Photoprotective composition for protecting the skin from visible light
Patent Information
- Application Number
- EP2023715126
- Authority / Receiving Office
- EP · EP
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2022-03-30
- Filing Date
- 2023-03-28
- Publication Date
- 2025-02-05
AI Technical Summary
Conventional light protection preparations primarily focus on shielding the skin from UV and IR radiation but fail to adequately address the damaging effects of visible light, which can cause hyperpigmentation and premature skin aging.
A light protection composition combining a UV filter with composite particles made of mica coated with metal oxides, antioxidants like carnosine, and glass, which scatters, absorbs, and reflects visible light, thereby protecting the skin from the harmful effects of UV, IR, and visible radiation.
The composition effectively reduces melanin formation and hyperpigmentation, and counteracts the activation of matrix metalloproteinases responsible for collagen breakdown, providing comprehensive protection against the negative consequences of visible light exposure.
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Abstract
Description
[0001] STADA ARZNEIMITTEL AG Hamburg, March 28, 2023
[0002] Our reference: S 3496 / SG
[0003] STADA Pharmaceuticals AG
[0004] Stadastraße 2-18, 61118 Bad Vilbel, Germany
[0005] Sunscreen composition to protect the skin from visible light
[0006] The present invention relates to a sunscreen composition for protecting the skin from UV radiation and visible light, which contains, in addition to at least one UV filter, a combination of at least one composite particle, at least one antioxidant and at least one glass.
[0007] The damaging effects of the ultraviolet portion of solar radiation (280 nm–400 nm) on the skin have long been known. Numerous chemical and physical filter substances have been developed to protect the skin from both UVA and UVB radiation. These filters, when applied to the skin in the form of pharmaceutical or cosmetic compositions, reduce the effects of UVA and UVB rays. UV radiation accounts for approximately 5% of sunlight. UVB radiation primarily causes sunburn and DNA damage and penetrates the basal layer of the skin. UVA radiation primarily causes DNA oxidation and immunosuppression and penetrates the dermis.
[0008] The damaging effects of the infrared portion of sunlight (760 nm–1400 nm) on the skin are also well known. The IR component accounts for approximately 45% of sunlight and penetrates deep into the skin—down to the hypodermis. Infrared light activates the production of matrix metalloproteinase-1 (MMP-1), a collagenase, in the fibroblasts of human skin. This leads to collagen degradation via the activation of the MAPK signaling pathway, thus contributing to premature skin aging.
[0009] Recent studies have shown that visible light (400 nm–760 nm) can also have a damaging effect on the skin. Visible light is not only an essential component of sunlight and essential for life on Earth, but also part of artificial light. It comprises approximately 50% of the total solar spectrum and penetrates deep into the skin. About 20% reaches the hypodermis.
[0010] Dupont et al. describe sunlight-induced skin damage in the International Journal of Cosmetic Science, 1-9, 2013. Visible light can produce inflammatory cytokines such as IL-1, IL-6, IL-8, and matrix-degrading enzymes such as MMP-1 and MMP-9 (in vitro), free radicals (in vivo), the formation of oxidized DNA bases, and pigmentation in individuals with darker skin.
[0011] Visible light can trigger what is known as hyperpigmentation in the skin.
[0012] For example, Duteil et al., in Pigment Cell Melanoma Res. 27, 822-826, 2014, describes the influence of visible light, especially from the higher-energy range, on the skin and observes dose-dependent hyperpigmentation that lasts for 3 months.
[0013] Furthermore, as is already known for UVA and IR radiation, visible light can also lead to premature skin aging by activating matrix metalloproteinases, particularly MMP-1. EP 1 591 105 demonstrated that IR radiation upregulates MMP-1 and thus leads to premature skin aging. Antioxidants were proposed as a solution that intervene in the MMP-1 upregulation process. Zastrow et al. published in Skin Pharmacol. Physiol. 22, 31-44, 2009, the free radicals (mainly ROS: reactive oxygen species) produced by UV and visible light, determined using electron paramagnetic resonance spectroscopy. Accordingly, 50% of the total oxidative skin load is caused by visible light.
[0014] The effects of UV radiation on the skin can be reduced by applying UV filters to the skin. Sunscreen compositions containing UV filters are applied to the skin.
[0015] There was therefore a need for sunscreen preparations that not only protect the skin from damage caused by UV and IR radiation, but also from visible light and its negative effects on the skin.
[0016] The object of the present invention is therefore to improve conventional sunscreen preparations which contain at least one UV filter and to provide a way of protecting the skin from the effects of visible light.
