Compositions against osmotic stress
A synergistic combination of rosel extract and glycine betaine in cosmetic compositions addresses osmotic stress, improving skin hydration and reducing stress-induced damage, enhancing skin health and appearance.
Patent Information
- Application Number
- JP2024544449
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2022-01-26
- Publication Date
- 2025-01-30
AI Technical Summary
Existing cosmetic compositions lack synergistic protection against osmotic stress, which is caused by exposure to ultraviolet rays, air pollution, and chemical substances, leading to skin issues such as wrinkles, thinning, drying, and dullness.
A combination of a rosel extract from Hibiscus Sabdariffa L. and a betaine compound, specifically glycine betaine, is formulated in a specific ratio and concentration to provide synergistic protection against osmotic stress, enhancing skin hydration and reducing stress-induced cell damage.
The combination effectively reduces stress-induced skin damage, improving skin appearance by minimizing wrinkles, thinning, drying, and dullness, providing enhanced protection against osmotic stress factors.
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Abstract
Description
[Technical field]
[0001] The present disclosure relates to the field of cosmetic or dermatological compositions. In particular, the present invention relates to novel cosmetic and / or dermatological compositions for topical application comprising a roselle extract and a betaine compound.
[0002] The present invention also relates to the cosmetic use of said composition, in particular to combat signs of stressor-induced osmoregulation of the epidermis, such as the appearance of fine lines and wrinkles, atrophy, thinning, dryness, laxity, dull appearance, or uneven surface of the skin. [Background technology]
[0003] Skin is one of the most important organs of the human body. It exists at the outermost part of the body as a barrier to protect the human body from the adverse effects of the external environment. Keratinocytes at different stages of differentiation constitute the five-layer structure of the epidermis of the skin, such as the stratum corneum, stratum lucidum, stratum granulosum, stratum spinosum, and stratum basale, from the outside to the inside. The epidermis composed of keratinocytes performs a barrier function to inhibit the transmission of foreign substances and prevent transepidermal water loss. However, with the development of modern society, skin cells face a continuous threat of osmotic pressure due to continuous exposure to ultraviolet rays, air pollution, dry environments, chemicals, etc. As an agent for protecting skin cells subjected to such stress, French Patent No. 2877843 discloses the use of betaine in the field of cosmetics to combat skin aging and damage.
[0004] Furthermore, as a cosmetic composition for protecting the skin from different types of stress, US Patent Application Publication No. 2010 / 0166814 provides a composition comprising a combination of at least two osmolytes selected from the group comprising taurine or a derivative thereof, inositol, betaine, and trehalose.
[0005] Recently, it has been reported that the use of betaine in combination with various plant extracts can not only achieve moisturization, but also achieve the additional beneficial effects brought by various plant extracts.For example, Chinese Patent No. 104523490 reports that betaine is used in combination with moisturizing plant extracts and whitening plant extracts to provide a peeling composition with whitening and moisturizing effects.Furthermore, US Patent Application Publication No. 2016 / 0287658 reports that the combination of betaine and bamboo sap can significantly increase the water content in the stratum corneum.Chinese Patent No. 105411900 teaches that the combination of betaine and Leontopodium alpinum extract can enhance the effect of Leontopodium alpinum.
[0006] Hibiscus sabdariffa L. is a plant of the genus Hibiscus in the family Mayacaceae, and has value as a food ingredient, natural colorant, and medical use.It is used in anti-allergy compositions in Chinese Patent No. 108653090 due to its antioxidant properties and tyrosinase inhibitory effects.In addition, as described in Chinese Patent No. 104523490, Hibiscus sabdariffa flower extract is referred to as a skin-whitening plant extract. Summary of the Invention [Problem to be solved by the invention]
[0007] To the best of the inventors' knowledge, the synergistic protective properties of a combination of a Roselle extract and a betaine compound against osmotic stress have not been disclosed.
[0008] The inventors have intensively investigated to solve the problem of providing combinations capable of providing synergistic protective properties against osmotic stress.
[0009] As a result, the inventors have found that betaine compounds and roselle extract can be combined in a specific manner to provide synergistic protective properties against osmotic stress.
[0010] In other words, in a first aspect, the present application provides a composition, in particular a cosmetic and / or dermatological composition for topical application, comprising a roselle extract and at least a betaine compound selected from the group consisting of betaine, its salts, and analogues thereof.
[0011] In one embodiment of the present application, the betaine compound is glycine betaine.
[0012] In another embodiment of the present application, the roselle extract is derived from the calyx or fruit of roselle.
[0013] In a further embodiment of the present application, the Roselle extract is extracted by a water-based extraction process.
[0014] In a further embodiment of the present application, the betaine compound and the roselle extract are present in a weight ratio of from 3:1 to 3:10, preferably from 3:1 to 6:10, more preferably from 9:5 to 9:10.
[0015] In a further embodiment of the application, the betaine compound is present in an amount ranging from 0.01% to 0.2% by weight, preferably from 0.03% to 0.1% by weight, relative to the total weight of the composition.
[0016] In a further embodiment of the present application, the roselle extract is present in an amount ranging from 0.01% to 0.1% by weight, preferably from 0.02% to 0.1% by weight, more preferably from 0.05% to 0.1% by weight relative to the total weight of the composition.
[0017] In a second aspect, the present application provides a non-therapeutic cosmetic treatment process comprising topical application of the composition described above to keratinous material, such as skin.
[0018] In one embodiment of the present application, the process is to combat signs of stressor-induced osmoregulation of the epidermis, such as the appearance of fine lines and wrinkles, atrophy, thinning, dryness, looseness, dull appearance, or uneven surface of the skin.
[0019] In another embodiment of the present application, the stress factor is UV radiation, chemical and / or osmotic stress.
[0020] In a third aspect, the present application provides the cosmetic use of a composition as defined above for caring for, protecting and / or making up the skin of the body or face, or for caring for the hair.
[0021] In one embodiment of the application, said use is for combating signs of stressor-induced osmoregulation of the epidermis, such as the appearance of fine lines and wrinkles, atrophy, thinning, dryness, looseness, dull appearance, or uneven surface of the skin.
[0022] In another embodiment of the present application, the stress factor is UV radiation, chemical and / or osmotic stress.
[0023] The composition, by containing a combination of betaine compounds and roselle extract in an appropriate ratio and concentration range, can provide synergistic protective properties against osmotic stress, thereby reducing stress-induced cellular damage and combating signs of stressor-induced osmoregulation of the epidermis, such as the appearance of fine lines and wrinkles, atrophy, thinning, dryness, laxity, dull appearance, or uneven surface of the skin. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS
[0024] I. Definition Hereinafter, unless otherwise indicated, the limits of value ranges are included within the scope, in particular in the expressions "between" and "from".
[0025] Unless otherwise defined, all technical and scientific terms used herein have the same meaning as commonly understood by one of ordinary skill in the art to which this invention belongs. When a definition of a term herein conflicts with a meaning commonly understood by one of ordinary skill in the art to which this invention belongs, the definition set forth herein shall apply.
[0026] Throughout this application, the term "comprising" should be interpreted as embracing all specifically mentioned features and, optionally, additional unspecified features. As used herein, use of the term "comprising" also discloses embodiments in which no features are present other than those specifically mentioned (i.e., "consisting of").
[0027] As used herein, the term "skin cells" refers to cells that make up the skin, including, but not limited to, keratinocytes, melanocytes, fibroblasts, T cells, and the like.
[0028] As used herein, the term "UV radiation" refers to ultraviolet radiation in the UVA and UVB wavelength ranges.
