Sunscreen compositions comprising human milk oligosaccharides
By adding neutral core human milk oligosaccharides composed of galactose, N-acetylglucosamine and glucose monosaccharides to the sunscreen products, the difficulty of improving the sunscreen coefficient (SPF) in the prior art was solved, and a significant improvement in SPF was achieved.
Patent Information
- Application Number
- CN202380075392.5
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Priority Date
- 2022-10-28
- Filing Date
- 2023-10-27
- Publication Date
- 2025-06-06
AI Technical Summary
Existing sunscreen products have difficulties in improving sunscreen coefficient (SPF), mainly due to the limited number of approved sunscreen active agents worldwide.
A neutral core human milk oligosaccharide consisting of galactose, N-acetylglucosamine and glucose monosaccharides are introduced to enhance the SPF of the composition by adding it to the sunscreen product.
The SPF of the sunscreen active ingredient was significantly increased, and in vitro measurements showed an increase of SPF by 20% to 100%.
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Abstract
Description
Technical Field
[0001] The present invention relates to compositions comprising at least one sunscreen active and having improved sun protection factor (SPF) performance, and methods of improving sun protection factor (SPF) performance. Background Art
[0002] The use of compositions comprising sunscreen active agents, also called sunscreen products, is very common today. The sunscreen active agents in such compositions protect keratin materials, such as, in particular, the skin, from damage caused by UV radiation, including damage by UVA and UVB rays, which are known not only to cause wrinkles on the skin, but also to promote the development of skin diseases, such as lupus erythematosus and melanoma and non-melanoma skin cancers. Therefore, in order to obtain ultimate skin protection, there is an increasing demand for sunscreen products with a high SPF (sun protection factor).
[0003] The standard measure for determining the degree of protection provided by a composition comprising a sunscreen active against UV radiation is the sun protection factor (SPF). However, increasing the SPF of a composition comprising a sunscreen active can be difficult given the limited number of sunscreen actives approved worldwide.
[0004] Therefore, there is a continuing need for natural ingredients that can increase the SPF of sunscreen actives in compositions. Summary of the invention
[0005] Surprisingly, it has now been found that certain human milk oligosaccharides, i.e. neutral core human milk oligosaccharides composed of galactose, N-acetylglucosamine and glucose monosaccharides, such as lacto-N-tetraose (LNT) or lacto-N-neotetraose (LNnT), are able to significantly increase the SPF of compositions comprising at least one sunscreen active ingredient.
[0006] Thus, in a first embodiment, the present invention relates to a composition for keratin materials (eg hair or skin) comprising at least one sunscreen active and at least one neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine and glucose monosaccharides.
[0007] The present invention also relates to an emulsion composition for keratin materials (e.g., hair or skin) comprising at least one sunscreen active and at least one neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine and glucose monosaccharides. Preferably, the composition is in the form of an oil-in-water (O / W) emulsion.
[0008] The present invention also relates to a method of increasing the sun protection factor (SPF) of a composition comprising at least one sunscreen active, the method comprising adding to the composition at least one neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine and glucose monosaccharides in an amount effective to increase the SPF of the composition.
[0009] The present invention also relates to the use of neutral core human milk oligosaccharides composed of galactose, N-acetylglucosamine and glucose monosaccharides for increasing the sun protection factor (SPF) of a composition comprising at least one sunscreen active.
[0010] The present invention also relates to a method for preparing a composition having improved sun protection factor (SPF) performance, comprising adding to the composition during the preparation of the composition at least one neutral core human milk oligosaccharide consisting of galactose, N-acetylglucosamine and glucose monosaccharides. It is known that the improved performance is to be compared with a composition not comprising the neutral core human milk oligosaccharide as defined herein.
[0011] The present invention also relates to a method of preparing a composition comprising combining at least one sunscreen active with at least one neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine and glucose monosaccharides.
[0012] According to the invention, there is also provided the use of the compositions according to the invention for protecting the skin against the effects of skin aging, in particular against UV-induced skin aging, such as in particular the development of wrinkles, and as sunscreen compositions.
[0013] Finally, the subject of the present invention is a method for the cosmetic treatment of keratinous materials, such as in particular the skin, wherein a composition as defined herein is applied to said keratinous materials, such as in particular the skin. This method is particularly suitable for protecting the skin from the adverse effects of UV-radiation, such as in particular sunburn and / or photoaging. DETAILED DESCRIPTION
[0014] The term "keratin material" refers to the skin (body, face, eye contour, scalp), hair, eyelashes, eyebrows, body hair, nails and / or lips. Preferably, in all embodiments, the keratin material is skin.
[0015] As used herein, the term 'neutral core human milk oligosaccharides' (neutral core HMO) refers to a family of structurally diverse unconjugated glycans that are abundant and unique to human milk and are composed of galactose, N-acetylglucosamine and glucose monosaccharide units preferably interconnected by β-(1-3) or β-(1-4) bonds. Preferably, in all embodiments herein, galactose is D-galactose and glucose is D-glucose.
[0016] SPF according to the invention is understood to be measured by the in vitro SPF method, as described in ISO 24443 (In vitro sunscreen UVA photoprotection determination, 01.06.2012) and exemplified in the examples.
[0017] In all embodiments of the present invention, preferably, the neutral core human milk oligosaccharide is a trisaccharide, a tetrasaccharide, a hexasaccharide, an octasaccharide or a decasaccharide, wherein trisaccharides, tetrasaccharides and hexasaccharides are particularly preferred. Tetrasaccharides are most preferred.
[0018] In all embodiments of the present invention it is further advantageous that the oligosaccharides are linear oligosaccharides, ie unbranched oligosaccharides.
[0019] Exemplary oligosaccharides according to the present invention are shown below
[0020]
[0021] In all embodiments of the invention it is further advantageous that the oligosaccharide is characterized by a terminal D-galactose linked to an N-acetyl-d-glucosamine (GlcNAc) unit via a β-(1-3) or β-(1-4) bond.
[0022] Furthermore, in all embodiments of the present invention, it is also preferred that the oligosaccharide is characterized by D-galactose linked to a reducing terminal D-glucose via a β-(1-4) bond.
[0023] Particularly suitable neutral core human oligosaccharides according to the invention are listed in Table 1
[0024]
[0025] Advantageously, in all embodiments of the 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, it is most preferred to use lacto-N-(neo)tetraose, ie lacto-N-tetraose (CAS No.: 14116-68-8) and / or lacto-N-neotetraose (CAS No.: 13007-32-4).
[0027] The HMOs according to the invention may be isolated from breast milk or may be produced chemically or biochemically according to methods well known in the art.
[0028] For the purposes of the present invention, the origin of the HMO is not important. Obviously, HMO from different sources can be used.
[0029] In the composition according to the invention, the total amount of the neutral core HMO according to the invention is preferably at least 0.01 wt.-%, more preferably at least 0.1 wt.-%, even more preferably at least 0.2 wt.-%, such as at least 0.3 wt.-% or at least 0.5 wt.-%, 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 wt.-%, more preferably from the range of 0.1 to 7.5 wt.-%, most preferably from the range of 0.2 to 5 wt.-%, based on the total weight of the composition. Further suitable ranges are 0.25 to 5 wt.-%, 0.5 to 4 wt.-%, 0.1 to 3 wt.-%, 0.25 to 3 wt.-% and 0.3 to 3 wt.-%. According to the invention, a particularly preferred range is 0.1 to 5 wt.-%, more preferably 0.25 to 3 wt.-%, such as 0.25 to 1.5 wt.-%, 0.5 to 5 wt.-%, or 0.5 to 4 wt.-%.
[0030] Preferably, in all embodiments of the invention, the neutral-core HMO according to the invention is present in an amount effective to increase the SPF (measured in vitro) of the composition by at least 20%, preferably at least 30%, more preferably at least 50%, most preferably at least 100% (including all ranges and subranges therebetween, for example 25% to 35%, 20% to 300%, 30% to 250%, 30% to 200%) and all ranges and subranges therebetween.
[0031] It is well understood that the composition according to the invention may include one or more HMOs. However, preferably, the composition according to the invention includes one or two, more preferably only one HMO, for example most preferably selected from LNT and / or LNnT. In all embodiments of the invention, the most preferred HMO is LNT, since the increase in SPF caused by it is particularly significant.
