Permeation blocking composition for reducing transdermal penetration of sunscreen

Abstract

The invention discloses a permeation prevention composition for reducing percutaneous permeation of a sun-screening agent, and belongs to the technical field of cosmetics. The permeation-blocking composition comprises a film-forming agent and a plant extract, the film-forming agent is composed of trimethylsiloxy silicate ester, polydimethylsiloxane and an acrylic acid (ester) / polytrimethylsiloxane methacrylate copolymer, and the plant extract is a mixture of a kappaphycus alvarezii extract and a caesalpinia spinosa fruit extract. According to the composition, through the synergistic effect of all the components, the good permeation preventing and film forming effects are achieved, the raw materials are wide in source, the preparation method is simple, safety and stability are high, storage and transportation are convenient, and the good application prospect is achieved.

Description

Technical Field

[0001] This application relates to the technical field of cosmetics, and specifically relates to an anti-permeation composition for reducing the percutaneous penetration of sunscreen agents. Background Art

[0002] Entering the 21st century, the economy has promoted the rapid development of industry. The impact of humans on the natural environment has become increasingly large. The protective effect of the ozone layer has weakened, and the intensity of ultraviolet rays in sunlight poses a threat to human health, showing serious consequences such as short-term sunburn or long-term effects of skin erythema, photoaging, tissue damage, and skin cancer. Therefore, sunscreen cosmetics have gradually become one of the essential cosmetics in life. Thus, how to develop and promote a sunscreen product to prevent the damage of ultraviolet rays to human health has become the latest research hotspot in the cosmetics industry.

[0003] Common sunscreen agents include physical sunscreen agents (physical shielding agents) and chemical absorbers. Among them, titanium dioxide and zinc oxide in physical sunscreen agents have a strong effect of reflecting ultraviolet rays, but there are also certain drawbacks. For example, some physical sunscreen agents are not easy to apply evenly; ethylhexyl methoxycinnamate and ethylhexyl salicylate in chemical sunscreen agents have strong ultraviolet absorption, but there is a certain skin permeability. Therefore, how to prevent sunscreen agents from penetrating into the skin is the current research hotspot.

[0004] Therefore, based on the above problems, there is an urgent need to provide a sunscreen anti-permeation composition that is safe to use, has good sunscreen anti-permeation effect, and strong stability for market selection. Summary of the Invention

[0005] The purpose of the present invention is to provide an anti-permeation composition for reducing the percutaneous penetration of sunscreen agents, which is prepared by compounding a plant extract and a film-forming agent, has high safety, good product stability, and excellent sunscreen anti-permeation effect.

[0006] To achieve the above purpose, the present invention adopts the following technical solutions:

[0007] In the first aspect, the present invention provides an anti-permeation composition for reducing the percutaneous penetration of sunscreen agents, and the anti-permeation composition comprises the following components in parts by weight:

[0008] Film-forming agent 5.5 - 22 parts:

[0009] Plant extract 0.1 - 1 part;

[0010] The film-forming agent is composed of a copolymer of trimethylsiloxysilicate, polydimethylsiloxane, and acrylate / polymethyltrimethoxysiloxysilicate with a mass ratio of 1:0.1 - 0.2, and the plant extract is a mixture of Kappaphycus striatum extract and Caesalpinia spinosa fruit extract;

[0011] The copolymer of polydimethylsiloxane and acrylate / polymethyltrimethoxysiloxysilane methacrylate is purchased from Dow (Zhangjiagang) Investment Co., Ltd., trade name: DOWSIL TM FA4003 DM Silicone Acrylate; the plant extract is purchased from SILAB company, product model: FILMEXEL.

[0012] Preferably, the barrier composition comprises the following components in parts by weight:

[0013] Film-forming agent: 11.5 parts;

[0014] Plant extract: 0.2 part;

[0015] The film-forming agent is composed of trimethylsiloxysilicate, polydimethylsiloxane and a copolymer of acrylate / polymethyltrimethoxysiloxysilane methacrylate in a mass ratio of 10:1.5.