[0017] It has surprisingly been found that sunscreen compositions comprising at least one UV filter and a combination of at least one composite particle, at least one antioxidant, and at least one glass protect the skin from UV radiation, IR radiation, and visible light, or their negative effects. The composite particle according to the invention contains a substrate core made of natural mica, synthetic mica (INCI: Synthetic Fluorphlogopite), bismuth oxychloride, silicon dioxide, aluminum oxide, aluminum borosilicate, glass, boron nitride, or mixtures thereof, to which at least one metal oxide layer is applied.
[0018] The substrate core preferably comprises mica, selected from natural mica (mica), synthetic mica (INCI: Synthetic Fluorphlogopite), and a mixture thereof. In a particularly preferred embodiment, it comprises natural mica.
[0019] In another particularly preferred embodiment of the invention, the substrate core consists of natural mica, synthetic mica, or a mixture thereof. In a very particularly preferred embodiment of the invention, the substrate core consists of natural mica.
[0020] If the composition contains more than one composite particle, these have different substrate cores and / or different coatings
[0021] In a preferred embodiment of the invention, the substrate core is in the form of a thin platelet.
[0022] In a further preferred embodiment of the invention, the substrate core is in the form of a semitransparent or transparent thin platelet. The composite particle according to the invention comprises
[0023] - a substrate core
[0024] - a first coating on the substrate core made of a first metal oxide - optionally further layers on the first coating made of further metal oxides, in particular a second layer made of a second metal oxide.
[0025] In a preferred embodiment of the invention, the composite particle comprises
[0026] - a substrate core made of mica
[0027] - a first coating on the substrate core made of a first metal oxide
[0028] - optionally further layers on the first coating of further metal oxides, in particular a second layer of a second metal oxide.
[0029] Advantageous first, second, and further metal oxides are, for example, titanium(IV) oxide, iron oxide, aluminum oxide, silicon dioxide, zirconium oxide, cobalt oxide, tin(II) oxide, tin(IV) oxide, nickel oxide, and mixtures of these oxides. Titanium(IV) oxide and tin(IV) oxide are preferred. The metal oxides of the adjacent layers are preferably different from one another. Layers of identical metal oxides may be arranged alternately. In a preferred embodiment of the invention with two metal oxide layers, one is made of tin(IV) oxide and the other of titanium(IV) oxide.
[0030] In a preferred embodiment of the invention, the composite particle is composed of mica, titanium dioxide, and tin oxide, wherein the mica substrate core is surrounded by layers of titanium dioxide (INCI nomenclature for titanium(IV) oxide) and tin oxide (INCI nomenclature for tin(IV) oxide). Alternating layers of titanium dioxide and tin oxide are preferably present. The titanium dioxide can be present in various modifications, e.g., in the anatase modification or the rutile modification. To provide titanium dioxide layers in rutile form, the mica substrate core is first pre-coated with a thin layer of tin(IV) oxide, onto which titanium(IV) oxide is then applied, which is in rutile form after subsequent annealing. In a preferred embodiment, the mica substrate core is therefore coated with a layer of tin(IV) oxide, on which a layer of titanium dioxide, preferably in rutile form, is located.
[0031] The preferred composite particle has the INCI name “Titanium Dioxide (and) Mica (and) Tin Oxide”.
[0032] The composite particle in the sense of the invention preferably consists exclusively of inorganic materials, i.e. is preferably an inorganic composite particle,
[0033] According to a preferred embodiment, the composite particle comprises, in addition to the substrate core, which preferably consists of mica, exclusively one or more metal oxide layers, so that the composite particle according to this embodiment is free of coatings made of non-metal oxides, in particular free of coatings made of stearoyl glutamate, disodium stearoylglutamate, silicones, dimethicone, methicone, s imethicone, stearic acid, cetyl phosphate, polysaccharides, polyacrylates, polyethers, and polyethersilanes.
[0034] According to a preferred embodiment of the invention, the effect of the composite particle is based on light scattering, absorption, reflection, and / or interference of light by the thin, highly refractive metal oxide layers. By varying layer thicknesses, for example, the path length difference between the radiation component reflected by an outer metal oxide layer and the radiation component initially transmitted into the outer layer, which is then reflected by the substrate surface or the metal oxide surface of the inner layer, can be varied.
