Photoprotective composition

Abstract

The present invention relates to photoprotective personal care compositions that provide a high sun protection factor along with protection against UVA and UVB-induced inflammation and oxidative stress, which is achieved by compositions containing a combination of oil-soluble sunscreens, water-soluble sunscreens, and nonionic surfactants with HLB values in the range of 9-20, along with specific vitamins.

Description

[Technical Field]

[0001] The present invention relates to photoprotective compositions that provide a high sun protection factor. Furthermore, the topical compositions are formulated to provide high protection against UV-induced inflammatory and oxidative stress that can be caused by the small amounts of UV rays that penetrate the sunscreen layer and reach the skin. [Background technology]

[0002] Solar radiation contains approximately 5% ultraviolet (UV) radiation, with wavelengths between 200 and 400 nm. UV radiation is further divided into three regions: 320–400 nm (UV-A), 280–320 nm (UV-B), and 200–280 nm (UV-C). A significant portion of UV-C radiation is absorbed by the ozone layer. Scientific studies have shown that short-term exposure to UV-A and UV-B radiation can cause skin pigmentation, redness, and local inflammation, while continuous or prolonged exposure can lead to sunburn, melanoma, wrinkles, and the formation of age spots. UV radiation is also believed to cause significant damage to hair. Therefore, it is desirable to protect human skin and other keratinous substrates from the harmful effects of both UV-A and UV-B radiation. This is achieved by cosmetic compositions that provide a high SPF (sun protection factor).

[0003] A variety of cosmetic preparations have been reported to prevent and / or protect skin from the harmful effects of ultraviolet radiation.Many organic sunscreens capable of absorbing UV-A rays have been reported in the cosmetic field, and one particularly useful sunscreen is t-butyl methoxydibenzoylmethane (also known as avobenzone, sold as Parsol® 1789).Various UV-B sunscreens are also known and used in personal care compositions for protection from UV-B rays.Many cosmetic manufacturers prefer to include UV-A and UV-B sunscreens in photoprotective compositions to provide full-spectrum protection against UV radiation. Summary of the Invention [Problem to be solved by the invention]

[0004] One such patent by the applicant is published as EP2575748B1, which discloses a composition providing a high SPF. This publication discloses only the use of certain oil-soluble sunscreens. The effectiveness of the sunscreen in this patent is enhanced by the inclusion of certain nonionic surfactants in combination with fatty acids and, optionally, certain specific polymers. With the advent of many water-soluble sunscreens, the inventors have experimented with combining oil-soluble and water-soluble sunscreens to provide better SPF. While the inclusion of oil-soluble and water-soluble sunscreens ensures high sun protection, this approach has two problems. Increasing the amount of such sunscreen does not provide a proportional increase in sun protection; rather, efficacy plateaus. Second, increasing the amount of sunscreen simultaneously increases costs. Even with very high sunscreen loadings, there will always be residual amounts of UV rays (both UVA and UVB) that penetrate the sunscreen layer, causing irritation and oxidative stress to the skin. On the one hand, the inventors want to provide high sun protection, but on the other hand, they want to provide a sunscreen at the lowest possible cost to the consumer, while keeping skin irritation and oxidative stress as low as possible.

[0005] Additionally, visible light, such as blue light, has also been reported to produce undesirable effects, such as aging and pigmentation. Therefore, there is also a need to provide compositions that provide protection against visible light, such as blue light.

[0006] The inventors have achieved this by using both water- and oil-soluble sunscreens, by using certain nonionic surfactants, and by using certain vitamins, namely vitamin B3 and vitamin C, which have been shown to interact synergistically in such compositions to provide enhanced anti-inflammatory and protection against oxidative stress.

[0007] It is therefore an object of the present invention to provide a photoprotective composition containing both oil-soluble and water-soluble sunscreens that provides a high SPF while offering good protection against UV-induced inflammation and oxidative stress.

[0008] Another object of the present invention is to provide a photoprotective personal care composition that provides high SPF and excellent protection against UV-induced irritation and oxidative stress while imparting desirable sensory properties to the skin.

[0009] Another object of the present invention is to provide a photoprotective personal care composition that provides protection against visible light-induced, eg, blue light-induced, oxidative stress.

[0010] Another object of the present invention is to provide a photoprotective personal care composition that provides protection against visible light, e.g., blue light, induced oxidative stress while delivering desirable sensory properties to the skin. [Means for solving the problem]

[0011] A first aspect of the present invention is (i) 0.1 to 10 wt. % of an oil-soluble sunscreen; (ii) 0.2 to 5 wt. % of a water-soluble sunscreen; (iii) 0.1 to 5 wt. % of a nonionic surfactant having an HLB value in the range of 9 to 20; (iv) 0.1 to 3% by weight of a vitamin B3 compound, derivative or precursor thereof; (v) 0.01 to 5% by weight of vitamin C or a derivative thereof A photoprotective composition comprising: The present invention relates to a photoprotective composition, wherein the composition further comprises 3 to 25% by weight of one or more saturated fatty acids.

[0012] Another aspect of the present invention relates to a method of providing photoprotection with a Sun Protection Factor (SPF) of at least 15, comprising applying the composition of the first aspect onto the desired skin surface.

[0013] Yet another aspect of the present invention relates to a method of protecting skin against UVA and UVB induced inflammation and oxidative stress comprising applying the composition of the first aspect onto the desired skin surface.

