Sunscreen composition containing human milk oligosaccharides
Neutral core human milk oligosaccharides like lacto-N-tetraose and lacto-N-neotetraose enhance SPF in sunscreen compositions, addressing the limitation of existing activators and offering substantial UV protection.
Patent Information
- Authority / Receiving Office
- JP · JP
- Patent Type
- Applications
- Current Assignee / Owner
- DSM IP ASSETS BV
- Filing Date
- 2023-10-27
- Publication Date
- 2026-04-22
AI Technical Summary
There is a need for natural ingredients that can increase the Sun Protection Factor (SPF) of sunscreen compositions, as the number of approved sunscreen activators is limited, and existing methods struggle to enhance SPF effectively.
Incorporating neutral core human milk oligosaccharides, such as lacto-N-tetraose and lacto-N-neotetraose, composed of galactose, N-acetylglucosamine, and glucose monosaccharides, into sunscreen compositions to enhance their SPF properties.
The addition of these oligosaccharides significantly increases the SPF of sunscreen compositions by at least 20% to 300%, providing enhanced protection against UV radiation.
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Abstract
Description
Detailed description of the invention
[0001] The present invention relates to a composition containing at least one sunscreen activator and having improved sun protection index (SPF) properties, and to a method for improving sun protection index (SPF) properties.
[0002] The use of compositions containing sunscreen activators (also called sunscreens) is very common today. Sunscreen activators in such compositions protect keratinous substances, particularly the skin, from damage caused by UV radiation, including damage from both UVA and UVB rays, which are known to cause wrinkles and contribute to the development of skin diseases such as lupus erythematosus, as well as melanoma and non-melanoma skin cancer. Therefore, the need for sunscreens with high SPF (Sun Protection Factor) is increasing to achieve ultimate skin protection.
[0003] The standard measure for determining the amount of protection a composition containing sunscreen activators provides against UV radiation is the sun protection factor (SPF). However, given the limited number of sunscreen activators approved worldwide, increasing the SPF of compositions containing sunscreen activators can be challenging.
[0004] Therefore, there is still a need for preferably natural ingredients that can increase the SPF of the sunscreen active ingredients in the composition.
[0005] Surprisingly, it is now known that certain human milk oligosaccharides, namely lacto-N-tetraose (LNT) or lacto-N-neotetraose (LNnT), which are neutral core human milk oligosaccharides composed of galactose, N-acetylglucosamine, and glucose monosaccharides, can significantly increase the SPF of compositions containing at least one sunscreen active ingredient.
[0006] Accordingly, in the first embodiment, the present invention relates to a composition for keratinous substances (e.g., hair or skin) comprising at least one sunscreen activator and at least one neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine, and glucose monosaccharide.
[0007] The present invention also relates to an emulsion composition for keratinous substances (e.g., hair or skin) comprising at least one sunscreen activator and at least one neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine, and glucose monosaccharide. Preferably, the composition is in the form of an oil-in-water (O / W) emulsion.
[0008] The present invention also relates to a method for increasing the sun protection index (SPF) of a composition comprising at least one sunscreen activator, the method comprising adding at least one neutral core human milk oligosaccharide, comprising galactose, N-acetylglucosamine, and glucose monosaccharide, to the composition in an amount effective for increasing the SPF of the composition.
[0009] The present invention also relates to the use of a neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine, and glucose monosaccharide to enhance the sun protection index (SPF) of a composition comprising at least one sunscreen activator.
[0010] The present invention also relates to a method for preparing a composition having improved sun protection index (SPF) properties, comprising adding at least one neutral core human milk oligosaccharide, comprising galactose, N-acetylglucosamine, and glucose monosaccharide, to the composition during the preparation of the composition. It is understood that the improved properties are comparable to those of a composition that does not contain the neutral core human milk oligosaccharide as defined herein.
[0011] The present invention further relates to a method for preparing a composition comprising combining at least one sunscreen activator with at least one neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine, and glucose monosaccharide.
[0012] The use of the composition of the present invention as a sunscreen composition for protecting the skin from the effects of skin aging, particularly wrinkles (especially from UV-induced skin aging), and for sun protection, is also in accordance with the present invention.
[0013] Finally, the subject matter of the present invention is a method for the cosmetic treatment of keratinous substances, particularly skin, where compositions as defined herein are applied particularly to the keratinous substances, particularly skin. This method is particularly suitable for protecting the skin from the harmful effects of ultraviolet radiation, such as sunburn and / or photoaging.
[0014] The term "keratinous material" means skin (body, face, eye contours, scalp), hair, eyelashes, eyebrows, body hair, nails, and / or lips. Preferably, in all embodiments, the keratinous material is skin.
[0015] As used herein, the term “neutral core human milk oligosaccharide” (neutral core HMO) refers to a family of structurally diverse unconjugated glycans constructed from galactose, N-acetylglucosamine, and glucose monosaccharide units that are very abundant and unique in human milk and are preferably linked to one another through β-(1-3) or β-(1-4) bonds. Preferably, in all embodiments herein, galactose is D-galactose and glucose is D-glucose.
[0016] The SPF according to the present invention is understood to be measured by the in vitro SPF method outlined in ISO 24443 (Determination of sunscreen UVA photoprotection in vitro, 01.06.2012) and illustrated in the examples.
[0017] In all embodiments of the present invention, preferably, the neutral core human milk oligosaccharide is a trisaccharide, tetrasaccharide, hexasaccharide, octasaccharide or decasaccharide, with trisaccharides, tetrasaccharides and hexasaccharides being particularly preferred. Tetrasaccharides are most preferred.
[0018] In all embodiments of the present invention, it is further advantageous for the oligosaccharide to be a linear oligosaccharide, i.e., unbranched.
[0019] Exemplary oligosaccharides according to the present invention are represented below.
Chemical formula
[0020] In all embodiments of the present invention, it is further advantageous for the oligosaccharide to be characterized by a terminal D-galactose linked through a β-(1-3) or β-(1-4) bond to an N-acetyl-D-glucosamine (GlcNAc) unit.
[0021] In addition, in all embodiments of the present invention, it is also preferred for the oligosaccharide to be characterized by a D-galactose linked through a β-(1-4) bond to a reducing end D-glucose.
[0022] Particularly suitable neutral core human oligosaccharides according to the present invention are listed in Table 1.
[0023]
Table 1
[0024]
Table 2
[0025] Advantageously, in all embodiments of the present invention, lacto-N-triose II, LNT, LNnT, LNH, LNnH, pLNH and pLNnH and mixtures thereof are used.
[0026] In all embodiments of the present invention, the use of lacto-N-(neo)tetraose, namely lacto-N-tetraose (CAS No: 14116-68-8) and / or lacto-N-neotetraose (CAS No: 13007-32-4), is most preferred.
[0027] The HMO according to the present invention can be isolated from breast milk, or the HMO can be produced chemically or biochemically according to methods well known in the art.
[0028] For the purposes of this invention, the source of the HMO is not essential. It is clear that HMOs from various sources can be used.
[0029] The total amount of neutral core HMO in the composition according to the present invention is preferably at least 0.01% by weight, more preferably at least 0.1% by weight, and even more preferably at least 0.2% by weight, for example at least 0.3% by weight or at least 0.5% by weight, based on the total weight of the composition. In particular, the amount of neutral core HMO is selected from the range of 0.01 to 10% by weight, more preferably in the range of 0.1 to 7.5% by weight, and most preferably in the range of 0.2 to 5% by weight, based on the total weight of the composition. Further suitable ranges are 0.25 to 5% by weight, 0.5 to 4% by weight, 0.1 to 3% by weight, 0.25 to 3% by weight, and 0.3 to 3% by weight. Particularly preferred ranges according to the present invention are 0.1 to 5% by weight, more preferably 0.25 to 3% by weight, for example at 0.25 to 1.5% by weight or 0.5 to 5% by weight, or 0.5 to 4% by weight.
[0030] Preferably, in all embodiments of the present invention, the neutral core HMO according to the present invention is present in an amount effective in increasing the SPF (measured in vitro) of the composition by at least 20%, preferably at least 30%, more preferably at least 50%, and most preferably at least 100% (including all and partial ranges between these, e.g., 25% to 35%, 20% to 300%, 30% to 250%, 30% to 200%, and all and partial ranges between them).
[0031] It is well understood that the compositions according to the present invention may contain one or more HMOs. However, preferably, the compositions according to the present invention contain one or two, more preferably only one HMO, for example, selected from the group most preferably LNT and / or LNnT. In all embodiments of the present invention, the most preferred HMO is LNT because it results in a particularly significant increase in SPF.