[0029] The term "stress" as used herein refers to stress conditions to which skin cells may be exposed, such as ultraviolet light, air pollution, dry environment, chemicals, or osmotic stress. Here, osmotic stress refers to physiological dysfunction caused by a sudden change in solute concentration around the cell, which causes a sudden change in water movement across its cell membrane. Under hypertonic conditions - conditions of high concentration of either salt, substrate, or any solute in the supernatant - water is drawn out of the cell by osmosis.
[0030] As used herein, the term "synergistic protective properties" refers to a protective effect provided by the combined use of two active ingredients, e.g., at least one betaine compound of the present invention (e.g., trimethylglycine) and a Roselle extract (e.g., an extract from Hibiscus sabdariffa L.), that is greater than the sum of the protective effects of the two active ingredients when used alone at the same dosage.
[0031] Unless otherwise specified, all numbers expressing quantities of ingredients and the like used herein should be understood as being modified by the term "about."
[0032] Unless otherwise specified, all percentages referred to herein are percentages by weight and all documents referred to herein are incorporated by reference in their entirety.
[0033] II. Roselle Extract The composition of the present invention contains roselle extract from Hibiscus sabdariffa L. (also called rosella or roselle), a plant of the genus Hibiscus in the family Mayacaceae, which has value as a food ingredient, natural colorant, and medical use. The extract from Hibiscus sabdariffa L. provides skin texture, feel, hydration, moisturization, and improvement of the appearance of fine lines and wrinkles, atrophy, thinning, dryness, laxity, dull appearance, or uneven surface of the skin, or other undesirable skin conditions.
[0034] The roselle extract used herein can be obtained from a plant part selected from the group consisting of flowers, seeds, leaves, fruits, calyx, or roots of Hibiscus sabdariffa L. Preferably, the roselle extract used herein can be obtained from a plant part selected from the group consisting of flowers, calyx, and fruits of Hibiscus sabdariffa L. More preferably, the roselle extract used herein can be obtained from the fruits of Hibiscus sabdariffa L.
[0035] The roselle extract used herein may be an aqueous or aqueous / alcoholic extract of plant parts.Preferably, the roselle extract used herein can be extracted by aqueous extraction process.Preferably, the roselle extract used herein can be purchased from Lucas Meyer Cosmetics Company under the trade name Hibiscus Sabdariffa Extract, which is obtained by aqueous extraction in the presence of enzymes and pH adjustment, followed by freeze-drying.Hibiscus Sabdariffa Extract is also commercially available under CAS number 84775-96-2 or EC number 283-920-7.
[0036] The roselle extract used herein may be present in an amount of 0.01% to 0.1% by weight, preferably 0.02% to 0.1% by weight, more preferably 0.05% to 0.1% by weight, based on the total weight of the composition. In one embodiment, the roselle extract contained in the composition may be present in an amount of 0.01%, 0.02%, 0.03%, 0.04%, 0.05%, 0.06%, 0.07%, 0.08%, 0.09%, or 0.1% by weight, based on the total weight of the composition.
[0037] Without wishing to be bound by theory, it is believed that when the amount of roselle extract is less than 0.01% by weight based on the total weight of the composition, the amount of roselle extract is too small to exhibit a synergistic effect with the following betaine compound, however, when the amount is more than 0.1% by weight based on the total weight of the composition, it may have a negative effect on skin cells due to high concentration of cytotoxicity.
[0038] III. Betaine Compounds The composition of the present invention contains at least a betaine compound selected from the group consisting of betaine, its salts, and its analogs. As used herein, the term "betaine" is the general name for an inner salt formed with a quaternary ammonium as the cation in one molecule and an anion of an acid, especially a carboxylic acid.
[0039] Betaine compounds suitable for use in the compositions of the present invention include those known to be useful in cosmetic or dermatological compositions.
[0040] In one embodiment, the betaine used herein may be selected from the group consisting of histidine betaine, glycine betaine, proline betaine, phenylalanine betaine, tyrosine betaine, tryptophan betaine, leucine betaine, isoleucine betaine, valine betaine, glutamic acid betaine, alanine betaine, aspartic acid betaine, lysine betaine, and arginine betaine, depending on the amino acid involved.
[0041] In another embodiment, the betaine used herein may be selected from the group consisting of alkyl betaines, alkyl amido betaines, alkyl sulfobetaines, and imidazolinium betaines, in particular alkyl N-betaines, alkyl N-sulfobetaines, acyl N-betaines, alkyl N-substituted aminopropionic acids, alkyl imidazolinium betaines, etc.
[0042] Additionally, betaine compounds suitable for use in the compositions of the present invention include the salts and analogs of betaine listed above.
[0043] In one embodiment, the salt of betaine may be an organic acid salt, an inorganic acid salt, or a base salt of the above betaine, particularly betaine hydrochloride, betaine hydrobromide, betaine hydroiodide, betaine chloroaurate, betaine hydrazide hydrochloride, etc.
[0044] In a preferred embodiment, the betaine used herein may be glycine betaine, also called trimethylglycine, having the following structure:
[0045] [ka]
[0046] In a preferred embodiment, the betaine used herein may be glycine betaine, commercially available under the CAS number 107-43-7.
[0047] Furthermore, the term "analog" as used herein refers to any compound having properties similar to betaine, particularly trimethylglycine.
[0048] The betaine compound used herein may be present in an amount of 0.01% to 0.2% by weight, preferably 0.03% to 0.1% by weight, based on the total weight of the composition. In one embodiment, the betaine compound contained in the composition of the present invention may be present in an amount of 0.01%, 0.02%, 0.03%, 0.04%, 0.05%, 0.06%, 0.07%, 0.08%, 0.09%, 0.1% or 0.2% by weight, based on the total weight of the composition.
[0049] Without wishing to be bound by theory, it is believed that when the amount of betaine compound is less than 0.01% by weight based on the total weight of the composition, the amount of betaine compound is too small to show synergistic effect with Roselle extract.However, when the amount is more than 0.1% by weight based on the total weight of the composition, it does not increase synergistic effect, and therefore is not preferred from the viewpoint of cost.
[0050] The composition of the present invention contains a Roselle extract and at least a betaine compound as defined above. In one embodiment, the betaine compound and the Roselle extract are in a weight ratio of 3:1 to 3:10, preferably 3:1 to 6:10, more preferably 9:5 to 9:10.
[0051] IV. Other Ingredients The composition of the present invention may be in solid, semi-solid, or liquid form, and may be in solution, emulsion, suspension, or anhydrous form. When in solution or suspension form, the composition may contain about 1-99.9%, preferably about 5-95%, more preferably about 10-90% water. When in emulsion form, the composition may contain about 1-99%, preferably about 5-90%, more preferably about 10-85% water and about 1-99%, preferably about 5-90%, more preferably about 5-75% oil. When in anhydrous form, the composition may contain about 10-99% oil and 10-99% solidifying agent.
[0052] The compositions of the present invention may contain other ingredients, including but not limited to those described herein, so long as the synergistic protective effect of the compositions of the present invention is not affected.