[0014] Yet another aspect of the present invention relates to a method of protecting skin against visible light, e.g., blue light, induced oxidative stress, comprising applying the composition of the first aspect onto the desired skin surface. DETAILED DESCRIPTION OF THE INVENTION

[0015] These and other aspects, features, and advantages will become apparent to those skilled in the art upon reading the following detailed description and the appended claims. For the avoidance of doubt, any feature of one aspect of the present invention may be utilized in any other aspect of the present invention. The word "comprising" is intended to mean "including," but not necessarily "consisting of" or "composed of." In other words, the listed steps or options need not be exhaustive. It should be noted that the examples set forth in the following description are intended to clarify the invention, but are not intended to limit the invention to those exact examples.

[0016] Similarly, all percentages are weight / weight percent unless otherwise specified. Except in the working and comparative examples, or unless expressly indicated otherwise, all numbers in the description and claims expressing amounts of materials or reaction conditions, physical properties of materials, and / or uses should be understood to be modified by the word "about." Numerical ranges expressed in the format "from x to y" are understood to be inclusive of x and y. When multiple preferred ranges for a particular feature are described in the format "from x to y," it is clear that all ranges combining the different endpoints are also contemplated.

[0017] The photoprotective compositions of the present invention are intended for use in personal care or cosmetic applications and may also be referred to as personal care or cosmetic compositions. As used herein, "personal care composition" is intended to include compositions for topical application to sun-exposed areas of human skin and / or hair. Such compositions may be classified as leave-on or rinse-off and include products applied to the human body to improve appearance, cleansing, odor control, or overall beauty. The compositions of the present invention can be in the form of a liquid, lotion, cream, foam, stick, or gel. Non-limiting examples of such sunscreen compositions include leave-on skin lotions, creams, antiperspirants, deodorants, foundations, mascaras, sunscreen lotions, and wash-off shampoos, conditioners, and shower gels. The compositions of the present invention are preferably leave-on compositions.

[0018] As used herein, "skin" includes the skin of the face and body (e.g., neck, chest, back, arms, armpits, hands, feet, and scalp), and particularly those parts thereof that are exposed to sunlight. The compositions of the present invention are also suitable for application to other keratinous substrates of the human body other than skin, such as, for example, hair, in which case the product may be formulated with the specific purpose of improving photoprotection.

[0019] The compositions of the present invention comprise 0.1 to 10% by weight of an oil-soluble sunscreen. By oil-soluble, we mean an organic sunscreen having a water solubility of less than 10 g / L, preferably less than 5 g / L, and more preferably less than 2 g / L. Thus, most oil-soluble sunscreens used in the present invention have a water solubility of 0 to 2 g / L. It is believed that oil-soluble sunscreens can be of the UV-B or UV-A type. It is preferred that compositions of the present invention comprise 1 to 8% by weight of such sunscreens.

[0020] If an oil-soluble UVB sunscreen is included, it is preferably octyl salicylate, 3,3,5-trimethylcyclohexyl 2-hydroxybenzoate, ethylhexyl salicylate, 2-ethylhexyl 2-cyano-3,3-diphenyl-2-propenoate (also known as octocrylene), 2-ethylhexyl-4-methoxycinnamate or octyl methoxycinnamate, ethylhexyl triazone, 3-benzylidene camphor, cinoxate, diethylhexyl butamido triazone, para-aminobenzoic acid (PABA), ethyl dihydroxypropyl PABA, ethylhexyl dimethoxybenzylidene dioxoimidazoline propionate, isoamyl p-methoxycinnamate, isopentyl trisiloxane trimethoxycinnamate, benzyl isopropyl salicylate, isopropyl methoxycinnamate, 4-methylbenzylidene camphor, PEG-25 PABA, and one or more of pentyl dimethyl PABA. More preferred oil-soluble UVB sunscreens are selected from one of octyl salicylate, 3,3,5-trimethylcyclohexyl 2-hydroxybenzoate, ethylhexyl salicylate, 2-ethylhexyl 2-cyano-3,3-diphenyl-2-propenoate, and 2-ethylhexyl-4-methoxycinnamate, and even more preferred are one or more of 2-ethylhexyl-4-methoxycinnamate, ethylhexyl salicylate, and 2-ethylhexyl 2-cyano-3,3-diphenyl-2-propenoate. Some of the well-known brands under which the above sunscreens are sold are Octisalate®, Homosalate®, Neo Heliopan®, Neo Heliopan® AV, Neo Heliopan® OS, Octocrylene®, and Parsol® MCX. Oil-soluble UV-B sunscreens have a λmax of 280 to 320 nm.

[0021] The compositions of the present invention may contain an organic oil-soluble UVA sunscreen, which, if present, is selected from one or more of dibenzoylmethane compounds, diethylaminohydroxybenzoylhexylbenzoate, and methyl anthranilate. Of the oil-soluble UVA sunscreens, dibenzoylmethane compounds are the most preferred. Suitable dibenzoylmethane compounds are selected from one or more of t-butyl methoxydibenzoylmethane, 2-methyl dibenzoylmethane, 4-methyl dibenzoylethane, 4-isopropyl dibenzoylmethane, 4-tert-butyl dibenzoylmethane, 2,4-dimethyl dibenzoylmethane, 2,5-dimethyl dibenzoylmethane, 4,4'-diisopropyl dibenzoylmethane, 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 t-butyl methoxydibenzoylmethane. It is commercially available as Parsol 1789.

[0022] The compositions of the present invention may contain both organic oil-soluble UVB and organic UVA sunscreens. Alternatively, there are specific oil-soluble sunscreens that have both UVA and UVB screening efficacy. These are selected from one or more of bis-ethylhexyloxyphenol methoxyphenyl triazine, drometrizole trisiloxane, benzophenone, and its derivatives. The most preferred is bis-ethylhexyloxyphenol methoxyphenyl triazine, commercially available as Tinosorb S.