[0016] In a second aspect, the present invention provides an application of the barrier composition described in the first aspect in the preparation of a sunscreen composition.

[0017] In a third aspect, the present invention provides a sunscreen composition, which comprises the barrier composition described in the first aspect.

[0018] Preferably, the addition amount of the barrier composition is 1-1.5 wt%.

[0019] Preferably, the sunscreen composition is a sunscreen, a sunscreen lotion or a sunscreen spray.

[0020] Preferably, the sunscreen composition further comprises one or more of a sunscreen agent, a moisturizer, a skin conditioner, a thickener, an antioxidant, a chelating agent, a skin feel regulator, a pH regulator, an emulsifier, a solvent.

[0021] More preferably, the sunscreen agent is selected from at least one of disodium phenyl dibenzimidazole tetrasulfonate, a mixture of ethylhexyl methoxycinnamate and butylated hydroxytoluene, a mixture of titanium dioxide, isododecane, polyhydroxystearic acid, stearic acid and aluminum hydroxide, ethylhexyl salicylate, diethylamino hydroxybenzoyl hexyl benzoate, bis-ethylhexyloxyphenol methoxyphenyl triazine, ethylhexyl triazone, a mixture of zinc oxide, diethylhexyl carbonate, polyhydroxystearic acid and triethoxysilane octyl, diethylhexyl butamido triazone, homosalate.

[0022] More preferably, the moisturizer is selected from dipropylene glycol and / or 1,2-hexanediol.

[0023] Further preferably, the skin conditioner is selected from at least one of niacinamide, polydimethylsiloxane, diisopropyl sebacate, isododecane, and octyl polymethylsiloxane.

[0024] Further preferably, the thickener is selected from at least one of sodium chloride, dimethyldistearylammonium lithium montmorillonite, and dextrin palmitate.

[0025] Further preferably, the antioxidant is selected from hydroxyacetophenone.

[0026] Further preferably, the chelating agent is selected from disodium EDTA.

[0027] Further preferably, the skin feel regulator is selected from poly(methyl methacrylate) cross polymer and / or silica.

[0028] Further preferably, the pH regulator is selected from tromethamine.

[0029] Further preferably, the emulsifier is selected from PEG-10 polydimethylsiloxane and / or cetyl PEG / PPG-10 / 1 polydimethylsiloxane.

[0030] Further preferably, the solvent is selected from deionized water.

[0031] Fourthly, the present invention provides a preparation method of the sunscreen composition described in the third aspect, and the preparation method includes the following steps:

[0032] (1) Mix deionized water, dipropylene glycol, niacinamide, sodium chloride, 1,2-hexanediol, tromethamine, disodium phenyl dibenzimidazole tetrasulfonate, hydroxyacetophenone, disodium EDTA, and plant extract, heat to 70-75 °C, stir until completely dissolved, and cool to 40-45 °C to obtain Phase A;

[0033] (2) Mix a part of polydimethylsiloxane, a mixture of ethylhexyl methoxycinnamate and butylated hydroxytoluene, titanium dioxide and a mixture of isododecane, polyhydroxystearic acid, stearic acid, and aluminum hydroxide, ethylhexyl salicylate, diethylamino hydroxybenzoyl hexyl benzoate, diisopropyl sebacate, isododecane, bis-ethylhexyloxyphenol methoxyphenyl triazine, octyl polymethylsiloxane, ethylhexyl triazone, PEG-10 polydimethylsiloxane, dimethyldistearylammonium lithium montmorillonite, cetyl PEG / PPG-10 / 1 polydimethylsiloxane, zinc oxide and a mixture of diethylhexyl carbonate, polyhydroxystearic acid, and triethoxysilane octyl, and dextrin palmitate, heat to 80-85 °C, stir evenly, and cool to 40-45 °C to obtain Phase B;

[0034] (3) Mix polydimethylsiloxane, copolymer of acrylate / polymethyltrimethoxysiloxysilicate, remaining polydimethylsiloxane, trimethylsiloxysilicate, methyl methacrylate cross-linked polymer, and silica evenly to obtain Phase C;

[0035] (4) Add Phase C to Phase B and disperse evenly to obtain Phase E;

[0036] (5) Add Phase A to Phase E, stir evenly, cool down to below 38 °C, and discharge to obtain the sunscreen composition.