[0053] A. Moisturizer The compositions of the present invention may contain one or more humectants. When present, they may range from about 0.1-75%, preferably from about 0.5-70%, more preferably from about 0.5-40%. Examples of suitable humectants include glycols, sugars, and the like. Suitable glycols include polyethylene glycols and polypropylene glycols, such as PEG 4-10, which are polyethylene glycols in monomeric or polymeric form and have 4-10 repeating ethylene oxide units, as well as C 1~6 Alkylene glycols, such as propylene glycol, butylene glycol, pentylene glycol, etc. Suitable sugars are also suitable humectants, some of which are also polyhydric alcohols. Examples of such sugars include glucose, fructose, honey, hydrogenated honey, inositol, maltose, mannitol, maltitol, sorbitol, sucrose, xylitol, xylose, etc. Urea is also suitable. Preferably, the humectant used in the composition of the present disclosure is C 1~6 , preferably C 2~4 Alkylene glycols, most particularly butylene glycol.
[0054] B. Plant extracts The compositions of the present invention may contain one or more additional plant extracts other than Roselle extract, if present, suggested ranges being about 0.0001-20%, preferably about 0.0005-15%, more preferably about 0.001-10%. Suitable plant extracts include extracts from plants (herbs, roots, flowers, fruits, seeds) such as yeast fermented extract, Padina pavonica extract, Thermus thermophilis fermented extract, Camelina sativa seed oil, Boswellia serrata extract, olive extract, Acacia dealbata extract, Acer saccharinum (sugar maple, Acidopholus, Acorus, Aesculus, Agaricus, Agave, Agrimonia, algae, aloe, citrus, Brassica, cinnamon, orange, apple, blueberry, cranberry, peach, pear, lemon, lime, pea, seaweed, caffeine, green tea, chamomile, willow bark, mulberry, poppy, and flowers, fruits, vegetables, etc., including those listed on pages 1646-1660 of the CTFA Cosmetic Ingredient Handbook, Eighth Edition, Volume 2.Further examples include, but are not limited to, Glycyrrhiza glabra, Salix nigra, Macrocycstis pyrifera, Pyrus malus, Saxifraga sarmentosa, Vitis vinifera, Morus nigra, Scutellaria baicalensis, Anthemis nobilis, Salvia sclarea, Rosmarinus officianalis, Citrus limonum, Panax ginseng, Siegesbeckia orientalis, Fructus mume, Ascophyllum nodosum, Glycine soja extract, Beta vulgaris, Haberlea rhodopensis, Polygonum cuspidatum, Citrus aurantium dulcis, Vitis vinifera, Selaginella tamariscina, Humulus lupulus, Citrus reticulata Peel, Punica granatum, Asparagopsis, Curcuma longa, Menyanthes trifoliata, Helianthus annuus, Hordeum vulgare, Cucumis sativus, Evernia prunastri, Evernia furfuracea, Kola acuminata, and mixtures thereof.
[0055] C. Surfactants The compositions of the present invention may contain one or more surfactants, especially when in emulsion form. However, such surfactants may also be used when the composition is a solution, suspension, or anhydrous. When present, the surfactant may range from about 0.001 to 30% by weight of the total composition, preferably from about 0.005 to 25% by weight, more preferably from about 0.1 to 20% by weight. Suitable surfactants may be silicone or organic, nonionic, anionic, amphoteric, or zwitterionic.
[0056] 1. Organic nonionic surfactants The compositions of the present invention may contain one or more non-ionic organic surfactants. Suitable non-ionic surfactants include alkoxylated alcohols or ethers formed by the reaction of an alcohol with an alkylene oxide, usually ethylene oxide or propylene oxide. Suitable alcohols include mono-, di-, or polyhydric short chain (C 1~6 ) alcohol, cholesterol, aromatic or aliphatic saturated or unsaturated fats (C 12~40 ) Alcohol, etc.
[0057] Cholesterol or aromatic or aliphatic saturated or unsaturated fatty alcohols that may have 6 to 40, preferably about 10 to 30, more preferably about 12 to 22 carbon atoms are suitable. Examples include oleyl alcohol, cetearyl alcohol, cetyl alcohol, stearyl alcohol, isostearyl alcohol, behenyl alcohol, etc. Examples of such ingredients include oleth 2-100, steareth 2-100, beheneth 5-30, ceteareth 2-100, ceteth 2-100, and cholesterol 2-100, where the number range refers to the number of repeating ethylene oxide units, for example, ceteth 2-100 means ceteth with the number of repeating ethylene oxide units ranging from 2 to 100. Derivatives of alkoxylated alcohols, such as their phosphate esters, are also suitable.
[0058] Some preferred organic nonionic surfactants include oleth-3, oleth-5, oleth-3 phosphate, cholestrol-24, ceteth-24, and the like.
[0059] Also suitable are alkoxylated alcohols formed from monohydric, dihydric, or polyhydric short chain alcohols, e.g., those having about 1 to 6 carbon atoms. Examples include glucose, glycerin, or alkylated derivatives thereof. Examples include glycereth 2-100, gluceth 2-100, methyl gluceth 2-100, etc. More preferred are methyl gluceth-20, glycereth-26, etc.
[0060] Another type of alkoxylated alcohol is a suitable surfactant, including ethylene oxide polymers with varying numbers of repeating EO groups, commonly referred to as PEG 12-200. More preferred is PEG-75, which may be purchased from Dow Chemical under the trade name Carbowax PEG-3350.
[0061] Other suitable nonionic surfactants include alkoxylated sorbitan and alkoxylated sorbitan derivatives. For example, alkoxylation, especially ethoxylation, of sorbitan provides polyalkoxylated sorbitan derivatives. Esterification of polyalkoxylated sorbitan provides sorbitan esters such as polysorbates. For example, polyalkoxylated sorbitan is C 6~30 , preferably C 12~22 It can be esterified with fatty acids. Examples of such components include polysorbates 20-85, sorbitan oleate, sorbitan sesquioleate, sorbitan palmitate, sorbitan sesquiisostearate, sorbitan stearate, etc.
[0062] 2. Silicone or silane surfactants Also suitable are various types of silicone or silane surfactants. Examples include organosiloxanes substituted with ethylene oxide or propylene oxide groups, such as PEG dimethicones, which are dimethicones substituted with polyethylene glycols, including those having the INCI names PEG-1 dimethicone, PEG-4 dimethicone, PEG-8 dimethicone, PEG-12 dimethicone, PEG-20 dimethicone, etc.
[0063] Also suitable are silanes substituted with ethoxy or propoxy groups, or both, such as the various types of PEG methyl ether silanes, such as bis-PEG-18 methyl ether dimethyl silane.
[0064] Further examples of silicone surfactants include those having the common names dimethicone copolyol, cetyl dimethicone copolyol, and the like.
[0065] D. Biological materials The compositions of the present invention may contain various types of biological materials, such as those derived from cells, fermented materials, etc. When present, such materials may range from about 0.001 to 30%, preferably from about 0.005 to 25%, more preferably from about 0.01 to 20%. Examples include cellular RNA or DNA, or fragments of probiotic microorganisms. RNA fragments are particularly preferred.
[0066] E. Thickener Suitable thickening agents may be incorporated into the compositions of the present invention, with suggested ranges, if present, being from about 0.01 to 30%, preferably from about 0.1 to 20%, more preferably from about 0.5 to 15% by weight of the total composition.
[0067] Examples of thickening agents include animal, vegetable, mineral, silicone, or synthetic waxes that may have melting points in the range of about 30-150°C. Examples of such waxes include waxes made by Fischer-Tropsch synthesis, such as polyethylene or synthetic waxes; or bayberry, candelilla, ozokerite, acacia, beeswax, ceresin, cetyl esters, flower wax, citrus wax, carnauba wax, jojoba wax, Japan wax, polyethylene, microcrystalline, rice bran, lanolin wax, mink, montan, bayberry, ouricury, ozokerite, palm kernel wax, paraffin, avocado wax, apple wax, shellac wax, salvia wax, spent grain wax, grape wax, and polyalkylene glycol derivatives thereof, such as PEG 6-20 beeswax, or PEG-12 carnauba wax; or esters thereof of fatty acids or fatty alcohols, such as hydroxystearic acid (e.g., 12-hydroxystearic acid), tristearin, tribehenin, and the like.
