High spf gel composition comprising nicotinamide
Patent Information
- Application Number
- CN202580009600.0
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2024-02-23
- Filing Date
- 2025-01-08
- Publication Date
- 2026-11-03
AI Technical Summary
In the prior art, the addition of vitamin B compounds such as nicotinamide to gel compositions at high concentrations leads to a loss of color stability, while making it difficult to maintain high SPF and good sensory properties.
A stable gel composition is formed by adding specific proportions of oil-soluble and water-soluble sunscreens, aqueous and oil-phase thickeners, humectants, sensory modifiers, vitamin B3 compounds, and antioxidants to the composition, comprising 0.1 to 25% oil-soluble sunscreens, 0.1 to 5% water-soluble sunscreens, 0.25 to 5% aqueous thickeners, 0.5 to 10% oil-phase thickeners, 0.5 to 15% humectants, 0.5 to 10% sensory modifiers, 0.01 to 10% vitamin B3 compounds, and 0.01 to 10% antioxidants.
It achieves high SPF color stability, reduces the generation of reactive oxygen species, and provides excellent sensory properties and sun protection effect.
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Abstract
Description
Technical Field
[0001] This invention relates to photoprotective personal care compositions that provide a high sun protection factor (SPF). Specifically, this invention relates to personal care compositions in gel form that provide a high SPF and are color-stable. Background Technology
[0002] The applicant’s co-pending application WO 2023 / 217920 (Unilever) discloses a photoprotective personal care composition that provides a high SPF and very good sensory properties that consumers expect when applying such a composition to the skin. Specifically, it discloses a gel composition that provides a high SPF, wherein the composition comprises a combination of an oil-soluble sunscreen agent, a water-soluble sunscreen agent, an aqueous phase thickener, an oil phase thickener, a moisturizer, and a selection of sensory modifiers.
[0003] However, it has been found that when vitamin B compounds, such as nicotinamide, which are water-soluble, are added to such gel compositions in increased amounts, it tends to lead to a loss of gel color stability.
[0004] Therefore, there is a need to overcome the drawbacks associated with existing technologies and to provide gel compositions that not only offer high SPF and the good sensory properties expected by consumers (such as low greasiness and good spreadability), but also provide color stability.
[0005] It has been found that when selected antioxidants are incorporated into the gel compositions of the present invention, the problems encountered are resolved and color stability is provided. It has also been found that color-stable gels reduce reactive oxygen species generated due to external factors (e.g., exposure to sunlight) and / or due to internal factors (e.g., intracellular reactions). Summary of the Invention
[0006] Therefore, the present invention relates to a personal care composition comprising: (i) 0.1 to 25% by weight of oil-soluble sunscreen agents, (ii) 0.1 to 5% by weight of water-soluble sunscreen agent, (iii) 0.25 to 5% by weight of an aqueous thickener, wherein the aqueous thickener is selected from one or two of polysaccharide gums and synthetic polymers, wherein the synthetic polymers are selected from ammonium acryloyl dimethyl taurate / VP copolymers and ammonium acryloyl dimethyl taurate / behenol polyether-25 methacrylate crosspolymers. (iv) 0.5% to 10% of an oil-phase thickener, said oil-phase thickener being selected from one or more of the following: C 18 To C 36 Fatty acid esters, C8 to C 16Fatty acid esters; polymeric oil-phase thickeners; and particles selected from organically modified clays, hydrophobically modified fumed silica, and aerogels. (v) 0.5 to 15% by weight of a humectant, said humectant being selected from glycerin or glycol. (vi) 0.5 to 10% by weight of a sensory modifier, said sensory modifier being selected from one or more of the following: modified starch, silica microspheres, and polymers of dimethicone / vinyl dimethicone crosslinked polymers with silica. (vii) 0.01 to 10% by weight of vitamin B3 compounds; and (viii) 0.01 to 10% by weight of an antioxidant selected from dilaurate thiodipropionate (Tinogard DA), pentaerythritol tetra(di-tert-butylhydroxyhydrocinnamate) ester (Tinogard TT), tris(tetramethylhydroxypiperidinol) citrate (Tinogard Q), vitamin C or derivatives thereof, and mixtures thereof, wherein the vitamin C derivative is selected from sodium ascorbate palmitate and sodium ascorbate phosphate.