[0023] The composition of the present invention contains 0.2 to 5% by weight of a water-soluble sunscreen agent.

[0024] By water-soluble sunscreen, we mean that the sunscreen, whether UVA or UVB, has a water solubility of greater than 10 g / L, preferably greater than 50 g / L, at 25° C. Most water-soluble sunscreens used in the present invention have a water solubility in the range of 10-100 g / L.

[0025] Preferred water-soluble UVB sunscreens for use in the present invention are phenylbenzimidazole sulfonic acid (PBSA), benzophenone-4, or benzylidene camphorsulfonic acid, preferably PBSA. PBSA, also known as ensulizole, is commercially available as Eusolex 232 (Merck KGaA). PBSA is also available under the trade names Neo Heliopan Hydro (Symrise), Parsol HS (DSM), and Sunsafe ES (Uniproma). Certain water-soluble sunscreens exist that have both UVA and UVB screening efficacy. Such sunscreens provide both UVA and UVB protection, and include, for example, benzophenone-4 (sold as Sulisobenzone). However, in the present invention, benzophenone-4 can be included as a water-soluble UV-B sunscreen.

[0026] Preferred UVA sunscreens for use in the present invention are one or more of phenyldibenzimidazole tetrasulfonate disodium salt (Neoheliopan AP) or terephthalylidene dicamphorsulfonic acid (TDSA). Phenyldibenzimidazole tetrasulfonate disodium salt is also known as bisdisulizole disodium salt. It is commercially available as Neoheliopan AP (manufactured by Symrise Shanghai Ltd.) or Sunsafe DPDT (manufactured by Uniproma).

[0027] Terephthalylidene dicamphorsulfonic acid (TDSA), also known as ecamsul, is commercially available as Mexoryl SX (US Pat. No. 4,585,597) from L'Oreal or Sunsafe TDSA (Uniproma). It can be used as the parent acid or its salt to provide the desired benefits.

[0028] The composition preferably contains 0.1 to 5% by weight, more preferably 1 to 3% by weight, of a water-soluble UVA sunscreen.The composition preferably contains 0.1 to 5% by weight, more preferably 1 to 4% by weight, of a water-soluble UVB sunscreen.

[0029] Water-soluble sunscreens for inclusion in the compositions of the present invention are generally commercially available in their acid form. When included in the composition in their acid form (pre-neutralized form), i.e., having sulfonic acid groups (—SO₃H), the composition further contains a neutralizing agent to convert the acid form to a salt form, which is known to be active as a sunscreen, except for Mexoryl SX, which can act as a sunscreen with or without neutralization. When included, the neutralizing agent is preferably present in an amount of 0.05% to 4% by weight of the composition, more preferably 0.2% to 2% by weight. Preferred neutralizing agents are inorganic or organic alkalis. Preferred organic alkalis are amines such as triethanolamine and diethanolamine. Based on the inventors' observations, inorganic alkalis are particularly preferred. Alkali metal hydroxides are preferred. The most preferred metal hydroxides for inclusion as neutralizing agents in the compositions of the present invention are sodium hydroxide or potassium hydroxide.

[0030] The composition of the present invention comprises a nonionic surfactant having an HLB value in the range of 9 to 20. More preferably, the nonionic surfactant is selected from those having an HLB value in the range of 12 to 20, and even more preferably from 12 to 18.

[0031] HLB is calculated using the Griffin method, HLB = 20 × Mh / M, where Mh is the molecular mass of the hydrophilic portion of the molecule and M is the molecular mass of the whole molecule, giving results on an arbitrary scale of 0 to 20.

[0032] Preferably, the nonionic surfactant having an HLB value in the range of 9 to 20 is selected from one or more of fatty alcohol ethoxylates, fatty acid ethoxylates, alkylphenol ethoxylates, and polyoxyethylene sorbitan alkyl esters.

[0033] Examples of fatty alcohol ethoxylates that may be used as nonionic surfactants in the composition include polyoxyethylene lauryl ether (HLB=16.9; commercially available as Brij® 35), polyoxyethylene (20) cetyl ether (HLB=16; commercially available as Brij® 58), polyethylene glycol octadecyl ether (HLB=18.8; commercially available as Brij® 700), and laureth-9 (C12EO9; HLB=14.3; commercially available as Brij® L9).

[0034] Examples of alkylphenol ethoxylates that may be used as nonionic surfactants in the composition include octylphenol ethoxylate (HLB=15.5; commercially available as Triton® X165), octylphenol ethoxylate (HLB=17.6; commercially available as Triton® X405), and octylphenol ethoxylate (HLB=18.4; commercially available as Triton® X705).

[0035] Examples of polyoxyethylene sorbitan alkyl esters that may be used as nonionic surfactants in the composition include polyoxyethylene sorbitan monolaurate (HLB=13.3; commercially available as Tween® 21), polyoxyethylene sorbitan monolaurate (HLB=16.7; commercially available as Tween® 20), polyoxyethylene sorbitan monopalmitate (HLB=15.6; commercially available as Tween® 40), and polyoxyethylene sorbitan monostearate (HLB=14.9; commercially available as Tween® 60).

[0036] Fatty acid ethoxylates are available in the Myrj class. Suitable examples of commercially available nonionic surfactants for use in compositions of this class are Myrj S40 (PEG-40 stearate), Myrj S50 (PEG-50 stearate) or Myrj 59 (PEG-100 stearate).

[0037] Preferably, the composition comprises 0.2-5 wt. %, more preferably 0.5-4 wt. %, even more preferably 1-3 wt. % of a nonionic surfactant having an HLB in the range of 9-20.