[0032] As used herein, the term “sunscreen activator” refers to a compound that absorbs light in the UVB and / or UVA range (also known as a UVA, UVB, and broadband (UVA&B) filter). Preferably, such a compound has an E1 / 1 value of at least 150, more preferably at least 180, and most preferably at least 190 (i.e., λ max The absorption layer has a thickness of 1 cm and a UV absorbance of 1%. The maximum lambda value (λ) max It is well understood by those skilled in the art that the wavelength along the absorption spectrum of the sunscreen activator having its strongest photon absorption (also called the maximum absorption wavelength) is in the UV range, i.e., in the range of 280 to 400 nm. Preferably, in all embodiments of the present invention, the maximum lambda value is selected in the range of 300 to 380 nm, most preferably in the range of 300 to 370 nm. Furthermore, it is well understood by those skilled in the art that UV filters used in sunscreens do not substantially absorb light in the visible range (i.e., wavelengths above 400 nm) (as this results in highly undesirable discoloration in the industry).
[0033] Accordingly, the present invention relates to a composition comprising at least one sunscreen activator and at least one neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine, and glucose monosaccharide, wherein the sunscreen activator has a lambda maximum value (i.e., maximum absorption wavelength) selected in the range of 280 to 400 nm, preferably in the range of 300 to 380 nm, and most preferably in the range of 300 to 370 nm.
[0034] Preferred UVA filters generally absorb radiation in the 320-400 nm region of the ultraviolet spectrum. Examples of preferred UVA absorbers include dibenzoylmethane or dialkylaminohydroxybenzoylalkylbenzoate.
[0035] A preferred UVB filter absorbs radiation in the 280–320 nm region of the ultraviolet spectrum. Examples of preferred UVB absorbers include cinnamate, diphenyl acrylate, benzalmalonate, triazine, and salicylate.
[0036] A preferred broadband UV filter provides substantial broad-spectrum protection from both UVA and UVB rays. Examples of preferred broadband absorbers include micronized organic UV filters such as methylenebis-benzotriazolyltetramethylbutylphenol.
[0037] Preferably, in all embodiments of the present invention, the composition does not contain lutein.
[0038] The sunscreen activator present in the composition of the present invention may be an organic sunscreen activator (organic UV filter) and / or an inorganic sunscreen activator (inorganic UV filter), such as a physical barrier agent such as titanium dioxide or zinc oxide. Furthermore, the sunscreen activator present in the composition of the present invention may be soluble in water, soluble in non-aqueous materials, and / or insoluble. The preferred sunscreen activator according to the present invention is an organic sunscreen activator.
[0039] Preferably, in all embodiments of the present invention, a combination of two or more, preferably three or more, and more preferably four or more different UV filters is used, for example, a combination of 2 to 10, 3 to 9, or 4 to 7 different UV filters. Advantageously, the two or more, preferably two or more, preferably three or more, and more preferably four or more different UV filters are selected from the group of organic UV filters having all the preferences and definitions given herein.
[0040] Preferably, in all embodiments of the present invention, the total amount of all sunscreen activators in the composition according to the present invention is selected from about 1 to about 50% by weight of the total weight of the composition, preferably from about 3 to about 40% by weight of the total weight of the composition, more preferably from about 5 to about 30% by weight, about 10 to about 25% by weight, and about 15 to about 25% by weight (including all and partial ranges between these).
[0041] Furthermore, in all embodiments of the present invention, the total amount of UV filters present in the composition according to the present invention is preferably selected such that the SPF of the final composition (in vitro SPF measured as outlined in ISO 24443 Determination of sunscreen UVA photoprotection in vitro, 01.06.2012, as illustrated in the examples) is at least 10, preferably at least 15, and more preferably at least 20.
[0042] Particularly useful organic UV filters in the present invention include anthranilates, cinnamic acid derivatives, dibenzoylmethane derivatives, salicylic acid derivatives, camphor derivatives, triazine derivatives, for example, U.S. Patent No. 4,367,390, European Patent No. 863145, European Patent No. 517104, European Patent No. 570838, European Patent No. 796851, European Patent No. 775698, European Patent No. 878469, and European Patent No. 933 Disclosed in Patent No. 376, European Patent No. 507691, European Patent No. 507692, European Patent No. 790243, and European Patent No. 944624; benzophenone derivatives; β,β-diphenyl acrylate derivatives; benzotriazole derivatives; benzalmalonate derivatives; benzimidazole derivatives; imidazoline; bisbenzoazolyl disclosed in European Patent No. 669323 and U.S. Patent No. 2,463,264. Derivatives; p-aminobenzoic acid (PABA) derivatives; methylenebis(hydroxyphenylbenzotriazole) derivatives disclosed in U.S. Patent Nos. 5,237,071 and 5,166,355, UK Patent No. 2303549, German Patent No. 19726184 and European Patent No. 893119; screening polymers and screening silicones, for example, those disclosed in International Publication No. 93 / 04665. Examples include dimers derived from α-alkylstyrene, such as those disclosed in German Patent No. 19855649; 4,4-diarylbutadiene disclosed in European Patent No. 0967200, German Patent No. 19746654, German Patent No. 19755649, European Patent Application Publication No. A-1008586, European Patent No. 1133980 and European Patent No. 133981; and mixtures thereof.
[0043] For example, as sunscreen activators that are generally active in the UV-A and / or UV-B regions, as shown below by their INCI names, are p-aminobenzoic acid (PABA) derivatives, particularly PABA, ethyl PABA, ethyl dihydroxypropyl PABA, ethylhexyldimethyl PABA, glyceryl PABA, or PEG-25. PABA, salicylic acid derivatives, especially homosalate (HMS), ethylhexyl salicylate (EHS), dipropylene glycol salicylate, or TEA salicylate; dibenzoylmethane derivatives, especially butyl methoxydibenzoylmethane (BMDBM), or isopropyl dibenzoylmethane; cinnamic acid derivatives, especially ethylhexyl methoxycinnamate (OMS), isopropyl methoxycinnamate, isoamyl methoxycinnamate, cinoxate, DEA methoxycinnamate, diisopropyl methylcinnamate, or ethylhexanoactoglyceryl dimethoxycinnamate; β,β-diphenyl acrylate derivatives, especially octocrylene (OC) or etocrylene; benzophenone, especially benzophenone-1, benzophenone-2, benzophenone-3, or oxybenzone, benzophenone-4, benzophenone-5, benzophenone Non-6, benzophenone-8, benzophenone-9, benzophenone-12, or n-hexyl 2-(4-diethylamino-2-hydroxybenzoyl) benzoate (DHHB), benzylidene camphor derivatives, especially 3-benzylidene camphor, 4-methylbenzylidene camphor, benzylidene camphor sulfonic acid, camphor benzalkonium methosulfate, terephthalylidene dicamphor sulfonic acid, or polyacrylamide methylbenzylidene, benzimidazole derivatives, especially phenylbenzimidazole sulfonic acid (HS), or phenyldibenzimidazole tetrasulfonate disodium, triazine derivatives, especially bis-ethylhexyloxyphenol methoxyphenyl triazine (BEMT), ethylhexyl triazone (EHT), diethylhexyl butamide triazone (DBT), or 2,4,Insoluble organic sunscreen activators such as 6-tris(diisobutyl4'-aminobenzalmalonate)-s-triazine, benzotriazole derivatives, especially drometrizole trisiloxane, or methylenebisbenzotriazolyltetramethylbutylphenol (MBBT), trisbiphenyltriazine (A2B) (generally in the form of an aqueous dispersion of active UV filters, e.g., DSM Nutritional Examples include products sold under the trade names PARSOL® MAX (MBBT) by Products or Tinosorb® A2B (A2B) by BASF, anthranilic acid derivatives, particularly menthyl anthranilic acid, imidazoline derivatives, particularly ethylhexyl dimethoxybenzylidene dioxoimidazoline propionate, benzalmalonate derivatives, particularly polyorganosiloxanes containing benzalmalonate functional groups (e.g., commercially available under the INCI name: Polysilicone-15), 4,4-diarylbutadiene derivatives, particularly 1,1'-dicarboxy(2,2'-dimethylpropyl)-4,4-diphenylbutadiene, and mixtures thereof.