[0007] Furthermore, the present invention also relates to a method for providing light protection with a sun protection factor (SPF) of at least 30, the method comprising the step of applying the composition of any one of the preceding claims to a desired skin surface. Detailed Implementation
[0008] These and other aspects, features, and advantages will become clear to those skilled in the art upon reading the following detailed description and appended claims. For the avoidance of doubt, any feature of one aspect of the invention may be used in any other aspect of the invention. The word “comprising” is intended to mean “including” but not necessarily “consisting of” or “comprises of”. In other words, the listed steps or options need not be exhaustive. It should be noted that the examples given in the following description are intended to illustrate the invention and are not intended to limit the invention to those examples alone. Similarly, unless otherwise stated, all percentages are weight / weight percentages. Except where expressly indicated in the operational examples and comparative examples or elsewhere, all figures in this specification and claims indicating the amount of material or reaction conditions, the physical properties of the material, and / or uses should be understood to be modified by the word “about”. Numerical ranges expressed in the format “x to y” should be understood to include both x and y. When multiple preferred ranges are described in the format “x to y” for a particular feature, it should be understood that all ranges combining different endpoints are also covered.
[0009] The photoprotective compositions of the present invention are intended for personal care or cosmetic purposes and may also be referred to as personal care compositions or cosmetic compositions. As used herein, "personal care composition" means a composition intended for topical application to sun-exposed areas of human skin and / or hair. Such compositions can be categorized as leave-in or rinse-off and include any product applied to the human body for the purpose of improving appearance, cleanliness, odor control, or general aesthetics. The compositions of the present invention (the compositions) may be in liquid or gel form, preferably in gel form. Non-limiting examples of such sunscreen compositions include leave-in skin products such as antiperspirants, deodorants, sunscreen gels, and rinse-off shampoos, conditioners, facial cleansers, and body washes. The compositions of the present invention are preferably leave-in compositions.
[0010] As used herein, “skin” means the skin on the face and body (e.g., neck, chest, back, arms, armpits, hands, legs, and scalp), especially the parts exposed to sunlight. The compositions of the present invention also relate to application on any other human keratin matrix besides skin, such as hair, wherein the product can be formulated to have a specific purpose of improving photoprotection.
[0011] The compositions of the present invention comprise 0.1 to 25% by weight of an oil-soluble sunscreen agent. Oil-soluble means those organic sunscreen agents having a solubility in water of less than 10 g / L, preferably less than 5 g / L, more preferably less than 2 g / L. The oil-soluble sunscreen agent can be of UV-B or UV-A type. Preferably, the compositions according to the present invention comprise 0.1 to 20% by weight, preferably 1 to 15% by weight of a UVB oil-soluble sunscreen agent. Further preferably, the compositions of the present invention comprise 0.1 to 5% by weight, preferably 1 to 4% by weight of a UVA oil-soluble sunscreen agent.
[0012] When it includes an oil-soluble UVB sunscreen agent, it is preferably one or more of the following: octyl salicylate (Eusolex) ®OS), 3,3,5-trimethylcyclohexyl 2-hydroxybenzoate, ethylhexyl salicylate, 2-cyano-3,3-diphenyl-2-acrylate 2-ethylhexyl ester (also known as octocrylene), 2-ethylhexyl 4-methoxycinnamate or octyl methoxycinnamate, ethylhexyl triazine, 3-benzyl camphor, cinnoxalate, diethylhexylbutamidotriazine, p-aminobenzoic acid (PABA), dihydroxypropyl PABA ethyl ester, dimethoxybenzyl dioxoimidazoline propionate ethylhexyl ester, p-methoxycinnamate isoamyl ester, isopentyl trimethoxycinnamate trisiloxane, isopropyl benzyl salicylate, isopropyl methoxycinnamate, 4-methylbenzyl camphor, PEG-25 PABA and dimethyl PABA pentyl ester. More preferably, oil-soluble UVB sunscreen agents are selected from one or more of octyl salicylate, 2-ethylhexyl 2-cyano-3,3-diphenyl-2-acrylate, and octyl methoxycinnamate.
[0013] Some well-known brands that sell the above sunscreen agents include Octisalate®, Homosalate®, Neo Heliopan®, Neo Heliopan® AV, Neo Heliopan® OS, Octocrylene®, and Parsol® MCX. The maximum wavelength (λ) of oil-soluble UV-B sunscreen agents is 280 to 320 nm.
[0014] The compositions of the present invention may comprise an organic, oil-soluble UVA sunscreen agent. When included, it is selected from one or more of dibenzoylmethane compounds, hexyl diethylaminohydroxybenzoylbenzoate, and methyl anthranilate. Dibenzoylmethane compounds are most preferably used in oil-soluble UVA sunscreen agents. Suitable dibenzoylmethane compounds are selected from one or more of the following: tert-butylmethoxydibenzoylmethane, 2-methyldibenzoylmethane, 4-methyldibenzoylethane, 4-isopropyldibenzoylmethane, 4-tert-butyldibenzoylmethane, 2,4-dimethyldibenzoylmethane, 2,5-dimethyldibenzoylmethane, 4,4'-diisopropyldibenzoylmethane, 2-methyl-5-isopropyl-4'-methoxydibenzoylmethane, 2-methyl-5-tert-butyl-4'-methoxydibenzoylmethane, 2,4-dimethyl-4'-methoxydibenzoylmethane, and 2,6-dimethyl-4-tert-butyl-4'-methoxydibenzoylmethane. The most preferred dibenzoylmethane compound is tert-butylmethoxydibenzoylmethane, which can be used as a Parsol... ® Obtained from 1789 Merchant Purchase.