[0038] The compositions of the present invention contain a vitamin B3 compound, a derivative, or a precursor thereof. This includes compounds that are carboxylic acid-functionalized heteroaromatic compounds. These may be selected from one or more of nicotinic acid, picolinic acid, nicotinic acid salts, niacinamide, and picolinamide. It is preferably one or both of niacinamide and picolinamide, and most preferably niacinamide. The vitamin B3 compound is typically present in an amount of 0.1 to 5% by weight, preferably 0.5 to 3% by weight, of the composition.

[0039] This composition contains 0.01 to 5% by weight of vitamin C or its derivatives. Vitamin C (ascorbic acid, ascorbate) is a simple, low-molecular-weight carbohydrate that is essential to the body as a water-soluble vitamin. Vitamin C exists in oxidized and reduced forms, namely, L-dehydroascorbic acid and L-ascorbic acid. Vitamin C is involved in the formation of the dermal skin barrier and collagen, and plays a physiological role in the cell signaling pathways of cell proliferation and differentiation related to skin oxidation prevention, wrinkle anti-aging, and the onset and progression of various skin diseases.

[0040] Vitamin C or its derivatives that can be used in the present invention are one or more of the following:

[0041] Sodium ascorbyl phosphate: Sodium ascorbyl phosphate is an active and stable vitamin C derivative ingredient for the cosmetic industry. It can release vitamin C in the skin, protect skin cells, promote collagen formation, inhibit the formation of senile keratosis, and lighten dark skin.

[0042] 3-O-Ethyl ascorbic acid: 3-O-Ethyl ascorbic acid promotes collagen production, which significantly improves the structure of skin cells and the overall condition of the skin.

[0043] Ascorbyl Methylsilanol Pectin: It is a known antioxidant and is known to help improve skin texture as well as reduce signs of aging and dark spots.

[0044] Magnesium ascorbyl phosphate (MAP): Magnesium ascorbyl phosphate (MAP) has all the functions of vitamin C and is very stable. It has excellent antioxidant and protective effects, effectively resists UV light, and promotes collagen production. This product is recommended for whitening / beautifying skin applications as well as anti-aging and anti-wrinkle products.

[0045] Ascorbic acid: Vitamin C (L-ascorbic acid), USP, is the naturally occurring, active form of vitamin C. It is a powerful antioxidant (shown to be able to protect skin from oxidative damage). It can improve the appearance of aging, fragile skin. It is widely used as an added ingredient in skin-lightening products to improve hyperpigmentation and age spots.

[0046] [ka] Ascorbyl Glucoside: Ascorbyl glucoside is a highly stable, water-soluble vitamin C derivative. It is resistant to degradation and has the same whitening, sun protection, and anti-aging effects as ascorbic acid.

[0047] Tetrahexyldecyl Ascorbate: Tetrahexyldecyl ascorbate is a very stable, oil-soluble vitamin C ester, but lacks inherent antioxidant potential because all hydroxyl groups are esterified. It has excellent skin penetration and, as a result, provides high cytoprotection against UV-B light. It can improve the appearance of aging and fragile skin. It is widely used as an additive ingredient in skin-lightening products to improve hyperpigmentation and dark spots.

[0048] Aminopropyl ascorbyl phosphate: It is a stabilized vitamin C derivative. It is ideal for whitening, anti-wrinkle, and antioxidant applications.

[0049] Vitamin C or a derivative thereof is preferably present in an amount of 0.01 to 2% by weight of the composition, more preferably 0.05 to 1.5% by weight. Vitamin C is preferably present in the composition in capsule form. The most suitable vitamin C or a derivative thereof for use in the present invention is sodium ascorbyl phosphate, available from BASF as SAP, DSM as Stay C50, Vivimed as sodium ascorbyl phosphate, Uniproma as PromaCare SAP, and Chemspec Chemicals Pvt. Ltd. as sodium ascorbyl phosphate.

[0050] The composition comprises 3-25% by weight of one or more saturated fatty acids. The one or more saturated fatty acids are preferably C10-C22 fatty acids, more preferably C16-C18 fatty acids. Most preferably, the one or more saturated fatty acids are stearic acid, palmitic acid, or a mixture thereof. The one or more saturated fatty acids are often hystric acid, which is essentially (generally about 90-95%) a mixture of stearic acid and palmitic acid. Preferred hystric acid has 40-65% saturated C16 fatty acids and 34-58% saturated C18 fatty acids, or 52-58% saturated C16 fatty acids and 40-47% saturated C18 fatty acids. It is particularly preferred that the composition comprises 4-23% by weight of fatty acids, more preferably 5-20% by weight, even more preferably 6-17% by weight, even more preferably 8-15% by weight, and even more preferably 10-12% by weight of the composition. Without wishing to be bound by theory, the inventors believe that the inclusion of one or more saturated fatty acids enhances skin hydration by trapping moisture in the skin and reducing evaporation to the surrounding atmosphere.Apart from this advantage, it is also recognized that the oil-soluble sunscreen agent can be distributed evenly on the skin, thereby enhancing SPF.

[0051] The composition may optionally contain 0.4 to 10% by weight of a humectant. Polyhydric alcohol-type humectants can be used as cosmetically acceptable carriers. Preferably, the humectant is at least one of propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol, sorbitol, hydroxypropyl sorbitol, hexylene glycol, 1,3-butylene glycol, isoprene glycol, 1,2,6-hexanetriol, glycerol, ethoxylated glycerol, and propoxylated glycerol. Preferred humectants are selected from one or more of glycerol, sorbitol, propylene glycol, and 1,3-butylene glycol. Glycerol is the most preferred humectant. The amount of humectant is preferably 1 to 10% by weight, more preferably 2 to 8% by weight, of the composition. Without wishing to be bound by theory, the inventors believe that the inclusion of a humectant provides a hydrating effect. Separately, it has been observed that maintaining a water-soluble sunscreen in a dissolved form enhances the SPF.