[0044] Particularly preferred organic sunscreen activators (organic UV filters) according to the present invention include homosalate (e.g., sold under the trade name "PARSOL® HMS"), ethylhexyl salicylate (e.g., sold under the trade name "PARSOL® EHS"), polysilicone-15 (especially sold under the trade name "PARSOL® SLX"), ethylhexyl methoxycinnamate (e.g., sold under the trade name "PARSOL® MCX"), octocrylene (e.g., sold under the trade name "PARSOL® 340"), phenylbenzimidazole sulfonic acid (e.g., sold under the trade name "PARSOL® HS") or its salts, for example, those formed during the preparation of a composition using a neutralizing agent such as triethanolamine of sodium hydroxide, bis-ethylhexyloxyphenol methoxyphenyl triazine (e.g., sold under the trade name "PARSOL® SHIELD"), ethylhexyl triazone (e.g., "PARSOL® EHT") Examples include diethylhexylbutamide triazone (for example, marketed under the trade name Uvasaorb HEB), methylenebisbenzotriazolyltetramethylbutylphenol (for example, marketed under the trade name "PARSOL® MAX"), trisbiphenyltriazine (for example, marketed under the trade name Uvinul A2B), butylmethoxydibenzoylbenzomethane (in particular marketed under the trade name "Parsol 1789"), diethylaminohydroxybenzoylhexylbenzoate (for example, marketed under the trade name Uvinul A Plus), and mixtures thereof.
[0045] The most preferred organic sunscreen activator (organic UV filter) used in all embodiments of the present invention is selected from the group consisting of ethylhexyl salicylate, polysilicone-15, ethylhexyl methoxycinnamate, octocrylene, phenylbenzimidazole sulfonic acid or its salts, bisethylhexyloxyphenol methoxyphenyl triazine, ethylhexyl triazone, diethylhexyl butamide triazone, methylene bisbenzotriazolyltetramethylphenol, butyl methoxydibenzoylmethane, diethylamino hydroxybenzoyl hexyl benzoate, and any mixture thereof.
[0046] In all embodiments of the present invention, the (total) amount of organic UV filter in the composition according to the present invention is selected from the range of 0.5 to 30% by weight, more preferably 1 to 25% by weight, most preferably 1 to 25% by weight, for example, from 1 to 15% by weight, based on the total weight of the composition. Further preferred amounts are selected from the range of 5 to 30% by weight, 10 to 30% by weight, 15 to 30% by weight, 5 to 25% by weight, 10 to 25% by weight, or 15 to 25% by weight, based on the total weight of the composition.
[0047] In all embodiments of the present invention, the amount of ethylhexyl salicylate in the composition according to the present invention is advantageously selected from the range of 0.5 to 10% by weight, preferably 0.5 to 9% by weight, 0.5 to 8% by weight, 0.5 to 7% by weight, 0.5 to 6% by weight, 0.5 to 5% by weight, for example, 1 to 10% by weight, 2 to 10% by weight, 3 to 10% by weight, or 2 to 7.5% by weight, based on the total weight of the composition.
[0048] In all embodiments of the present invention, the amount of polysilicone-15 in the composition according to the present invention is advantageously selected from the range of 0.4 to 10% by weight, preferably 0.4 to 9% by weight, 0.4 to 8% by weight, 0.4 to 7% by weight, 0.4 to 6% by weight, 0.4 to 5% by weight, 0.4 to 4% by weight, 0.4 to 3% by weight, 0.5 to 3% by weight, 0.8 to 9% by weight, 0.8 to 8% by weight, 0.8 to 7% by weight, 0.8 to 6% by weight, 0.8 to 5% by weight, 0.8 to 4% by weight, or 0.8 to 3% by weight, for example, 1 to 5% by weight, 1 to 3% by weight, 1 to 2.5% by weight, or 1.5 to 2.5% by weight.
[0049] In all embodiments of the present invention, the amount of ethylhexyl methoxycinnamate in the composition according to the present invention is advantageously selected from the range of 0.5 to 10% by weight, preferably 0.5 to 9% by weight, 0.5 to 8% by weight, 0.5 to 7% by weight, 0.5 to 6% by weight, 0.5 to 5% by weight, for example, 1 to 10% by weight, 2 to 10% by weight, 3 to 10% by weight, or 2 to 7.5% by weight, based on the total weight of the composition.
[0050] In all embodiments of the present invention, the amount of octocrylene in the composition according to the present invention is advantageously selected from a range of 0.5 to 15% by weight, preferably from a range of 0.5 to 10% by weight, 0.5 to 8% by weight, 1 to 10% by weight, 2 to 10% by weight, 3 to 10% by weight, for example, from a range of 5 to 10% by weight, 6 to 10% by weight, or 7 to 10% by weight, based on the total weight of the composition.
[0051] In all embodiments of the present invention, the amount of phenylbenzimidazole sulfonic acid or a salt thereof in the composition according to the present invention is advantageously selected from the range of 0.5 to 5% by weight, preferably 0.5 to 4% by weight, 0.5 to 3% by weight, 1 to 2.5% by weight, 1 to 3% by weight, or 1 to 4% by weight, based on the total weight of the composition.
[0052] In all embodiments of the present invention, the amount of bisethylhexyloxyphenol methoxyphenyl triazine in the composition according to the present invention is advantageously selected from the range of 0.4 to 10% by weight, preferably 0.4 to 9% by weight, 0.4 to 8% by weight, 0.4 to 7% by weight, 0.4 to 6% by weight, 0.4 to 5% by weight, 0.4 to 4% by weight, 0.4 to 3% by weight, 0.5 to 3% by weight, 0.8 to 9% by weight, 0.8 to 8% by weight, 0.8 to 7% by weight, 0.8 to 6% by weight, 0.8 to 5% by weight, 0.8 to 4% by weight, or 0.8 to 3% by weight, for example, 1 to 5% by weight, 1 to 3% by weight, 1 to 2.5% by weight, or 1.5 to 2.5% by weight.
[0053] In all embodiments of the present invention, the amount of ethylhexyl triazone in the composition according to the present invention is advantageously selected from the range of 0.4 to 10% by weight, preferably 0.4 to 9% by weight, 0.4 to 8% by weight, 0.4 to 7% by weight, 0.4 to 6% by weight, 0.4 to 5% by weight, 0.4 to 4% by weight, 0.4 to 3% by weight, 0.5 to 3% by weight, 0.8 to 9% by weight, 0.8 to 8% by weight, 0.8 to 7% by weight, 0.8 to 6% by weight, 0.8 to 5% by weight, 0.8 to 4% by weight, or 0.8 to 3% by weight, for example, 1 to 5% by weight, 1 to 3% by weight, 1 to 2.5% by weight, or 1.5 to 2.5% by weight.
[0054] In all embodiments of the present invention, the amount of diethylhexylbutamide triazone in the composition according to the present invention is advantageously selected from the range of 0.4 to 10% by weight, preferably 0.4 to 9% by weight, 0.4 to 8% by weight, 0.4 to 7% by weight, 0.4 to 6% by weight, 0.4 to 5% by weight, 0.4 to 4% by weight, 0.4 to 3% by weight, 0.5 to 3% by weight, 0.8 to 9% by weight, 0.8 to 8% by weight, 0.8 to 7% by weight, 0.8 to 6% by weight, 0.8 to 5% by weight, 0.8 to 4% by weight, 0.8 to 3% by weight, for example, 1 to 5% by weight, 1 to 3% by weight, or 1.5 to 3% by weight.
[0055] In all embodiments of the present invention, the amount of methylenebisbenzotriazolyltetramethylbutylphenol in the composition according to the present invention (for example, based on a dispersion of MBBT of approximately 45-55% by weight, commercially available under the trade name PARSOL MAX) is advantageously selected in the range of 0.5-10% by weight, preferably 1-10% by weight, more preferably 2-10% by weight, and most preferably 2-6% or 3-6% by weight, based on the total weight of the composition.
[0056] In all embodiments of the present invention, the amount of butylmethoxydibenzoylmethane in the composition according to the present invention is advantageously selected from the range of 0.4 to 10% by weight, preferably 0.4 to 9% by weight, 0.4 to 8% by weight, 0.4 to 7% by weight, 0.4 to 6% by weight, 0.4 to 5% by weight, 0.4 to 4% by weight, 0.4 to 3% by weight, 0.5 to 3% by weight, 0.8 to 9% by weight, 0.8 to 8% by weight, 0.8 to 7% by weight, 0.8 to 6% by weight, 0.8 to 5% by weight, 0.8 to 4% by weight, or 0.8 to 3% by weight, for example, 1 to 5% by weight, 2 to 5% by weight, 3 to 5% by weight, or 3.5 to 5% by weight.
