentation pathway.
[0016] The beneficial effects of the hair care compositions of the present invention described above can surprisingly lead to an observable reduction in high levels of age-related functional changes in individual hair pigmentation and / or the appearance of gray or white hair.
[0017] In addition to reducing age-related functional changes in hair pigmentation, the combination of ingredients in the hair care compositions of the present invention also provides beneficial improvements in other age-related hair properties. For example, the hair care compositions of the present invention can provide a beneficial increase in hair volume, such as a synergistic increase in hair volume. The hair care compositions of the present invention can provide a beneficial increase in hair thickness, such as a synergistic increase in hair thickness. The hair care compositions of the present invention can provide a beneficial increase in hair count, such as a synergistic increase in hair count. The hair care compositions of the present invention can provide a beneficial increase in hair strength / reduction in hair loss, such as a synergistic increase in hair strength / reduction in hair loss. The hair care compositions of the present invention can also provide observable hair fiber repair, such as a synergistic hair fiber repair.
[0018] In addition to reducing age-related functional changes in hair pigmentation, the combination of ingredients in the hair care compositions of the present invention also provides beneficial improvements in scalp health. For example, the hair care compositions of the present invention can provide a beneficial reduction in scalp inflammation, such as a synergistic reduction in scalp inflammation. The hair care compositions of the present invention can also provide a beneficial reduction in scalp itching. The hair care compositions of the present invention can also provide a beneficial scavenging of reactive oxygen species (ROS), resulting in a reduction in oxidative stress in the scalp / hair follicles, such as a synergistic reduction in oxidative stress in the scalp / hair follicles. The hair care compositions of the present invention can also provide a beneficial reduction in oxidized lipid substances in the scalp / hair follicles, such as a synergistic reduction in oxidized lipid substances in the scalp / hair follicles. The hair care compositions of the present invention can also provide beneficial improvements in sebum control, such as a synergistic improvement in sebum control. The hair care compositions of the present invention can also provide beneficial improvements in scalp health and barrier properties, such as a synergistic improvement in scalp health and barrier properties. The hair care compositions can also provide beneficial improvements in scalp microbiome balance, such as a synergistic improvement in scalp microbiome balance. Detailed Implementation
[0019] The aspects and embodiments of the invention will now be discussed. Further aspects and embodiments will be apparent to those skilled in the art. All references herein are incorporated by way of citation.
[0020] In this invention, the term "extract" refers to any isolated substance obtained by extraction from a raw material. For example, an extract is obtained by dissolving the raw material in a solvent (e.g., water or alcohol) and then concentrating and / or purifying the substance separated from the raw material, such as by evaporating the solvent.
[0021] (i) Taxifenesin glucoside The compositions of the present invention contain taurine glucoside.
[0022] Preferably, at least a portion of the taxonomycin glucoside is taxonomycin α-D-glucoside. A suitable method for preparing taxonomycin α-D-glucoside is described in WO 2007 / 144368.
[0023] In a preferred embodiment, the hair care composition of the present invention further comprises taurine.
[0024] For example, a mixture of taxine and taxine glucoside can be prepared by stopping the reaction according to WO 2007 / 144368 before complete conversion, for example after about half of the taxine has been converted to obtain a mixture of about 1:1.
[0025] Taxifenin glucoside and taxifenin may be present in a weight ratio of 100:0 to about 40:60. Preferably, the weight ratio of taxifenin glucoside to taxifenin is 90:10 to 40:60, more preferably 70:30 to 50:50, and most preferably about 60:40.
[0026] The amount of taurine glucoside in the hair care composition of the present invention may be, for example, 0.0001% to 0.50% of the total weight of the composition, more preferably 0.0005% to 0.025% of the total weight of the composition, more preferably 0.0007% to 0.009% of the total weight of the composition, such as 0.0009% to 0.007% of the total weight of the composition, such as 0.001% to 0.004% of the total weight of the composition, such as 0.001% to 0.002% of the total weight of the composition.
[0027] In the hair care composition of the present invention, a portion of the taurine glucoside may be replaced by taurine. In particular, up to 60%, preferably up to 50%, and even more preferably up to 40% of the taurine glucoside may be replaced by taurine.
[0028] In some embodiments, the taxonaisin glucoside and / or taxonaisin of the present invention can be derived from European larch (Larix Europaea Wood). For example, taxonaisin glucoside and / or taxonaisin can be contained in European larch extract.
[0029] The amount of European larch extract in the composition is, for example, 0.0001% to 0.1% of the total weight of the composition, more preferably 0.001% to 0.01% of the total weight of the composition, and most preferably 0.002% to 0.008% of the total weight of the composition.
[0030] Preferably, the ratio of PPAR activator to European larch extract is 1:0.0001 to 1:1, more preferably 1:0.0005 to 1:0.1, and even more preferably 1:0.001 to 1:0.01. In some embodiments, the ratio of PPAR activator to European larch extract is 1:0.001 to 1:0.008.
[0031] (ii) N-acetyrosine The compositions of the present invention contain N-acetyltyrosine.
[0032] The amount of N-acetyltyrosine in the hair care composition of the present invention can be, for example, 0.01% to 30% of the total weight of the composition, more preferably 0.05% to 20% of the total weight of the composition, and even more preferably 0.1% to 5% of the total weight of the composition. Most preferably, it is 0.15% to 0.9% of the total weight of the composition, for example, 0.15% to 0.4% of the total weight of the composition.
[0033] In the hair care composition of the present invention, the weight ratio of taurine glucoside to N-acetyltyrosine is preferably 1:500 to 1:1, more preferably 1:300 to 1:50, and most preferably 1:200 to 1:100, for example about 1:150.
[0034] Compositions comprising taxine glucoside and / or N-acetyltyrosine can be as described, for example, in EP3873483A1 (incorporated herein by reference). Taxine glucoside and / or N-acetyltyrosine can also be supplied to the compositions of the present invention by means of the commercially available material Darkenyl™ from Givaudan.
[0035] (iii) Peroxisome proliferator-activated receptor activator The hair care composition of the present invention contains a peroxisome proliferator-activated receptor activator.
[0036] The term "peroxisome proliferator-activated receptor activator" refers to a compound, preferably a lipid, that activates the nuclear receptor PPAR. In this invention, the activated PPAR receptor is the [α] subtype. The PPAR [α] activator is a lipid.