[0068] Also suitable as thickening agents are silicas, silicates, silica silylate, and their alkali metal or alkaline earth metal derivatives. These silicas and silicates are generally found in particulate form and include silica, silica silylate, magnesium aluminum silicate, and the like.
[0069] Silicone elastomers can also be used as thickeners. Such elastomers include those formed by addition reaction cure, by reacting an SiH-containing diorganosiloxane and an organopolysiloxane with terminal olefinic unsaturation, or an alpha-omega diene hydrocarbon, in the presence of a platinum metal catalyst. Such elastomers can also be formed by other reaction methods, such as condensation cure of an organopolysiloxane composition in the presence of an organotin compound via a dehydrogenation reaction between a hydroxyl-terminated diorganopolysiloxane and an SiH-containing diorganopolysiloxane or an alpha-omega diene, or by condensation cure of an organopolysiloxane composition in the presence of an organotin compound or a titanate ester using a condensation reaction between a hydroxyl-terminated diorganopolysiloxane and a hydrolyzable organosiloxane. They may also be formed by other reaction methods, such as peroxide cure of an organopolysiloxane composition that is thermally cured in the presence of an organic peroxide catalyst.
[0070] One type of elastomer that may be suitable can be prepared by addition reaction curing an organopolysiloxane or alpha-omega diene having at least two lower alkenyl groups in each molecule, and an organopolysiloxane having at least two silicon-bonded hydrogen atoms in each molecule, and a platinum type catalyst. The lower alkenyl groups, such as vinyl, can be present at any position in the molecule, although terminal olefinic unsaturation at one or both molecular ends is preferred. The molecular structure of this component may be linear, branched linear, cyclic, or network. These organopolysiloxanes are exemplified by methylvinylsiloxane, methylvinylsiloxane-dimethylsiloxane copolymer, dimethylvinylsiloxy terminated dimethylpolysiloxane, dimethylvinylsiloxy terminated dimethylsiloxane-methylphenylsiloxane copolymer, dimethylvinylsiloxy terminated dimethylsiloxane-diphenylsiloxane-methylvinylsiloxane copolymer, trimethylsiloxy terminated dimethylsiloxane-methylvinylsiloxane copolymer, trimethylsiloxy terminated dimethylsiloxane-methylphenylsiloxane-methylvinylsiloxane copolymer, dimethylvinylsiloxy terminated methyl(3,3,3-trifluoropropyl)polysiloxane, and dimethylvinylsiloxy terminated dimethylsiloxane-methyl(3,3,-trifluoropropyl)siloxane copolymer, decadiene, octadiene, heptadiene, hexadiene, pentadiene, or tetradiene, or tridiene.
[0071] Curing proceeds by addition reaction of silicon-bonded hydrogen atoms in the dimethylmethylhydrogensiloxane with the siloxane or alpha-omega diene under catalysis using the catalysts described herein. In order to form a highly crosslinked structure, the methylhydrogensiloxane must contain at least two silicon-bonded hydrogen atoms in each molecule to optimize its function as a crosslinker.
[0072] Catalysts used in the addition reaction of silicon-bonded hydrogen atoms and alkenyl groups are specifically exemplified by chloroplatinic acid (possibly dissolved in an alcohol or ketone and the solution optionally aged), chloroplatinic acid-olefin complexes, chloroplatinic acid-alkenylsiloxane complexes, chloroplatinic acid-diketone complexes, platinum black, and platinum on a carrier.
[0073] The example of silicone elastomer suitable for use in the composition of the present invention can be in powder form or can be dispersed or solubilized in a solvent such as volatile or non-volatile silicone, or a silicone compatible vehicle such as paraffinic hydrocarbon or ester.Examples of silicone elastomer powder include vinyl dimethicone / methicone silsesquioxane crosspolymers such as Shin-Etsu's KSP-100, KSP-101, KSP-102, KSP-103, KSP-104, KSP-105, hybrid silicone powder containing fluoroalkyl groups such as Shin-Etsu's KSP-200, which is a fluorosilicone elastomer, and hybrid silicone powder containing phenyl groups such as Shin-Etsu's KSP-300, which is a phenyl-substituted silicone elastomer, and DC9506 from Dow Coming. Examples of silicone elastomer powders dispersed in silicone compatible vehicles include dimethicone / vinyl dimethicone crosspolymers provided by various suppliers, including 9040 or 9041 from Dow Corning Corporation, SFE839 from GE Silicones, or KSG-15, 16, 18 from Shin-Etsu Silicones. KSG-15 has the CTFA name Cyclopentasiloxane / Dimethicone / Vinyl Dimethicone Crosspolymer. KSG-18 has the INCI name Phenyl Trimethicone / Dimethicone / Phenyl Vinyl Dimethicone Crosspolymer. Silicone elastomers can also be purchased from Grant Industries under the trade name Gransil. Also suitable are silicone elastomers with long chain alkyl substitution, such as lauryl dimethicone / vinyl dimethicone crosspolymers supplied by Shin Etsu under the trade names KSG-31, KSG-32, KSG-41, KSG-42, KSG-43, and KSG-44.Crosslinked organopolysiloxane elastomers useful in the present invention, and processes for making them, are further described in U.S. Pat. No. 4,970,252 to Sakuta et al., issued Nov. 13, 1990; U.S. Pat. No. 5,760,116 to Kilgour et al., issued Jun. 2, 1998; U.S. Pat. No. 5,654,362 to Schulz, Jr. et al., issued Aug. 5, 1997; and Japanese Patent Application Publication No. 61-18708, assigned to Pola Kasei Kogyo KK, each of which is incorporated herein by reference in its entirety.
[0074] Polysaccharides may be suitable aqueous phase thickening agents, including naturally occurring materials such as agar, agarose, Alcaligenes polysaccharides, algin, alginic acid, acacia gum, amylopectin, chitin, dextran, acacia gum, cellulose gum, gelatin, gellan gum, hyaluronic acid, hydroxyethylcellulose, methylcellulose, ethylcellulose, pectin, sclerotium gum, xanthan gum, pectin, trehelose, gelatin, and the like.
[0075] Also suitable are different types of synthetic polymer thickeners. One type includes acrylic polymer thickeners composed of monomers A and B, where A is selected from the group consisting of acrylic acid, methacrylic acid, and mixtures thereof, and B is selected from the group consisting of C1-22 alkyl acrylates, C1-22 alkyl methacrylates, and mixtures thereof. Acrylic polymer solutions include those sold under the trade name Sepigel® by Seppic, Inc., or those sold under the trade name Aristoflex®.
[0076] Also suitable are acrylic polymer thickeners that are copolymers of A, B, and C monomers, where A and B are as defined above and C has the general formula:
[0077] [ka] wherein Z is -(CH2) m m is 1 to 10, n is 2 to 3, o is 2 to 200, and R is C 10~30 It is a straight or branched chain alkyl. An example of the secondary thickener mentioned above is a copolymer where A and B are defined as above, C is CO, and n, o, and R are as above defined. An example of such a secondary thickener is the acrylates / steareth-20 methacrylate copolymer sold by Rohm & Haas under the trade name Acrysol ICS-1.