[0052] The compositions of the present invention comprise 0.25 to 5% by weight of a polymer of (a) dimethicone / vinyl dimethicone crosspolymer and (b) silica. The dimethicone / vinyl dimethicone crosspolymer can be present with or without silica. Various polymers of the above type can be used in the present invention. Preferred polymers according to the present invention, dimethicone / vinyl dimethicone crosspolymer, are available as KM-9729, DOWSIL™ EP-9215, SeraSnow SP 13, DOWSIL™ 9506 Powder, and Specsil SPD. An even more preferred polymer according to the present invention is dimethicone / vinyl dimethicone crosspolymer (and) silica, available as DOWSIL™ 9701 Cosmetic Powder. Other suitable polymers that can be used are listed below.

[0053] Dimethicone / vinyl dimethicone crosspolymer (and) silica (and) butylene glycol, available as DOWSIL™ EP-9801 Hydro Cosmetic Powder; Dimethicone (and) Dimethicone / Vinyl Dimethicone Crosspolymer (and) Dimethicone Crosspolymer (and) Beeswax (and) Silica (and) Silica Silylate, available as DOWSIL™ 9576 Smooth Away Elastomer; Available as SSP100 Dimethicone / vinyl dimethicone crosspolymer (and) polymethylsilsesquioxane (and) silica dimethyl silylate; Dimethicone / vinyl dimethicone crosspolymer (and) lauroyl lysine available as DOWSIL™ EP-9289 LL; Hydrophobically modified silica preferably selected from silica silylate available as DOWSIL™ VM-2270 AerogelFine particles, HDK® H2000; and Silica dimethyl silylate available as HDK® H15, HDK® H20, HDK® H30, HDK® H18.

[0054] The polymer is contained in an amount of 0.25 to 5% by weight, preferably 0.5 to 4% by weight, more preferably 1 to 3% by weight of the composition.

[0055] Without wishing to be bound by theory, the inventors believe that the inclusion of the polymer reduces shine and provides a matte effect to the skin with sensory benefits.

[0056] The compositions of the present invention may further comprise a modified starch, preferably aluminum starch octenyl succinate. Aluminum starch octenyl succinate is a chemically modified starch, particularly an esterified starch. Such aluminum starch octenyl succinate is commercially available from suppliers such as Akzo Nobel and Nouryon under the names Dry Flo® Pure and Dry Flo® PC. Various other suppliers also sell it under their own brand names. In cosmetics and personal care products, aluminum starch octenyl succinate is used in the formulation of lotions, powders, makeup, and underarm deodorants. It is used as a thickener and binder, anti-caking agent, and oil absorbent. The compositions may further comprise aluminum starch octenyl succinate combined with other ingredients to achieve other benefits. For example, an ingredient with the INCI name starch aluminum octenyl succinate (and) acrylate copolymer (and) magnesium carbonate can be included. This is available from Nouryon as NATRASORB® HFB. Its natural ingredient content is 81%, and suggested uses include humidity-resistant products, oil-control products, anhydrous products, antiperspirant sticks, sunscreens, and dry shampoos for various benefits, such as oil absorption, syneresis relief, and fragrance retention. The Nouryon ingredient literature discloses crosslinked aluminum starch octenyl succinate surface-treated with acrylate copolymer and magnesium carbonate. The modified starch preferably comprises 0.5 to 10% by weight of the composition, more preferably 0.5 to 5% by weight. Of these, when included, the polymer preferably comprises 0.2 to 3% by weight of the composition; when included, the silica microspheres comprise 0.2 to 3% by weight; and when included, the modified starch comprises 0.5 to 4% by weight of the composition. Without wishing to be bound by theory, the inventors believe that the inclusion of modified starch provides the following benefits: even distribution of sunscreen to increase SPF while absorbing sebum and oil, good spreadability and slipperiness with a smooth, powdery feel.

[0057] The content of water in the composition is preferably 35 to 90% by weight, more preferably 50 to 85% by weight, and even more preferably 50 to 80% by weight.

[0058] In addition to the components disclosed above, the composition may, and preferably does, contain other ingredients to perform one or more functions of the present invention, including a cosmetically acceptable carrier. Emollient materials can serve as the cosmetically acceptable carrier. These can be in the form of silicone oils, natural or synthetic esters, and hydrocarbons. The amount of emollient can range anywhere from 0.1 to 25% by weight of the composition, preferably 1 to 10% by weight. Silicone oils can be divided into volatile and non-volatile varieties. As used herein, the term "volatile" refers to materials that have a measurable vapor pressure at ambient temperature. Preferably, the volatile silicone oil is selected from cyclic (cyclomethicone) or linear polydimethylsiloxanes containing 3 to 9, preferably 5 to 6, silicon atoms.

[0059] Non-volatile silicone oils useful as emollient materials include polyalkyl siloxanes, polyalkylaryl siloxanes, and polyether siloxane copolymers. Essentially non-volatile polyalkyl siloxanes useful herein include, for example, polyalkyl siloxanes having a viscosity of 5×10 at 25° C. 6 ~0.1m 2 Among the preferred nonvolatile emollients useful in the present compositions are polydimethylsiloxanes having a viscosity of 1×10 / s at 25° C. 5 ~4×10 4 m 2 There is a polydimethylsiloxane with a viscosity of 1 / s.