[0057] In all embodiments of the present invention, the amount of diethylaminohydroxybenzoylhexyl benzoate in the composition according to the present invention is advantageously selected from the range of 0.5 to 10% by weight, preferably 0.5 to 9% by weight, 0.5 to 8% by weight, 0.5 to 7% by weight, 0.5 to 6% by weight, 0.5 to 5% by weight, 0.5 to 4% by weight, 0.5 to 3% by weight, 1 to 10% by weight, 1 to 9% by weight, 1 to 8% by weight, 1 to 7% by weight, 1 to 6% by weight, 1 to 5% by weight, 2 to 5% by weight, 3 to 5% by weight, for example, 2.5 to 6% by weight, 3 to 6% by weight, 4 to 6% by weight, or 3.5 to 5.5% by weight.
[0058] Particularly preferred combinations of organic UV filters in all embodiments of the present invention include combinations of DHHB, EHT, BEMT, OMC, polysilicone-15, DBT, and MBBT or BMDBM, EHS, OC, and BEMT, which are optionally further combined with HS as illustrated.
[0059] In a preferred embodiment, the composition according to the present invention comprises only an organic UV filter.
[0060] In another preferred embodiment, the composition further comprises one or more inorganic UV filters.
[0061] As used herein, the term “inorganic UV filter” refers to any metal oxide particles that have the UV filter properties defined above and are therefore useful for incorporation into a composition as a UV filter. Such inorganic UV filters are well known to those skilled in the art and are often referred to as micronized or ultrafine particle UV filters, particularly micronized or ultrafine particle titanium dioxide or zinc oxide.
[0062] The particle size of such inorganic UV filters is not particularly limited. Generally, a suitable (primary) particle size for efficient UV light absorption is selected in the range of 2 to 200 nm.
[0063] In all embodiments of the present invention, the (total) amount of inorganic UV filter in the composition according to the present invention is preferably selected from the range of 0.5 to 30% by weight, more preferably from the range of 1 to 30% by weight, and most preferably from the range of 2 to 30% by weight, based on the total weight of the composition. Further preferred amounts are selected from the range of 1 to 25% by weight, 1 to 20% by weight, 1 to 15% by weight, 3.0 to 25% by weight, 4 to 25% by weight, 5 to 20% by weight, or 10 to 25% by weight.
[0064] More advantageously, the (total) amount of inorganic titanium dioxide UV filter in the composition according to the present invention is selected from the range of 0.5 to 15% by weight, preferably 1 to 15% by weight, more preferably 2 to 10% by weight, and most preferably 2 to 6% by weight or 3 to 6% by weight, based on the total weight of the composition.
[0065] More advantageously, the (total) amount of inorganic zinc oxide UV filter in the composition according to the present invention is selected from the range of 0.5 to 25% by weight, preferably 1 to 20% by weight, more preferably 2 to 20% by weight, and most preferably 5 to 20% by weight or 7.5 to 20% by weight, based on the total weight of the composition.
[0066] Preferably, when present in the composition according to the present invention, the ratio (w / w) of titanium dioxide UV filter to zinc oxide UV filter is selected from the range of 1:5 to 5:1, preferably 1:2 to 2:1. More preferably, the amount of zinc oxide in the composition according to the present invention is greater than the amount of titanium dioxide, for example, in the range of 5:1 to 1.25:1, most preferably in the range of 2.5:1 to 1.25:1.
[0067] In a particular embodiment, the composition according to the present invention preferably comprises only an inorganic UV filter.
[0068] According to the present invention, it is advantageous for the inorganic UV filter to have a surface coating. The surface coating may include providing a thin hydrophilic or hydrophobic inorganic or organic layer on the metal oxide particles by a method known in itself. According to the present invention, various surface coatings may also include water. As a result of the surface treatment, hydrophilic, amphiphilic, or hydrophobic properties are imparted to the metal oxide.
[0069] Examples of inorganic surface coatings suitable for the purposes of the present invention include aluminum oxide (Al2O3), aluminum hydroxide Al(OH)3, aluminum oxide hydrate (also known as alumina, CAS number 1333-84-2), sodium hexametaphosphate (NaPO3)6, and sodium metaphosphate (NaPO3). n These include silicon dioxide (SiO2) (also known as silica, CAS number: 7631-86-9) and iron oxide (Fe2O3). These inorganic surface coatings may exist alone, in combination, and / or in particular in combination with organic coating materials as outlined below.
[0070] Examples of organic surface coatings suitable for use in the present invention include plant or animal aluminum stearate, fatty acids such as stearic acid and lauric acid, dimethylpolysiloxane (also known as dimethicone), methylpolysiloxane (methicone), simethicone, trimethoxycaprylylsilane, triethoxycaprylylsilane, octyltrimethoxysilane, and cetyl phosphate, such as potassium cetyl phosphate, and any mixture thereof.
[0071] These organic surface coatings may exist alone, in combination, and / or in combination with inorganic coating materials.
[0072] The crystalline form of titanium dioxide can be any crystalline or amorphous form. For example, titanium dioxide can be any type of amorphous, rutile, anastase, brookite, or a mixture thereof. In all embodiments of the present invention, the crystalline form of titanium dioxide is preferably rutile.
[0073] Furthermore, it is preferable that the zinc oxide is a white powder consisting of zinc oxide existing as a wurtzite-type crystalline structure.
[0074] Titanium dioxide UV filters for use according to the present invention (including any pre-dispersions thereof) are available, for example, from DSM Nutritional Products Ltd. as PARSOL® TX (INCI: titanium dioxide, silica, dimethicone), from Tayca as Micro titanium dioxide MT-01, or from Ishihara Sangyo Co., Ltd. as TTO-55I. Double-coated titanium dioxide having an inner alumina coating and an outer simethicone coating (for example, commercially available from EMD Chemicals Inc / Rona as Eusolex T-2000) is also preferred.
[0075] Zinc oxide UV filters for use according to the present invention (including any predispersions thereof) are available, for example, from BASF as Z-Cote or Z-Cote HP1 (2% dimethicone coating), from Tayca as MZ-505S (5% methicone coating), or from DSM Nutritional Products Ltd as PARSOL® ZX (2-3.5% triethoxycaprylylsilane coating).
[0076] In certain embodiments, the composition according to the present invention comprises, as an inorganic UV filter, at least one double-coated titanium dioxide and at least one coated zinc oxide, most preferably without further ultrafine metal oxide particles (i.e., one double-coated titanium dioxide and one coated zinc oxide).
[0077] Most preferably, in all embodiments of the present invention, the titanium dioxide UV filter is a double-coated titanium dioxide, more preferably a double-coated titanium dioxide having an inner silica and an outer organic coating, or a silica-coated titanium dioxide.
[0078] The inner silica coating layer of the double-coated titanium dioxide preferably consists of at least 0.5% by weight of inorganic silica (based on titanium dioxide). More preferably, the inner coating layer consists of 0.5% to 50% by weight, most preferably 1% to 20% by weight of inorganic silica (based on titanium dioxide).
[0079] The outer coating of the double-coated titanium dioxide is preferably selected from a class of organic coatings, such as silicone oil (e.g., simethicone, methicone, dimethicone, polysilicone-15), alkylsilane (e.g., octyltrimethoxysilane), olefinic acid (e.g., stearic acid), or polyol (e.g., glycerol), and can be applied to the titanium dioxide particles by methods known to those skilled in the art, for example, the method described in FI57124. The outer coating is preferably selected from the group consisting of simethicone, methicone, dimethicone, polysilicone-15, stearic acid, and octyltrimethoxysilane. Most preferably, the outer coating is dimethicone. More preferably, the amount of the outer coating layer is at least 0.25% by weight based on titanium dioxide. The amount of the outer coating is preferably selected from the range of 0.5% to 50% by weight, most preferably from 0.5% to 10% by weight, based on titanium dioxide.
[0080] In all embodiments of the present invention, the double-coated titanium dioxide according to the present invention preferably has a titanium dioxide content selected from the range of 70 to 95% by weight and a silicon dioxide content selected from the range of 5 to 20% by weight, for example, a titanium dioxide content selected from the range of 80 to 90% by weight and a silicon dioxide content selected from the range of 10 to 15% by weight (provided that the total content of titanium dioxide and silicon dioxide is selected from the range of 90 to 100% by weight).