[0035] The composite particle, particularly the preferred one made of mica, titanium dioxide, and tin oxide, reflects visible light. The composite particle is commercially available, for example, from BASF under the names Cellini, Cloisonne, Duochrome, Flamenco, Gemtone, or Timica; from Merck under the names Timiron, Colorona, Xirona, Ronaflair, Ronaflair Balance Red, Ronaflair Balance Gold, Ronaflair Balance Blue, or Ronaflair Balance Green; from Kobo under the names KTZ, Kobopearl Perpetua!, or K-Ray; or from Eckart under the names Syncrystal.
[0036] The composite particle preferably has a particle size determined by laser diffraction of 1 μm to 200 μm, more preferably of 1 μm to 100 μm, and most preferably of less than 15 μm (80% within this range). In one embodiment of the invention, the particle size determined by laser diffraction is 1 to 15 μm.
[0037] The composite particle composed of mica, titanium dioxide, and tin oxide (INCI: Titanium Dioxide (and) Mica (and) Tin Oxide) typically has a particle size determined by laser diffraction of less than 15 μm (80% within this range), preferably between 4 and 10 μm, and a particle size distribution of D50 determined by laser diffraction in the range of 4 to 10 μm, preferably in the range of 6.0 to 8.5 μm.
[0038] The composite particle can be produced by processes familiar to those skilled in the art, such as the comminution and classification of titanium dioxide-coated mica flakes (natural mica), which may be precoated with tin(IV) oxide, the hydrolysis of titanium salt solutions in aqueous mica suspension, where the mica may also be precoated with tin(IV) oxide, or vapor deposition. Exemplary production processes are described in US 4,086,100, US 4,038,099, EP 0271 767, and US 4,867,794. The composite particle is typically used in cosmetic formulations as an effect pigment or as a functional filler.
[0039] Luster or effect pigments are used in many areas of technology, particularly in decorative coatings, paints, varnishes, printing inks, and cosmetic formulations. They typically consist of platelet-shaped substrates coated with thin metal oxide layers. The optical effect of these pigments is based on the directed reflection of light from the predominantly parallel platelets. Interference colors are created by the reflection of light at the interfaces between layers with different refractive indices.
[0040] Functional fillers are used in a range of cosmetic products to adjust important sensory and optical properties. While color pigments, dyes, colorants, and perfumes add body and character to cosmetics, functional filler pigments adjust subtle properties such as viscosity, hardness, flow, volume, skin feel, transparency, and soft-focus effects, which are crucial for the haptic properties of a cosmetic product. Since functional fillers do not generally determine the predominant properties of cosmetics such as color or odor, they are usually odorless, white powders that create a pleasant skin feel. Functional fillers contribute significantly to the optical appearance of cosmetics on the skin through their light-scattering and matting properties.Incident light is reflected by the filler particles to a greater or lesser extent in all directions; this is often referred to as diffuse reflection. High scattering often results in a whitish appearance and the optical concealment of the skin, whereas low scattering leads to high transparency both in the formulation and on the skin. In addition, interference effects, particularly low-gloss interference effects, can also occur, which contribute, for example, to correcting skin tone. The composite particles are present in the sunscreen compositions according to the invention in an amount of 0.01 to 2 wt. %, preferably 0.05 to 1.5 wt. %, and particularly preferably 0.1 to 1 wt. %.
[0041] According to the invention, the composite particles are preferably contained in a concentration such that they are barely or not at all visually perceptible to the observer.
[0042] The sunscreen preparations according to the invention are preferably not make-up products (decorative cosmetics).
[0043] The antioxidant used according to the invention is preferably selected from the group consisting of: amino acids (e.g. glycine, histidine, tyrosine, tryptophan) and their derivatives, imidazoles (e.g. urocanic acid) and their derivatives, peptides such as D, L-camosine, D-camosine, L-camosine and their derivatives (e.g. anserine), suitable phenylpropane bodies, in particular caffeic acid and its derivatives, e.g. esters of caffeic acid, carotenoids (e.g. lycopene, lutein), carotenes (e.g. α-carotene, β-carotene) and their derivatives, lipoic acid and its derivatives (e.g. dihydrolipoic acid), aurothioglucose, propylthiouracil and other thiols (e.g.Thioredoxin, glutathione, cysteine, cystine, cystamine and their glycosyl, N-acetyl, methyl, ethyl, propyl, amyl, butyl and lauryl, palmitoyl, oleyl, γ-lionyl, cholesteryl and glyceryl esters) and their salts, dilauryl thiodipropionate, distearyl thiodipropionate, thiodipropionic acid and their derivatives (esters, ethers, peptides, lipids, nucleotides, nucleosides and their salts) and sulfoximine compounds (e.g. buthionine sulfoximines, homocysteine sulfoximine, buthionine sulfine, penta-, hexa-, heptathionine sulfoximine) in very low tolerated doses (e.g. μmol to μmol / kg), furthermore (metal) chelators (e.g. a-hydroxy fatty acids, palmitic acid, phytic acid, lactoferrin), a-hydroxy acids (e.g. citric acid, lactic acid, malic acid), humic acid, bile acid, bile extracts, bilirubin, biliverdin, EDTA, EGTA and their derivatives, unsaturated fatty acids and their derivatives (e.g. γ-linolenic acid, linoleic acid, oleic acid), folic acid and its derivatives, alanine diacetic acid, flavonoids (e.g.Rutin and its derivatives, e.g. troxerutin), polyphenols, catechins, ubiquinone and ubiquinol and their derivatives, vitamin C and its derivatives (e.g. ascorbyl palmitate, Mg ascorbyl phosphate, ascorbyl acetate), tocopherols and their derivatives (e.g. vitamin E acetate), as well as coniferyl benzoate of benzoin resin, rutinic acid and its derivatives, ferulic acid and its derivatives, butylhydroxytoluene, butylhydroxyanisole, nordihydroguaiatric acid, nordihydroguaiatric acid.