[0037] Peroxisome proliferator-activated receptors (PPARs) are a known family of nuclear hormone receptors, with three subtypes [α], [β], and [γ] distributed across different tissues. The PPAR [α] subtype (hereinafter referred to as PPAR [α]) is present in the skin. Lipid activators of PPAR [α], such as linoleic acid, are well known in the art. These activators have been shown to accelerate the development of the skin-epidermal barrier in vitro (Hanley et al., (1997) J. Clin. Inv 100, 705-712). However, it is not disclosed or implied in the art that PPAR [α] activators may be used in cosmetic compositions to reduce the aforementioned age-related functional changes in hair.
[0038] One established and widely accepted method for demonstrating PPAR activation and thereby identifying PPAR lipid activators is reporter gene assays. Therefore, lipids acting as PPAR[α] activators can be readily identified by those skilled in the art as compounds that induce luciferase or chloramphenicol acetyltransferase (CAT) expression in reporter gene assays, the complete protocol of which is provided by Kliewer et al. (1992) Nature, 358, 771-774.
[0039] Therefore, if a lipid compound passes this in vitro reporter gene assay, i.e., it induces the expression of luciferase or CAT in the reporter gene assay, then it is a lipid PPAR[α] activator.
[0040] In a preferred embodiment of the invention, the lipid PPAR[α] activator is a compound that activates the reporter gene at least twice the background level.
[0041] The lipid PPAR[α] activators that meet the reporter gene assay criteria are selected from C10-C18 saturated fatty acids (preferably branched, or if straight, preferably hydroxylated), C10-C20 monounsaturated fatty acids, and C10-C22 polyunsaturated fatty acids.
[0042] Fatty acids can be straight-chain or branched, saturated or unsaturated, and can be substituted, for example, by hydroxylation, such as α-hydroxy or β-hydroxy derivatives. The corresponding alcohols, triglycerides, and phospholipids of any of these acids are also suitable for this invention. Preferred derivatives include those derived from the substitution of the carboxyl group of the acid, such as esters (e.g., triglycerides, monoglycerides, diglycerides, phosphate esters), amides (e.g., ceramide derivatives), and salts (e.g., alkali metal and alkaline earth metal salts, ammonium salts). In the case of triglyceride derivatives, all isomers at all positions on the glycerol backbone are included.
[0043] Oils rich in fatty acid triglycerides are therefore also suitable for this invention. Such oils are commercially available and include coriander seed oil (rich in apigenin), parsley seed oil (rich in apigenin), evening primrose oil (rich in gamma-linolenic acid), borage seed oil (rich in gamma-linolenic acid), shea butter (rich in oleic and linoleic acids), fish oil and its concentrates (rich in DHA and EPA), crambling oil (rich in erucic acid), flaxseed oil (rich in alpha-linolenic acid), almond oil (rich in oleic acid), and cottonseed oil (rich in linoleic acid).
[0044] According to the present invention, preferred PPAR[α] activators are 12-hydroxystearic acid, cis-octadecanoic acid, trans-7-octadecanoic acid, cis-5,8,11,14,17-eicosapentaenoic acid, cis-4,7,10,13,16,19-docosahexaenoic acid, conjugated linoleic acid (C9,T11), columbinic acid, trans-linolenic acid, trans-ricinoleic acid, octadecanoic acid, 2-hydroxystearic acid, α-linolenic acid, arachidonic acid, cis-11,14-eicosadienoic acid, conjugated linoleic acid (T10,C12), conjugated linoleic acid (T9,T11), and conjugated linoleic acid (C9,T11 and T10). (a 50:50 mixture of C12), coriander acid, transoleic acid, monocarboxylic acid, cinnamon oleic acid, stearylene acid, arborvitae extract or trans isoleic acid.
[0045] Other suitable PPAR activators include cis-11,14,17-eicosalicylic acid, cis-5-eicosalicylic acid, cis-8,11,14-eicosalicylic acid, hexadecanoic acid, palmitoleic acid, trans-rockapinic acid, trans-trans-farnesol, cis-13,16-docosadienoic acid, cis-isooleic acid, cis-11-eicosalicylic acid, cis-13,16,19-docosatrienoic acid, cis-13-octadecenoic acid, cis-15-octadecenoic acid, cis-7,10,13,16-docosatraenoic acid, transoleic acid, gamma-linolenic acid, geranilic acid, geraniylgeranilic acid, linoleic acid, oleic acid, rockapinic acid, phytanoic acid, terpineic acid, trans-13-octadecenoic acid, or tridecyl salicylic acid (TDS).
[0046] Other suitable PPAR activators include chickpea extract (red clover phytoestrogens), safflower extract, pomegranate saponifiable hydrolysate extract, buglossoides extract (octadecanoic acid plant extract), or zanthalene (extract from Sichuan pepper), thereby using any mixture of PPAR activators described herein within the scope of this invention.
[0047] In embodiments of the present invention, the lipid PPAR[α] activator is phellandic acid, conjugated linoleic acid, 12-hydroxystearic acid, ricinoleic acid, or a mixture thereof.
[0048] In the most preferred embodiment of the present invention, the lipid PPAR[α] activator is 12-hydroxystearic acid.
[0049] Typically, the lipid PPAR[α] activator accounts for 0.0001% to 8.0% of the composition by weight, for example 0.0002% to 8.0%, preferably 0.05% to 8.0%, more preferably 1% to 6%, and most preferably 1.5% to 4.5%. In embodiments of the invention, the composition has 1.5% to 4% by weight, and in yet another embodiment, 1.5% to 3.5% by weight of the PPAR activator.
[0050] Typically, 12-hydroxystearic acid accounts for 0.0001% to 8.0% of the composition by weight, for example 0.0002% to 8.0%, preferably 0.05% to 8.0%, more preferably 1% to 6%, and most preferably 0.5% to 4.5%. In embodiments of the invention, the composition has 0.8% to 4% by weight, and in yet another embodiment, 1% to 3% by weight of 12-hydroxystearic acid.
[0051] Preferably, the weight ratio of the lipid PPAR[α] activator to N-acetyltyrosine is 1:0.01 to 1:5; more preferably, the weight ratio is 1:0.02 to 1:3; and even more preferably, 1:0.05 to 1:1. In some embodiments, the weight ratio is 1:0.06 to 1:0.2.