[0015] The compositions of the present invention may comprise both organic oil-soluble UVB and organic UVA sunscreens. Alternatively, certain oil-soluble sunscreens possessing both UVA and UVB shielding properties exist. These are selected from one or more of the following: bis(ethylhexyloxyphenol) methoxyphenyl triazine, cresoltrazol trisiloxane, benzophenone, and their derivatives. The most preferred is bis(ethylhexyloxyphenol) methoxyphenyl triazine, commercially available from Tinosorb S.
[0016] The compositions of the present invention comprise 0.1 to 5% by weight of a water-soluble sunscreen agent. A water-soluble sunscreen agent, whether UVA or UVB type, means that the sunscreen agent has a solubility in water at 25°C greater than 10 g / L, preferably greater than 50 g / L.
[0017] Preferred water-soluble UVB sunscreens used in this invention are phenylbenzimidazole 5-sulfonic acid (PBSA), benzophenone-4, or benzyl camphorsulfonic acid, preferably PBSA. PBSA, also known as Ensulizole, is commercially available as Eusolex 232 (from Merck KGaA). PBSA is also available under the brand names Neo Heliopan Hydro (from Symrise), Parsol HS (from DSM), and Sunsafe ES (from Uniproma). Certain water-soluble sunscreens exist that provide both UVA and UVB protection. Such sunscreens offer protection against both UVA and UVB, such as benzophenone-4 (sold as Sulisobenzone). However, for the purposes of this invention, benzophenone-4 may be included as a water-soluble UV-B sunscreen.
[0018] Preferred UVA sunscreens used in this invention are one or more of disodium phenyl dibenzimidazole tetrasulfonate (Neohelipan AP) or terephthalic acid dicamphor sulfonic acid (TDSA). Among these, disodium phenyl dibenzimidazole tetrasulfonate is preferred, and is also known as bisdisulizole disodium. It is commercially available as Neo heliopan AP (from Symrise Shanghai Ltd) or Sunsafe DPDT (from Uniproma).
[0019] Terephthalimide dicamphor sulfonic acid (TDSA), also known as Ecamsule, is commercially available as L'Oreal's MexorylSX (US 4,585,597) or Sunsafe TDSA (from Uniproma). It can be used as a parent acid or its salt to provide the desired benefits. The composition preferably contains 0.1 to 5% by weight, more preferably 1 to 4% by weight, of a water-soluble sunscreen agent. Preferably, the composition contains both UVA and UVB water-soluble sunscreen agents. Most preferably, it includes one or both of 2-phenylbenzimidazole-5-sulfonic acid and disodium phenyldibenzimidazole tetrasulfonate.
[0020] Water-soluble sunscreens included in the compositions of the present invention are generally commercially available in acid form. When included in the composition in acid form (pre-neutralized form), i.e., having a sulfonic acid group (-SO3H), the composition further includes a neutralizing agent to convert the acid form into a salt form in which it is known to be active as a sunscreen, except for Mexoryl SX, which can function as a sunscreen in both neutralized and unneutralized states. When included, the neutralizing agent is preferably 0.05 to 4% by weight of the composition, more preferably 0.2 to 2%. The neutralizing agent is preferably an inorganic or organic base. The organic base is preferably an amine, such as triethanolamine or diethanolamine. The inventors of the present invention have observed that inorganic bases are particularly preferred. Alkali metal hydroxides are preferred. The most preferred metal hydroxide included in the compositions of the present invention as a neutralizing agent is sodium hydroxide or potassium hydroxide. Stabilizing the salt form of the water-soluble sunscreen in the gel composition while still obtaining the desired SPF enhancement and desired tactile sensory properties is a particularly challenging problem. The inventors of this invention have solved this problem by specifically selecting features (iii) to (vi) claimed in this invention, namely, aqueous thickeners, oil thickeners, humectants, and sensory modifiers.