[0081] Preferably, the double-coated titanium dioxide has an average primary particle size in the range of 2 to 100 nm, more preferably in the range of 5 to 50 nm, and most preferably in the range of 10 to 25 nm, and a secondary particle size of 0.025 to 1 μm, for example, preferably 0.05 to 0.075 μm.
[0082] A particularly suitable double-coated titanium dioxide according to the present invention contains a rutile-type titanium dioxide (TiO2) core having a double coating of silica (inner coating) and dimethicone (outer coating), and has a titanium dioxide content in the range of at least 75% by weight, preferably 82-87% by weight, and a silicon dioxide content in the range of at least 10% by weight, preferably 10.5-14.5% by weight, and an average particle size distribution D of 25-100 nm, preferably 40-80 nm. n It has a molecular weight of 50 (analyzed by laser diffraction measurement using Malvern Mastersizer 2000), and this double-coated titanium dioxide is commercially available, for example, from DSM nutritional products Ltd as PARSOL® TX (INCI: titanium dioxide, silica, dimethicone).
[0083] In all embodiments of the present invention, zinc oxide is most preferably either uncoated or coated with triethoxycaprylylsilane. The zinc oxide is most preferably a white powder consisting of zinc oxide existing as a wurtzite-type crystalline structure coated with triethoxycaprylylsilane, with a zinc oxide content of 96-98% and a triethoxycaprylylsilane content of 2-3.5%, and an average particle size of 90-130 nm (analyzed by laser diffraction measurement with Malvern Mastersizer 2000), and is commercially available from DSM nutritional products Ltd as PARSOL® ZX.
[0084] Unless otherwise specified in this specification, all given parts and percentages are by weight, based on the total weight of the composition.
[0085] Preferably, the neutral core human milk oligosaccharide, composed of galactose, N-acetylglucosamine, and glucose monosaccharide, and the sunscreen activator are present in the composition and method of the present invention in a weight ratio of 1:50 to 1:1, preferably 1:40 to 1:7.5, more preferably 1:30 to 1:5, for example, 1:25 to 1:15. Preferably, the amount of sunscreen activator is greater than the amount of HMO on a weight basis.
[0086] Since the compositions according to the present invention are intended for topical application, it is well understood that they include physiologically acceptable media, i.e., media compatible with skin, mucous membranes, and keratinous materials such as keratin fibers. In particular, physiologically acceptable media are cosmetically acceptable carriers. Therefore, it will be well understood by those skilled in the art that the compositions according to the present invention are topical compositions.
[0087] As used herein, the term “cosmetically acceptable carrier” refers to all carriers and / or excipients and / or diluents conventionally used in topical cosmetic compositions, particularly skincare formulations.
[0088] The exact amount of the support will depend on the actual amounts of the UV filter and all other optional components (e.g., other active ingredients) that a person skilled in the art would classify as different from the support.
[0089] In a favorable embodiment, the composition according to the present invention comprises, based on the total weight of the composition, 50% to 99%, preferably 60% to 98%, more preferably 70% to 98%, for example, particularly 80% to 95% of the carrier.
[0090] In particularly advantageous embodiments, the carrier in all embodiments of the present invention is further composed of at least 30% by weight, more preferably at least 40% by weight, and most preferably at least 45% by weight of water, for example, particularly 50-90% by weight, 50-80% by weight, 50-79% by weight, or 50-60% by weight of water.
[0091] In particular, the compositions according to the present invention are cosmetic or pharmaceutical compositions, preferably cosmetic (non-therapeutic) compositions.
[0092] In one embodiment, the composition according to the present invention is applied to the keratinized tissue of mammals, for example, particularly human skin or human scalp and hair.
[0093] The term "cosmetic composition" as used in this application refers to cosmetic compositions as defined in the title "Kosmetika" of Roempp Lexikon Chemie, 10th edition 1997, Georg Thieme Verlag Stuttgart, New York, and cosmetic compositions as disclosed in A. Domsch, "Cosmetic Compositions", Verlag fuer chemische Industrie (ed. H. Ziolkowsky), 4th edition, 1992.
[0094] Preferred compositions according to the present invention include skincare formulations, decorative formulations, and functional formulations.
[0095] Examples of skincare formulations include, in particular, photoprotective formulations, anti-aging formulations, formulations for the treatment of photoaging, body oils, body lotions, body gels, treatment creams, skin protective ointments, skin powders, moisturizing gels, moisturizing sprays, moisturizers for the face and / or body, skin tanning formulations (i.e., compositions for artificial / sunless tanning and / or browning of human skin), such as self-tanning creams and skin whitening formulations.
[0096] Examples of decorative formulations include, in particular, lipsticks, eyeshadows, mascaras, dry and moist makeup formulations, blushes and / or powders.
[0097] Examples of functional formulations include, but are not limited to, cosmetics or pharmaceutical compositions containing active ingredients such as hormone preparations, vitamin preparations, plant extract preparations, anti-aging preparations, and / or antimicrobial (antibacterial or antifungal) preparations.
[0098] In certain embodiments, the compositions according to the present invention are photoprotective formulations (sun care products, sunscreens) such as sunscreen lotions, sunscreen creams, sunscreen oils, sunscreen blockers, or day care creams having an SPF. Sunscreen creams, sunscreen lotions, and sunscreen lotions are of particular interest.
[0099] The compositions of the present invention (including carriers) may contain conventional auxiliaries and additives such as preservatives / antioxidants, fatty substances / oils, organic solvents, silicones, thickeners, softeners, emulsifiers, defoamers, aesthetic components such as fragrances, surfactants, fillers, anionic, cationic, nonionic or amphoteric polymers or mixtures thereof, propellants, acidifying or basicizing agents, dyes, colorants / colorants, abrasives, absorbents, chelating agents and / or metal ion sequestering agents, essential oils, skin coolants, astringents, pigments, or any other components commonly incorporated into such compositions.
[0100] According to the present invention, the composition according to the present invention may contain further components such as skin whitening; sun protection; treatment of hyperpigmentation; components for preventing or reducing acne, wrinkles, fine lines, atrophy and / or inflammation; chelating agents and / or metal ion sequestering agents; anti-lipidation and slimming agents (e.g., phytanic acid); firming agents; moisturizing and activating agents; self-tanning agents; analgesics; and agents for improving elasticity and skin barrier properties; and carriers and / or excipients or diluents that have been conventionally used in compositions.
[0101] Unless otherwise specified, the excipients, additives, diluents, etc. described below are suitable for the compositions according to the present invention. The required amounts of cosmetics, dermatological adjuvants, and additives can be easily determined by those skilled in the art based on the desired product.
[0102] Additional components may be added to the oil phase, the aqueous phase, or individually, as deemed appropriate. The method of addition can be readily adapted by those skilled in the art.
[0103] Examples of cosmetic excipients, diluents, auxiliaries, additives, and active ingredients commonly used in the skincare industry and suitable for use in the cosmetic compositions of the present invention are, for example, but are not limited to, those listed in the International Cosmetic Ingredient Dictionary & Handbook by the Personal Care Product Council.
[0104] The cosmetic active ingredients useful in this specification may, in some cases, provide two or more benefits or function through two or more mechanisms of action.
[0105] Naturally, those skilled in the art will select the above-mentioned optional additional components, auxiliaries, diluents, and additives, and / or their amounts, with care, such that the favorable properties inherently associated with the combination according to the present invention are not adversely affected or substantially affected by the intended additions.
[0106] In all embodiments of the present invention, preferred compositions are emulsions containing an oil phase and an aqueous phase, such as particularly O / W, W / O, Si / W, W / Si, O / W / O, W / O / W multiple, or Pickering emulsions. The amount of oily phase (i.e., the phase containing all oils and fats) present in such an emulsion is preferably at least 10% by weight, for example, in the range of 10 to 60% by weight, preferably 15 to 50% by weight, and most preferably 15 to 45% by weight, based on the total weight of the composition.
[0107] In a more preferred embodiment, the composition according to the present invention, as outlined herein, is an O / W emulsion comprising an oil phase dispersed in an aqueous phase in the presence of an O / W emulsifier. The preparation of such an O / W emulsion is well known to those skilled in the art and is illustrated in the examples.