[0052] Preferably, the weight ratio of the lipid PPAR[α] activator to taxine glucoside is from 1:0.00001 to 1:1, more preferably from 1:0.0001 to 1:0.1, and even more preferably from 1:0.0002 to 1:0.01. In some embodiments, the weight ratio of the PPAR activator to taxine glucoside is from 1:0.0005 to 1:0.002.
[0053] Preferably, the weight ratio of 12-hydroxystearic acid to N-acetyltyrosine is from 1:0.01 to 1:5, more preferably from 1:0.02 to 1:3, and even more preferably from 1:0.05 to 1:1. In some embodiments, the weight ratio of 12-hydroxystearic acid to N-acetyltyrosine is from 1:0.06 to 1:0.2.
[0054] Preferably, the weight ratio of 12-hydroxystearic acid to taxine glucoside is from 1:0.00001 to 1:1, more preferably from 1:0.0001 to 1:0.1, and even more preferably from 1:0.0002 to 1:0.01. In some embodiments, the weight ratio of 12-hydroxystearic acid to taxine glucoside is from 1:0.0005 to 1:0.002.
[0055] In an alternative preferred embodiment, the hair care composition comprises: (i) Taxonitrile glucoside; (ii) N-acetyltyrosine; and (iii) 12-hydroxystearic acid.
[0056] In a preferred embodiment, the hair care composition comprises: (i) 0.0005% to 0.25% of piperidine glucoside; (ii) 0.05% to 20% N-acetyltyrosine; and (iii) 0.0001% to 3% of 12-hydroxystearic acid.
[0057] In a preferred embodiment, the hair care composition comprises: (i) 0.0005% to 0.25% of piperidine glucoside; (ii) 0.05% to 20% N-acetyltyrosine; and (iii) 0.01% to 3% of 12-hydroxystearic acid.
[0058] Most preferably, the hair care composition comprises: (i) 0.0007% to 0.009% of taxine glucoside; (ii) 0.1% to 5% N-acetyltyrosine; and (iii) 0.1% to 2% of 12-hydroxystearic acid.
[0059] Product form and other ingredients The hair care compositions of the present invention may also contain other beneficial active agents, such as, for example, zinc salts. Zinc can act as an inhibitor of enzymes associated with hair loss. Therefore, enzyme inhibition can advantageously lead to a reduction in hair loss or thinning.
[0060] The zinc salts suitable for use in this invention include zinc sulfate, zinc gluconate, zinc chloride, zinc pyrithione, or combinations thereof. Preferably, the composition comprises zinc sulfate, zinc gluconate, zinc chloride, or combinations thereof. More preferably, the composition comprises zinc gluconate, zinc chloride, or combinations thereof. Most preferably, the composition comprises zinc chloride.
[0061] The amount of zinc salt in the hair care composition of the present invention may be, for example, 0.00001% to 5% of the total weight of the composition, and preferably 0.0001% to 3% of the total weight of the composition, more preferably 0.001% to 1% of the total weight of the composition, even more preferably 0.01% to 0.1% of the total weight of the composition, and most preferably 0.01% to 0.05% of the total weight of the composition, for example, at most 0.03% concentration.
[0062] The compositions used in this invention (as described above) may contain additional active substances for improving the physical and / or aesthetic properties of the scalp and / or hair. Examples include amino acids, vitamins, minerals and / or antioxidants, emollients, moisturizers, sunscreens, anti-irritants, exfoliants, plant extracts (such as pomegranate, birch, green tea, chamomile and licorice extracts) and mixtures thereof, preservatives (such as sodium benzoate, potassium sorbate, phenoxyethanol, pentylene glycol and sodium metabisulfite), pH adjusters and fragrances (such as essential oils, flower oils, natural extracts from resins, gums, balsams, legumes, mosses and other plants, as well as synthetic aromatic materials).
[0063] In some embodiments, the compositions of the present invention preferably further comprise a thickener. Suitable thickeners are selected from polyacrylic acid, crosslinked polymers of acrylic acid, copolymers of acrylic acid with hydrophobic monomers, copolymers of carboxylic acid-containing monomers with acrylates, crosslinked copolymers of acrylic acid with acrylates, heteropolysaccharide gums, and crystalline long-chain acrylic derivatives. Long-chain acrylic derivatives are ideally selected from ethylene glycol stearate, alkanolamides of fatty acids having 16 to 22 carbon atoms, and mixtures thereof. Ethylene glycol distearate and polyethylene glycol 3-distearate are preferred long-chain acrylic derivatives because they impart pearlescent properties to the composition. Polyacrylic acid is commercially available as Carbopol 420, Carbopol 488, or Carbopol 493. Polymers of acrylic acid crosslinked with multifunctional agents can also be used; these are commercially available as Carbopol 910, Carbopol 934, Carbopol 941, and Carbopol 980. An example of a suitable copolymer of carboxylic acid-containing monomers and acrylates is Carbopol 1342. All Carbopol (trademark) materials are available from Goodrich. Suitable crosspolymers of acrylic acid and acrylate are Pemulen TR1 or Pemulen TR2. Suitable heteropolysaccharide gums are xanthan gum, such as xanthan gum available as Kelzan mu.
[0064] The hair care composition of the present invention may also contain a penetration enhancer.
[0065] According to the present invention, a "penetration enhancer" can be understood as a compound that can penetrate the skin (e.g., scalp) to reversibly reduce barrier resistance and improve the bioavailability of active substances to, for example, hair follicles and hair bulbs.
[0066] In some embodiments, the penetration enhancer is selected from glycols, such as polyethylene glycol; phospholipids, such as in the form of one or more liposomes; nonionic emulsifiers, such as polysorbate, lauryl ketone, isohexadecane, dodecane, DMSO, ethanol, decanol, isosorbide dimethyl ether and / or combinations thereof.
[0067] In some embodiments, the penetration enhancer is present in an amount of 0.01% to 20% of the total weight of the composition, more preferably at least 0.1% of the weight of the composition, even more preferably at least 1%, even more preferably at least 2%, and most preferably at least 6%. Preferably, the penetration enhancer is present in an amount not exceeding 15% of the weight of the composition, even more preferably not exceeding 10%, even more preferably not exceeding 8%, and most preferably not exceeding 3%.
[0068] In some embodiments, the penetration enhancer is selected from ethanol, isosorbide dimethyl ether, or combinations thereof. Preferably, the penetration enhancer is a combination of isosorbide dimethyl ether and ethanol.
[0069] In some preferred embodiments, the penetration enhancer comprises isosorbide dimethyl ether.