[0032] As used herein, the term 'sunscreen active' refers to compounds that absorb light in the UVB and / or UVA range (also known as UVA-, UVB- and broad spectrum (UVA&B) filters). Preferably, such compounds have an E1 / 1 value (ie, max The UV absorbance of the absorption layer with a thickness of 1 cm at a concentration of 1% is at least 150, more preferably at least 180, and most preferably at least 190. It is well understood by those skilled in the art that the λmax (λ max), i.e. the wavelength in the absorption spectrum at which the sunscreen active has 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 invention, λmax is taken from the range of 300 to 380 nm, most preferably from the range of 300 to 370 nm. Furthermore, it is well understood by the person skilled in the art that UV-filters used as sunscreens do not absorb substantially light in the visible range (i.e. wavelengths > 400 nm), since this discolors them, which is highly undesirable in the industry.
[0033] Therefore, the present invention relates to a composition comprising at least one sunscreen active and at least one neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine and glucose monosaccharides, wherein the λmax (i.e. the maximum absorption wavelength) of the sunscreen active is within the range of 280 to 400 nm, preferably within the range of 300 to 380 nm, most preferably within the range of 300 to 370 nm.
[0034] Preferred UVA filters typically absorb radiation in the 320 to 400 nm region of the ultraviolet spectrum. Examples of preferred UVA absorbers include dibenzoylmethane or dialkylaminohydroxybenzoylalkyl benzoates.
[0035] Preferred UVB filters absorb radiation in the 280 to 320 nm region of the ultraviolet spectrum. Examples of preferred UVB absorbers include cinnamate, diphenylacrylate, benzalmalonate, triazines and salicylates.
[0036] Preferred broad spectrum UV filters provide substantially broad spectrum protection against both UVA and UVB rays.Examples of preferred broad spectrum absorbers include micronized organic UV-filters such as methylene bisbenzotriazolyl tetramethylbutylphenol.
[0037] Preferably, in all embodiments of the invention, the composition does not comprise lutein.
[0038] The sunscreen active agent present in the composition of the invention may be an organic sunscreen active agent (organic UV-filter) and / or an inorganic sunscreen active agent (inorganic UV-filter), for example a physical blocking agent, such as titanium dioxide or zinc oxide. Furthermore, the sunscreen active agent present in the composition of the invention may be soluble in water, soluble in non-aqueous materials and / or insoluble. Preferred sunscreen active agents according to the invention are organic sunscreen active agents.
[0039] Preferably, in all embodiments of the present invention, a combination of two or more, preferably three or more, even 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, even more preferably four or more different UV filters are selected from organic UV filters with all the preferences and definitions given herein.
[0040] Preferably, in all embodiments of the present invention, the total amount of all sunscreen actives in the composition according to the invention is taken in the range from about 1 to about 50 wt.-% relative to the total weight of the composition, preferably from about 3 to about 40 wt.-% relative to the total weight of the composition, more preferably from about 5 to about 30 wt.-%, about 10 to 25 wt.-% or about 15 to 25 wt.-% relative to the total weight of the composition, including all ranges and sub-ranges therebetween.
[0041] In all embodiments of the present invention, it is also preferred that the amount of all UV filters present in the composition according to the invention is chosen so that the SPF (in vitro SPF measured as described in ISO 24443 In vitro sunscreen UVA photoprotection determination, 01.06.2012, as exemplified in the examples) of the final composition is at least 10, preferably at least 15, more preferably at least 20.
[0042] Particularly useful organic UV-filters herein include anthranilates; cinnamic acid derivatives; dibenzoylmethane derivatives; salicylic acid derivatives; camphor derivatives; triazine derivatives, such as those disclosed in patent applications U.S. Pat. No. 4,367,390, EP 863 145, EP 517 104, EP 570 838, EP 796 851, EP 775 698, EP 878 469, EP 933376, EP 507 691, EP 507 692, EP 790 243 and EP 944 624; benzophenone derivatives; β,β-diphenylacrylate derivatives; benzotriazole derivatives; benzylidenemalonate derivatives; benzimidazole derivatives; imidazolines; such as those disclosed in patent EP 669 323 and U.S. Pat. No. 2,463,264; p-aminobenzoic acid (PABA) derivatives; methylenebis(hydroxyphenylbenzotriazole) derivatives as disclosed in U.S. Pat. Nos. 5,237,071 and 5,166,355, GB 2 303 549, DE 197 26 184 and EP 893 1 19; barrier polymers and barrier silicones, such as those disclosed in particular in WO 93 / 04665; dimers derived from α-alkylstyrene, such as those disclosed in DE 198 55 649; 4,4-diarylbutadiene, such as those disclosed in EP 0 967 200, DE 197 46 654, DE 197 55 649, EP-A-1 008586, EP 1 133 980 and EP 133 981; and mixtures thereof.
[0043] By way of illustration, mention may be made of, as sunscreen actives generally active in the UV-A and / or UV-B region (indicated hereinafter by their INCI names): para-aminobenzoic acid (PABA) derivatives, in particular PABA, ethyl PABA, ethyl dihydroxypropyl PABA, ethylhexyl dimethyl PABA, glyceryl PABA or PEG-25 PABA; salicylic acid derivatives, in particular homosalate (HMS), ethylhexyl salicylate (EHS), dipropylene glycol salicylate or TEA salicylate; dibenzoylmethane derivatives Bioagents, in particular butyl methoxydibenzoylmethane (BMDBM) or isopropyl dibenzoylmethane; cinnamic acid derivatives, in particular ethylhexyl methoxycinnamate (OMS), isopropyl methoxycinnamate, isoamyl methoxycinnamate, cinoxate, DEA methoxycinnamate, diisopropyl methyl cinnamate or glyceryl ethylhexanoate dimethoxycinnamate, β,β-diphenylacrylate derivatives, in particular octocrylene (OC) or etocrylene, benzophenones, in particular benzophenone-1, benzophenone-2, benzophenone-3 or oxybenzone, dibenzoylmethane Benzophenone-4, benzophenone-5, benzophenone-6, benzophenone-8, benzophenone-9, benzophenone-12 or n-hexyl 2-(4-diethylamino-2-hydroxybenzoyl)benzoate (DHHB), benzylidene camphor derivatives, in particular 3-methylbenzylidene camphor, 4-methylbenzylidene camphor, benzylidene camphor sulfonic acid, camphor benzalkonium methyl sulfate, terephthalylidene camphor sulfonic acid or polyacrylamide methyl benzylidene, benzimidazole derivatives, in particular phenylbenzimidazole sulfonic acid (HS) or disodium phenyldibenzimidazole tetrasulfonate, triazine derivatives, In particular, bis-ethylhexyloxyphenol methoxyphenyl triazine (BEMT), ethylhexyl triazone (EHT), diethylhexyl butamido triazone (DBT) or 2,4,6-tris(diisobutyl 4'-amino-benzylidenemalonate)-s-triazine, benzotriazole derivatives, in particular drometrizole trisiloxane, or insoluble organic sunscreen actives, such as methylenebisbenzotriazolyl tetramethylbutylphenol (MBBT) and tris-biphenyl triazine (A2B), which are usually sold in the form of aqueous dispersions of active UV filters, for example under the trade name MAX (MBBT) (from DSM Nutritional Products) or A2B (A2B) (from BASF), anthranilic acid derivatives, in particular menthol anthranilate, imidazoline derivatives, in particular ethylhexyl dimethoxybenzylidene dioxoimidazolinium propionate, benzylmalonate derivatives, in particular polyorganosiloxanes comprising benzylmalonate functional groups (for example commercially available under the INCI name: Polysilicone-15), 4,4-diarylbutadiene derivatives, in particular 1,1'-dicarboxy(2,2'-dimethylpropyl)-4,4-diphenylbutadiene, and mixtures thereof.