[0044] Trihydroxybutyrophenone, uric acid and its derivatives, mannose and its derivatives, zinc and its derivatives (e.g. ZnO, ZnSO4), selenium and its derivatives (e.g. selenomethionine), stilbenes and their derivatives (e.g. stilbene oxide, trans-stilbene oxide) and the derivatives (salts, esters, ethers, sugars, nucleotides, nucleosides, peptides and lipids) phytoene, D-biotin, coenzyme Q10, α-glycosylrutin, carnitine, carosin, natural and / or synthetic isoflavonoids, creatine, taurine and / or ß-alanine as well as 8-hexadecene-1,16-dicarboxylic acid as well as Vitis Vinifera (Grape) seed extract, oat extract, Cichorium intubybus (chicory) leaf extract, Leontopodium Alpinum Extract (Edelweiss), Green tea extract, curcumin, silymarin, apigenin, resveratrol, or emblica. They can be used individually or in combination with several antioxidants.
[0045] The antioxidant is present in the sunscreen compositions according to the invention in an amount of 0.001 to 20 wt. o / o, preferably 0.01 to 10 wt.%, particularly preferably 0.01 to 5 wt.% and in particular 0.05 to 2 wt.%.
[0046] In a preferred embodiment, the antioxidant is a peptide, particularly preferably the dipeptide carnosine (ß-alanyl-L-histidine). Carnosine is composed of the amino acids ß-alanine and L-histidine. It occurs naturally in the human body. Carnosine is commercially available, for example, from Symrise under the name Dragosme. Carnosine is present in the sunscreen compositions according to the invention in an amount of 0.001 to 10 wt. preferably 0.01 to 1 wt.%, particularly preferably 0.01 to 0.5 wt.%.
[0047] Different antioxidants can be used simultaneously in the sunscreen preparations according to the invention.
[0048] Glass is an amorphous, non-crystalline solid^ obtained by cooling and solidifying a melt of an inorganic mixture without crystallization. A distinction is made between synthetic and natural glass, with natural glass being preferred according to the invention.
[0049] According to a preferred embodiment, the glass consists predominantly of silicon dioxide.
[0050] The synthetic glass used according to the invention is preferably selected from the group consisting of: E, A, C, ECR glass, borosilicate glass, silicate glass, aluminum silicate glass, window glass, and laboratory glass. The glass used according to the invention is particularly preferably an E, C, ECR glass, or a borosilicate glass.
[0051] A typical composition of these glasses is as follows:
[0052] Table 1: Glasses In a preferred embodiment of the invention, the synthetic glass is used in the form of glass flakes.
[0053] The glass flakes according to the invention are produced from the melt using known processes, such as tube blowing or the spin-molding process. The glass flakes are particularly preferably produced using the spin-molding process, as described, for example, in EP 0 289 240 or WO 2005 / 063637.
[0054] The glass flakes made of synthetic glass used in the light protection composition preferably have a thickness of < 10 μm as determined by electron microscopy and preferably a particle size distribution D50 as determined by laser diffraction of < 500 μm, particularly preferably < 200 μm and very particularly preferably < 100 μm.
[0055] The natural glass used according to the invention is preferably selected from the group consisting of obsidian and perlite.
[0056] Different glasses can be used simultaneously in the light protection devices according to the invention.