[0070] In one embodiment, the isosorbide dimethyl ether is contained in an amount of 0.01% to 10% of the total weight of the composition, or in an alternative, in an amount of 0.1% to 5% of the total weight of the composition, or in an amount of 1% to 3% of the total weight of the composition, such as 2.5% of the total weight of the composition.
[0071] In some implementations, the penetration enhancer comprises ethanol.
[0072] Preferably, ethanol is present in an amount of 0.01% to 20% of the total weight of the composition, more preferably at least 0.1%, even more preferably at least 1%, even more preferably at least 2%, and most preferably at least 3%. Preferably, ethanol is present in an amount not exceeding 15% of the weight of the composition, even more preferably not exceeding 10%, even more preferably not exceeding 8%, and most preferably not exceeding 7%.
[0073] Preferably, the weight ratio of the penetration enhancer to N-acetyltyrosine is 1:0.001 to 1:10, more preferably 1:0.01 to 1:5, and even more preferably 1:0.03 to 1:1. In some embodiments, the weight ratio of the penetration enhancer to N-acetyltyrosine is 1:0.1 to 1:0.5.
[0074] Preferably, the weight ratio of the penetration enhancer to taxine glucoside is 1:0.00001 to 1:1; more preferably, the weight ratio is 1:0.00005 to 1:0.1; and even more preferably, 1:0.0001 to 1:0.01. In some embodiments, the weight ratio is 1:0.001 to 1:0.005.
[0075] Preferably, the weight ratio of isosorbide dimethyl ether to N-acetyltyrosine is from 1:0.001 to 1:5, more preferably from 1:0.01 to 1:1, and even more preferably from 1:0.03 to 1:0.1. In some embodiments, the weight ratio of isosorbide dimethyl ether to N-acetyltyrosine is from 1:0.05 to 1:0.09.
[0076] Preferably, the weight ratio of isosorbide dimethyl ether to taxonomycin glucoside is from 1:0.00001 to 1:1, more preferably from 1:0.00005 to 1:0.1, and even more preferably from 1:0.0001 to 1:0.01. In some embodiments, the weight ratio of isosorbide dimethyl ether to taxonomycin glucoside is from 1:0.002 to 1:0.006.
[0077] Preferably, the weight ratio of ethanol to N-acetyltyrosine is from 1:0.0001 to 1:5, more preferably from 1:0.001 to 1:1, and even more preferably from 1:0.01 to 1:0.5. In some embodiments, the weight ratio of ethanol to N-acetyltyrosine is from 1:0.02 to 1:0.05.
[0078] Preferably, the weight ratio of ethanol to taxonomycin glucoside is from 1:0.00001 to 1:1, more preferably from 1:0.00005 to 1:0.1, and even more preferably from 1:0.0001 to 1:0.01. In some embodiments, the weight ratio of ethanol to taxonomycin glucoside is from 1:0.001 to 1:0.005.
[0079] In some embodiments of the invention, the hair care composition also contains additional antioxidants. For example, the compositions of the invention may also contain epigallocatechin gallate and / or epigallocatechin gallyl glucoside.
[0080] Epigallocatechin gallate (EGCG, also known as epigallocatechin-3-gallate) is an ester of epigallocatechin and gallic acid, and is a type of catechin. Epigallocatechin gallate may contribute to hair growth. A suitable method for preparing epigallocatechin galloyl α-D-glucoside is described in WO 2007 / 144368.
[0081] The amount of epigallocatechin gallate glucoside can be from 0.00001 to 0.60% by weight, more preferably from 0.00010 to 0.060% by weight, and most preferably from 0.00015 to 0.0045% by weight.
[0082] The sources of epigallocatechin gallate and / or epigallocatechin galloglycoside that may be included in the compositions of the present invention include tea leaf extract. Preferably, the amount of tea leaf extract in the hair care compositions of the present invention may be, for example, 0.0001% to 1% of the total weight of the composition, and more preferably 0.0005% to 0.1% of the total weight of the composition, more preferably 0.0009% to 0.01% of the total weight of the composition, and even more preferably 0.0009% to 0.005% of the total weight of the composition.
[0083] In a preferred embodiment, the hair care composition of the present invention comprises glycine. Glycine may be used at a concentration of 0.001% to 0.50% of the total weight of the composition, more preferably 0.001% to 0.30% of the total weight of the composition, and most preferably 0.001% to 0.008% of the total weight of the composition.
[0084] In some embodiments of the invention, the composition comprises one or more cosmetically or pharmaceutically acceptable solvents, such as glycerin, propylene glycol, butylene glycol, ethoxylated or propoxylated diethylene glycol, propanol, or isopropanol, to help dissolve the active ingredient of the composition.
[0085] In some embodiments, the hair care composition comprises a first active component and a second active component. The first and second active components may optionally be blended with further ingredients and components to form the hair care composition of the present invention.
[0086] In some embodiments, the first active component comprises: (i) Taxonitrile glucoside; and (ii) N-acetyltyrosine.
[0087] The amount of taurine glucoside in the first active component may be, for example, 0.01% to 0.50% of the total weight of the first active component, more preferably 0.05% to 0.25% of the total weight of the first active component, and most preferably 0.07% to 0.15% of the total weight of the first active component, for example, about 0.10% of the total weight of the first active component.
[0088] The ratio of taxanein glucoside to taxanein in the first active component can be as described above for the total hair care composition.
[0089] In some embodiments, the first active component, taxonomyl glucoside and / or taxonomyl, may be derived from European larch. For example, taxonomyl glucoside and / or taxonomyl may be contained in European larch extract.
[0090] The amount of European larch extract in the first active component may be, for example, 0.01% to 0.1% of the total weight of the first active component, more preferably 0.05% to 0.8% of the total weight of the first active component, and most preferably 0.1% to 0.7% of the total weight of the first active component, for example, about 0.55% of the total weight of the first active component.
[0091] The amount of N-acetyltyrosine in the hair care active agent of the present invention may be, for example, 1.0% to 30% of the total weight of the first active component, more preferably 10% to 20% of the total weight of the first active component, and most preferably 15% to 20% of the total weight of the first active component, for example, about 17.5%.
[0092] The first active ingredient may include glycine. For example, glycine may be used in an amount of 0.01% to 1% of the total weight of the first active ingredient, more preferably 0.10% to 0.80% of the total weight of the first active ingredient, and most preferably 0.20% to 0.60% of the total weight of the first active ingredient, such as about 0.55% of the total weight of the first active ingredient.