[0078] Also suitable are acrylate-based anionic amphiphilic polymers containing at least one hydrophilic unit and at least one allyl ether unit containing a fatty chain, the hydrophilic unit containing an ethylenically unsaturated anionic monomer, more specifically a vinyl carboxylic acid such as acrylic acid, methacrylic acid, or a mixture thereof, and the allyl ether unit containing a fatty chain is represented by the formula: CH2=CR'CH2OB n R where R' represents H or CH3, B represents an ethyleneoxy radical, n is zero or an integer ranging from 1 to 100, and R represents a hydrocarbon radical selected from alkyl, arylalkyl, aryl, alkylaryl, and cycloalkyl radicals containing 8 to 30 carbon atoms, preferably 10 to 24, and even more particularly 12 to 18 carbon atoms. In this case, R' represents H, n is equal to 10, and R represents stearyl (C 18) radical. Anionic amphiphilic polymers of this type have been described and prepared in U.S. Pat. Nos. 4,677,152 and 4,702,844, both of which are incorporated herein by reference in their entirety. Among these anionic amphiphilic polymers are polymers formed from 20-60% by weight of acrylic acid and / or methacrylic acid, 5-60% by weight of lower alkyl methacrylates, 2-50% by weight of the above-mentioned fatty chain-containing allyl ethers, and 0-1% by weight of crosslinking agents which are well-known copolymerizable polyethylenically unsaturated monomers, such as diallyl phthalate, allyl (meth)acrylate, divinylbenzene, (poly)ethylene glycol dimethacrylate, and methylene bisacrylamide. One commercially available example of such a polymer is a crosslinked terpolymer of methacrylic acid, ethyl acrylate, stearyl alcohol or steareth-10 polyethylene glycol (having 10 EO units) ether, in particular those sold by Allied Colloids under the names SALCARE SC80 and SALCARE SC90, which are aqueous emulsions containing 30% crosslinked terpolymer of methacrylic acid, ethyl acrylate, and steareth-10 allyl ether (40 / 50 / 10).
[0079] Also suitable are acrylate copolymers such as Polyacrylate-3, which is a copolymer of methacrylic acid, methyl methacrylate, methylstyrene isopropyl isocyanate, and PEG-40 behenate monomers; Polyacrylate-10, which is a copolymer of sodium acryloyldimethyltaurate, sodium acrylate, acrylamide, and vinylpyrrolidone monomers; or Polyacrylate-11, which is a copolymer of sodium acryloyldimethylacryloyldimethyltaurate, sodium acrylate, hydroxyethyl acrylate, lauryl acrylate, butyl acrylate, and acrylamide monomers.
[0080] Also suitable are crosslinked acrylate-based polymers in which one or more of the acrylic groups may have a substituted long chain alkyl (6-40, 10-30, etc.) group, such as acrylate / C10-30 alkyl acrylate crosslinked polymers, which are copolymers of C10-30 alkyl acrylate with one or more monomers of acrylic acid, methacrylic acid, or one of their simple esters, crosslinked with an allyl ether of sucrose or an allyl ether of pentaerythritol. Such polymers are commonly sold under the tradenames Carbopol or Pemulen and have the CTFA name Carbomer.
[0081] One particularly suitable type of aqueous phase thickener is an acrylate-based polymer thickener sold by Clariant under the Aristoflex trademark, such as Aristoflex AVC, which is an ammonium acryloyldimethyltaurate / VP copolymer; Aristoflex AVL, the same polymer found in AVC dispersed in a mixture containing caprylic / capric triglyceride, trilaureth-4, and polyglyceryl-2 sesquiisostearate; or Aristoflex HMB, which is an ammonium acryloyldimethyltaurate / beheneth-25 methacrylate crosspolymer.
[0082] Various polyethylene glycol (PEG) derivatives with degrees of polymerization ranging from 1,000 to 200,000 are also suitable as thickening agents. Such components are designated by "PEG" followed by the degree of polymerization in thousands, e.g., PEG-45M, which means a PEG having 45,000 repeating ethylene oxide units. Examples of suitable PEG derivatives include PEG 2M, 5M, 7M, 9M, 14M, 20M, 23M, 25M, 45M, 65M, 90M, 115M, 160M, 180M, etc.
[0083] Also suitable are polyglycerols, where the number of repeating glycerol moieties ranges from 15 to 200, preferably from about 20 to 100. Examples of suitable polyglycerols include those having CTFA names such as polyglycerol-20, polyglycerol-40, etc.
[0084] F.Oil When the composition of the present invention is in emulsion form, the composition will contain an oil phase. An oily component is desirable for its skin moisturizing and protective properties. Suitable oils include, but are not limited to, silicone, ester, vegetable oil, synthetic oil, and those described herein. The oil may be volatile or non-volatile, and is preferably in the form of a pourable liquid at room temperature. The term "volatile" means that the oil has a measurable vapor pressure, or a vapor pressure of at least about 2 mm of mercury at 20°C. The term "non-volatile" means that the oil has a vapor pressure of less than about 2 mm of mercury at 20°C.
[0085] 1. Volatile oils Suitable volatile oils generally have a viscosity in the range of about 0.5 to 5 centistokes at 25° C. and include linear silicones, cyclic silicones, paraffinic hydrocarbons, or mixtures thereof.
[0086] (a) Volatile silicone Cyclic silicones are one type of volatile silicone that may be used in the composition. Such silicones have the general formula:
[0087] [ka] where n=3 to 6, preferably 4, 5, or 6.
[0088] Linear volatile silicones are also suitable, such as those having the general formula: (CH3)3Si-O-[Si(CH3)2-O] n -Si(CH3)3 In the formula, n=0, 1, 2, 3, 4, or 5, preferably 0, 1, 2, 3, or 4.
[0089] Cyclic and linear volatile silicones are available from a variety of commercial sources, including Dow Corning Corporation and General Electric. Dow Corning's linear volatile silicones are sold under the trade names Dow Corning 244, 245, 344, and 200 fluid. These fluids include hexamethyldisiloxane (viscosity 0.65 centistokes (abbreviated cst)), octamethyltrisiloxane (1.0 cst), decamethyltetrasiloxane (1.5 cst), dodecamethylpentasiloxane (2 cst), and mixtures thereof, all with viscosity measurements at 25°C.
[0090] Suitable branched volatile silicones include alkyl trimethicones, such as methyl trimethicone, branched volatile silicones having the general formula:
[0091] [ka]
[0092] Methyl trimethicone can be purchased from Shin-Etsu Silicones under the trade name TMF-1.5, having a viscosity of 1.5 centistokes at 25°C.
[0093] (b) Volatile paraffinic hydrocarbons Also suitable are various straight or branched chain paraffinic hydrocarbons having 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, or 20 carbon atoms, more preferably 8 to 16 carbon atoms. Suitable hydrocarbons include pentane, hexane, heptane, decane, dodecane, tetradecane, tridecane, and C 6 alkyl ethers such as those disclosed in U.S. Pat. Nos. 3,439,088 and 3,818,105, both of which are incorporated herein by reference. 8~20Isoparaffins are included.
[0094] Preferred volatile paraffinic hydrocarbons have a molecular weight of 70 to 225, preferably 160 to 190, a boiling point range of 30 to 320, preferably 60 to 260° C., and a viscosity of less than about 10 cst. at 25° C. Such paraffinic hydrocarbons are available from EXXON under the ISOPARS trademark and from Permethyl Corporation. 12 Isoparaffins are manufactured by Permethyl Corporation under the trade name Permethyl 99A. 16 Isoparaffins such as isohexadecane (having the trade name Permethyl R) are also suitable.