[0057] The glass platelets made of synthetic glass are contained in the light protection compositions according to the invention in an amount of 0.01 to 5 wt.%, preferably 0.01 to 2 wt.%, particularly preferably 0.05 to 1.5 wt.% and especially preferably 0.1 to 1 wt.%.
[0058] The glass used according to the invention is particularly preferably a hydrated, natural glass, with periite glass being very particularly preferred.
[0059] Periite is a naturally occurring glass of volcanic origin that forms when lava cools rapidly. It has a water content of 2-6 wt.%. At approximately 900 °C, thermal expansion occurs; the evaporating water causes it to expand, forming swollen particles that can then be used, preferably in crushed form, in light-shielding preparations.
[0060] The periite used according to the invention is preferably an expanded and crushed periite with the INCI name: Perlite.
[0061] The perite used, with the INCI name Perlite, preferably has an average particle size D50 determined by laser diffraction of approximately 15 to 30 μm, preferably approximately 20 to 30 μm, particularly preferably approximately 20 μm. The perlite according to the invention, with the INCI name Perlite, can be produced, for example, as described in WO 02 / 11882.
[0062] Perlite with the INCI name Perlite is commercially available, for example, from the company Imerys under the names ImerCare® 20P, ImerCare® 25P or ImerCare® 30P.
[0063] Perlite (INCI name) is contained in the sunscreen compositions according to the invention in an amount of 0.01 to 2 wt.%, preferably 0.05 to 1.5 wt.%, particularly preferably 0.1 to 1 wt.%.
[0064] The topically administered sunscreen composition according to the invention further comprises at least one UV filter. It can be selected from inorganic and organic UV filters.
[0065] Advantageous inorganic UV filters are metal oxides, in particular oxides of titanium (amorphous or crystalline in the rutile and / or anatase form) or zinc, in the INCI nomenclature Titanium Dioxide or Zinc Oxide. If inorganic pigments are present, they are preferably used in micronized form, preferably in particle sizes smaller than 100 μm. They are preferably present in amounts of 1-25 wt.%, in particular 1-10 wt.%. The inorganic light protection filters can be coated, for example, with silicon dioxide, silicon dioxide hydrate, aluminum oxide, aluminum stearate, stearic acid, trimethoxycaprylylsilane, glycerin, methicone, dimethicone, hydrogen dimethicone, simethicone, polysilicone-15, alkylsilanes or mixtures thereof.
[0066] Such titanium (IV) oxide pigments are commercially available, for example, from Tayca under the trade name MT100T, from BASF under the trade name Uvinul TiO2, from Merck under the trade name Eusolex T-Avo or from DSM Nutritional Products under the trade name PARSOL® TX.
[0067] Zinc oxide pigments are available, for example, from BASF under the trade name Z-Cote HP1 or from Symrise under the trade name Zinc Oxide NDM.
[0068] Organic UV filters used according to the invention are oil-soluble or water-soluble UV-A and / or UV-B filters as well as so-called broadband filters.
[0069] Preferred oil-soluble UV filters are:
[0070] Esters of cinnamic acid, for example according to the INCI nomenclature Ethylhexyl Methoxycinnamate (Neo Heliopan AV, Parsol MCX) or Isoamyl p-Methoxycinnamate (Aeo Heliopan E 1000);
[0071] - Benzophenones, for example according to the INCI nomenclature Benzophenone-3 (Neo Heliopan BB), Benzophenone-4 (Uvinul MS 40) or Diethylamino Hydroxybenzoyl Hexyl Benzoate (Uvinul A Plus);
[0072] - Triazine derivatives, for example, according to the INCI nomenclature, Ethylhexyl Triazone (Uvinul T150), Diethylhexyl Butamido Triazone (Uvasorb HEB); Bis-Ethylhexyloxyphenol Methoxyphenyl Triazine (Tinosorb S); Ethylhexyl Bis-Isopentylbenzoxazolylphenyl Melamine (Uvasorb K2A) and / or Tris-Biphenyl Triazine (Tinosorb A2B);
[0073] - Dibenzoylmethane derivatives, for example according to the INCI nomenclature Butyl Methoxy dibenzoylmethane (Parsol 1789);
[0074] Octocrylene (Neo Heliopan 303); salicylic acid derivatives, for example, according to the INCI nomenclature, homosalate (Neo Heliopan HMS) and / or ethylhexyl salicylate (Neo Heliopan OS),'
[0075] - Benzotriazole derivatives, for example according to the INCI nomenclature Methylene Bis-Benzotriazolyl Tetramethylbutylphenol (Tinosorb M) and / or Drometrizole Trisiloxane (Mexoryl XL);
[0076] Oil-soluble UV filters, if present, are preferably present in amounts of 0.1-15% by weight, preferably 0.5-10% by weight, in particular 0.5-8% by weight or 1-6% by weight, in the compositions to be administered topically.