[0093] The first active ingredient may include tea leaf extract. For example, the tea leaf extract may be included in an amount of 0.01% to 1.5% of the total weight of the first active ingredient, more preferably 0.05% to 1% of the total weight of the first active ingredient, and most preferably 0.08% to 0.5% of the total weight of the first active ingredient, such as about 0.1% of the total weight of the first active ingredient.
[0094] The first active ingredient may include epigallocatechin gallate glucoside. For example, epigallocatechin gallate glucoside may be included in an amount of 0.001% to 0.60% of the total weight of the first active ingredient, more preferably 0.010% to 0.060% of the total weight of the first active ingredient, and most preferably 0.015% to 0.045% of the total weight of the first active ingredient, such as about 0.03% of the total weight of the first active ingredient.
[0095] The first active ingredient may include a preservative, such as sodium metabisulfite. For example, the preservative may be included in an amount of 0.01% to 1.00% of the total weight of the first active ingredient, more preferably 0.10% to 0.750% of the total weight of the first active ingredient, and most preferably 0.45% to 0.55% of the total weight of the first active ingredient, such as about 0.50% of the total weight of the first active ingredient.
[0096] In some embodiments, the first active component may comprise a zinc salt, preferably zinc chloride. For example, the zinc salt may be included in an amount of 0.01% to 1% of the total weight of the first active component, more preferably 0.05% to 0.5% of the total weight of the first active component, and most preferably 0.08% to 0.2% of the total weight of the first active component, such as about 0.1% of the total weight of the first active component.
[0097] The first active ingredient may contain one or more cosmetically or pharmaceutically acceptable solvents, such as glycerin, propylene glycol, butylene glycol, ethoxylated or propoxylated diethylene glycol, ethanol, propanol, or isopropanol, to help dissolve the active ingredient of the first active ingredient.
[0098] For example, glycerin may be included in an amount of 1% to 95% of the total weight of the first active component, more preferably 10% to 80% of the total weight of the first active component, most preferably 20% to 60% of the total weight of the first active component, such as about 50% of the total weight of the first active component.
[0099] The first active ingredient may be present in the hair care composition in an amount of 0.001% to 20% of the total weight of the composition, for example, in an amount of 0.005% to 10% of the total weight of the composition, more preferably in an amount of 0.01% to 5% of the total weight of the composition, more preferably in an amount of 0.1% to 3% of the total weight of the composition, and most preferably in an amount of 0.5% to 2% of the total weight of the composition, for example, in an amount of about 1% of the total weight of the composition.
[0100] The first active component can be provided, for example, as Darkenyl™, a commercially available material from Givaudan.
[0101] In some embodiments, the second active component comprises: (iii) At least one lipid PPAR[α] activator selected from: C10-C18 saturated fatty acids, preferably branched, or if straight-chain, preferably derivatized with hydroxyl groups; C10-C20 monounsaturated fatty acids; and C10-C22 polyunsaturated fatty acids.
[0102] PPAR activators are as defined above.
[0103] The hair care compositions of the present invention are primarily intended for application to the hair and / or scalp of human subjects to improve hair properties.
[0104] Preferably, the hair care composition is selected from shampoo-free hair compositions, hair masks, leave-in hair care compositions, and pre-treatment hair care compositions, and most preferably from shampoo-free hair compositions, hair masks, and leave-in compositions. The pre-treatment composition is preferably a leave-in hair care composition. The hair care composition of the present invention can also be a "shampoo-free" composition to be applied to the hair and then partially rinsed off.
[0105] The wash-off compositions used in this invention are typically left on wet hair for 1 to 2 minutes before being rinsed off. Typically, about 1 g to about 50 g of the composition is applied to the hair or scalp.
[0106] The hair mask used in this invention is typically left on the hair for 3 to 10 minutes, preferably 3 to 5 minutes, more preferably 4 to 5 minutes, before rinsing it off.
[0107] The leave-in compositions used in this invention are typically applied to the hair and left on the hair for more than 10 minutes, and preferably applied to the hair after washing and not rinsed off until the next wash.
[0108] Based on total weight, the hair care composition of the present invention typically contains about 20% to about 95% water, preferably at least 30% by weight, more preferably at least 40% by weight, even more preferably at least 50% by weight, and even more preferably at least 60% by weight or even at least 70% by weight, but generally not exceeding 94% by weight, preferably not exceeding 93% by weight, more preferably not exceeding 92% by weight, even more preferably not exceeding 91% by weight, and even more preferably not exceeding 90% by weight or even not exceeding 80% by weight. Other organic solvents, such as lower alkyl alcohols and polyols, may also be present. Examples of lower alkyl alcohols include C1 to C6 monohydric alcohols, such as ethanol and isopropanol. Examples of polyols include propylene glycol, hexanediol, glycerol, and propylene glycol. Mixtures of any of the above-mentioned organic solvents may also be used.
[0109] Preferably, the composition comprises a polyol. The polyol may be selected from glycerol, propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol, sorbitol, hydroxypropyl sorbitol, hexanediol, 1,3-butanediol, isopentyl glycol, ethoxylated glycerol, propoxylated glycerol, or mixtures thereof. The most preferred polyol is glycerol, also known as glycerin. The amount of the polyol may be from 0.1% to 20% by weight of the composition, preferably from 0.5% to 15%, and more preferably any value in the range of 2% to 10%.
[0110] Uses and methods In a further aspect, the present invention relates to the non-therapeutic use of the hair care compositions of the present invention.
[0111] In some embodiments, the present invention relates to the non-therapeutic use of the hair care compositions of the present invention for reducing the appearance of gray or white hair in an individual, for reducing age-related functional changes in hair pigmentation, for increasing melanin production in gray hair, for increasing cell proliferation, for increasing melanocyte proliferation, for increasing the level and / or activity of tyrosinase, and for increasing gene and / or protein expression in hair-related pigmentation pathways.
[0112] In some embodiments, the present invention relates to the non-therapeutic use of the hair care compositions of the present invention for reducing age-related functional changes in hair pigmentation and for improving hair volume, increasing hair thickness, increasing hair count, improving hair strength, reducing hair loss, and / or for fiber repair.