[0044] Organic sunscreen active agents (organic UV filters) that are particularly preferred according to the invention include homosalate (e.g. sold under the trade name “ HMS”), ethylhexyl salicylate (e.g. sold under the trade name “ EHS"), polysilicone-15 (especially sold under the trade name " SLX”), ethylhexyl methoxycinnamate (e.g. sold under the trade name “ MCX”), octocrylene (e.g., sold under the trade name “ 340”), phenylbenzimidazole sulfonic acid (e.g. sold under the trade name “ HS") or a salt thereof, for example formed during preparation of the composition with a neutralizing agent such as triethanolamine or sodium hydroxide, bis-ethylhexyloxyphenol methoxyphenyl triazine (for example sold under the trade name " SHIELD”), ethylhexyl triazone (e.g. sold under the trade name “ EHT”), diethylhexyl butyramido triazone (for example, sold under the trade name Uvasaorb HEB), methylene bisbenzotriazolyl tetramethylbutylphenol (for example, sold under the trade name MAX", tris-biphenyltriazine (sold for example under the trade name Uvinul A2B), butyl methoxydibenzoylmethane (sold especially under the trade name "Parsol 1789"), diethylaminohydroxybenzoyl hexyl benzoate (sold for example under the trade name Uvinul A Plus), and mixtures thereof.
[0045] In all embodiments according to the invention, the most preferred organic sunscreen actives (organic UV filters) are selected from ethylhexyl salicylate, polysilicone-15, ethylhexyl methoxycinnamate, octocrylene, phenylbenzimidazole sulfonic acid or its salts, bis-ethylhexyloxyphenol methoxyphenyl triazine, ethylhexyl triazone, diethylhexyl butamido triazone, methylene bisbenzotriazolyl tetramethylbutylphenol, butyl methoxydibenzoylmethane, diethylaminohydroxybenzoyl hexyl benzoate and any mixtures thereof.
[0046] In all embodiments of the present invention, the (total) amount of organic UV filters in the composition according to the invention is taken in the range of 0.5 to 30 wt.-%, more preferably in the range of 1 to 25 wt.-%, most preferably in the range of 1 to 25 wt.-%, for example 1 to 15 wt.-%, based on the total weight of the composition. Further suitable amounts are taken in the range of 5 to 30 wt.-%, 10 to 30 wt.-%, 15 to 30 wt.-%, 5 to 25 wt.-%, 10 to 25 wt.-% or 15 to 25 wt.-%, based on the total weight of the composition.
[0047] In all embodiments of the invention, the amount of ethylhexyl salicylate in the composition according to the invention is advantageously taken in the range of 0.5 to 10 wt.-%, preferably in the range of 0.5 to 9 wt.-%, 0.5 to 8 wt.-%, 0.5 to 7 wt.-%, 0.5 to 6 wt.-%, 0.5 to 5 wt.-%, for example in the range of 1 to 10 wt.-%, 2 to 10 wt.-%, 3 to 10 wt.-% or 2 to 7.5 wt.-%, 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 invention is advantageously taken in the range of 0.4 to 10 wt.-%, preferably in the range of 0.4 to 9 wt.-%, 0.4 to 8 wt.-%, 0.4 to 7 wt.-%, 0.4 to 6 wt.-%, 0.4 to 5 wt.-%, 0.4 to 4 wt.-%, 0.4 to 3 wt.-%, 0.5 to 3 wt.-%, 0.8 to 9 wt.-%, 0.8 to 8 wt.-%, 0.8 to 7 wt.-%, 0.8 to 6 wt.-%, 0.8 to 5 wt.-%, 0.8 to 4 wt.-%, 0.8 to 3 wt.-%, for example in the range of 1 to 5 wt.-%, 1 to 3 wt.-%, 1 to 2.5 wt.-% or 1.5 to 2.5 wt.-%, based on the total weight of the composition.
[0049] In all embodiments of the invention, the amount of ethylhexyl methoxycinnamate in the composition according to the invention is advantageously taken in the range of 0.5 to 10 wt.-%, preferably in the range of 0.5 to 9 wt.-%, 0.5 to 8 wt.-%, 0.5 to 7 wt.-%, 0.5 to 6 wt.-%, 0.5 to 5 wt.-%, for example in the range of 1 to 10 wt.-%, 2 to 10 wt.-%, 3 to 10 wt.-% or 2 to 7.5 wt.-%, based on the total weight of the composition.
[0050] In all embodiments of the invention, the amount of octocrylene in the composition according to the invention is advantageously taken in the range of 0.5 to 15 wt.-%, preferably in the range of 0.5 to 10 wt.-%, 0.5 to 8 wt.-%, 1 to 10 wt.-%, 2 to 10 wt.-%, 3 to 10 wt.-%, for example in the range of 5 to 10 wt.-%, 6 to 10 wt.-% or 7 to 10 wt.-%, based on the total weight of the composition.
[0051] In all embodiments of the present invention, the amount of phenylbenzimidazole sulfonic acid or its salt in the composition according to the invention is advantageously taken in the range of 0.5 to 5 wt.-%, preferably in the range of 0.5 to 4 wt.-%, 0.5 to 3 wt.-%, 1 to 2.5 wt.-%, 1 to 3 wt.-% or 1 to 4 wt.-%, based on the total weight of the composition.
[0052] In all embodiments of the present invention, the amount of bis-ethylhexyloxyphenol methoxyphenyl triazine in the composition according to the invention is advantageously taken in the range of 0.4 to 10 wt.-%, preferably in the range of 0.4 to 9 wt.-%, 0.4 to 8 wt.-%, 0.4 to 7 wt.-%, 0.4 to 6 wt.-%, 0.4 to 5 wt.-%, 0.4 to 4 wt.-%, 0.4 to 3 wt.-%, 0.5 to 3 wt.-%, 0.8 to 9 wt.-%, 0.8 to 8 wt.-%, 0.8 to 7 wt.-%, 0.8 to 6 wt.-%, 0.8 to 5 wt.-%, 0.8 to 4 wt.-%, 0.8 to 3 wt.-%, for example in the range of 1 to 5 wt.-%, 1 to 3 wt.-%, 1 to 2.5 wt.-% or 1.5 to 2.5 wt.-%, based on the total weight of the composition.
[0053] In all embodiments of the present invention, the amount of ethylhexyl triazone in the composition according to the invention is advantageously taken in the range of 0.4 to 10 wt.-%, preferably in the range of 0.4 to 9 wt.-%, 0.4 to 8 wt.-%, 0.4 to 7 wt.-%, 0.4 to 6 wt.-%, 0.4 to 5 wt.-%, 0.4 to 4 wt.-%, 0.4 to 3 wt.-%, 0.5 to 3 wt.-%, 0.8 to 9 wt.-%, 0.8 to 8 wt.-%, 0.8 to 7 wt.-%, 0.8 to 6 wt.-%, 0.8 to 5 wt.-%, 0.8 to 4 wt.-%, 0.8 to 3 wt.-%, for example in the range of 1 to 5 wt.-%, 1 to 3 wt.-%, 1 to 2.5 wt.-% or 1.5 to 2.5 wt.-%, based on the total weight of the composition.
[0054] In all embodiments of the present invention, the amount of diethylhexyl butanamido triazone in the composition according to the invention is advantageously taken in the range of 0.4 to 10 wt.-%, preferably in the range of 0.4 to 9 wt.-%, 0.4 to 8 wt.-%, 0.4 to 7 wt.-%, 0.4 to 6 wt.-%, 0.4 to 5 wt.-%, 0.4 to 4 wt.-%, 0.4 to 3 wt.-%, 0.5 to 3 wt.-%, 0.8 to 9 wt.-%, 0.8 to 8 wt.-%, 0.8 to 7 wt.-%, 0.8 to 6 wt.-%, 0.8 to 5 wt.-%, 0.8 to 4 wt.-%, 0.8 to 3 wt.-%, for example in the range of 1 to 5 wt.-%, 1 to 3 wt.-%, or 1.5 to 3 wt.-%, based on the total weight of the composition.
[0055] In all embodiments of the present invention, the amount of methylenebisbenzotriazolyltetramethylbutylphenol (based on about 45-55 wt.-% of MBBT dispersion, for example commercially available under the trade name PARSOLMAX) in the composition according to the invention is advantageously taken in the range of 0.5 to 10 wt.-%, preferably in the range of 1 to 10 wt.-%, more preferably in the range of 2 to 10 wt.-%, most preferably in the range of 2 to 6 wt.-% or 3 to 6 wt.-%, based on the total weight of the composition.