[0077] Preferred water-soluble UV filters are:
[0078] - salts of 2-phenylbenzimidazole-5-sulfonic acid, for example according to the INCI nomenclature Phenylbenzimidazole Sulfonic Acid (Neo Heliopan Hydro), as well as the sulfonic acid itself;
[0079] Sulfonic acid derivatives of dibenzimidazole, such as according to the INCI nomenclature Disodium Phenyl Dibenzimidazole Tetrasulfonate (Neo Heliopan AP) '
[0080] Camphor and dicamphorsulfonic acid derivatives, such as Benzylidene Camphor Sulfonic Acid (Mexoryl ST) and Terephthalylidene Dicamphor Sulfonic Acid (Mexoryl SX) according to the INCI nomeclature\
[0081] The water-soluble UV filters, if included, are also preferably contained in amounts of 0.1-15 wt.%, preferably 0.5-10 wt.%, in particular 0.5-8 wt.% or 1-6 wt.%, in the compositions to be administered topically.
[0082] In a preferred embodiment of the invention, the topically administered sunscreen compositions according to the invention comprise a
[0083] - Coinposite particles comprising a substrate core of mica (INCI: Mica) surrounded by layers of tin (IV) oxide (INCI: Tin oxide) and titanium (IV) oxide (INCI: Titanium Dioxide),
[0084] - Carnosine and
[0085] - Perlite.
[0086] Most preferably, the composite particle comprising a substrate core of mica surrounded by layers of tin(IV) oxide (INCI: Tin oxide) and titanium(IV) oxide (INCI: Titanium Dioxide) has a particle size determined by laser diffraction of 1 to 15 μm, preferably between 4 to 10 μm, and an average particle diameter D50 determined by laser diffraction in the range of between 4 to 10 μm, preferably in the range of 6.0 to 8.5 μm.
[0087] The sunscreen composition according to the invention can comprise other conventional additives, such as emulsifiers (o / w, w / o), surfactants, film formers, gel formers, thickeners, fats, oils, waxes, active substances / active ingredients, preservatives, solvents, emollients, dyes and / or pigments and additives such as humectants, perfumes, defoamers, bactericides, buffers, salts, chelating agents, lubricants, propellants or the like.
[0088] The topically administered sunscreen composition can be formulated, for example, as an emulsion, such as an oil-in-water emulsion, a water-in-oil emulsion, a silicone-in-water emulsion, a water-in-silicone emulsion, a double emulsion, such as a W1 / 0 / W2 or O1 / W / O2 system, a multiple emulsion, such as a W1 / O1 / W2 / O2 / W3 or O1 / W1 / O2 / W2 system, an aqueous or solvent-based formulation, a tonic, shampoo, or conditioner, and can preferably be provided or applied to the skin in the form of a cream, ointment, paste, lotion, gel, hydrodispersion gel, aerosol, spray, or stick.
[0089] According to the invention, the claimed sunscreen compositions are applied topically to the skin to protect it from the damaging effects of visible light, in particular high-energy visible light with a wavelength of 400 to 500 nm, so-called blue light, such as pigmentation. The applicant has surprisingly found that the use of the sunscreen compositions according to the invention protects the skin from visible-light-induced melanin formation, in particular from hyperpigmentation.
[0090] Hyperpigmentation is caused by a local overproduction of melanin, which leads to the formation of pigment spots. It is a localized hyperactivity of melanocytes, which are normally present in normal numbers. It occurs particularly on areas of the body exposed to sunlight. Topical application of the sunscreen compositions according to the invention protects the skin from overproduction of melanin caused by visible light.
[0091] In addition, exposure to visible light on the skin leads to activation of the formation of matrix petalloproteinases, particularly MMP-1, which is responsible for collagen degradation in the skin.
[0092] By applying the sunscreen preparation according to the invention to the skin, the upregulation of MMP-1 caused by visible light is also counteracted. The present invention therefore further relates to a mixture of substances, ie the sunscreen preparation according to the invention, comprising at least one UV filter and a combination of
[0093] - at least one composite particle,
[0094] - at least one antioxidant and
[0095] - at least one glass for topical application in a method for protecting the skin from visible light damage, wherein according to a preferred embodiment the visible light damage is caused by activation of the formation of MMP-1 and wherein according to a particularly preferred embodiment this damage is premature skin aging and wherein according to a further embodiment the visible light damage is hyperpigmentation.