[0060] Another type of emollient is the ester emollient, which is an alkyl ester of saturated fatty acids having 10 to 24 carbon atoms, such as behenyl neopentanoate, isononyl isonanoate, isopropyl myristate, and octyl stearate. Alternatively, they are ether esters, such as fatty acid esters of ethoxylated saturated fatty alcohols. Alternatively, they are polyhydric alcohol esters, such as ethylene glycol mono- and di-fatty acid esters, diethylene glycol mono- and di-fatty acid esters, polyethylene glycol (200-6000) mono- and di-fatty acid esters, propylene glycol mono- and di-fatty acid esters, polypropylene glycol 2000 monostearate, ethoxylated propylene glycol monostearate, glyceryl mono- and di-fatty acid esters, polyglycerol polyfatty acid esters, ethoxylated glyceryl monostearate, 1,3-butylene glycol monostearate, 1,3-butylene glycol distearate, polyoxyethylene polyol fatty acid esters, sorbitan fatty acid esters, and polyoxyethylene sorbitan fatty acid esters. Pentaerythritol, trimethylolpropane, and neopentyl glycol esters of C1-C30 alcohols are particularly useful. Alternatively, they are wax esters, such as beeswax, spermaceti, and tribehenin wax. Alternatively, they are sugar esters of fatty acids, such as sucrose polybehenate and sucrose polycottonseedate. Alternatively, they are natural ester emollients based primarily on mono-, di-, and triglycerides. Representative glycerides include sunflower seed oil, cottonseed oil, borage oil, borage seed oil, primrose oil, castor oil and hydrogenated castor oil, rice bran oil, soybean oil, olive oil, safflower oil, shea butter, jojoba oil, and combinations thereof. Animal-derived emollients are represented by lanolin oil and lanolin derivatives. The amount of natural esters can range from 0.1 to 20% by weight of the composition.

[0061] Suitable cosmetically acceptable carrier hydrocarbons include petrolatum, mineral oil, C8-C18 Isoparaffins include polybutenes, and especially isohexadecane, available commercially from Presperse Inc. as Permethyl® 101A.

[0062] Fatty alcohols having 10 to 30 carbon atoms are another useful category of cosmetically acceptable carriers. Illustrative of this category are stearyl alcohol, lauryl alcohol, myristyl alcohol, oleyl alcohol, and cetyl alcohol, as well as mixtures thereof. Thickeners can be utilized as part of the cosmetically acceptable carrier of compositions according to the present invention. Representative thickeners include crosslinked acrylates (e.g., Carbopol® 982 and Carbopol® Ultrez 10), hydrophobically modified acrylates (e.g., Carbopol 1382®), polyacrylamides (e.g., Sepigel® 305), acryloylmethylpropanesulfonic acid / salt polymers and copolymers (e.g., Aristoflex® HMB and AVC), cellulose derivatives, and natural gums. Useful cellulose derivatives include sodium carboxymethylcellulose, hydroxypropyl methocellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, ethyl cellulose, and hydroxymethyl cellulose. Natural gums suitable for the present invention include guar, xanthan, sclerotium, carrageenan, pectin, and combinations of these gums. Minerals may also be utilized as thickeners, particularly clays such as bentonite and hectorite, fumed silica, talc, calcium carbonate, and silicates such as magnesium aluminum silicate (Veegum®). Amounts of thickeners may range from 0.0001 to 10%, typically from 0.001 to 2.5%, optimally from 0.01 to 1% by weight of the composition. To improve sensory properties, emollients selected from the group of oils that do not form stiff gels at 12 HSA are preferred, particularly for products intended for application to the face. These include polypropylene glycol-14 butyl ether, otherwise known as Tegosoft® PBE, or PPG 15 stearyl ether, such as Tegosoft® E, other oils such as esters, specifically isopropyl myristate, isopropyl palmitate, and other oils may include castor oil and its derivatives.

[0063] The compositions of the present invention preferably contain a skin-whitening compound. Exemplary substances include placenta extract, lactic acid, arbutin, kojic acid, ferulic acid, and hydroquinone. More preferably, such skin-whitening compounds are tyrosinase inhibitors to complement the melanogenesis inhibitory activity of substituted monoamines, most preferably compounds selected from the group consisting of kojic acid, hydroquinone, and 4-substituted resorcinols. Also included are dicarboxylic acids represented by the formula HOOC-(CxHy)-COOH (where x = 4 to 20 and y = 6 to 40), such as azelaic acid, sebacic acid, oxalic acid, succinic acid, fumaric acid, octadecenedioic acid, or salts thereof or mixtures thereof, most preferably fumaric acid or its salts, particularly the disodium salt.

[0064] A combination of 12HSA and fumaric acid or its salts is particularly preferred, especially for skin lightening formulations. Amounts of these agents may range from 0.1 to 10%, preferably 0.5 to 2% by weight of the composition.

[0065] Colorants, opacifiers and abrasives may also be included in the compositions of the present invention. Each of these materials may range from 0.05 to 5%, preferably 0.1 to 3%, by weight of the composition.

[0066] Preservatives can be incorporated into the compositions of the present invention to protect against the growth of potentially harmful microorganisms. A traditional preservative suitable for the compositions of the present invention is an alkyl ester of para-hydroxybenzoic acid. Other preservatives that have come into use include hydantoin derivatives, propionate salts, and various quaternary ammonium compounds. Cosmetic chemists are familiar with appropriate preservatives and routinely select them to meet preservative load tests and provide product stability. Particularly preferred preservatives are iodopropynyl butylcarbamate, phenoxyethanol, caprylyl glycol, C1-6 parabens (especially methylparaben and / or propylparaben), imidazolidinyl urea, sodium dehydroacetate, and benzyl alcohol. Preservatives should be selected taking into account the use of the composition and possible incompatibilities between the preservative and other ingredients in the emulsion.