[0113] In some embodiments, the present invention relates to the non-therapeutic uses of the hair care compositions of the present invention for reducing age-related functional changes in hair pigmentation and for improving scalp health, reducing scalp inflammation, reducing scalp itching, reducing oxidative stress in the scalp / hair follicles, reducing oxidized lipid substances in the scalp / hair follicles, improving sebum control, improving the scalp barrier, and / or improving the balance of the scalp microbiome.
[0114] In some embodiments, the present invention relates to the non-therapeutic use of the hair care compositions of the present invention for reducing oxidative stress in melanocytes, preferably in hair follicles and / or scalp.
[0115] In some embodiments, the present invention relates to hair care compositions for reducing the appearance of gray or white hair in an individual, for reducing age-related functional changes in hair pigmentation, for increasing melanin production in gray hair, for increasing cell proliferation, for increasing melanocyte proliferation, for increasing tyrosinase levels and / or activity, and for increasing gene and / or protein expression in hair-related pigmentation pathways.
[0116] In some embodiments, the present invention relates to hair care compositions for reducing age-related functional changes in hair pigmentation and for improving hair volume, increasing hair thickness, increasing hair count, improving hair strength, reducing hair loss, and / or for fiber repair.
[0117] In some embodiments, the present invention relates to hair care compositions for reducing age-related functional changes in hair pigmentation and for improving scalp health, reducing scalp inflammation, reducing scalp itching, reducing oxidative stress in the scalp / hair follicles, reducing oxidized lipid substances in the scalp / hair follicles, improving sebum control, improving the scalp barrier, and / or improving the balance of the scalp microbiome.
[0118] In some embodiments, the present invention relates to hair compositions for reducing oxidative stress in melanocytes, preferably in hair follicles and / or scalp.
[0119] In a further aspect, the present invention relates to a treatment method comprising the hair care composition of the present invention.
[0120] In some embodiments, the present invention relates to a method for reducing the presence of gray or white hair in an individual, reducing age-related functional changes in hair pigmentation, increasing melanin production in gray hair, increasing cell proliferation, increasing melanocyte proliferation, increasing tyrosinase levels and / or activity, and increasing gene and / or protein expression in hair-related pigmentation pathways; said method comprising applying the hair care composition of the present invention to hair or scalp.
[0121] In some embodiments, the present invention relates to reducing age-related functional changes in hair pigmentation and to methods for improving hair volume, increasing hair thickness, increasing hair count, improving hair strength, reducing hair loss, and / or providing fiber repair; said methods include applying the hair care composition of the present invention to the hair or scalp.
[0122] In some embodiments, the present invention relates to methods for reducing age-related functional changes in hair pigmentation, and to methods for improving scalp health, reducing scalp inflammation, reducing oxidative stress in the scalp / hair follicles, reducing oxidative lipids in the scalp / hair follicles, improving sebum control, improving the scalp barrier, and / or improving the microbiome balance of the scalp; said methods include applying the hair care composition of the present invention to the hair or scalp.
[0123] In some embodiments, the present invention relates to a method for reducing oxidative stress in melanocytes, the method comprising applying the hair care composition of the invention to hair or scalp. Preferably, melanocytes in hair follicles and / or scalp.
[0124] The present invention also unexpectedly demonstrates that, compared with the control, the inclusion of 12-hydroxystearic acid (12-HSA) in the hair care composition without other active ingredients provides improved antioxidant activity.
[0125] Therefore, in a further aspect of the invention, 12-hydroxystearic acid is provided for non-therapeutic uses in reducing the occurrence of gray or white hair in an individual, in reducing age-related functional changes in hair pigmentation, and in increasing melanin production in gray hair.
[0126] In some embodiments, the present invention relates to the non-therapeutic uses of 12-hydroxystearic acid for reducing age-related functional changes in hair pigmentation and for improving hair volume, increasing hair thickness, increasing hair count, improving hair strength, reducing hair loss, and / or for fiber repair.
[0127] In some embodiments, the present invention relates to the non-therapeutic use of the 12-hydroxystearic acid of the present invention for reducing age-related functional changes in hair pigmentation and for improving scalp health, reducing scalp inflammation, reducing scalp itching, reducing oxidative stress in the scalp / hair follicles, and reducing oxidized lipid substances in the scalp / hair follicles.
[0128] In some embodiments, the present invention relates to the non-therapeutic use of 12-hydroxystearic acid for reducing oxidative stress in melanocytes, preferably in hair follicles and / or scalp.
[0129] In some embodiments, the present invention relates to 12-hydroxystearic acid for reducing the occurrence of gray or white hair in an individual, for reducing age-related functional changes in hair pigmentation, for increasing melanin production in gray hair, for increasing cell proliferation, for increasing melanocyte proliferation, for increasing tyrosinase levels and / or activity, and for increasing gene and / or protein expression in hair-related pigmentation pathways.
[0130] In some embodiments, the present invention relates to 12-hydroxystearic acid for reducing age-related functional changes in hair pigmentation and for improving hair volume, increasing hair thickness, increasing hair count, improving hair strength, reducing hair loss, and / or for fiber repair.
[0131] In some embodiments, the present invention relates to 12-hydroxystearic acid for reducing age-related functional changes in hair pigmentation, for improving scalp health, for reducing scalp inflammation, for reducing scalp itching, for reducing oxidative stress in the scalp / hair follicles, and for reducing oxidative lipid substances in the scalp / hair follicles.
[0132] In some embodiments, the present invention relates to 12-hydroxystearic acid for reducing oxidative stress in melanocytes, preferably in hair follicles and / or scalp.
[0133] In a further aspect, the present invention relates to a treatment method comprising 12-hydroxystearic acid.
[0134] In some embodiments, the present invention relates to a method for reducing the occurrence of gray or white hair in an individual, reducing age-related functional changes in hair pigmentation, increasing melanin production in gray hair, increasing cell proliferation, increasing melanocyte proliferation, increasing tyrosinase levels and / or activity, and / or increasing gene and / or protein expression in hair-related pigmentation pathways; said method comprising applying 12-hydroxystearic acid to hair or scalp.
[0135] In some embodiments, the present invention relates to a method for reducing age-related functional changes in hair pigmentation, and to a method for increasing hair volume, increasing hair thickness, increasing hair count, improving hair strength, reducing hair loss, and / or providing fiber repair; said method comprising applying 12-hydroxystearic acid to the hair or scalp.