[0096] A preferred embodiment of the invention is the light protection preparation according to the invention, comprising at least one UV filter and a combination of
[0097] - a composite particle comprising a substrate core of mica (INCI: Mica) surrounded by layers of tin (IV) oxide (INCI: Tin Oxide) and titanium (IV) oxide (INCI: Titanium Dioxide),
[0098] Carnosine and
[0099] - Perlite (INCI name) for topical application in a method for protecting the skin from visible light damage, wherein according to a preferred embodiment the visible light damage is caused by activation of the formation of MMP-1 and wherein according to a particularly preferred embodiment this damage is premature skin aging and wherein according to a further embodiment the visible light damage is hyperpigmentation.
[0100] The following comparative tests demonstrate the effect provided by the sunscreen preparations according to the invention:
[0101] Comparative tests:
[0102] The transmission of six sunscreen compositions A to F and the effect of topical application of six sunscreen compositions
[0103] A to F were tested for melanin formation in the skin. Of the tested sunscreen compositions A to F, A, C and E are in accordance with the invention and B, D and F represent the respective comparison formulations (quantities in wt.%). Sunscreen compositions A, B, C and D are lotions in the form of hydrodispersion gels. Sunscreen compositions E and F were formulated as sprays. x in Table 2 means that the additive or
[0104] UV filter is included in the formulation:
[0105] Table 2: Sunscreen compositions
[0106] Comparative tests photometric measurement of transmission:
[0107] The transmission T [%] of the light stabilizers A to C was determined using a Perkin Elmer Lambda 900 spectrometer in the range of 400-800 nm and in the HEV range of 400-500 nm. The film thickness of the sample was 0.1 mm. Undiluted samples were measured. The measured values correspond to the average of
[0108] 10 measurements. The protective effect [%] is given, determined according to:
[0109] Protective effect [%] = [1- Tproduct / Tplacebo] x 100.
[0110] The samples were tested for the effectiveness of the combination according to the invention: Determination of the protective effect of the sunscreen composition A in relation to B, C in relation to D and E in relation to F.
[0111] With the sunscreen compositions A, C and E according to the invention, a protective effect in the range 400 - 800 nm between 47% and 56% and in the range 400 - 500 nm between 51% and 71% was achieved, with the protective effect in the range 400 - 800 nm increasing from formulation A via B to C, and in the range 400 - 500 nm increasing from formulation C via A to B.
[0112] Preclinical assessment of cosmetic formulations on melanin formation after visible light irradiation:
[0113] The protective effect of the photoprotective compositions according to the invention against visible light-induced melanin formation, in particular against hyperpigmentation, was demonstrated in a preclinical study on melanin formation following visible light irradiation on human skin explants.
[0114] For this purpose, skin explants from a healthy volunteer of Fitzpatrick skin type III were treated on 4 consecutive days with the investigated sunscreen compositions A to F at a dosage of 25-30 mg / cm 2 treated. 24 hours after the first treatment, the investigated sunscreen compositions were removed, and the skin explants were exposed to a defined physiologically relevant dose of visible light (480 J / cm2) (Hydrosun 750, KG1 filter). 24 hours after the fourth treatment, the skin explants were histologically evaluated using Fontana-Masson staining. In the Fontana-Masson stain, melanin is visualized as a black precipitate. The evaluated parameter was the percentage of melanin per corresponding area of the basal and prickle cell layers of the epidermis.
[0115] Treatment of the skin explants with the sunscreens A, C, and E according to the invention leads to a reduction in melanin formation of between 50% and 71%, while the sunscreens B, D, and F tested only led to a reduction in melanin formation of between 27% and 54%. It can be seen that the sunscreen preparations A, C, and E according to the invention each cause a significantly greater reduction in melanin formation than the corresponding comparison compositions B, D, and F, which do not contain the combination according to the invention.
[0116] In all samples A, C and E, the use of the inventive combination of titanium dioxide, mica, tin oxide, carnosine and perlite resulted in a significant reduction in the transmission of the sunscreen preparation in the visible radiation range and a significant reduction in melanin formation compared to the respective comparison formulations B, D and F, which increased from formulation C via E to A.