[0021] The compositions of the present invention comprise an aqueous thickener. The aqueous thickener may be selected from one or more of (i) polysaccharide gums and (ii) synthetic polymers selected from (a) ammonium acryloyl dimethyl taurate / VP copolymers and (b) ammonium acryloyl dimethyl taurate / betaine-25 methacrylate crosslinked polymers. Of these, polysaccharide gums are most preferred. Preferred polysaccharide gums included in the compositions of the present invention are one or more of xanthan gum, guar gum, cellulose gum, tara gum, gellan gum, gum arabic, sclerotium gum, carrageenan, and locust bean gum. The most preferred polysaccharide gum is xanthan gum. Xanthan gum is commercially available from CP Kelco as Keltrol CG-V. The synthetic polymer ammonium acryloyl dimethyl taurate / VP copolymer is commercially available as Aristoflex AVC, and the ammonium acryloyl dimethyl taurate / betaine-25 methacrylate crosslinked polymer is commercially available as Aristoflex HMB. In a particularly preferred aspect of the invention, the mixture may include both polysaccharide gums such as xanthan gum and synthetic polymers Aristoflex AVC and Aristoflex HMB. The aqueous thickener is present in an amount of 0.25 to 5% by weight of the composition, preferably 0.5 to 4%, and most preferably 1 to 3%.
[0022] The compositions of the present invention comprise an oil-phase thickener selected from one or more of the following: C 18 To C 36 Fatty acid esters, C8 to C 16 Fatty acid esters; polymerized oil-phase thickeners; and particles selected from organically modified clays, hydrophobically modified fumed silica, and aerogels. Among these, C 18 To C 36 Fatty acid esters are the preferred choice.
[0023] Suitable commercially available C 18 To C 36 Fatty acid esters are C 18-36 Syncrowax HGLC, C 18-36 Syncrowax ERLC (ethylene glycol ester), Syncrowax HRC (glyceryl tris(hydroxystearate) ester), Naturchem GMHS (glyceryl hydroxystearate), Thixcin R (glyceryl tris(12-hydroxystearate) ester), C 16-18 Triglycerides, C 16-24Triglycerides (Cremeol HF-62-SPC). A particularly preferred oil-phase thickener used in the compositions of the present invention is available from Croda Personal Care as Syncrowax HGLC. It has a melting point of 60-70°C and also acts as a structural aid, crystallinity modifier, and emulsion stabilizer.
[0024] C8-C 16 An example of a fatty acid ester is hydrogenated cocoyl glycerol ester (Softisan 100).
[0025] The polymeric oil thickeners that may be included are sorbitol / sebacic acid copolymer sorbate (Syncrowax ORM), trisorbin (and) sorbitol / sebacic acid copolymer sorbate (Syncrowax OSW), dextrin palmitate (Dextrin Palmitate LDXP, HDXP, and HDXP-KL), amide-terminated polyamides (OleoCraft LP-20, MP-30, HP-31, and MP-32), ester-terminated polyamides (Uniclear 100VG and C75V), stearoyl inulin (Rheopearl ISK2), and polyacrylic acid C. 10-30 Alkyl ester (Intellimer IPA 13-6 polymer), polyacrylic acid C 10-30 Alkyl ester-MP 48C (IntellimerIPA 13-1 polymer) and PVP (FlexiThix) TM (Thickener).
[0026] The particles that act as oil phase thickeners may be selected from one or more of the following: organic modified clays such as cationic surfactants containing sepiolite, montmorillonite, hydrophobic or bentonite, fumed silica, hydrophobically modified fumed silica, and aerogels such as Dow Corning VM-2270 aerogel fine particles and Aerosil® R 972 (Silica Silyate-Evonik).
[0027] The content of the oil phase thickener is preferably 0.5 to 10% by weight of the composition, more preferably 0.8 to 5%, and even more preferably 1% to about 3%.
[0028] The compositions of the present invention comprise a humectant selected from glycols or glycerin. The glycol is preferably selected from one or more of propylene glycol, butylene glycol, and caprylyl glycol. The humectant used in the present invention is one or both of glycerin and caprylyl glycol. The composition comprises 0.5 to 15%, preferably 1 to 10%, more preferably 1 to 8% of the humectant by weight of the composition.
[0029] The composition comprises a sensory modifier selected from one or more of the following: - Modified starch, - Silica microspheres, and - A polymer of dimethicone / vinyl dimethicone crosslinked polymer and silica.
[0030] Of these, one or both of the silica microspheres and the polymer are most preferably included in the composition.
[0031] The polymer used as a sensory modifier is preferably a dimethylpolysiloxane / vinyldimethylpolysiloxane crosslinked polymer (and) silica. The dimethylpolysiloxane / vinyldimethylpolysiloxane crosslinked polymer (and) silica can be sourced from Dow Corning as DOWSIL. TM 9701 cosmetic powder is obtained and is also known as DC 9701. Silica microspheres are available from Kobo as MSS-500 / 3H.