[0136] In some embodiments, the present invention relates to a method for reducing age-related functional changes in hair pigmentation, and to a method for improving scalp health, reducing scalp inflammation, reducing oxidative stress in the scalp / hair follicles, and reducing oxidized lipid substances in the scalp / hair follicles; said method comprising applying 12-hydroxystearic acid to hair or scalp.
[0137] In some embodiments, the present invention relates to a method for reducing oxidative stress in melanocytes, the method comprising applying 12-hydroxystearic acid to hair or scalp. Preferably, it is applied to melanocytes in hair follicles and / or scalp.
[0138] The features disclosed in the foregoing specification or the appended claims may be used alone or in any combination of these features to implement the invention, when appropriate.
[0139] While the present invention has been described in conjunction with the foregoing exemplary embodiments, many equivalent modifications and variations will be apparent to those skilled in the art upon which this disclosure is given. Therefore, the exemplary embodiments of the invention described above are considered illustrative rather than restrictive. Various changes may be made to the described embodiments without departing from the spirit and scope of the invention.
[0140] To avoid any ambiguity, any theoretical explanations provided herein are intended to enhance the reader's understanding. The inventor does not wish to be bound by any of these theoretical explanations. Any section headings used herein are for organizational purposes only and should not be construed as limiting the subject matter described.
[0141] Throughout this specification, including the following claims, unless the context otherwise requires, the words “comprising” and “including”, as well as variations such as “comprising,” “containing,” and “including”, shall be understood to imply inclusion of the said integer or step or group of integers or steps, but do not exclude any other integer or step or group of integers or steps.
[0142] It should be noted that, as used in the specification and appended claims, the singular forms “a,” “an,” and “the” include plural indicators unless the context clearly specifies otherwise. A range may be expressed herein as from “about” one particular value and / or to “about” another particular value. When expressing such a range, another embodiment includes from one particular value and / or to another particular value. Similarly, when a value is expressed as an approximation using the antecedent “about,” it should be understood that the particular value forms another embodiment. The term “about” with respect to numerical values is optional and means, for example, + / - 10%.
[0143] The invention will now be further described with reference to the following embodiments. Unless otherwise stated, all percentages are weight percentages based on total weight.
[0144] Example Fill the container with deionized water. Separately disperse the carbomer and then add it to the container to ensure proper hydration. Heat the container to 70-75°C and add 12-HSA and Montanov 68. TM Add to a container, then add the preservative, including pentylene glycol, until dissolved. Cool the container to room temperature. Once 35°C or lower is reached, add Darkeyl™ while continuing to mix. Add the remaining ingredients and mix. The pH of the solution is then adjusted to 4.5-5.0 as needed using sodium hydroxide and / or citric acid solution.
[0145] Example 1: Hair care shampoo Table 1
[0146] Example 2 - Catalase Activity Assay Adult primary human epidermal melanocytes were cultured in T75 flasks in melanocyte culture medium supplemented with a mixture of melanocyte growth factors and antibiotics, the T75 flasks being maintained at 37°C in a humidified chamber with 5% CO2. Cells were then transferred in microtiter plates at approximately 5 × 10⁻⁶ cells / mL. 4 Cells were further passaged at a density of [number] cells / well and incubated for 24 hours at 37°C in a humidified chamber containing 5% CO2, as described above. After 24 hours, the cells were treated with the desired concentration of test material or a combination of test materials and 5 μM menadione, and incubated for another 6 hours as described above. Catalase activity of the cells after incubation was assessed using a catalase colorimetric activity kit. Experiments were performed in duplicate (n=2) on three different donor cells (n=3). Data are expressed as % catalase activity compared to menadione.
[0147] Concentration of test material in cell culture medium : Darkenyl™ (available from Givaudan) - 0.005% containing taurine glucoside / acetyltyrosine 12-Hydroxystearic acid (12-HSA) - 0.00024% Statistical analysis For each test, the mean of two replicates from three different experiments was used to show the percentage difference compared to the menadione-treated control. A t-test was used to assess statistical significance for comparing the menadione control with the corresponding treatment.
[0148] To identify synergistic combinations, a t-test is performed to compare the combination data with individual data using JMP. For a combination to be considered synergistic, it should exhibit statistical significance across all individuals.
[0149] Table 2
[0150] Menaquinone induces oxidative stress in melanocytes by producing reactive oxygen species (ROS).
[0151] The antioxidant effect of the test material on menadione-stressed melanocytes was assessed by comparing catalase activity in treated and untreated stressed cells. Increased catalase activity indicated an enhanced ability of cells to reduce oxidative stress.
[0152] Surprisingly, compared with untreated stressed cells and stressed cells treated with only one or two active substances, cells treated with a combination of taurine glucoside and N-acetyltyrosine with 12-HSA showed a statistically significant synergistic increase in catalase activity. Catalase activity was also improved compared with that in unstressed control cells.
[0153] Experiments have shown that a combination of active ingredients, including taurine glucoside, N-acetyltyrosine, and 12-HSA, effectively reduces oxidative stress in hair follicle melanocytes associated with unwanted hair graying and age-related hair changes.
[0154] Example 3 - Determination of dichlorofluorescein diacetate (DCFDA) Adult primary human epidermal melanocytes were cultured in melanocyte culture medium supplemented with a mixture of melanocyte growth factors and antibiotics in a humidified chamber at 37°C in T75 flasks. The cells were further cultured in microplates at approximately 5 x 10⁻⁶ wells. 4Cells were passaged at a density of [number] cells / well and incubated for 24 hours in a humidified chamber at 37°C and 5% CO2 under the conditions described above. After 24 hours, cells were treated with the desired concentration of the test substance or a combination of test substances and 5 µM menadione, and incubated for another 6 hours under the conditions described above. Following incubation, ROS levels were assessed by incubating cells in DCFDA dye for 45 minutes. Cells were then washed, and fluorescence was measured at excitation wavelength 485 nm and emission wavelength 535 nm. Experiments were performed in duplicate (n=2) on three different donor cells (n=3). Data are expressed as % ROS levels compared to menadione.
[0155] Concentration of test substances in cell culture medium: Darkenyl containing taurine glucoside / acetyltyrosine TM (From Givaudan) - 0.005% 12-Hydroxystearic acid (12-HSA) - 0.00024% Statistical analysis For each test, data were presented as the percentage difference relative to the menadione-treated control, using the mean of two replicates from three independent experiments. The significance of comparisons between the menadione control and the corresponding treatment group was assessed using a t-test.