[0056] In all embodiments of the invention, the amount of butyl methoxydibenzoylmethane in the composition according to the invention is advantageously taken in the range of 0.4 to 10 wt.-%, preferably in the range of 0.4 to 9 wt.-%, 0.4 to 8 wt.-%, 0.4 to 7 wt.-%, 0.4 to 6 wt.-%, 0.4 to 5 wt.-%, 0.4 to 4 wt.-%, 0.4 to 3 wt.-%, 0.5 to 3 wt.-%, 0.8 to 9 wt.-%, 0.8 to 8 wt.-%, 0.8 to 7 wt.-%, 0.8 to 6 wt.-%, 0.8 to 5 wt.-%, 0.8 to 4 wt.-%, 0.8 to 3 wt.-%, for example in the range of 1 to 5 wt.-%, 2 to 5 wt.-%, 3 to 5 wt.-% or 3.5 to 5 wt.-%, based on the total weight of the composition.
[0057] In all embodiments of the invention, the amount of diethylaminohydroxybenzoyl hexyl benzoate in the composition according to the invention is advantageously taken in the range of 0.5 to 10 wt.-%, preferably in the range of 0.5 to 9 wt.-%, 0.5 to 8 wt.-%, 0.5 to 7 wt.-%, 0.5 to 6 wt.-%, 0.5 to 5 wt.-%, 0.5 to 4 wt.-%, 0.5 to 3 wt.-%, 1 to 10 wt.-%, 1 to 9 wt.-%, 1 to 8 wt.-%, 1 to 7 wt.-%, 1 to 6 wt.-%, 1 to 5 wt.-%, 2 to 5 wt.-%, 3 to 5 wt.-%, for example in the range of 2.5 to 6 wt.-%, 3 to 6 wt.-%, 4 to 6 wt.-% or 3.5 to 5.5 wt.-%, based on the total weight of the composition.
[0058] Particularly preferred organic UV-filter combinations in all embodiments of the present invention include the combination of DHHB, EHT, BEMT, OMC, polysilicone-15, DBT and MBBT or the combination of BMDBM, EHS, OC and BEMT, optionally further in combination with HS, as exemplified.
[0059] In a preferred embodiment, the compositions according to the invention comprise exclusively organic UV filters.
[0060] In another preferred embodiment, the composition further comprises one or more inorganic UV-filters.
[0061] The term 'inorganic UV-filter' as used herein refers to any metal oxide particles having UV-filtering properties as defined above and therefore useful for incorporation into the composition as a UV-filter. Such inorganic UV-filters are well known to those skilled in the art and are generally referred to as micronized or finely divided UV filters, such as in particular micronized or finely divided titanium dioxide and zinc oxide.
[0062] The particle size of such inorganic UV-filters is not particularly limited. Typically, suitable (primary) particle sizes for effective UV-light absorption are taken from the range of 2 to 200 nm.
[0063] In all embodiments of the present invention, the (total) amount of inorganic UV filters in the composition according to the invention is preferably taken in the range of 0.5 to 30 wt.-%, more preferably in the range of 1 to 30 wt.-%, most preferably in the range of 2 to 30 wt.-%, based on the total weight of the composition. Further suitable amounts are taken in the range of 1 to 25 wt.-%, 1 to 20 wt.-%, 1 to 15 wt.-%, 3.0 to 25 wt.-%, 4 to 25 wt.-%, 5 to 20 wt.-% or 10 to 25 wt.-%.
[0064] Even more advantageously, the (total) amount of inorganic titanium dioxide UV filters in the composition according to the invention is taken in the range of 0.5 to 15 wt.-%, preferably in the range of 1 to 15 wt.-%, more preferably in the range of 2 to 10 wt.-%, most preferably in the range of 2 to 6 wt.-% or 3 to 6 wt.-%, based on the total weight of the composition.
[0065] Even more advantageously, the (total) amount of inorganic zinc oxide UV filters in the composition according to the invention is taken in the range of 0.5 to 25 wt.-%, preferably in the range of 1 to 20 wt.-%, more preferably in the range of 2 to 20 wt.-%, most preferably in the range of 5 to 20 wt.-% or 7.5 to 20 wt.-%, based on the total weight of the composition.
[0066] Preferably, if present in the composition according to the invention, the ratio (w / w) of titanium dioxide UV-filter to zinc oxide UV-filter is taken in the range of 1 :5 to 5: 1, preferably in the range of 1 :2 to 2: 1. Even more preferably, the amount of zinc oxide in the composition according to the invention is higher 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, it is preferred that the compositions according to the invention comprise only inorganic UV filters.
[0068] According to the invention, it is advantageous if the inorganic UV filter is surface-coated. The surface coating can consist in providing the metal oxide particles with a thin hydrophilic or hydrophobic inorganic or organic layer by methods known per se. According to the invention, the different surface coating layers can also include water. Due to the surface treatment, the metal oxide is given hydrophilic, amphiphilic or hydrophobic properties.
[0069] Examples of inorganic surface coating materials suitable for the purpose of the present invention include aluminum oxide (Al 2 O 3 ), aluminum hydroxide Al(OH) 3 , Alumina hydrate (also known as: Alumina, CAS-No.: 1333-84-2), Sodium hexametaphosphate (NaPO 3 ) 6 、Sodium metaphosphate (NaPO 3 ) n 、Silicon dioxide (SiO 2 ) (also known as: silica, CAS-No.: 7631-86-9) and iron oxide (Fe 2 O 3 ). These inorganic surface coating layers may be present alone, in combination and / or in combination with organic coating materials, in particular those described below.
[0070] Examples of organic surface coating materials suitable for use in the present invention include plant or animal aluminum stearate, fatty acids such as stearic acid and lauric acid, polydimethylsiloxane (also known as: dimethicone), polymethylsiloxane (methicone), simethicone, trimethoxycaprylylsilane, triethoxycaprylylsilane, octyltrimethoxysilane and cetyl phosphates such as potassium cetyl phosphate and any mixtures thereof.
[0071] These organic surface coating materials may be present alone, in combination and / or in combination with inorganic coating materials.
[0072] The crystal form of titanium dioxide can be any crystalline or amorphous type. For example, titanium dioxide can be any type of amorphous, rutile, anatase, brookite or a mixture thereof. Preferably, in all embodiments of the present invention, the crystal form of titanium dioxide is rutile.
[0073] Also preferably, the zinc oxide is a white powder consisting of zinc oxide in a wurtzite crystal structure.
[0074] The titanium dioxide UV filters used according to the invention (including any predispersions thereof) are available, for example, from DSM Nutritional Products Ltd. as TX (INCI: titanium dioxide, silicon dioxide, dimethicone), available from Tayca as Micro Titanium Dioxide MT-01 or from Ishihara Sangyo Kaisha as TTO-55I. Also suitable is a double coated titanium dioxide having an inner coating of alumina and an outer coating of simethicone, available for example from EMD chemicals Inc. / Rona as Eusolex T-2000.
[0075] The zinc oxide UV filters used according to the invention (including any predispersions thereof) are available, for example, from BASF as Z-Cote or Z-Cote HP1 (2% dimethicone coated), from Tayca as MZ-505S (5% methicone coated) or from DSM Nutritional Products Ltd as ZX (2-3.5% triethoxyoctylsilane coating) was obtained.
[0076] In a specific embodiment, the composition according to the invention comprises as inorganic UV-filters at least one doubly coated titanium dioxide and at least one coated zinc oxide, most preferably without any other finely divided metal oxides being present (ie one doubly coated titanium dioxide and one coated zinc oxide).
[0077] Most preferably in all embodiments according to the invention the titanium dioxide UV-filter is a double coated titanium dioxide, even more preferably a double coated titanium dioxide having a silica inner coating and an organic outer coating, or a silica coated titanium dioxide.
[0078] Preferably, the silica inner coating of the double coated titania consists of at least 0.5 wt.-% of inorganic silica (based on titania). Further, preferably, the inner coating consists of 0.5 wt.-% to 50 wt.-%, most preferably 1 wt.-% to 20 wt.-% of inorganic silica (based on titania).