[0032] Preferred modified starches are aluminum starch octenyl succinate or sodium starch, more preferably aluminum starch octenyl succinate. Aluminum starch octenyl succinate is a chemically modified starch, particularly starch that has undergone esterification. This aluminum starch octenyl succinate is available from suppliers such as Akzo Nobel or Nouryon under the names Dry Flo® Pure and Dry Flo® PC. Various other suppliers sell it under their own brand names. In cosmetic and personal care products, aluminum starch octenyl succinate is used in the formulation of lotions, powders, makeup, and underarm deodorants. It acts as a thickener and binder, an anti-caking agent, and an oil absorbent. The composition may contain aluminum starch octenyl succinate that is further blended with other ingredients to provide additional benefits. For example, it may contain an ingredient with the INCI name aluminum starch octenyl succinate (and) acrylate copolymer (and) magnesium carbonate. It is available from Nouryon as NATRASORB® HFB. It contains 81% natural ingredients and is recommended for various applications including moisture-wicking products, oil-controlling products, anhydrous products, antiperspirants, sunscreens, and dry shampoos, offering multiple benefits such as oil absorption, relief from dehydration and shrinkage, and fragrance retention. Literature from Nouryon discloses that it is cross-linked aluminum starch octenyl succinate surface-treated with acrylate copolymers and magnesium carbonate.
[0033] The sensory modifier is present in an amount of 0.5 to 10% by weight of the composition, preferably 1 to 8%, more preferably 1 to 5%. Among these, the polymer is preferably 0.2 to 3% by weight when included, the silica microspheres are 0.2 to 3% by weight when included, and the modified starch is 0.5 to 4% by weight when included.
[0034] The composition comprises a vitamin B3 compound. Preferably, the vitamin B3 compound is selected from nicotinamide, pyridinecarboxamide, isonicotinamide, N-cyclopropylnicotinamide, N-cyclobutylnicotinamide, N-cyclopentylnicotinamide, N-cyclohexylnicotinamide, and mixtures thereof. More preferably, the vitamin B3 compound is nicotinamide, pyridinecarboxamide, isonicotinamide, and mixtures thereof. Even more preferably, the vitamin B3 compound is nicotinamide.
[0035] The composition contains 0.01 to 10% by weight, preferably 0.1 to 9% by weight, preferably 0.5 to 8% by weight, preferably 1 to 7% by weight, preferably 2 to 6% by weight, preferably 3 to 5% by weight, for example 4% by weight of a vitamin B3 compound.
[0036] The composition further comprises an antioxidant selected from vitamin C or its derivatives (e.g., sodium ascorbate palmitate and sodium ascorbate phosphate), dilauryl thiodipropionate (Tinogard DA), pentaerythritol tetra(di-tert-butylhydroxycinnamate) ester (Tinogard TT), tris(tetramethylhydroxypiperidinol) citrate (Tinogard Q), and mixtures thereof. More preferably, the antioxidant is selected from vitamin C or its derivatives (e.g., sodium ascorbate palmitate and sodium ascorbate phosphate), dilauryl thiodipropionate, and mixtures thereof. Even more preferably, the selected antioxidant is any one of sodium ascorbate phosphate and dilauryl thiodipropionate, or a mixture thereof.
[0037] The composition comprises 0.01 to 10% by weight, preferably 0.1 to 9% by weight, preferably 1 to 8% by weight, preferably 2 to 7% by weight, preferably 3 to 6% by weight, preferably 4 to 5% by weight of an antioxidant.
[0038] Within the scope of the gel compositions of this invention, components such as vitamin B3 compounds, due to their water-soluble properties, such as nicotinamide (water-soluble at 20°C of 1000 g / L), are present in the aqueous phase of the composition. However, it has been found that due to the high water solubility of such vitamin B3 compounds, when such components are incorporated in increased amounts into gels disclosed in the prior art, the gel composition tends to become discolored, i.e., it tends to lead to a loss of color stability.
[0039] The inventors of this invention have discovered that when a selected antioxidant is added to a gel composition, it prevents loss of color stability despite containing an increased amount (e.g., 3% by weight) of a water-soluble compound such as vitamin B3 (i.e., nicotinamide). It also results in a reduction of reactive oxygen species generated due to external and / or internal factors (such as those mentioned above).
[0040] The compositions of the present invention are preferably substantially free of emulsifiers. Emulsifiers are typically anionic, nonionic, cationic, and amphoteric surfactants or surface-active agents. A few examples include glyceryl stearate, glycol stearate, and stearamide AMP. Therefore, the compositions are preferably substantially free of such emulsifiers. Preferably, "substantially free of emulsifiers" means that the emulsifier content is less than or equal to 2% by weight, more preferably less than 2% by weight, even more preferably less than 1.5% by weight, further more preferably less than 1% by weight, and most preferably less than 0.5% by weight, ideally not present in the compositions of the present invention. Alternatively, the compositions preferably contain 0 to 2% by weight, more preferably 0.1 to 1.5% by weight, even more preferably 0.25 to 1% by weight, and still more preferably 0.5 to 0.75% by weight of emulsifier.