[0117] Further example formulations:
[0118] Formulation 1 : Spray Formulations 2-5: Hydrodispersion gels Formulations 6-9: Hydrodispersion gels
[0119] Formulation 10: Lotion
[0120] Formulation 11 : W / O Cream
[0121] Formulation 12: O / W emulsion
[0122] Formulation 13: O / W emulsion
Claims
REQUIREMENTS 1. Sunscreen composition for protecting the skin against UV radiation and visible light, comprising at least one UV filter and a combination of - at least: one composite particle - at least one antioxidant and - at least one glass, 2. Light protection composition according to claim 1, characterized in that the composite particle comprises: - a substrate core of mica, bismuth oxychloride, silicon dioxide, aluminum oxide, aluminum borosilicate, glass, bomitride or mixtures thereof - a first coating on the substrate core consisting of a first metal oxide - possibly further layers on the first coating made of further metal oxides, in particular a second layer made of a second metal oxide.
3. Light protection composition according to claim 1 or 2, characterized in that the composite particle comprises a substrate core made of mica.
4. Sunscreen composition according to claim 2 or 3, characterized in that the mica is selected from natural mica, synthetic mica (INCI: Synthetic Fluorphlogopite) or a mixture thereof, preferably natural mica, 5. A sun protection composition according to one of claims 2 to 4, characterized in that the first, second and further metal oxides are selected from titanium(IV) oxide, iron oxide, aluminum oxide, silicon dioxide, zirconium oxide, cobalt oxide, tin(IV) oxide, Zmn(II) oxide, nickel oxide and mixtures of these oxides, preferably from titanium dioxide (INCI nomenclature for titanium(IV) oxide) and tin oxide (INCI nomenclature for tin(IV) oxide), wherein the first metal oxide is particularly preferably tin oxide and the second metal oxide is titanium dioxide.
6. Light protection composition according to any one of claims 1 to 5, characterized in that the glass is selected from synthetic glass, natural glass or mixtures thereof, 7. Light protection composition according to one of claims 1 to 6, characterized in that the glass is Perlite (INCI name), 8. Light protection composition according to one of claims 1 to 7, characterized in that the content of composite particles in the light protection preparation is 0.01 to 2 wt.%, preferably 0.05 to 1.5 wt.%, particularly preferably 0.1 to 1 wt.%.
9. A light protection composition according to any one of claims 1 to 8, characterized in that the content of antioxidants in the light protection preparation is 0.001 to 20 wt.%, preferably 0.01 to 10 wt.%, particularly preferably 0.01 to 5 wt.% and particularly 0.05 to 2 wt.%.
10. Light protection composition according to one of claims 1 to 9, characterized in that the glass content in the light protection preparation is 0.01 to 5 wt.%, preferably 0.01 to 2 wt.%, particularly preferably 0.05 to 1.5 wt.% and particularly 0.1 to 1 wt.%.
11. Light protection composition according to one of claims 1 to 10, characterized in that the UV filter is selected from Ethylhexyl Methoxycinnamate, Isoamyl p-Methoxycinnamate, Benzophenone-3, Benzophenone-4, Diethylamino Hydroxy benzoyl Hexyl Benzoate, Ethylhexyl Triazone, Diethylhexyl Butamido Triazone, Bis-Ethylhexyloxyphenol Methoxyphenyl Triazine, Ethylhexyl Bis-Isopentylbenzoxazolylphenyl Melamine, Tris-Biphenyl Triazine, Butyl Methoxy-dibenzoylmethane, Octocrylene, Homosalate, Ethylhexyl Salicylates, Methylene Bis-benzotriazolyl Tetramethylbutylphenol, Drometrizole Trisiloxane, Phenylbenzimid-azole Sulfonic Acid, Disodium Phenyl Dibenzimidazole Tetrasulfonate, Benzylidene Camphor Sulfonic Acid, Terephthalylidene Dicamphor Sulfonic Acid, Titanium Dioxide, Zinc Oxide.
12. Sunscreen composition according to one of claims 1 to 11, characterized in that the UV filter is titanium dioxide.
13. Light protection composition according to one of claims 1 to 12, characterized in that the composite particles have a particle size determined by laser diffraction in the range of 1 μm to 200 μm, particularly preferably from 1 μm to 100 μm and most preferably of less than 15 μm (80% within this range).
14. Use of a sunscreen composition according to any one of claims 1 to 13 for protecting the skin from pigmentation caused by visible light, preferably hyperpigmentation.
15. A sun protection composition according to any one of claims 1 to 13 for topical application in a method for protecting the skin from damage caused by visible light.
16. Light protection composition according to claim 15, characterized in that the damage caused by visible light is caused by activation of the formation of matrix metalloproteinase-1.
17. A sunscreen composition according to claim 15 or 16, characterized in that the damage caused by visible light is premature skin aging.
18. A sunscreen composition according to claim 15, characterized in that the damage caused by visible light is hyperpigmentation.