[0079] The outer coating material of the double coated titanium dioxide is preferably selected from organic coating materials, such as silicone oils (e.g. simethicone, methyl silicone oil, dimethicone, polysilicone-15), alkyl silanes (e.g. octyl tri(methyl)ethoxysilane), olefinic acids (e.g. stearic acid) or polyols (e.g. glycerol), and can be applied to the titanium dioxide particles by methods known to those skilled in the art (e.g. the method described in FI57124). Preferably, the outer coating material is selected from simethicone, methyl silicone oil, dimethicone, polysilicone-15, stearic acid and octyl trimethoxysilane. Most preferably, the outer coating material is dimethicone. Even more preferably, the amount of the outer coating layer is at least 0.25 wt.-% based on titanium dioxide. Preferably, the amount of the outer coating layer is taken in the range of 0.5 wt.-% to 50 wt.-% based on titanium dioxide, most preferably in the range of 0.5 wt.-% to 10 wt.-% 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 in the range of 70-95 wt.-% and a silicon dioxide content in the range of 5-20 wt.-%, for example preferably a titanium dioxide content in the range of 80-90 wt.-% and a silicon dioxide content in the range of 10 to 15 wt.-%, with the proviso that the total content of titanium dioxide and silicon dioxide is in the range of 90-100 wt.-%.
[0081] Preferably, the average primary particle size of the double-coated titanium dioxide is in the range of 2 to 100 nm, more preferably in the range of 5 to 50 nm, most preferably in the range of 10 to 25 nm, and the secondary particle size is between 0.025 and 1 μm, such as preferably between 0.05 and 0.075 μm.
[0082] According to the present invention, particularly suitable double-coated titanium dioxide comprises rutile titanium dioxide (TiO 2 ) core, and the titanium dioxide content is at least 75wt.-%, preferably in the range of 82-87wt.-%, the silicon dioxide content is at least 10wt.-%, preferably in the range of 10.5 to 14.5wt.-%, and the average particle size distribution D n 50 is 25 to 100 nm, preferably 40 to 80 nm (laser diffraction measurement analysis by Malvern Mastersizer 2000), and the double-coated titanium dioxide can be obtained from DSM Nutritional Products Ltd. TX (INCI: titanium dioxide, silicon dioxide, dimethicone) was purchased.
[0083] Most preferably, in all embodiments of the present invention, the zinc oxide is uncoated or coated with triethoxyoctylsilane. Most preferably, the zinc oxide consists of zinc oxide coated with triethoxyoctylsilane in a wurtzite crystal structure, with a zinc oxide content of 96-98%, a triethoxyoctylsilane content of 2-3.5%, and an average particle size of 90 to 130 nm (analyzed by Malvern Mastersizer 2000 laser diffraction measurement), which is available from DSM Nutritional Products Ltd. as Purchased from ZX.
[0084] If not otherwise specified in this specification, any given parts and percentages are by weight and are based on the total weight of the composition.
[0085] Preferably, neutral core human milk oligosaccharides composed of galactose, N-acetylglucosamine and glucose monosaccharides and sunscreen actives are present in the compositions and methods of the invention in a weight ratio of 1:50 to 1:1, preferably 1:40 to 1:7.5, preferably 1:30 to 1:5, for example 1:25 to 1: 15. Preferably, the sunscreen active is present in excess of the HMO on a weight basis.
[0086] Since the compositions according to the invention are intended for topical application, it is well understood that they comprise a physiologically acceptable medium, i.e. a medium compatible with keratinous substances such as the skin, mucous membranes and keratinous fibers. In particular, a physiologically acceptable medium is a cosmetically acceptable carrier. Therefore, it will be understood by those skilled in the art that the compositions according to the invention are topical compositions.
[0087] As used herein, the term 'cosmetically acceptable carrier' refers to all carriers and / or excipients and / or diluents commonly used in topical cosmetic compositions, such as, in particular, skin care preparations.
[0088] The exact amount of carrier will depend on the actual level of UV-filter as well as any other optional ingredients that one of ordinary skill in the art would classify as different from a carrier (eg, other active ingredients).
[0089] In an advantageous embodiment, the composition according to the invention comprises from 50% to 99%, preferably from 60% to 98%, more preferably from 70% to 98%, such as in particular from 80% to 95% of carrier, based on the total weight of the composition.
[0090] In a particularly advantageous embodiment, the carrier in all embodiments of the invention furthermore consists of at least 30 wt.-%, more preferably at least 40 wt.-%, most preferably at least 45 wt.-% water, such as in particular 50 to 90 wt.-%, 50 to 80 wt.-%, 50 to 79 wt.-% or 50 to 60 wt.-% water.
[0091] In particular, the composition according to the invention is a cosmetic or pharmaceutical composition, preferably a cosmetic (non-therapeutic) composition.
[0092] In one embodiment, the composition according to the invention is applied to mammalian keratinous tissue, such as in particular to human skin or human scalp and hair.
[0093] The term "cosmetic composition" as used herein refers to Cosmetic compositions as defined under the heading "Kosmetika" in Lexikon Chemie (10th edition, 1997, Georg Thieme Verlag Stuttgart, New York) and disclosed in A. Domsch, "Cosmetic Compositions", Verlag für chemische Industrie (by H. Ziolkowsky), 4th edition, 1992.
[0094] Preferred compositions according to the invention are skin care preparations, decorative preparations and functional preparations.
[0095] Examples of skin care preparations are, in particular, photoprotective preparations, anti-aging preparations, preparations for treating photoaging, body oils, body lotions, body gels, therapeutic creams, skin protection ointments, skin powders, moisturizing gels, moisturizing sprays, face and / or body moisturizers, skin tanning preparations (i.e. artificial / sunless tanning and / or browning compositions for human skin), for example self-tanning creams, and skin-lightening preparations.
[0096] Examples of decorative preparations are in particular lipsticks, eye shadows, mascaras, dry and wet make-up preparations, blushers and / or powders.
[0097] Examples of functional preparations are cosmetic 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, but are not limited thereto.
[0098] In a specific embodiment, the composition according to the invention is a photoprotective preparation (sun protection product, sunscreen product), such as a sunscreen milk, sunscreen lotion, sunscreen cream, sunscreen oil, sunblock or day care cream with SPF. Of particular interest are sunscreen creams, sunscreen lotions and sunscreen milks.
[0099] The compositions of the present invention (including carriers) may include conventional adjuvants and additives, such as preservatives / antioxidants, fatty substances / oils, organic solvents, silicones, thickeners, emollients, emulsifiers, defoamers, cosmetic ingredients (e.g. fragrances, surfactants, fillers, anionic, cationic, nonionic or amphoteric polymers or mixtures thereof), propellants, acidulants or alkalizers, dyes, pigments / colorants, abrasives, absorbents, chelating agents and / or sequestering agents, essential oils, skin sensates, astringents, pigments or any other ingredient usually formulated in such compositions.
[0100] According to the present invention, the composition of the present invention may include other ingredients, such as ingredients for skinlighting; ingredients for preventing tanning; ingredients for treating hyperpigmentation; ingredients for preventing or reducing acne, wrinkles, fine lines, atrophy and / or inflammation; chelating agents and / or sequestrants; anti-cellulite and slimming agents (such as phytanic acid), firming agents, moisturizing and energizing agents, self-tanning agents, soothing agents, and agents that improve elasticity and skin barrier, as well as carriers and / or excipients or diluents commonly used in compositions.
[0101] If not otherwise stated, the excipients, additives, diluents, etc. mentioned below are suitable for the compositions according to the invention. A person skilled in the art can easily determine the necessary amounts of cosmetic and dermatological auxiliaries and additives depending on the desired product.
[0102] The additional ingredients may be added to the oil phase, the water phase or separately, as appropriate. The manner of addition may be easily adjusted by those skilled in the art.
[0103] Examples of cosmetic excipients, diluents, adjuvants, additives and active ingredients commonly used in the skin care industry that are suitable for use in the cosmetic composition of the present invention are described, for example, in the International Cosmetic Ingredient Dictionary & Handbook of the Personal Care Product Council, but are not limited thereto.
[0104] In some cases, the cosmetic active ingredients useful herein may provide more than one benefit, or operate via more than one mode of action.
[0105] Of course, the person skilled in the art will carefully choose the abovementioned optional additional ingredients, adjuvants, diluents and additives and / or their amounts so that the advantageous properties inherently associated with the combination according to the invention are not or not substantially adversely affected by the envisaged additions.
[0106] In all embodiments of the present invention, preferred compositions are emulsions containing an oil phase and an aqueous phase, such as in particular O / W, W / O, Si / W, W / Si, O / W / O, W / O / W multiple emulsions or pickering emulsions. The amount of oil phase (i.e. the phase comprising all oils and fats) present in such emulsions is preferably at least 10 wt.-%, such as in the range of 10 to 60 wt.-%, preferably in the range of 15 to 50 wt.-%, most preferably in the range of 15 to 45 wt.-%, based on the total weight of the composition.