[0067] Preservatives are preferably used in amounts ranging from 0.01% to 2% by weight of the composition, including all ranges encompassed therein. A particularly preferred combination is octocrylene and caprylyl glycol, as caprylyl glycol has been disclosed to enhance UVA and UVB protection. The compositions of the present invention can include a wide range of other optional ingredients. The CTFA Cosmetic Ingredient Handbook, Second Edition, 1992, incorporated herein by reference in its entirety, describes a wide variety of non-limiting cosmetic and pharmaceutical ingredients commonly used in the skin care industry that are suitable for use in the compositions of the present invention. Examples include antioxidants, binders, biological additives, buffers, colorants, astringents, fragrances, opacifiers, conditioners, exfoliants, pH adjusters, natural extracts, essential oils, skin sensates, skin soothing agents, and skin healing agents.

[0068] The composition of the present invention is preferably non-solid.The composition of the present invention is preferably a leave-on composition.Such a composition is applied to the skin and remains there for a long time.Rather, since leave-on compositions are not intended to be rinsed off, they need to be non-irritating, and therefore it is necessary to minimize the total level of surfactants and the total level of anionic surfactants in leave-on compositions.The total level of anionic surfactants in the composition of the present invention is preferably 10% or less, more preferably less than 8%, most preferably at most 5%, and optimally at most 3%.

[0069] The compositions of the present invention are preferably in lotion form. The compositions of the present invention provide a sun protection factor (SPF) of at least 15.

[0070] Method of using the composition The compositions according to the invention are primarily intended as products for topical application to human skin, in particular as agents for protecting against solar radiation and for preventing or reducing pigmentation, the appearance of wrinkled or aged skin, or age spots.

[0071] At the time of use, a small amount of the composition, for example 1 to 5 mL, is applied to the exposed area of skin from a suitable container or applicator and then spread over and / or rubbed into the skin using the hands or fingers or a suitable device, as needed.

[0072] According to another aspect, a method of providing photoprotection is disclosed comprising applying a composition of the present invention, the method providing a SPF of at least 15, preferably at least 20, more preferably at least 25, and ideally at least 30.

[0073] The individual sun protection factor (SPF) for each subject is the amount of energy (J / m) required to produce minimal erythema on protected skin. 2 It is defined as the ratio of the amount of energy required to produce minimal erythema in untreated skin (dose in units or seconds of exposure time) to the amount of energy required to produce minimal erythema in untreated skin and is calculated as follows:

[0074]

number

[0075] Yet another aspect of the present invention relates to a method of protecting skin against UVA and UVB induced inflammation and oxidative stress, comprising applying to the desired skin surface a composition of the first aspect. Preferably, the method is non-therapeutic / cosmetic in nature.

[0076] Yet another aspect of the present invention relates to a method of protecting skin against visible light, e.g., blue light, induced oxidative stress, comprising applying to the desired skin surface a composition of the first aspect. Preferably, the method is non-therapeutic / cosmetic in nature.

[0077] The above summarizes the present invention, but it will be apparent to those skilled in the art that modifications, variations, and variations can be made without departing from the scope and spirit of the invention as described and claimed herein. The invention will now be further described in the following non-limiting examples. [Example]

[0078] Examples A to C and 1: Compositions tested for SPF, and anti-inflammatory and antioxidant effects: The following compositions shown in Table 1 were prepared. Table-1

[0079] [Table 1]

[0080] In the table above, Stay C50 is sodium ascorbyl phosphate manufactured by DSM.

[0081] Using the above samples, the SPF and UVAPF values were measured according to the following procedure.

[0082] Thin film transmittance measurements were performed using a Labsphere UV transmittance analyzer. For this test, 70x70mm PMMA plates with a roughness of approximately 6µm from Schoenberg GmbH & Co were used. The transmittance of various compositions was measured using the procedure described below. 2The sample was applied to a PMMA plate and evenly distributed and spread using a syringe. The PMMA plate was allowed to dry for 30 minutes. After the drying period, the sample plate was exposed to UV light, and a transmittance scan was recorded. This scan provides the transmittance as a function of wavelength (290-400 nm) for a given sample. Six to nine different spots were scanned per plate. The same procedure was repeated for two or three plates. Therefore, the reported data are the average of 12 to 18 readings. A reference transmittance scan was obtained using a blank PMMA plate, sprinkled with glycerin, without any sample on it. The transmittance values were used to obtain SPF and UVAPF values using the UV-2000s application provided with the instrument.

[0083] Percent transmittance (and therefore SPF) was measured at time zero (line 0 min) for in vitro SPF. The same plates were exposed to simulated sunlight and transmittance was measured at designated intervals from 0 to 60 h. Average absorbance at 310 nm and 355 nm was recorded to determine % UVB and UVA photostability, respectively. UV was measured at an irradiance of 550 W / m at a distance of approximately 20 cm. -2 The generated energy was generated using a solar simulator (Atlas kW system) using the

[0084] The SPF and UVAPF values are summarized in Table 2 below. Table-2:

[0085] [Table 2]

[0086] The data in the above table show that the SPF and UVAPF values of the composition according to the invention (Example 1) are similar in magnitude to a composition according to the invention having the same amount of sunscreen but without vitamins (B3 and C), i.e. Example C.

[0087] Additionally, Examples C1 and C2 were prepared containing either vitamin B3 or vitamin C, but not both, and their compositions are shown in Table 3 below. Table-3

[0088] [Table 3]

[0089] Samples from Examples A-C, C1, C2 and Example 1 were subjected to UVA and UVB irradiation in separate experiments and the anti-inflammatory effect (IL1a levels) and antioxidant effect (ROS levels) were measured using the protocols provided below.