[0095] 2. Non-volatile oil A variety of non-volatile oils are also suitable for use in the compositions of the present invention. Non-volatile oils generally have a viscosity of greater than about 5-10 centistokes at 25° C. and can range in viscosity up to about 1,000,000 centipoise at 25° C. Examples of non-volatile oils include, but are not limited to: (a) Ester Suitable esters are mono-, di-, and triesters. The composition may comprise one or more esters selected from the group, or a mixture thereof.
[0096] (i) Monoesters A monoester is defined as an ester formed by the reaction of a monocarboxylic acid having the formula R-COOH, where R is a linear or branched, saturated or unsaturated alkyl having 2 to 45 carbon atoms, or phenyl, with an alcohol having the formula R-OH, where R is a linear or branched, saturated or unsaturated alkyl having 2 to 30 carbon atoms, or phenyl. Both the alcohol and the acid may be substituted with one or more hydroxyl groups. Either the acid or alcohol, or both, may be a "fatty" acid or alcohol, and may have from about 6 to 30 carbon atoms, more preferably 12, 14, 16, 18, or 22 carbon atoms, in linear or branched, saturated or unsaturated form. Examples of monoester oils that may be used in the compositions of the present invention include hexyl laurate, butyl isostearate, hexadecyl isostearate, cetyl palmitate, isostearyl neopentanoate, stearyl heptanoate, isostearyl isononanoate, stearyl lactate, stearyl octanoate, stearyl stearate, isononyl isononanoate, and the like.
[0097] (ii) Diester Suitable diesters are reaction products of dicarboxylic acids with aliphatic or aromatic alcohols or aliphatic or aromatic alcohols having at least two substituted hydroxyl groups with monocarboxylic acids. The dicarboxylic acids may contain from 2 to 30 carbon atoms and may be in linear or branched, saturated or unsaturated form. The dicarboxylic acids may be substituted with one or more hydroxyl groups. The aliphatic or aromatic alcohols may also contain from 2 to 30 carbon atoms and may be in linear or branched, saturated or unsaturated form. Preferably, one or more of the acids or alcohols is a fatty acid or alcohol, i.e., contains from 12 to 22 carbon atoms. The dicarboxylic acid may also be an alpha hydroxy acid. The esters may be in dimeric or trimeric form. Examples of diester oils that may be used in the compositions of the present invention include diisostearyl malate, neopentyl glycol dioctanoate, dibutyl sebacate, dicetyl dimer dilinoleate, dicetyl adipate, diisocetyl adipate, diisononyl adipate, diisostearyl dimer dilinoleate, diisostearyl fumarate, diisostearyl malate, dioctyl malate, and the like.
[0098] (iii) Triester Suitable triesters include the reaction products of tricarboxylic acids with aliphatic or aromatic alcohols, or the reaction products of aliphatic or aromatic alcohols having three or more substituted hydroxyl groups with monocarboxylic acids. As with the mono- and diesters described above, the acids and alcohols contain 2 to 30 carbon atoms and may be saturated or unsaturated, straight or branched chain, and may be substituted with one or more hydroxyl groups. Preferably, one or more of the acids or alcohols is a fatty acid or alcohol containing 12 to 22 carbon atoms. Examples of triesters include triarachydin, tributyl citrate, triisostearyl citrate, triC citrate, triisostearyl ... 12~13Examples of such esters include esters of arachidonic acid, citric acid, or behenic acid, such as alkyl, tricaprylin, tricaprylyl citrate, tridecyl behenate, trioctyldodecyl citrate, tridecyl behenate, or tridecyl cocoate, tridecyl isononanoate, and the like.
[0099] Esters suitable for use in the compositions of the present invention are further described under the category of "Esters" in the CTFA Cosmetic Ingredient Dictionary and Handbook, Eleventh Edition, 2006, the text of which is incorporated herein by reference in its entirety.
[0100] (b) Hydrocarbon oil It may be desirable to incorporate one or more non-volatile hydrocarbon oils into the compositions of the present invention. Suitable non-volatile hydrocarbon oils include paraffinic hydrocarbons and olefins, preferably those having more than about 20 carbon atoms. Examples of such hydrocarbon oils include C 24~28 Olefin, C 30~45 Olefin, C 20~40 These include isoparaffins, hydrogenated polyisobutene, polyisobutene, polydecene, hydrogenated polydecene, mineral oil, pentahydrosqualene, squalene, squalane, and mixtures thereof. In one preferred embodiment, such hydrocarbons have a molecular weight in the range of about 300 to 1000 Daltons.
[0101] (c) Glyceryl esters of fatty acids Synthetic or naturally occurring glyceryl esters of fatty acids, or triglycerides, are also suitable for use in the present compositions. Both vegetable and animal sources may be used. Examples of such oils include castor oil, lanolin oil, C 10~18These include triglycerides, caprylic / capric / triglycerides, sweet almond oil, apricot kernel oil, sesame oil, camelina sativa oil, tamanu seed oil, coconut oil, corn oil, cottonseed oil, linseed oil, ink oil, olive oil, coconut oil, illipe oil, rapeseed oil, soybean oil, grapeseed oil, sunflower seed oil, and walnut oil.
[0102] Also suitable are synthetic or semi-synthetic glyceryl esters, such as fatty acid mono-, di-, and triglycerides, which are modified natural fats or oils, e.g., mono-, di-, or triesters of polyols, such as glycerin. In one example, the fat (C 12~22 ) The carboxylic acid is reacted with one or more repeating glyceryl groups, glyceryl stearate, diglyceryl diisostearate, polyglyceryl-3 isostearate, polyglyceryl-4 isostearate, polyglyceryl-6 ricinoleate, glyceryl dioleate, glyceryl diisotearate, glyceryl tetraisostearate, glyceryl trioctanoate, diglyceryl distearate, glyceryl linoleate, glyceryl myristate, glyceryl isostearate, PEG castor oil, PEG glyceryl oleate, PEG glyceryl stearate, PEG glyceryl tallowate, and the like.
[0103] (d) Non-volatile silicone Non-volatile silicone oils (both water-soluble and water-insoluble) are also suitable for use in the present compositions. Such silicones preferably have a viscosity ranging from about greater than 5 to 800,000 cst, preferably 20 to 200,000 cst at 25° C. Suitable water-insoluble silicones include amine-functional silicones such as amodimethicone.
[0104] For example, such non-volatile silicones may have the general formula:
[0105] [ka] wherein R and R′ are each independently selected from the group consisting of 1~30 A is a linear or branched, saturated or unsaturated alkyl, phenyl, or aryl, trialkylsiloxy, x and y are each independently 1 to 1,000,000, provided that at least one of x or y is present, and A is an alkylsiloxy end cap unit. A is a methylsiloxy end cap unit, particularly trimethylsiloxy, R and R' are each independently C 1~30 Linear or branched alkyl, phenyl, or trimethylsiloxy, more preferably C 1~22 Preferably, at least one R is a fatty alkyl (C 12 , C 14 , C 16 , C 18 , C 20 , or C 22 ), where R is methyl, and A is a trimethylsiloxy end-cap unit, provided that such alkyl dimethicones are pourable liquids at room temperature. Phenyl trimethicone can be purchased from Dow Corning Corporation under the trade name 556 Fluid. Trimethylsiloxy phenyl dimethicone can be purchased from Wacker-Chemie under the trade name PDM-1000. Cetyl dimethicone, also called liquid silicone wax, can be purchased from Dow Corning as Fluid 2502, or from DeGussa Care & Surface Specialties under the trade name Abil Wax 9801 or 9814.