[0108] In one advantageous embodiment, the O / W emulsifier is a phosphate ester emulsifier. Preferred phosphate ester emulsifiers include C8-10 alkylethyl phosphate, C9-15 alkyl phosphate, C20-22 alkyl phosphate, ceteareth-2 phosphate, ceteareth-5 phosphate, ceteth-8 phosphate, ceteth-10 phosphate, cetyl phosphate, C6-10 pareth-4 phosphate, C12-15 pareth-2 phosphate, C12-15 pareth-3 phosphate, ceteareth-2 phosphate DEA, cetyl phosphate DEA, oleth-3 phosphate DEA, potassium cetyl phosphate, deceth-4 phosphate, deceth-6 phosphate, and trilaureth-4 phosphate. In all embodiments of the present invention, particularly preferred phosphate ester emulsifiers are C8-C25 alkyl phosphates, particularly C20-22 alkyl phosphates and cetyl phosphates, and especially their respective potassium salts. A particular preferred phosphate ester emulsifier according to the present invention is, for example, potassium cetyl phosphate, which is commercially available as Amphisol® K at DSM Nutritional Products Ltd Kaiseraugst.
[0109] Further preferred O / W emulsifiers according to the present invention include PEG-30 dipolyhydroxystearate, PEG-4 dilaurate, PEG-8 dioleate, PEG-40 sorbitol oleate, PEG-7 glyceryl cocoate, PEG-20 glyceryl almond oil, PEG-25 hydrogenated castor oil, glyceryl stearate (and) PEG-100 stearate, PEG-7 oleate, PEG-8 oleate, PEG-8 laurate, PEG-60 glyceryl almond oil, PEG-20 methyl glucose sesquistearate, PEG-40 stearate, and stearin It contains PEG-100 acid, PEG-80 sorbitan laurate, steareth-2, steareth-12, oleth-2, ceteth-2, laureth-4, oleth-10, oleth-10 / polyoxyl-10 oleyl ether, ceteth-10, isosteareth-20, ceteareth-20, oleth-20, steareth-20, steareth-21, ceteth-20, isoceteth-20, laureth-23, steareth-100, glyceryl stearate citrate, glyceryl stearate (self-emulsifying type), stearic acid, salts of stearic acid, and polyglyceryl-3 methylglucose distearate. Further preferred emulsifiers include sorbitan oleate, sorbitan sesquioleate, sorbitan isostearate, sorbitan trioleate, lauryl glucoside, decyl glucoside, sodium stearoyl glutamate, sucrose polystearate, and hydrated polyisobutene. In addition, one or more synthetic polymers can be used as emulsifiers. For example, PVP eicosene copolymer, acrylate / C10-30 alkyl acrylate crosspolymer, acrylate / steareth-20 methacrylate copolymer, PEG-22 / dodecyl glycol copolymer, PEG-45 / dodecyl glycol copolymer, and mixtures thereof.
[0110] Another particularly suitable type of O / W emulsifier is a nonionic self-emulsifying system derived from olive oil, known, for example, as cetearyl olive oil fatty acid (INCI name) and sorbitan olive oil fatty acid (chemical composition: sorbitan ester and cetearyl ester of olive oil fatty acid), sold under the trade name OLIVEM 1000.
[0111] More preferably are commercially available polymer emulsifiers, such as hydrophobized polyacrylic acids like (acrylates / alkyl acrylate (C10-30)) crosspolymers sold by Lubrizol under the trade names Pemulen(registered trademark) TR-1 and TR-2.
[0112] Another type of emulsifier that is particularly suitable is a polyglycerol ester or diester of fatty acids (i.e., a polymer in which fatty acids are bonded by esterification with polyglycerin), also called polyglyceryl esters / diesters, such as Isolan GPS [INCI name (diisostearate / polyhydroxystearate / sebacic acid) polyglyceryl-4 (i.e., a diester of a mixture of isostearate, polyhydroxystearate and sebacic acid with polyglycerin-4)], commercially available from Evonik, or Dehymuls PGPH [INCI polyglyceryl-2 dipolyhydroxystearate], commercially available from BASF.
[0113] Polyalkylene glycol ethers, such as Brij 72 (polyoxyethylene(2) stearyl ether) or Brij 721 (polyoxyethylene(21) stearyl ether), available from Croda, are also preferred.
[0114] Particularly advantageous O / W emulsifiers according to the present invention include polyglyceryl-3 methyl glucose distearate, lauryl glucoside (and) polyglyceryl-2 dipolyhydroxystearate, glyceryl citrate stearate, sodium cetearyl sulfate, cetearyl glucoside; polyglyceryl-6 stearate (and) polyglyceryl-6 behenate, cetearyl olivate (and) sorbitan olivate, arachidyl alcohol (and) behenyl One or more of the following: alcohols (and) arachidyl glucosides, cetearyl alcohol (and) coconut oil alkyl glucosides, coconut oil alkyl glucosides (and) coconut alcohols, PEG-100 stearate (and) glyceryl stearate, sodium stearoyl glutamate, steareth-20, steareth-21, steareth-25, steareth-2, ceteareth-25, and ceteareth-6 (all listed by their INCI names).
[0115] In one embodiment, according to the present invention, it is particularly preferable that the composition contains, as an emulsifier or at least a co-emulsifier, a C8-C25 alkyl phosphate, preferably a C20-22 alkyl phosphate and / or a cetyl phosphate, most preferably a cetyl phosphate, for example, potassium cetyl phosphate.
[0116] In another embodiment, according to the present invention, it is particularly preferable that the composition contains polyglyceryl-6 stearate and / or polyglyceryl-6 behenate as an emulsifier, preferably in the presence of cetyl phosphate, more preferably potassium cetyl phosphate, as a co-emulsifier.
[0117] Each of these at least one O / W, Si / W emulsifier is preferably used in an amount ranging from 0.5 to 10% by weight, particularly 0.5 to 5% by weight, for example most specifically 0.5 to 4% by weight or 0.5 to 3% by weight, based on the total weight of the composition.
[0118] When a phosphate ester emulsifier having all the definitions and preferences given herein is used as a coemulsifier, the amount thereof is preferably selected based on the total weight of the composition in the range of 0.1 to 1% by weight, for example particularly in the range of 0.25 to 0.75% by weight, most specifically in the range of 0.3 to 0.7% by weight or 0.4 to 0.6% by weight.
[0119] Suitable W / O or W / Si emulsifiers according to the present invention include polyglyceryl-2-dipolyhydroxystearic acid, PEG-30 dipolyhydroxystearic acid, cetyl dimethicone copolyol, polyglyceryl-3 diisostearate polyglycerol ester of oleic acid / isostearate, polyglyceryl-6 hexalicinoleate, polyglyceryl-4 oleate, PEG-8 propylene glycol oleic acid / coconut oil fatty acid, magnesium stearate, sodium stearate, potassium laurate, potassium ricinoleate, sodium coconut fatty acid, sodium talusate, potassium castrate, sodium oleate, and mixtures thereof. Further preferred W / Si emulsifiers are lauryl polyglyceryl-3 polydimethylsiloxyethyl dimethicone, and / or PEG-9 polydimethylsiloxyethyl dimethicone, and / or cetyl PEG / PPG-10 / 1 dimethicone, and / or PEG-12 dimethicone crosspolymer, and / or PEG / PPG-18 / 18 dimethicone. At least one W / O emulsifier is used in an amount of preferably about 0.001 to 10% by weight, more preferably 0.2 to 7% by weight, based on the total weight of the composition.
[0120] The composition according to the invention further advantageously contains at least one surfactant adjuvant selected, for example, from the group consisting of monoglycerides and diglycerides and / or fatty alcohols. The surfactant adjuvant is generally used in an amount selected from the range of 0.1 to 10% by weight, particularly in the range of 0.5 to 7% by weight, most particularly in the range of 1 to 5% by weight, based on the total weight of the composition. Particularly suitable surfactant adjuvants are selected from the list of alkyl alcohols such as cetyl alcohol (Lorol C16, Lanette 16), cetearyl alcohol (Lanette O), stearyl alcohol (Lanette 18), behenyl alcohol (Lanette 22), polyhydroxystearic acid, glyceryl stearate, glyceryl myristate (Estol 3650), hydrogenated coco glyceride (Lipocire Na10) and mixtures thereof.
[0121] In all embodiments of the invention, it is particularly advantageous when the composition also contains cetyl alcohol and / or glyceryl stearate.