[0156] Table 3
[0157] Menadione induces oxidative stress in melanocytes by generating reactive oxygen species (ROS). The antioxidant effect of the test material on menadione-stressed melanocytes was assessed using a dichlorofluorescein diacetate assay to determine ROS levels in treated and untreated stressed cells. Decreased ROS levels indicated an enhanced ability of the active ingredient to reduce oxidative stress in cells.
[0158] Surprisingly, cells treated with 12-HSA showed a statistically significant reduction in ROS levels compared to untreated stressed cells. ROS levels were also reduced compared to those in unstressed control cells.
[0159] Experiments have shown that compositions containing 12-HSA effectively reduce oxidative stress in hair follicle melanocytes associated with undesirable graying of hair and age-related hair changes.
Claims
1. A hair care composition comprising: (i) Taxonitrile glucoside; (ii) N-acetyltyrosine; and (iii) At least one lipid peroxisome proliferator-activated receptor (PPAR) [α] activator, selected from: C10-C18 saturated fatty acids, preferably branched, or, if straight-chain, preferably hydroxylated; C10-C20 monounsaturated fatty acids; and C10-C22 polyunsaturated fatty acids.
2. The hair care composition according to any one of the preceding claims, wherein the lipid PPAR[α] activator is selected from 12-hydroxystearic acid, cis-octadecanoic acid, trans-7-octadecanoic acid, cis-5,8,11,14,17-eicosapentaenoic acid, cis-4,7,10,13,16,19-docosahexaenoic acid, conjugated linoleic acid (C9,T11), bromelain, trans-linolenic acid, and trans-castor oil. Acids, octadecanoic acid, 2-hydroxystearic acid, α-linolenic acid, arachidonic acid, cis-11,14-eicosadienoic acid, conjugated linoleic acid (t10, c12), conjugated linoleic acid (t9, t11), conjugated linoleic acid (a 50:50 mixture of c9, t11 and t10c12), coriander acid, trans-linoleic acid, monocarboxylic acid, piracetamic acid, ricinoleic acid, stearylene acid, arborvitae extract or trans-isooleic acid, cis-11, 14,17-Eicosatrienoic acid, cis-5-eicosatrienoic acid, cis-8,11,14-eicosatrienoic acid, hexadecanoic acid, palmitoleic acid, trans-pecinic acid, trans-trans-farnesol, cis-13,16-docosadienoic acid, cis-isooleic acid, cis-11-eicosatrienoic acid, cis-13,16,19-docosatrienoic acid, cis-13-octadecenoic acid, cis-15-octadecenoic acid, cis... Formula-7,10,13,16-docosahexaenoic acid, transoleic acid, gamma-linolenic acid, geranilic acid, geraniylgeranilic acid, linoleic acid, oleic acid, phellandrene, phytaneic acid, terpineic acid, trans-13-octadecenoic acid, tridecyl salicylic acid (TDS), chickpea extract (red clover phytoestrogens), safflower extract, pomegranate saponifiable hydrolysate extract, gromwell root (octadecanoic acid plant extract), or zanthoxylen (extract from zanthoxylen).
3. The hair care composition according to any one of the preceding claims, wherein the lipid PPAR[α] activator is selected from apigenin, conjugated linoleic acid, 12-hydroxystearic acid, ricinoleic acid, or mixtures thereof.
4. The hair care composition according to any one of the preceding claims, wherein the lipid PPAR[α] activator is 12-hydroxystearic acid.
5. The hair care composition according to any one of the preceding claims, wherein the lipid PPAR[α] activator is present in an amount of 0.05% to 8.0% by weight of the composition, preferably 1% to 6%, most preferably 1.5% to 4.5%; preferably the composition has 1.5% to 4% by weight, more preferably 1.5% to 3.5% by weight of PPAR activator.
6. The hair care composition according to any one of the preceding claims, wherein the amount of taurine glucoside in the hair care composition is 0.0001% to 0.50% of the total weight of the composition, more preferably 0.0005% to 0.25% of the total weight of the composition, even more preferably 0.0007% to 0.009% of the total weight of the composition, preferably 0.0009% to 0.007% of the total weight of the composition, and most preferably 0.001% to 0.004% by weight of the total weight of the composition.
7. The hair care composition according to any one of the preceding claims, wherein the amount of N-acetyltyrosine in the hair care composition is from 0.001% to 30% of the total weight of the composition, preferably from 0.05% to 20% of the total weight of the composition, more preferably from 0.1% to 5% of the total weight of the composition, more preferably from 0.15% to 0.9% of the total weight of the composition, and most preferably from 0.15% to 0.4% of the total weight of the composition.
8. The hair care composition according to any one of the preceding claims, wherein the weight ratio of taurine glucoside to N-acetyltyrosine is preferably 1:500 to 1:1, more preferably 1:300 to 1:50, and most preferably 1:200 to 1:100, for example about 1:
150.
9. The hair care composition according to any one of the preceding claims, wherein the weight ratio of the lipid PPAR[α] activator to N-acetyltyrosine is 1:0.01 to 1:5, more preferably 1:0.02 to 1:3, more preferably 1:0.05 to 1:1, and even more preferably 1:0.06 to 1:0.
2.
10. The hair care composition according to any one of the preceding claims, wherein the weight ratio of the lipid PPAR[α] activator to taxine glucoside is 1:0.00001 to 1:1, more preferably 1:0.0001 to 1:0.1, more preferably 1:0.0002 to 1:0.01, and even more preferably 1:0.0005 to 1:0.
002.
11. The non-therapeutic use of the hair care composition according to any of the preceding claims for reducing the appearance of gray or white hair in an individual, for reducing age-related functional changes in hair pigmentation, for reducing oxidative stress in the scalp / hair follicles, and for reducing oxidative lipid substances in the scalp / hair follicles.
12. The hair care composition according to any one of claims 1-10 for non-therapeutic use in reducing oxidative stress in melanocytes.
13. A method for reducing the appearance of gray or white hair in an individual, reducing age-related functional changes in hair pigmentation, reducing oxidative stress in the scalp / hair follicles, and reducing oxidized lipid substances in the scalp / hair follicles, the method comprising applying a hair care composition according to any one of claims 1-10 to the hair or scalp.
14. A method for reducing oxidative stress in melanocytes, the method comprising applying a hair care composition according to any one of claims 1-10 to hair or scalp.
15. Non-therapeutic use of 12-hydroxystearic acid to reduce oxidative stress in melanocytes.