[0107] According to an even more preferred embodiment, the composition according to the invention as described 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 O / W emulsions is well known to those skilled in the art and is illustrated in the examples.
[0108] In an advantageous embodiment, the O / W emulsifier is a phosphate emulsifier. Preferred phosphate emulsifiers are C8-10 alkyl ethyl 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, DEA-ceteareth-2 phosphate, DEA-ceteeth phosphate, DEA-oleth-3 phosphate, potassium cetyl phosphate, decereth-4 phosphate, decereth-6 phosphate and trilaureth-4 phosphate. In all embodiments of the present invention, particularly preferred phosphate emulsifiers are C8-C25 alkyl phosphates, such as in particular C20-22 alkyl phosphates and cetyl phosphate, in particular the potassium salts thereof. A particularly preferred phosphate emulsifier according to the present invention is potassium cetyl phosphate, for example available from DSM Nutritional Products Ltd Kaiseraugst as K is commercially available.
[0109] According to the present invention, other suitable O / W emulsifiers include PEG 30 dipolyhydroxystearate, PEG-4 dilaurate, PEG-8 dioleate, PEG-40 sorbitan full oleate, PEG-7 glyceryl cocoate, PEG-20 almond glycerides, PEG-25 hydrogenated castor oil, glyceryl stearate (and) PEG-100 stearate, PEG-7 olive oil, PEG-8 oleate, PEG-8 laurate, PEG-60 almond glycerides, PEG-20 methyl glucose sesquistearate, PEG-40 stearate, PEG-100 stearate, PEG-80 sorbitan laurate, stearic acid. Alcohol Polyeth-2, Steareth-12, Oleth-2, Ceteth-2, Laureth-4, Oleth-10, Oleth-10 / Polyoxyethylene 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), Stearic Acid, Stearate, Polyglyceryl-3-Methylglucose Distearate. Other suitable emulsifiers include sorbitan oleate, sorbitan sesquioleate, sorbitan isostearate, sorbitan trioleate, lauryl glucoside, decyl glucoside, sodium stearoyl glutamate, sucrose polystearate, and hydrated polyisobutylene. In addition, one or more synthetic polymers may be used as emulsifiers. For example, PVP eicosene copolymer, acrylates / C10-30 alkyl acrylate crosspolymer, acrylates / steareth-20 methacrylate copolymer, PEG-22 / dodecyl glycol copolymer, PEG-45 / dodecyl glycol copolymer, and mixtures thereof.
[0110] Another particularly suitable class of O / W emulsifiers are the nonionic self-emulsifying systems derived from olive oil, such as those known as (INCI name) cetearyl olivate and sorbitan olivate (chemical composition: sorbitan esters and cetearyl esters of olive oil fatty acids), sold under the trade name OLIVEM 1000.
[0111] Also suitable are commercially available polymeric emulsifiers, such as hydrophobically modified polyacrylic acids, such as acrylates / C10-30 alkyl acrylate crosspolymers, which are available from Lubrizol under the trade name TR-1 and TR-2 are commercially available.
[0112] Another particularly suitable class of emulsifiers are polyglycerol esters or diesters of fatty acids, also known as polyglycerol esters / diesters (i.e. polymers in which fatty acids are bound by esterification with polyglycerol), available, for example, from Evonik as Isolan GPS [INCI name Polyglyceryl-4 diisostearate / polyhydroxystearate / sebacate (i.e. a mixture of isostearic acid, polyhydroxystearic acid and sebacic acid with a diester of polyglyceryl-4)] or from BASF as Dehymuls PGPH (INCI Polyglyceryl-2 dipolyhydroxystearate).
[0113] Additionally suitable are polyalkylene glycol ethers, for example Brij 72 (polyoxyethylene (2) stearyl ether) or Brij 721 (polyoxyethylene (21) stearyl ether), obtainable, for example, from Croda.
[0114] Particularly advantageous O / W emulsifiers according to the invention are one or more of the following: Polyglyceryl-3 Methylglucose Distearate, Lauryl Glucoside (and) Polyglyceryl-2 Dipolyhydroxystearate, Glyceryl Stearate Citrate, Sodium Cetearyl Sulfate, Cetearyl Glucoside; Polyglyceryl-6 Stearate (and) Polyglyceryl-6 Behenate, Cetearyl Olivate (and) Sorbitan Olivate, Arachidyl (and) Behenyl Alcohol (and) Arachidyl Glucoside, Cetearyl Alcohol (and) Coco-Glucoside, Coco-Glucoside (and) Coconut Alcohol, 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 INCI name).
[0115] In one embodiment, it is particularly preferred according to the invention if the composition comprises C8-C25 alkyl phosphate, preferably C20-22 alkyl phosphate and / or cetyl phosphate, most preferably cetyl phosphate (such as in particular potassium cetyl phosphate) as emulsifier or at least as co-emulsifier.
[0116] In another embodiment, it is particularly preferred according to the invention if the composition comprises polyglyceryl-6 stearate and / or polyglyceryl-6 behenate as emulsifier, preferably in the presence of cetyl phosphate, more preferably potassium cetyl phosphate, as co-emulsifier.
[0117] The at least one O / W or Si / W emulsifier is preferably used in an amount of 0.5 to 10 wt.-%, such as in particular in the range of 0.5 to 5 wt.-%, such as most in particular in the range of 0.5 to 4 wt.-% or in the range of 0.5 to 3 wt.-%, based on the total weight of the composition.
[0118] If a phosphate emulsifier with all the definitions and preferences given herein is used as a co-emulsifier, its amount is preferably taken in the range of 0.1 to 1 wt.%, such as in particular in the range of 0.25 to 0.75 wt.%, such as most in particular in the range of 0.3 to 0.7 wt.% or in the range of 0.4 to 0.6 wt.%, based on the total weight of the composition.
[0119] According to the invention, suitable W / O- or W / Si-emulsifiers are polyglyceryl-2-dipolyhydroxystearate, PEG-30 dipolyhydroxystearate, cetyl dimethicone copolyol, polyglyceryl-3 diisostearate polyglyceryl esters of oleic / isostearate, polyglyceryl-6 hexaricinoleate, polyglyceryl-4-oleate, oleate / PEG-8 propylene glycol cocoate, magnesium stearate, sodium stearate, potassium laurate, potassium ricinoleate, sodium cocoate, sodium tallowate, potassium ricinoleate, sodium oleate and mixtures thereof. Other suitable 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. The at least one W / O emulsifier is preferably used in an amount of about 0.001 to 10 wt.-%, more preferably 0.2 to 7 wt.-%, relative to the total weight of the composition.
[0120] Furthermore, the composition according to the invention advantageously comprises at least one co-surfactant, for example mono- and di-glycerides and / or fatty alcohols. Co-surfactants are generally used in an amount taken in the range of 0.1 to 10 wt.-%, such as in particular in the range of 0.5 to 7 wt.-%, such as most in particular in the range of 1 to 5 wt.-%, based on the total weight of the composition. Particularly suitable co-surfactants are selected from the following list: alkyl alcohols, for example 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 coconut oil glycerides (Lipocire Na10) and mixtures thereof.
[0121] In all embodiments of the invention, it is particularly advantageous if the composition also comprises cetearyl alcohol and / or glyceryl stearate.
[0122] Advantageous embodiments of the composition of the invention also include those embodiments in which the composition comprises one or more oils selected from the group consisting of butylene glycol dicaprylate / dicaprate, phenethyl benzoate, C 12 -C 15Alkyl benzoate, dibutyl adipate, diisopropyl sebacate, dicaprylyl carbonate, di-C 12-13 Alkyl tartaric acid ester, diethylhexyl syringylidenemalonate, hydrogenated castor oil dimer, triheptyl, C 12-13 Alkyl lactate, C 16-17 alkyl benzoate, propylheptyl caprylate, caprylic / capric triglyceride, diethylhexyl 2,6-naphthalene dicarboxylate, octyldodecanol, ethylhexyl cocoate and phenethyl alcohol. Preferably, the composition according to the invention comprises the oils: dibutyl adipate, phenethyl benzoate, butylene glycol, phenethyl benzoate, phenethyl alcohol, C 12 -C 15 Alkyl benzoates, diisopropyl sebacate and mixtures thereof.