[0122] As an advantageous embodiment of the composition of the invention, the composition contains di(caprylic / capric acid) butylene glycol, phenethyl benzoate, alkyl benzoate (C 12 -C 15 ), dibutyl adipate, diisopropyl sebacate, dicaprylyl carbonate, dialkyl tartrate (C 12 - 13 ), butyl octyl salicylate, diethylhexyl malonate silicylene, hydrogenated castor oil dimer acid, triheptanoin, alkyl lactate (C 12 - 13 ), alkyl benzoate (C 16-17), also includes one or more oils selected from propylheptyl caprylate, caprylic / capric triglyceride, 2,6-naphthalenedicarboxylate diethylhexyl, octyldodecanol, coconut oil fatty acid ethylhexyl, and phenethyl alcohol. Preferably, the composition according to the present invention includes, as oil, dibutyl adipate, phenylethyl benzoate, butylene glycol, phenethyl benzoate, phenethyl alcohol, and C benzoate. 12 -C 15 It contains alkyl groups, diisopropyl sebacate, and mixtures thereof.
[0123] In a more advantageous embodiment of the present invention, the composition of the present invention preferably further comprises a preservative and / or preservative booster, selected from the group consisting of ethanol, phenoxyethanol, sodium benzoate, potassium sorbate, phenethyl alcohol, hydroxyactofenone, ethylhexylglycerin, hexylglycerin, glyceryl caprylate, 1,3-propanediol, 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol (caprylyl glycol), 1,2-decanediol and 2-methyl-1,3-propanediol and mixtures thereof, and most preferably selected from the group consisting of phenoxyethanol and ethylhexylglycerin and mixtures thereof. Where present, the preservative and / or preservative booster are used in an amount of preferably 0.01 to 5% by weight, more preferably 0.05 to 4% by weight, and most preferably 0.1 to 3.0% by weight, based on the total weight of the composition.
[0124] The present invention is advantageous when the formulation contains one or more alkanediols from the group consisting of 1,3-propanediol, 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, 1,2-decanediol, and 2-methyl-1,3-propanediol. When one or more alkanediols are present, they are used in an amount of preferably 0.1 to 7% by weight, more preferably 0.5 to 7% by weight, and most preferably 1.0 to 5.0% by weight, based on the total weight of the composition.
[0125] According to the present invention, it is even more advantageous when the emulsion composition of the present invention contains phenoxyethanol, ethylhexylglycerin, glyceryl caprylate and / or phenethyl alcohol, preferably phenoxyethanol and / or ethylhexylglycerin or glyceryl caprylate and / or phenethyl alcohol, most preferably phenoxyethanol and ethylhexylglycerin or glyceryl caprylate and phenethyl alcohol.
[0126] In another advantageous embodiment, the compositions according to the present invention do not contain any parabens, benzethonium chloride, piroctone olamine, lauroyl alginate, methylisothiazolinone, chloromethylisothiazolinone, bronopol, benzalkonium chloride, formaldehyde-releasing compounds, salicylic acid, triclosan, DMDM hydantoin, chlorphenesin, or IPBC (iodopropynyl butylcarbamate).
[0127] The composition according to the present invention may further contain one or more emollients that soothe and soften the skin. Examples of emollients include silicones (dimethicone, cyclomethicone), vegetable oils (grape seed oil, sesame seed oil, jojoba oil, etc.), butters (cocoa butter, shea butter), and petrolatum derivatives (petrolatum, mineral oil).
[0128] In another embodiment, the composition of the present invention includes limonene, citral, linalool, alpha-isomethyl ionone, geraniol, citronellol, 2-isobutyl-4-hydroxy-4-methyltetrahydropyran, 2-tert-pentylcyclohexyl acetate, 3-methyl-5-phenyl-1-pentanol, 7-acetyl-1,1,3,4,4,6-hexamethyltetraline, adipic acid diester, cinnamal, amyl salicylate, alpha-amyl cinnamaldehyde, alpha-methyl ionone, butylphenyl methylpropional, cinnamal, amyl cinnamyl alcohol, anise alcohol, benzoin, benzyl alcohol, benzyl benzoate, benzyl cinnamate, salicylic acid It may contain one or more fragrances selected from benzyl tate, bergamot oil, bitter orange oil, butylphenyl methylpropional, cardamom oil, cedrol, cinnamal, cinnamyl alcohol, citronellyl methylcrotate, citrus oil, coumarin, diethyl succinate, ethyl linalool, eugenol, Ebernia furfrasea extract, hornwort extract, farnesol, guaiawood oil, hexyl cinnamal, hexyl salicylate, hydroxycitronellal, lavender oil, lemon oil, linalyl acetate, mandarin oil, menthyl PCA, methylhexadecane, nutmeg oil, rosemary oil, sweet orange oil, terpineol, tonka bean oil, triethyl citrate, and vanillin.
[0129] The compositions of the present invention may, advantageously, include humectants. Humectants are compounds or mixtures of compounds that, after the cosmetic composition is applied to or spread on the skin surface, impart to the cosmetic composition a quality that reduces water loss from the stratum corneum (also known as transepidermal water loss (TEWL)) and / or has a favorable effect on the hydration of the stratum corneum.
[0130] Non-limiting examples of humectants advantageous for use in the present invention include glycerol, lactic acid and / or lactates, particularly sodium lactate, butylene glycol, propylene glycol, 1,3-propanediol, biosaccharide gum-1, wild soybean, ethylhexyloxyglycerol, pyrrolidone carboxylic acid, and urea. Particularly advantageous is the use of high molecular weight humectants from the group of polysaccharides that are water-soluble and / or water-swellable and / or can be gelled by the power of water. Particularly advantageous are, for example, hyaluronic acid, chitosan, and / or fucose-rich polysaccharides, the fucose-rich polysaccharides which are registered in Chemical Abstracts under registration number 178463-23-5 and are available, for example, from SOLABIA SA under the name Fucogel® 1000. Humidifiers can also be advantageously used, for example, as active anti-wrinkle ingredients to protect against the types of skin changes that occur with skin aging.
[0131] Particularly advantageous humectants used in the compositions according to the present invention are glycerin, sodium hyaluronate, isomerized sugar and / or 1,3-propanediol, in a total amount selected from a range of 0.1 to 5% by weight, more preferably 0.1 to 3% by weight, and even more preferably 0.5 to 3% by weight, based on the total weight of the composition.
[0132] While not essential, advantageously, the cosmetic compositions of the present invention may further include fillers that, for example, further improve the sensory and cosmetic properties of the formulation and have the effect of evoking or emphasizing a skin feel such as velvet or silk. Advantageous fillers in the sense of the present invention include starch and starch derivatives (e.g., tapioca starch, cross-linked starch phosphate, aluminum starch octenyl succinate, sodium starch octenyl succinate, etc.), Valvance pigments that essentially exhibit neither UV filtering nor coloring effects (e.g., Valvance Touch 210 or Valvance Touch 250), and / or Aerosils® (CAS No. 7631-86-9), and / or talc, and / or polyethylene, nylon, and dimethylsilylated silica.
[0133] The aqueous phase of the composition of the present invention may, advantageously, include commonly used cosmetic additives, for example, individually or in combination in each case, alcohols, particularly those with a low number of carbon atoms, preferably ethanol and / or isopropanol or polyols with a low number of carbon atoms, in addition to their ethers, preferably propylene glycol, glycerol, electrolytes, self-tanning agents, and also one or more thickeners, advantageously silicon dioxide, aluminum silicate, polysaccharides and / or derivatives thereof, thickeners that can be selected from the group of hyaluronic acid, xanthan gum, hydroxypropyl methylcellulose, particularly advantageously polyacrylates, preferably thickeners from the group of polyacrylates referred to as Carbopol (examples include 980, 981, 1382, 2984 and 5984 type carbopols). Further advantageous thickeners according to the present invention include those with the INCI name (acrylate / C10-30 alkyl acrylate crosspolymer) (e.g., Pemulen TR 1, Pemulen TR 2, Carbopol 1328 from Lubrizol), as well as Aristoflex AVC (INCI: (ammonium acryloyldimethyltaurate / VP) copolymer) and Simugel NS (INCI: (hydroxyethyl acrylate / sodium acryloyldimethyltaurate) copolymer (and) squalane (and) polysorbate 60).
[0134] According to the present invention, it is particularly preferable when the composition contains a thickening agent. Suitable thickening agents used in accordance with the present invention include xanthan gum, crosslinked acrylate / C10-C30 alkyl polymer, hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymer, and / or vinylpyrrolidone / hexadecane copolymer, preferably xanthan gum and / or hydroxyethyl acrylate / sodium acryloyldimethyl taurate, most preferably xanthan gum.
[0135] The amount of xanthan gum, if present, is preferably selected in the range of 0.1 to 1% by weight, more preferably in the range of 0.15 to 0.75% by weight, and most preferably in the range of 0.2 to 0.4% by weight, based on the total weight of the composition.