[0090] Primary skin keratinocytes were seeded onto cell culture plates and incubated in a 5% CO2 incubator at 37°C for 48 hours. Then, the cells were exposed to UVA (378 mJ / cm2) by placing a PMMA plate on top of the culture plate with or without a placebo / test formulation. 2 ) or UVB (15mJ / cm 2 ) were exposed to UV light. Bioactive agents (0.0125% Vitamin B3, 0.0025% SAP) were added alone or in combination to the cells in the culture medium after UV exposure. The culture plates were then incubated at 37°C for 6 hours in a 5% CO2 incubator. After 6 hours of incubation, intracellular ROS levels were measured by DCFDA assay, and IL1a in the supernatant was estimated using an IL1a ELISA kit.

[0091] The data are summarized in Tables 4 and 5 below. Table-4:

[0092] [Table 4] Table-5:

[0093] [Table 5]

[0094] The data in Table 4 above show that the composition according to the present invention (Example 1) provides overwhelmingly superior anti-inflammatory and antioxidant effects compared to sunscreen-containing compositions that do not contain vitamins (B3 and C), i.e., Example C, and other control compositions (Examples A and B). The data in Table 5 show that the inclusion of only one vitamin (either vitamin C in Example C1 or vitamin B3 in Example C2) does not provide superior effects compared to the inclusion of both vitamins (Example 1).

[0095] Furthermore, the compositions of Examples A, B, C and 1 shown in Table 1 were subjected to a test at 5.7 J / cm 2 The cells were exposed to a blue light source using a blue light LED light source, and the amount of ROS generated was estimated using the DCFDA assay as described above. The ROS generation value obtained from untreated cells was set to 100%. The values obtained when the compositions of Examples A, B, C, and 1 were used were as shown in Table 6 below. Table 6

[0096] [Table 6]

[0097] Thus, the data in Table 6 demonstrate that compositions according to the present invention provide protection from oxidative stress induced by visible light, eg, blue light.

Claims

1. (i) 0.1 to 10 wt. % of an oil-soluble sunscreen; (ii) 0.2 to 5 wt. % of a water-soluble sunscreen; (iii) 0.1 to 5 wt. % of a nonionic surfactant having an HLB value in the range of 9 to 20; (iv) 0.1 to 5% by weight of a vitamin B3 compound, derivative or precursor thereof; (v) 0.01 to 5% by weight of vitamin C or a derivative thereof A photoprotective composition comprising: A photoprotective composition wherein said composition further comprises 3-25% by weight of one or more saturated fatty acids.

2. 2. The composition of claim 1, wherein the vitamin B3 compound is niacinamide.

3. 3. The composition of claim 1, wherein the oil-soluble sunscreen is selected from a UV-B sunscreen selected from one or more of octyl salicylate, 3,3,5-trimethylcyclohexyl 2-hydroxybenzoate, ethylhexyl salicylate, 2-ethylhexyl 2-cyano-3,3-diphenyl-2-propenoate, 2-ethylhexyl-4-methoxycinnamate, and octyl methoxycinnamate; or a UV-A sunscreen selected from one or more of dibenzoylmethane compounds, diethylaminohydroxybenzoylhexyl α-benzoate, and methyl anthranilate.

4. 10. The composition of any one of the preceding claims, wherein the water-soluble sunscreen is selected from a UV-B sunscreen selected from one or more of 2-phenylbenzimidazole-5-sulfonic acid, benzophenone-4, and benzylidene camphorsulfonic acid; or a water-soluble UV-A sunscreen selected from one or more of phenyldibenzimidazole tetrasulfonate disodium and terephthalylidene dicamphorsulfonic acid.

5. A composition according to any one of the preceding claims, wherein the non-ionic surfactant has an HLB value in the range of 12 to 20.

6. 10. A composition according to any one of the preceding claims, wherein the nonionic surfactant is selected from one or more of fatty alcohol ethoxylates, fatty acid ethoxylates, alkylphenol ethoxylates, and polyoxyethylene sorbitan alkyl esters; preferably fatty alcohol ethoxylates or fatty acid ethoxylates.

7. 10. A composition according to any preceding claim, wherein the composition comprises 4 to 23% by weight of one or more saturated fatty acids.

8. 10. A composition according to any one of the preceding claims, wherein the one or more saturated fatty acids are selected from one or both of stearic acid and palmitic acid, preferably a mixture of stearic acid and palmitic acid.

9. A composition according to any preceding claim, further comprising 0.4 to 10% by weight of a humectant.

10. 10. The composition of claim 9, wherein the humectant is chosen from one or more of propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol, sorbitol, hydroxypropyl sorbitol, hexylene glycol, 1,3-butylene glycol, isoprene glycol, 1,2,6-hexanetriol, glycerol, ethoxylated glycerol, and propoxylated glycerol.

11. 10. The composition of any one of the preceding claims, further comprising 0.25 to 5% by weight of a polymer of (a) dimethicone / vinyl dimethicone crosspolymer and (b) silica.

12. 10. A composition according to any one of the preceding claims, further comprising a modified starch, preferably an aluminum octenyl succinate starch.

13. 10. A method of providing photoprotection with a Sun Protection Factor (SPF) of at least 15, comprising applying the composition of any one of the preceding claims onto the desired skin surface.

14. A method for protecting skin against UVA and UVB induced inflammation and oxidative stress, comprising applying a composition according to any one of claims 1 to 12.

15. A method for protecting skin against visible light-induced oxidative stress, comprising applying a composition according to any one of claims 1 to 12.

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