[0041] It should be understood that terms such as “substantially emulsifier-free” and “emulsifier-free” are used interchangeably and they mean the same thing.
[0042] Therefore, the composition is preferably an emulsifier-free gel composition comprising: (i) 0.1 to 25% by weight of oil-soluble sunscreen agents; (ii) 0.1 to 5% by weight of water-soluble sunscreen; (iii) 0.25 to 5% by weight of an aqueous thickener, wherein the aqueous thickener is selected from one or two of polysaccharide gums and synthetic polymers, wherein the synthetic polymers are selected from ammonium acryloyl dimethyl taurate / VP copolymers and ammonium acryloyl dimethyl taurate / behenol polyether-25 methacrylate crosslinked polymers; (iv) 0.5% to 10% of an oil-phase thickener, said oil-phase thickener being selected from one or more of the following: C 18 To C 36 Fatty acid esters, C8 to C 16 Fatty acid esters; polymeric oil-phase thickeners; and particles selected from organically modified clays, hydrophobically modified fumed silica, and aerogels. (v) 0.5 to 15% by weight of a humectant, said humectant being selected from glycerin or glycol; and (vi) 0.5 to 10% by weight of a sensory modifier, said sensory modifier being selected from one or more of the following: modified starch, silica microspheres, and polymers of dimethicone / vinyl dimethicone crosslinked polymers with silica. (vii) 0.01 to 10% by weight of vitamin B3 compounds; and (viii) 0.01 to 10% by weight of an antioxidant, said antioxidant being selected from vitamin C or its derivatives (e.g., sodium ascorbate palmitate and sodium ascorbate phosphate), dilauryl thiodipropionate and mixtures thereof.
[0043] Water is typically included in gel compositions as a cosmetically acceptable base. The water content can be 10 to 70% by weight of the composition, preferably 20 to 70%, and more preferably 20 to 65%.
[0044] Preferably, the composition further comprises a moisturizing agent, such as hyaluronic acid. Hyaluronic acid may be added to the composition as sodium hyaluronate. Preferably, the amount of hyaluronic acid added may be 0.1 to 10% by weight of the composition of the present invention, more preferably 1 to 8% by weight, more preferably 2 to 6% by weight, and more preferably 3 to 5% by weight.
[0045] In addition to the ingredients disclosed above, the composition may and preferably does contain other ingredients to achieve one or more functions of the invention, including a cosmetically acceptable carrier. Emollient materials may be used as cosmetically acceptable carriers. These may be in the form of silicone oils, natural or synthetic esters, and hydrocarbons. The amount of emollient may be from 0.1% to 25% by weight of the composition, preferably 1% and 10%. Silicone oils can be classified into volatile and non-volatile types. The term "volatile" as used herein refers to those materials that have a measurable vapor pressure at ambient temperature. Volatile silicone oils are preferably selected from cyclic (cyclic polydimethylsiloxanes) or linear polydimethylsiloxanes containing 3 to 9, preferably 5 to 6, silicon atoms.
[0046] Colorants, opacifiers, and abrasives may also be included in the compositions of the present invention. Each of these substances may constitute 0.05 to 5% of the weight of the composition, preferably 0.1 to 3%.
[0047] The compositions of the present invention provide an external sun protection factor (SPF) of preferably at least 30, more preferably at least 40, and even more preferably at least 50.
[0048] Furthermore, the present invention also relates to a method for providing sun protection with a sun protection factor (SPF) of at least 30, the method comprising the step of applying the composition of the present invention to a desired skin surface. Optionally, the method further comprises the step of washing off the composition applied in a previous step. If the method includes the step of washing off the composition, this step is preferably performed within 5 minutes, preferably within 4 minutes, preferably within 2 minutes, preferably within 1 minute, for example within 30 seconds, starting from the step of applying the composition.
[0049] The compositions according to the invention are primarily intended as products for topical application to human skin, particularly as agents for protection against solar radiation and for preventing or reducing pigmentation, wrinkles, or the appearance of aging skin, or age spots. Preferably, the method is cosmetic / non-therapeutic.
[0050] In use, a small amount of the composition, such as 1 to 5 ml, is applied to the skin from a suitable container or applicator, preferably to areas of skin exposed to or likely to be exposed to sunlight, and if necessary, spread and / or rubbed onto the skin with the hand or fingers or a suitable device.
[0051] Therefore, the present invention also relates to the use of the compositions of the present invention as described above for providing light protection of at least 30, preferably at least 40, preferably at least 50 SPF. Preferably, the use is non-therapeutic / cosmetic.
[0052] While the invention has been summarized above, it will be apparent to those skilled in the art that modifications, variations, and alterations can be made without departing from the scope and spirit of the invention as described and claimed herein. The invention is now further illustrated in the following non-limiting embodiments.