[0106] G. Sunscreen It may also be desirable to include one or more sunscreens in the compositions of the present invention. Such sunscreens include chemical UVA or UVB sunscreens or physical sunscreens in particulate form. The inclusion of a sunscreen in a composition containing a whitening active will provide additional protection to the skin during the day and promote the effectiveness of the whitening active on the skin. When present, the sunscreen may range from about 0.1 to 50%, preferably from about 0.5 to 40%, more preferably from about 1 to 35%.
[0107] 1. UVA Chemical Sunscreens If desired, the composition may contain one or more UVA sunscreens. The term "UVA sunscreen" refers to a compound that blocks UV radiation in the wavelength range of about 320 to 400 nm. Preferred UVA sunscreens are dibenzoylmethane compounds of the formula:
[0108] [ka] wherein R1 is H, OR, and NRR, and each R is independently H, C 1~20 R2 is H or OH; R3 is H, C 1~20 It is a straight or branched chain alkyl.
[0109] R1 is OR and R is C 1~20 R2 is H and R3 is C 1~20 It is preferred if it is a straight or branched chain alkyl, more preferably butyl.
[0110] Examples of suitable UVA sunscreen compounds of this general formula include 4-methyldibenzoylmethane, 2-methyldibenzoylmethane, 4-isopropyldibenzoylmethane, 4-tert-butyldibenzoylmethane, 2,4-dimethyldibenzoylmethane, 2,5-dimethyldibenzoylmethane, 4,4'-diisopropylbenzoylmethane, 4-tert-butyl-4'-methoxydibenzoylmethane, 4,4'-diisopropylbenzoylmethane, 2-methyl-5-isopropyl-4'-methoxydibenzoylmethane, 2-methyl-5-tert-butyl-4'-methoxydibenzoylmethane, etc. Particularly preferred is 4-tert-butyl-4'-methoxydibenzoylmethane, also called avobenzone. Avobenzone is commercially available under the trade name Parsol® 1789 from Givaudan-Roure and under the trade name Eusolex® 9020 from Merck & Co.
[0111] Another type of UVA sunscreen includes dicamphor sulfonic acid derivatives, such as ecamsule, a sunscreen sold under the trade name Mexoryl®, which is terephthalylidene dicamphor sulfonic acid having the formula:
[0112] [ka]
[0113] The composition may contain from about 0.001 to 20%, preferably from 0.005 to 5%, more preferably from about 0.005 to 3% by weight of a UVA sunscreen. In a preferred embodiment of the invention, the UVA sunscreen is avobenzone and is present at about 3% or less by weight of the total composition.
[0114] 2. UVB Chemical Sunscreens The term "UVB sunscreen" refers to a compound that blocks UV radiation in the wavelength range of about 290-320 nm. There are a variety of UVB chemical sunscreens, including alpha-cyano-beta, beta-diphenylacrylic acid esters as described in U.S. Pat. No. 3,215,724, the entirety of which is incorporated herein by reference. One specific example of an alpha-cyano-beta, beta-diphenylacrylic acid ester is octocrylene, which is 2-ethylhexyl 2-cyano-3,3-diphenylacrylate. In certain cases, the composition may contain up to about 10% octocrylene by weight of the total composition. Suitable amounts range from about 0.001 to 10% by weight. Octocrylene may be purchased from BASF under the trade name Uvinul® N-539.
[0115] Other suitable sunscreens include the benzylidene camphor derivatives described in U.S. Pat. No. 3,781,417, the entirety of which is incorporated herein by reference. Such benzylidene camphor derivatives have the general formula:
[0116] [ka] where R is p-tolyl or styryl, preferably styryl. Particularly preferred is 4-methylbenzylidene camphor, a fat-soluble UVB sunscreen compound sold by Merck under the trade name Eusolex 6300.
[0117] Also suitable are cinnamate derivatives having the general formula:
[0118] [ka] In the formula, R and R1 are each independently C 1~20 R is a straight or branched alkyl group. R is methyl and R is a branched C 1~10, preferably C8 alkyl. A preferred compound is ethylhexyl methoxycinnamate, also called octoxinate or octyl methoxycinnamate. The compound can be purchased from Givaudan Corporation under the trade name Parsol® MCX or from BASF under the trade name Uvinul® MC 80.
[0119] Mono-, di-, and triethanolamine derivatives of such methoxycinnamates, including diethanolamine methoxycinnamate, are also suitable. Cinoxate, an aromatic ether derivative of the above compound, is also acceptable. If present, cinoxate should be found at no more than about 3% by weight of the total composition.
[0120] Also suitable as UVB screening agents are various benzophenone derivatives having the following general formula:
[0121] [ka] In the formula, R to R9 are each independently H, OH, NaO3S, SO3H, SO3Na, Cl, R'', or OR'', and R'' is C 1~20 It is a straight or branched chain alkyl. Examples of such compounds include benzophenone 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, and 12. Particularly preferred are benzophenone derivatives such as benzophenone 3 (also called oxybenzone), benzophenone 4 (also called sulisobenzone), benzophenone 5 (sulisobenzone sodium), etc. Benzophenone 3 is most preferred.
[0122] Also suitable are certain menthyl salicylate derivatives having the general formula:
[0123] [ka] In the formula, R1, R2, R3, and R4 are each independently H, OH, NH2, or C 1~20It is a straight or branched chain alkyl. It is particularly preferred when R1, R2, and R3 are methyl and R4 is hydroxyl or NH2, and the compound has the name homomenthyl salicylate (also known as homosalate) or menthyl anthranilate. Homosalate is commercially available from Merck under the trademark Eusolex® HMS, and menthyl anthranilate is commercially available from Haarmann & Reimer under the trademark Heliopan®. If present, homosalate should be found at no more than about 15% by weight of the total composition.
[0124] Various aminobenzoic acid derivatives are suitable UVB absorbers, including those having the general formula:
[0125] [ka] In the formula, R1, R2, and R3 each independently represent H, C optionally substituted with one or more hydroxy groups. 1~20 R1 is H or C 1~8 Linear or branched alkyl, R2 and R3 are H or C 1~8 Particularly preferred are straight or branched chain alkyls. PABA, ethylhexyl dimethyl PABA (Padimate O), ethyl dihydroxypropyl PABA, and the like are particularly preferred. If present, Padimate O should be found at no more than about 8% by weight of the total composition.
[0126] Salicylate derivatives are also acceptable UVB absorbers. Such compounds have the general formula: where R is a straight or branched chain alkyl, including derivatives of the above compounds formed from mono-, di-, or triethanolamine. Octyl salicylate, TEA-salicylate, DEA-salicylate, and mixtures thereof are particularly preferred.
[0127] Generally, the amount of UVB chemical sunscreen present may range from about 0.001 to 45%, preferably from 0.005 to 40%, more preferably from about 0.01 to 35% by weight of the total composition.
[0128] If desired, the compositions of the present invention can be formulated to have a particular SPF (Sun Protection Factor) value ranging from about 1 to 50, preferably from about 2 to 45, and most preferably from about 5 to 30. Calculation of SPF values is well known in the art.
[0129] H. Vitamins and Antioxidants It may be desirable to incorporate one or more vitamins or antioxidants into the compositions of the present invention. If present, suggested ranges are about 0.001-20%, preferably about 0.005-15%, more preferably about 0.010-10%. Preferably, such vitamins, vitamin derivatives, and / or antioxidants function to scavenge free radicals in the form of singlet oxygen. Such vitamins may include tocopherol or derivatives thereof, such as tocopherol acetate, tocopherol ferulate; ascorbic acid or derivatives thereof, such as ascorbyl palmitate, magnesium ascorbyl phosphate; vitamin A or derivatives thereof, such as retinyl palmitate; or vitamins D, K, B, or derivatives thereof.