[0136] The oil phase of the composition of the present invention may also advantageously contain commonly used cosmetic auxiliaries, such as dextrin palmitate (Rheopearl KL2, Chiba Flour Milling), dextrin palmitate and C15-19 alkanes (TILAMAR FITS, DSM), polyurethane-79 and caprylic / caprylic triglyceride (Oilkemia 5S, Lubrizol), ethylene / propylene / styrene copolymer and butylene / ethylene / styrene copolymer and pentaerythrityltetra-di-t-butylhydroxyhydrocinnamate and squalane (Veggi Gel, Aiglon), dibutyl lauroyl glutamide and dibutyl ethylhexanoyl glutamide and octyldodecanol (AJK-OD246, Ajinomoto).
[0137] The amount of a thickening agent (e.g., an active thickening polymer), if present, is preferably selected in the range of 0.1 to 15% by weight, more preferably in the range of 0.5 to 10% by weight, and most preferably in the range of 1.0 to 8.0% by weight, based on the total weight of the composition.
[0138] The composition of the present invention requires a surprisingly small total amount of UV filter.
[0139] In another embodiment, the composition may have an SPF of at least 15, preferably at least 20, and most preferably at least 30.
[0140] According to the present invention, it is advantageous when the composition of the present invention includes a film-forming agent. A film-forming agent in the sense of the present invention is a substance having various compositions and is characterized by having the following properties. When the film-forming agent is dissolved in water or another suitable solvent and this solution is then applied to the skin, the film-forming agent forms a film after the solvent evaporates, and this film essentially fixes the UV filter to the skin and enhances the water resistance of the product.
[0141] It is particularly advantageous to select a film-forming agent from the group of polymers based on polyvinylpyrrolidone (PVP).
[0142] For example, vinylpyrrolidone copolymers such as PVP hexadecane copolymer and PVP eicosene copolymer, available from Ashland under trade names Antaron V216 and Antaron V220, are particularly preferred.
[0143] Similarly, further polymeric film-forming agents such as sodium polystyrene sulfonate (available from National Starch and Chemical Corp. under the trade name Flexan 130) and / or polyisobutene (available from Rewo under the trade name Rewopal PIB1000) are also advantageous. Further examples of suitable polymers include polyacrylamide (Sepigel 305), polyvinyl alcohol, PVP, PVP / VA copolymer, polyglycol, and acrylate / octylacrylamide copolymer (Dermacryl 79). It is equally advantageous to use hydrogenated castor oil dimer dilinoleate (CAS 646054-62-8, INCI hydrogenated castor oil dimer dilinoleate) (available from Higher Alcohol Industries, Ltd. under the name Risocast DA-H) or PPG-3 benzyl ether myristate (CAS 403517-45-3) (available from Croda Chemicals under the trade name Crodamol STS).
[0144] The compositions according to the present invention generally have a pH in the range of 3 to 10, preferably in the range of 4 to 8, and most preferably in the range of 4 to 7.5. This pH can be easily adjusted as needed using a suitable acid, such as citric acid, or a base, such as NaOH, or a suitable amine, such as tromethamine, according to standard methods in the art.
[0145] The amount of cosmetic composition applied to the skin is not definitive and can be easily adjusted by those skilled in the art. Preferably, the amount is 0.1 to 3 mg / cm³. 2 In the area of the skin, for example, preferably 0.1 to 2 mg / cm³ 2 In the skin area, most preferably 0.5 to 2 mg / cm³ 2 Selected within the skin area.
[0146] The following examples are provided to further illustrate the compositions and effects of the present invention. These examples are illustrative and are not intended to limit the scope of the present invention.
[0147] [Examples] [Brief explanation] The SPF-boosting effects of neutral core human milk oligosaccharides LNT and LNnT were investigated. For this purpose, various sunscreens were prepared according to standard methods in the art, as outlined in Tables 1a, 2a, and 3a.
[0148] [In vitro SPF measurement] In vitro SPF tests were performed on PMMA plates (Helioscreen HD6 plates, 5cm x 5cm, Sa roughness 6μm). Each formulation was administered at a dose of 32.5 mg (i.e., 1.3 mg / cm³). 2 The mixture was evenly applied onto a PMMA plate and allowed to dry for 15 minutes.
[0149] In vitro SPF was measured using a Labsphere 2000 UV Transmittance Analyzer. Each PMMA plate was measured nine times at different points on the plate, yielding 27 data points. The results were calculated as the average of these 27 data points.
[0150] [Table 3]
[0151] [Table 4]
[0152] [Table 5]
[0153] [Table 6]
[0154] [Table 7]
[0155] [Table 8]
[0156] [Table 9]
[0157] As shown in Tables 1b, 2b, and 3b, neutral core human milk oligosaccharides, composed of galactose, N-acetylglucosamine, and glucose monosaccharides, increase in vitro SPF by 34% to 194%.
Claims
1. A composition comprising at least one sunscreen activator that absorbs light in the UVB and / or UVA range, and at least one neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine, and glucose monosaccharide.
2. The composition according to claim 1, wherein the at least one sunscreen activator has a lambda maximum value selected in the range of 280 to 400 nm.
3. The composition according to claim 1 or 2, wherein the human milk oligosaccharide is selected from the group consisting of trisaccharides, tetrasaccharides, hexasaccharides, octasaccharides, or decasaccharides, preferably from the group consisting of trisaccharides, tetrasaccharides, and hexasaccharides, and most preferably from the group consisting of tetrasaccharides.
4. The composition according to any one of claims 1 to 3, wherein the galactose, N-acetylglucosamine, and glucose monosaccharide are linked to each other via β-(1-3) or β-(1-4) bonds.
5. The composition according to any one of claims 1 to 4, wherein the human milk oligosaccharide is selected from the group consisting of lacto-N-triose II, lacto-N-tetraose, lacto-N-neotetraose, lacto-N-hexaose, lacto-N-neohexaose, para-lacto-N-hexaose and para-lacto-N-neohexaose and mixtures thereof, preferably lacto-N-triose II, lacto-N-tetraose and / or lacto-N-neotetraose, most preferably lacto-N-tetraose and / or lacto-N-neotetraose.
6. The composition according to any one of claims 1 to 5, wherein the at least one neutral core human milk oligosaccharide is present in an amount effective for increasing the SPF of the composition.
7. The composition according to any one of claims 1 to 6, wherein the amount of neutral core human milk oligosaccharide in the composition is at least 0.2% by weight, preferably at least 0.3% by weight, and most preferably at least 0.5% by weight, based on the total weight of the composition.
8. The composition according to any one of claims 1 to 7, wherein the at least one sunscreen activator is preferably an organic sunscreen activator (organic UV filter) selected from the group consisting of homosalate, ethylhexyl salicylate, polysilicone-15, ethylhexyl methoxycinnamate, octocrylene, phenylbenzimidazole sulfonic acid or a salt thereof, bisethylhexyloxyphenol methoxyphenyl triazine, ethylhexyl triazone, diethylhexyl butamide triazone, methylene bisbenzotriazolyltetramethylbutylphenol, trisbiphenyl triazine, butyl methoxydibenzoylmethane, and diethylamino hydroxybenzoylhexyl benzoate, or preferably an inorganic UV filter (inorganic sunscreen activator (inorganic UV filter)) selected from the group consisting of titanium dioxide or zinc oxide and any mixture thereof.
9. The composition according to any one of claims 1 to 8, wherein the total amount of sunscreen activator in the composition is selected from 1 to 50% by weight, preferably 3 to 40% by weight, and most preferably 5 to 30% by weight, based on the total weight of the composition.
10. The composition according to any one of claims 1 to 9, comprising a carrier consisting of at least 30% by weight, more preferably at least 40% by weight, most preferably at least 45% by weight of water, for example, particularly 50 to 90% by weight of water.
11. The composition according to any one of claims 1 to 10, which is an emulsion.
12. The composition according to claim 11, wherein the composition is an O / W emulsion comprising an oily phase dispersed in an aqueous phase.
13. Use of the composition according to any one of claims 1 to 12 for protecting the skin from the effects of skin aging such as wrinkles, and as a sunscreen composition.
14. A method for preparing a composition, comprising adding at least one sunscreen activator and at least one neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine, and glucose monosaccharide to the composition during the preparation of the composition.
15. Use of at least one neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine, and glucose monosaccharide to increase the SPF of a composition containing at least one sunscreen activator.