[0053] Example Preparation of controls and according to the present invention: Briefly, the compositions shown in the table below are prepared as follows: Add glycerol, disodium EDTA, phenylbenzimidazole sulfonic acid (ensolidazole), and sodium hydroxide (to pH 7) to the water in the main container. Stir the mixture until the aqueous phase becomes clear and heat to 70°C. Prepare a solution in a separate beaker containing an oil phase thickener (if applicable), caprylyl glycol, ethylhexyl salicylate, octocrylene, and octyl methoxycinnamate (Parsol). ® MCX) and butylmethoxydibenzoylmethane (Parsol) ® The oil phase of (1789) was heated to 70°C. Aristoflex AVC and Aristoflex HMB were added to the master container under homogenization conditions. The aqueous phase was allowed to become a clear gel. Then, the oil phase was added to the master container under homogenization conditions at 3500 rpm. The mixture was homogenized for 10 minutes, followed by the addition of xanthan gum pre-dispersed in 5 mL of water. DC 245 and (if applicable) MSS 500 / 3H were mixed and added to the master container, and mixed for 10 minutes. If applicable, Dowsil 9701 was then added to the master container and mixing continued. Once the master container reached below 40°C, ethanol, fragrance, phenoxyethanol, nicotinamide, and antioxidants were added to the master container; and mixed for 10 minutes. When the formulation reached room temperature and had a homogeneous structure, it was removed from the homogenizer and stored in a container.
[0054] SPF measurement: The in vitro SPF and UVAPF values of the samples shown in Table 4 below were measured using the following procedure: Thin film transmittance was measured using a Labsphere UV transmittance analyzer. In this study, a 70 × 70 mm PMMA plate with a roughness of approximately 6 µm from Schönberg GmbH & Co. was used. The percentage of transmittance for various compositions was measured using the procedure outlined below. 2 mg / cm 2 The sample is applied to a PMMA plate, evenly distributed and spread using a syringe. The PMMA plate is dried for 30 minutes. After drying, the sample plate is exposed to UV light and a transmittance scan is recorded. This scan gives the transmittance of a given sample as a function of wavelength (290–400 nm). For a single plate, six to nine different points are scanned. The same procedure is repeated for two or three plates. Therefore, the reported data is the average of 12–18 readings. A reference transmittance scan is obtained using a blank plate, where no sample is present on the PMMA plate and glycerol is spread on it. The transmittance values are used to derive the SPF value using the UV-2000s application provided with the instrument.
[0055] The in vitro SPF (and therefore SPF) was measured at zero time (0-minute line). The same plate was exposed to simulated sunlight, and the percentage of transmittance was measured at designed time intervals from 0 to 60 minutes. Average absorbance at 310 and 355 nm was recorded to measure the percentage of UVB and UVA photostability, respectively. A solar simulator (Atlas kW system) was used at a distance of approximately 20 cm, employing a 550 W m² sensor. -2 The irradiance produces UV radiation.
[0056] Color stability: Color stability was measured as follows: The compositions in Table 3 below were incubated in an incubator at 45 to 50°C for 2 weeks to 3 months, for example, 1 month. After the desired incubation period, the color was measured using a colorimeter and expressed in Hunter Lab color space L*, a*, and b*, where L* is the black-white space, a* is the green-red space, and b* is the blue-yellow space. The L*, a*, and b* values of the compositions were also measured before incubation. These values were used to calculate the color change (expressed as Delta E (ΔE)). The smaller the ΔE, the more stable the color of the composition.
[0057] Cell culture and ultraviolet exposure: Keratinocytes (HaCaT cells) were sized at a density of 3.5 × 10⁻⁶. 4Cells were seeded at a density of 10 cells / well in 48-well plates and maintained in reconstituted DMEM medium as described above for 24 to 48 hours. Cells were exposed to UV light using a solar simulator containing a xenon arc lamp, if necessary. Cells not exposed to UV light served as a control. Prior to exposure, the composition was uniformly applied to PMMA plates (2 mg / cm²). 2 The plates were incubated in a 5% CO2 / 37℃ incubator for 6 hours. After incubation, cells were harvested, and ROS levels were measured using the DCFDA assay.
[0058] DCFDA assay method: Cells at 100 mJ / cm 2 Cells were exposed to UVA and not exposed to UVA, then incubated in a CO2 incubator at 37°C for 6 hours. After 6 hours, cells were washed with 1X PBS and treated with medium containing DCFDA reagent, then incubated in a CO2 incubator at 37°C for 30 minutes. Cells were then washed once with 1X PBS, followed by the addition of fresh PBS. The plates were then wrapped with aluminum foil, and readings were taken at an excitation wavelength of 485 nm and an emission wavelength of 535 nm. After background subtraction, the amount of ROS generated was calculated as a percentage of the control.