[0123] In a further advantageous aspect of the invention, the composition of the invention further comprises a preservative and / or a preservative enhancer, preferably selected from ethanol, phenoxyethanol, sodium benzoate, potassium sorbate, phenylethyl alcohol, hydroxyacetophenone, ethylhexylglycerol, hexylglycerol, glyceryl caprylate, 1,3-propylene glycol, 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol (octanediol), 1,2-decanediol and 2-methyl-1,3-propanediol and mixtures thereof, most preferably selected from phenoxyethanol and ethylhexylglycerol and mixtures thereof. When present, the preservative or preservative enhancer is preferably used in an amount of 0.01 to 5 wt.-%, more preferably in an amount of 0.05 to 4 wt.-%, most preferably in an amount of 0.1 to 3.0 wt.-%, respectively, based on the total weight of the composition.
[0124] According to the invention, it is advantageous if the formulation comprises one or more alkanediols selected from 1,3-propylene glycol, 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, 1,2-decanediol and 2-methyl-1,3-propanediol. When present, the one or more alkanediols are preferably used in an amount of 0.1 to 7 wt.%, more preferably in an amount of 0.5 to 7 wt.%, most preferably in an amount of 1.0 to 5.0 wt.%, based on the total weight of the composition.
[0125] According to the present invention, it is more advantageous if the emulsion composition of the present invention comprises phenoxyethanol, ethylhexylglycerin, caprylic acid glyceride and / or phenethyl alcohol, preferably comprises phenoxyethanol and / or ethylhexylglycerin or caprylic acid glyceride and / or phenethyl alcohol, most preferably phenoxyethanol and ethylhexylglycerin or caprylic acid glyceride and phenethyl alcohol.
[0126] In another advantageous aspect, the composition according to the invention does not contain any parabens, benzethonium chloride, piroctone olamine, lauroylarginat, methylisothiazolinone, chloromethylisothiazolinone, bronopol, benzalkonium chloride, formaldehyde-releasing compounds, salicylic acid, triclosan, DMDM hydantoin, chlorphenesin and IPBC (iodopropynyl butylcarbamate).
[0127] The composition according to the invention may also comprise one or more emollients for soothing and softening the skin. As examples, the emollients may be silicones (dimethicone, cyclomethicone), vegetable oils (grapeseed oil, sesame seed oil, jojoba oil, etc.), fats (cocoa butter, shea butter) and petroleum derivatives (petroleum jelly, mineral oil).
[0128] On the other hand, the composition of the present invention may include one or more fragrances selected from the following: limonene, citral, linalool, α-isomethyl ionone, geraniol, citronellol, 2-isobutyl-4-hydroxy-4-methyltetrahydropyran, 2-tert-amylcyclohexyl acetate, 3-methyl-5-phenyl-1-pentanol, 7-acetyl-1,1,3,4,4,6-hexamethyltetralin, diester of adipate, cinnamaldehyde, amyl salicylate, α-Amyl Cinnamal, α-Methyl Ionone, Butylphenyl Methylpropional, Cinnamaldehyde, Amyl Cinnamyl Alcohol, Anise Alcohol, Benzoin, Benzyl Alcohol, Benzyl Benzoate, Benzyl Cinnamate, Benzyl Salicylate, Bergamot Oil, Bitter Orange Oil, Butylphenyl Methylpropional, Cardamom Oil, Cedrol, Cinnamaldehyde, Cinnamyl Alcohol, Citronellol Methyl Crotonate, Citrus Oil, Coumarin, Diethyl Succinate, Ethyl Linalool, Eugenol, Oakmoss Lichen (Evernia furfuracea extract, Evernia prunastri extract, farnesol, guaiac wood oil, hexyl cinnamaldehyde, hexyl salicylate, hydroxycitronellal, lavender oil, lemon oil, linalyl acetate, mandarin oil, menthyl PCA, methylhexadecan, nutmeg oil, rosemary oil, sweet orange oil, pineneol, tonka bean oil, triethyl citrate, vanillin.
[0129] The composition of the invention may advantageously include a humectant. A humectant is a compound or mixture of compounds which imparts to the cosmetic composition the quality of reducing stratum corneum water loss, also known as transepidermal water loss (TEWL), and / or positively influencing stratum corneum hydration after application or distribution on the skin surface.
[0130] Non-limiting examples of advantageous humectants for use in the present invention include glycerol, lactic acid and / or lactates (especially sodium lactate), butylene glycol, propylene glycol, 1,3-propanediol, biosaccharide gum-1, Glycine soya, ethylhexylglycerol, pyrrolidone carboxylic acid and urea. It is further advantageous to use, in particular, a polymer humectant selected from polysaccharides that are water-soluble and / or swellable in water and / or can be gelled with the aid of water. For example, hyaluronic acid, chitosan and / or a polysaccharide rich in fucose, which is registered in Chemical Abstracts under registration number 178463-23-5, can be obtained, for example, from the company SOLABIA SA under the trade name HYDROGEN®. 1000. Moisturizers can also be used advantageously as active anti-wrinkle ingredients to protect the skin from changes such as those that occur with skin aging.
[0131] Particularly advantageous humectants in the composition according to the invention are glycerol, sodium hyaluronate, saccharide isomers and / or 1,3-propylene glycol, more preferably in a total amount in the range of 0.1 to 5 wt.-%, more preferably in the range of 0.1 to 3 wt.-%, even more preferably in the range of 0.5 to 3 wt.-%, based on the total weight of the composition.
[0132] The cosmetic composition according to the invention may also advantageously (but not necessarily) comprise fillers, which have the effect, for example, of further improving the sensory and cosmetic properties of the preparation and, for example, of causing or enhancing a velvety or silky skin feel. Advantageous fillers in the sense of the invention are starch and starch derivatives (e.g. tapioca starch, distarch phosphate, sodium starch octenylsuccinate or aluminum starch octenylsuccinate, etc.), Valvance pigments which do not have a major UV filtering effect and do not have a coloring effect (e.g. Valvance Touch 210 or 250) and / or (CAS No. 7631-86-9) and / or talc and / or polyethylene, nylon and silica dimethyl silylate.
[0133] The aqueous phase of the composition according to the invention can advantageously comprise customary cosmetic adjuvants, for example alcohols, in particular low-C alcohols, preferably ethanol and / or isopropanol, or low-C polyols, and their ethers, preferably propylene glycol, glycerol, electrolytes, self-tanning agents, and in particular one or more thickeners, which can advantageously be chosen from silicon dioxide, aluminum silicates, polysaccharides and / or derivatives thereof, for example hyaluronic acid, xanthan gum, hydroxypropyl methylcellulose, particularly advantageously from polyacrylates, preferably from the so-called Carbopols, examples being Carbomers of the 980, 981, 1382, 2984 and 5984 types, in each case alone or in combination. Other advantageous thickeners according to the invention are those with the INCI name Acrylates / C10-30 Alkyl Acrylate Crosspolymer (e.g. Pemulen TR 1, Pemulen TR2, Carbopol 1328 from Lubrizol), and also Aristoflex AVC (INCI: Ammonium Acryloyldimethyltaurate / VP Copolymer) and Simugel NS (INCI: Hydroxyethyl Acrylate / Sodium Acryloyldimethyltaurate Copolymer & Squalane & Polysorbate 60).
[0134] According to the present invention, it is further preferred if the composition comprises a thickener. Suitable thickeners for use according to the present invention include xanthan gum, crosslinked acrylates / C10-C30 alkyl acrylate polymers, hydroxyethyl acrylate / sodium acryloyldimethyl taurate copolymers and / or vinyl pyrrolidone / hexadecane copolymers, preferably xanthan gum and / or hydroxyethyl acrylate / sodium acryloyldimethyl taurate, most preferably xanthan gum.
[0135] If xanthan gum is present, its amount is preferably in the range of 0.1 to 1 wt.-%, more preferably in the range of 0.15 to 0.75 wt.-%, most preferably in the range of 0.2 to 0.4 wt.-%, based on the total weight of the composition.