[0130] Without wishing to be bound by theory, it is believed that delivery of roselle extract and betaine compounds can reduce stress-induced cellular damage and combat symptoms of stressor-induced osmoregulation of the epidermis, such as the appearance of fine lines and wrinkles, atrophy, thinning, dryness, flaccidity, dull appearance, or uneven surface of the skin.
[0131] The present invention therefore also relates to a non-therapeutic cosmetic treatment process for combating signs of stressor-induced osmoregulation of the epidermis, such as the appearance of fine lines and wrinkles, atrophy, thinning, dryness, looseness, a dull appearance or an uneven surface of the skin, comprising the topical application of a composition as defined above to a keratinous material such as the skin.
[0132] In one embodiment, the compositions of the present invention may be applied topically to the neck, face, neckline, back, hands, or areas of the body in an effective amount such that the combination of roselle extract and betaine compound can provide synergistic protective properties against osmotic stress.
[0133] The present invention also provides the use of a roselle extract and a betaine compound for the preparation of a medicament for treating symptoms of skin dehydration.
[0134] The invention will now be further described with reference to the following examples, which are given for purposes of illustration only. EXAMPLES
[0135] A. In Vitro Testing 1.Active preparation 1.2 g of Betaine (RDS 51-6709) was dissolved in 100 ml of water (stock concentration 1.2%) with magnetic stirring for complete dissolution. 0.5 g of Roselle extract (Hibiscus Sabdariffa extract, Lucas Meyer Cosmetics Company) was dissolved in 10 mL of water to achieve a 5% stock solution. The solution was then filtered through a 0.22 um filter to keep it sterile.
[0136] 2.Cell culture Normal Human Epidermal Keratinocytes (NHEK, FC-0007) purchased from Lifeline Cell Technology were incubated at 37°C, 95% humidity, and 5% CO2 in keratinocyte cell culture medium (DermaLife K Keratinocyte Medium Complete Kit, LL-0007, Lifeline cell technology) supplemented with growth factors and 1% penicillin / streptomycin (Thermo Fischer, Waltham, MA, USA). Cells were passaged when they reached 80% confluency.
[0137] 3. Cell culture medium components:
[0138] [Table 1]
[0139] 4. Establishment of hyperosmotic stress model NHEKs were seeded at a density of 4,000 / well in 96-well plates. After 24 hours of incubation, cells reached approximately 80% confluency. 4.38 mg / mL NaCl was added to the culture medium to achieve an osmolality of 450 in addition to a baseline of approximately 300 mOsm.
[0140] 5. Cell Treatment On day 1, NHEKs were seeded at 3,000 cells / well in 96-well plates with culture medium (DermaLife K Keratinocyte Medium Complete Kit). After 24 hours of attachment, two-active combination experiments were performed in vitro. 21 data points were used for dose and effect, including 4 concentrations for betaine, 7 concentrations for roselle extract, and their combinations as follows (Table 1). Cells were treated with combinations of these actives for 48 hours (diluted separately in cell culture medium and then mixed together to treat cells). Cells were then washed twice with Dulbecco's phosphate buffered saline (DPBS) and then incubated for 120 minutes in medium containing 10% alamarBlue™ Cell Viability Reagent (Thermo Fisher, Waltham, MA, USA). The incubated plates were measured for fluorescence at Ex 530 nm / Em 615 nm using a Perkin Elmer plate reader (VICTOR Nivo). Values are reported as RFU values.
[0141] 6. Cell protection rate The protective effect can be determined by the cell survival ratio (%) and the cell protection rate (%) as follows.
[0142]
number
[0143] 7. Combination index (CI) According to the theory proposed by Chou and Talalay (TING-CHAO CHOU. Theoretical Basis, Experimental Design, and Computerized Simulation of Synergism and Antagonism in Drug Combination Studies. Pharmacol Rev 58:621-681, 2006), the level of synergy can typically be measured and quantified by the drug combination index (CI, a quantitative measure of drug combination effect) from experimental dose-response data. The concentration of each compound, the protection ratio of each compound, or a combination of these two compound data were input into a computer for automatic analysis using CalcuSyn software. The combination index can be used to classify drug interactions as synergistic, additive, or antagonistic, as follows: CI<1 synergy CI=1 additive effect CI>1 antagonism
[0144] 8. Combination index: the effect of betaine and roselle extract concentrations, combination concentration ratio, and effect level.
[0145] The experiment was carried out with 4 levels of betaine and 7 levels of Roselle extract. The combination ratios indicate the ratio of betaine to Roselle extract by their mass concentrations. The synergy values are classified based on the calculated combination index.
[0146] [Table 2]
[0147] B. Formulation Examples The composition of the present invention containing roselle extract and a betaine compound is prepared as follows.
[0148] [Table 3]
[0149] The composition is prepared by thoroughly mixing these ingredients according to conventional methods.
[0150] While the present invention has been described in terms of preferred embodiments, it is not intended to limit the scope of the invention to the particular forms described, but on the contrary, it is intended to cover alternatives, modifications, and equivalents which may be included within the spirit and scope of the invention as defined by the appended claims.
Claims
1. A composition, in particular a cosmetic and / or dermatological composition for topical application, comprising a roselle extract and at least a betaine compound selected from the group consisting of betaine, its salts and analogues thereof.
2. The composition of claim 1 , wherein the betaine compound is glycine betaine.
3. The composition according to claim 1 or 2, wherein the roselle extract is derived from the fruit of roselle.
4. The composition according to any one of claims 1 to 3, wherein the Roselle extract is extracted by an aqueous extraction process.
5. 5. The composition according to any one of claims 1 to 4, wherein the betaine compound and the Roselle extract are present in a weight ratio of from 3:1 to 3:10, preferably from 3:1 to 6:10, more preferably from 9:5 to 9:
10.
6. The composition according to any one of the preceding claims, wherein the betaine compound is present in an amount ranging from 0.01% to 0.2% by weight, preferably from 0.03% to 0.1% by weight, relative to the total weight of the composition.
7. 7. The composition according to any one of claims 1 to 6, wherein the Roselle extract is present in an amount ranging from 0.01% to 0.1% by weight, preferably from 0.02% to 0.1% by weight, more preferably from 0.05% to 0.1% by weight, relative to the total weight of the composition.
8. A non-therapeutic cosmetic treatment process comprising the topical application of a composition as defined in any one of claims 1 to 7 to keratinous material such as the skin.
9. 9. The process of claim 8 for combating signs of stressor-induced osmoregulation dysregulation of the epidermis, such as the appearance of fine lines and wrinkles, atrophy, thinning, dryness, looseness, dull appearance, or uneven surface of the skin.
10. 10. The process according to claim 8 or 9, wherein the stress factor is UV radiation, chemical and / or osmotic stress.
11. Cosmetic use of a composition according to any one of claims 1 to 7 for caring for, protecting and / or making up the skin of the body or face or for caring for the hair.
12. 12. The use according to claim 11 for combating signs of stressor-induced osmoregulation dysregulation of the epidermis, such as the appearance of fine lines and wrinkles, atrophy, thinning, dryness, looseness, dull appearance, or uneven surface of the skin.
13. 13. The use according to claim 11 or 12, wherein the stress factor is UV radiation, chemical and / or osmotic stress.
Citation Information
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