[0059] Prepare the compositions shown in Table 1 as described above; and evaluate ROS generation as described above.
[0060] Table 1: Comparative compositions (Examples A and B), compositions of the present invention (Examples 1 and 2), and their ROS data
[0061] In addition, the additional compositions shown in the examples in Table 2 below were prepared, and their color stability was evaluated as previously described.
[0062] Table 2: Additional Examples
[0063] Table 3: Color Stability
[0064] When measured as described above, the compositions shown in Examples 1 to 6 obtained an in vitro SPF of 75 to 85 and an in vitro UVA protection factor (UVAPF) of 25 to 30.
[0065] Table 4: Additional Examples
Claims
1. A personal care composition comprising: (i) 0.1 to 25% by weight of oil-soluble sunscreen agents, (ii) 0.1 to 5% by weight of water-soluble sunscreen agent, (iii) 0.25 to 5% by weight of an aqueous thickener, wherein the aqueous thickener is selected from one or two of polysaccharide gums and synthetic polymers, wherein the synthetic polymers are selected from ammonium acryloyl dimethyl taurate / VP copolymers and ammonium acryloyl dimethyl taurate / behenol polyether-25 methacrylate crosspolymers. (iv) 0.5% to 10% of an oil-phase thickener, said oil-phase thickener being selected from one or more of the following: C 18 To C 36 Fatty acid esters, C8 to C 16 Fatty acid esters; polymeric oil-phase thickeners; and particles selected from organically modified clays, hydrophobically modified fumed silica, and aerogels. (v) 0.5 to 15% by weight of a humectant, said humectant being selected from glycerin or glycol. (vi) 0.5 to 10% by weight of a sensory modifier, said sensory modifier being selected from one or more of the following: modified starch, silica microspheres, and polymers of dimethicone / vinyl dimethicone crosslinked polymers with silica. (vii) 0.01 to 10% by weight of vitamin B3 compounds; and (viii) 0.01 to 10% by weight of an antioxidant selected from dilaurate thiodipropionate (Tinogard DA), pentaerythritol tetra(di-tert-butylhydroxyhydrocinnamate) ester (Tinogard TT), tris(tetramethylhydroxypiperidinol) citrate (Tinogard Q), vitamin C or derivatives thereof, and mixtures thereof, wherein the vitamin C derivative is selected from sodium ascorbate palmitate and sodium ascorbate phosphate.
2. The composition according to claim 1, wherein the oil-soluble sunscreen agent is selected from UV-B sunscreen agents or UV-A sunscreen agents, wherein the UV-B sunscreen agent is selected from one or more of octyl salicylate, 2-cyano-3,3-diphenyl-2-acrylate 2-ethylhexyl ester and octyl methoxycinnamate; and wherein the UV-A sunscreen agent is selected from dibenzoylmethane compounds.
3. The composition according to claim 2, comprising 0.1 to 5% by weight of an oil-soluble UVA sunscreen agent.
4. The composition according to claim 2 or 3, comprising 0.1 to 20% by weight of an oil-soluble UVB sunscreen agent.
5. The composition according to any one of the preceding claims, wherein the water-soluble sunscreen agent is selected from one or both of 2-phenylbenzimidazole-5-sulfonic acid and disodium phenyldibenzimidazole tetrasulfonate.
6. The composition according to any one of the preceding claims, wherein the polysaccharide gum is xanthan gum.
7. The composition according to any one of the preceding claims, wherein the diol is selected from one or more of propylene glycol, butanediol, and octyl glycol.
8. The composition according to any one of the preceding claims, wherein the sensory modifier is selected from one or two of silica microspheres and polymers of dimethicone / vinyl dimethicone crosslinked polymers and silica.
9. The composition according to any one of the preceding claims, comprising 10 to 70% by weight of water.
10. The composition according to any one of the preceding claims is substantially free of emulsifiers.
11. The composition according to any one of the preceding claims, wherein the vitamin B3 compound is selected from 1 to 7% by weight of nicotinamide, pyridinecarboxamide, isonicotinamide, N-cyclopropylnicotinamide, N-cyclobutylnicotinamide, N-cyclopentylnicotinamide, N-cyclohexylnicotinamide, and mixtures thereof.
12. The composition according to any one of the preceding claims, wherein the vitamin B3 compound is selected from nicotinamide.
13. The composition according to any one of the preceding claims, wherein the antioxidant is selected from vitamin C or its derivatives, such as sodium ascorbate palmitate and sodium ascorbate phosphate, dilauryl thiodipropionate and mixtures thereof.
14. The composition according to any one of the preceding claims, wherein the composition further comprises hyaluronic acid or a salt thereof.
15. A method of providing light protection with a sun protection factor (SPF) of at least 30, the method comprising the step of applying a composition according to any one of the preceding claims to a desired skin surface.
Citation Information
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