[0136] The oil phase of the composition of the present invention may also advantageously include conventional cosmetic adjuvants, such as oil phase thickeners, for example dextrin palmitate (Rheopearl KL2, Chiba Flour Milling), dextrin palmitate and C15-19 alkane (TILAMAR Fits, DSM), polyurethane-79 and caprylic / capric triglyceride (Oilkemia 5S, Lubrizol), ethylene / propylene / styrene copolymer and butylene / ethylene / styrene copolymer and pentaerythritol tetra-di-tert-butyl hydroxyhydrocinnamate and squalane (Veggi Gel, Aiglon), dibutyl lauroyl glutamine and dibutyl ethylhexanoyl glutamine and octyldodecanol (AJK-OD246, Ajinomoto).
[0137] If present, a thickener (eg a reactive thickening polymer) is preferably present in an amount in the range of 0.1 to 15 wt.-%, more preferably in the range of 0.5 to 10 wt.-%, most preferably in the range of 1.0 to 8.0 wt.-%, based on the total weight of the composition.
[0138] The total amount of UV filters contained in the compositions according to the invention is surprisingly low.
[0139] In another aspect, the composition has an SPF of at least 15, preferably at least 20, most preferably at least 30.
[0140] According to the invention, it is advantageous if the composition according to the invention comprises a film former. Film formers in the sense of the invention are substances of various compositions, characterized by the following properties: when the film former is dissolved in water or another suitable solvent and the solution is then applied to the skin, the film former forms a film after evaporation of the solvent, which film essentially serves to fix the UV filter on the skin, thereby increasing the water resistance of the product.
[0141] It is particularly advantageous if the film former is selected from polymers based on polyvinylpyrrolidone (PVP).
[0142] Particularly preferred are vinylpyrrolidone copolymers such as PVP hexadecane copolymer and PVP eicosene copolymer, which are available from Ashland under the trade names Antaron V216 and Antaron V220.
[0143] Also advantageous are other polymeric film formers, such as sodium polystyrene sulfonate, which is available under the trade name Flexan 130 from National Starch and Chemical Corp., and / or polyisobutylene, which is available under the trade name Rewopal PIB 1000 from Rewo. Examples of other suitable polymers are polyacrylamide (Sepigel 305), polyvinyl alcohol, PVP, PVP / VA copolymers, polyethylene glycol, acrylate / octylacrylamide copolymers (Dermacryl 79). Also advantageous is the use of hydrogenated castor oil dimer linoleate (CAS 646054-62-8, INCI hydrogenated castor oil dimer linoleate), which is available under the name Risocast DA-H from Kokyu Alcohol Kogyo, or PPG-3 benzyl ether myristate (CAS 403517-45-3), which is available under the trade name Crodamol STS from Croda Chemicals.
[0144] The composition according to the present invention typically has a pH in the range of 3 to 10, preferably in the range of 4 to 8, most preferably in the range of 4 to 7.5. The pH can be readily adjusted as required with a suitable acid (e.g. citric acid) or base (e.g. NaOH) or a suitable amine (e.g. tromethamine) according to standard methods in the art.
[0145] The amount of the cosmetic composition applied to the skin is not critical and can be easily adjusted by a person skilled in the art. The amount is preferably in the range of 0.1 to 3 mg / cm 2 In the skin range, for example, preferably 0.1 to 2 mg / cm 2 Within the skin, most preferably 0.5 to 2 mg / cm 2 Within the skin range.
[0146] The following examples are provided to further illustrate the compositions and effects of the present invention. These examples are merely illustrative and are not intended to limit the scope of the present invention in any way.
[0147] Example
[0148] Brief Description
[0149] The neutral core human milk oligosaccharides LNT and LNnT were evaluated for their SPF enhancing effect. To this end, various sunscreen products were prepared according to standard methods in the art as listed in Tables 1a, 2a and 3a.
[0150] In vitro SPF measurement
[0151] In vitro SPF tests were carried out on PMMA plates (HD6 plates from Helioscreen, 5 cm x 5 cm, Sa roughness = 6 μm): 32.5 mg of the corresponding formulation (i.e. 1.3 mg / cm 2 ) was evenly applied to the PMMA plate and allowed to dry for 15 minutes.
[0152] In vitro SPF was determined using a Labsphere 2000 UV Transmittance Analyzer: Each PMMA plate was measured 9 times at different points on the plate, resulting in 27 data points. The result was calculated as the average of these 27 data points.
[0153] Table 1a: Formulation 1
[0154]
[0155] Table 1b: Results
[0156] HMO HMO concentration External SPF SPF Enhancement Reference - 64.1 - Sialyl lactose (3-SL) (reference) 1% 75.9 +18% Lacto-N-neotetraose (LNnT) 1% 85.7 +34%
[0157] Table 2a: Formulation 2
[0158]
[0159] Table 2b: Results
[0160]
[0161] Table 3a: Formulation 3
[0162]
[0163] Table 3b: Results
[0164]
[0165] As shown in Tables 1b, 2b and 3b, neutral core human milk oligosaccharides composed of galactose, N-acetylglucosamine and glucose monosaccharides enhanced in vitro SPF by 34% to 194%.
Claims
1. A composition comprising at least one sunscreen active agent which 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 monosaccharides.
2. The composition according to claim 1, wherein the at least one sunscreen active agent has a lambda maximum selected in the range of 280 to 400 nm.
3. The composition according to claim 1 and / or 2, wherein the human milk oligosaccharide is selected from trisaccharides, tetrasaccharides, hexasaccharides, octasaccharides or decasaccharides, preferably selected from trisaccharides, tetrasaccharides and hexasaccharides, most preferably tetrasaccharides.
4. The composition according to any one or more of the preceding claims, wherein the galactose, N-acetylglucosamine and glucose monosaccharides are linked to each other via β-(1-3) or β-(1-4) bonds.
5. A composition according to any one or more of the preceding claims, wherein the human milk oligosaccharide is selected from lacto-N-triose II, lacto-N-tetraose, lacto-N-neotetraose, lacto-N-hexaose, lacto-N-neohexose, p-lacto-N-hexaose and p-lacto-N-neohexose and mixtures thereof, preferably selected from 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 or more of the preceding claims, wherein the at least one neutral core human milk oligosaccharide is present in an amount effective to increase the SPF of the composition.
7. The composition according to any one or more of the preceding claims, wherein the amount of neutral core human milk oligosaccharide in the composition is at least 0.2 wt.-%, preferably at least 0.3 wt.-%, most preferably at least 0.5 wt.-%, based on the total weight of the composition.
8. Composition according to any one or more of the preceding claims, wherein the at least one sunscreen active agent is an organic sunscreen active agent (organic UV-filter), preferably selected from homosalate, ethylhexyl salicylate, polysilicone-15, ethylhexyl methoxycinnamate, octocrylene, phenylbenzimidazole sulfonic acid or its salts, bis-ethylhexyloxyphenol methoxyphenyl triazine, ethylhexyl triazone, diethylhexyl butamido triazone, methylene bisbenzotriazolyl tetramethylbutylphenol, tris-biphenyl triazine, butyl methoxydibenzoylmethane, diethylaminohydroxybenzoyl hexyl benzoate, or an inorganic UV-filter (inorganic sunscreen active agent (inorganic UV-filter), preferably selected from titanium dioxide or zinc oxide and any mixtures thereof.
9. Composition according to any one or more of the preceding claims, wherein the total amount of sunscreen actives in the composition is taken in the range from 1 to 50 wt.-%, preferably 3 to 40 wt.-%, most preferably 5 to 30 wt.-%, based on the total weight of the composition.
10. Composition according to any one or more of the preceding claims, wherein the composition comprises a carrier consisting of at least 30 wt.% water, more preferably at least 40 wt.-% water, most preferably at least 45 wt.-% water, such as in particular 50 to 90 wt.-% water.
11. The composition according to any one or more of the preceding claims, wherein the composition is an emulsion.
12. The composition according to claim 11, wherein the composition is an O / W emulsion comprising an oil phase dispersed in an aqueous phase.
13. Use of a composition according to any one of claims 1 to 12 for protecting the skin from the effects of skin ageing, such as wrinkles, and as a sunscreen composition.
14. A method of preparing a composition comprising adding to the composition during the preparation of the composition at least one sunscreen active and at least one neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine and glucose monosaccharides.
15. Use of at least one neutral core human milk oligosaccharide composed of galactose, N-acetylglucosamine and glucose monosaccharides for increasing the SPF of a composition comprising at least one sunscreen active.
Citation Information
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