[0037] Compared with the prior art, the beneficial effects of the present invention are as follows: The present invention provides a sunscreen composition, which contains an anti-permeation composition for reducing the percutaneous penetration of sunscreen agents. The anti-permeation composition includes a film-forming agent and a plant extract. The film-forming agent is composed of trimethylsiloxysilicate, polydimethylsiloxane, and copolymer of acrylate / polymethyltrimethoxysiloxysilicate. The plant extract is a mixture of extracts of Kappaphycus alvarezii and fruits of Caesalpinia spinosa. Among them, the copolymer formed by cross-linking polydimethylsiloxane and acrylate / polymethyltrimethoxysiloxysilicate has characteristics such as comfort and breathability; the extracts of Kappaphycus alvarezii and fruits of Caesalpinia spinosa are used in combination, and a tight film can be spontaneously formed by cross-linking natural polysaccharides, which can achieve a better effect of tightening the skin and reduce the risk of irritation; through the synergistic effect of the film-forming agent and the plant extract, the anti-permeation composition of the present invention has a good anti-permeation film-forming effect, and has effects such as fast film-forming speed, low irritation, good breathability, and good makeup retention and adherence.

[0038] Description of the accompanying drawings of the specification:

[0039] Figure 1 : HPLC chromatogram of the reference substance of 35 wt% sunscreen agent A, homosalate;

[0040] Figure 2 : HPLC chromatogram of the permeation rate of homosalate in the anti-permeation composition 1;

[0041] Figure 3 : HPLC chromatogram of the permeation rate of homosalate in the anti-permeation composition ⑥. Detailed implementation manners

[0042] To better understand the present invention, the following describes the present invention in further detail with reference to specific embodiments. The terms used in the embodiments are for describing specific implementation manners and do not constitute a limitation on the protection scope of the present invention.

[0043] The experimental methods without specific conditions noted in the following examples are usually carried out under conventional conditions or according to the conditions recommended by the manufacturers. Unless otherwise stated, percentages and parts are calculated by weight.

[0044] The partial raw materials and their sources are as follows:

[0045] Trimethylsiloxysilicate: Purchased from: Wacker Chemie (China) Co., Ltd., product number: TMS 803

[0046] Copolymer of polydimethylsiloxane and acrylate / polymethyltrimethoxysilyl methacrylate: Purchased from Dow (Zhangjiagang) Investment Co., Ltd., trade name: DOWSIL TM FA 4003DM Silicone Acrylate.

[0047] Plant extract: A mixture of Kappaphycus alvarezii extract and Caesalpinia spinosa fruit extract, purchased from SILAB company, product model: FILMEXEL.

[0048] Except as specifically stated above, all chemical reagents used in the present invention are purchased from Shanghai Aladdin Biochemical Technology Co., Ltd.

[0049] An occlusive composition for reducing percutaneous penetration of sunscreen agents, and the specific components and mass parts are shown in Table 1.

[0050] Table 1 Components and their mass parts of the occlusive composition

[0051]

[0052]

[0053] A sunscreen composition, and its specific components are shown in Table 2.

[0054] Table 2 Components and their mass percentages of the sunscreen composition

[0055]

[0056]

[0057] Note: In the mixture of ethylhexyl methoxycinnamate and butylated hydroxytoluene, the mass ratio of ethylhexyl methoxycinnamate to butylated hydroxytoluene is 99.97:0.03;

[0058] In the mixture of titanium dioxide, isododecane, polyhydroxystearic acid, stearic acid and aluminum hydroxide, the mass ratio of titanium dioxide, isododecane, polyhydroxystearic acid, stearic acid and aluminum hydroxide is 45:40:5:5:5;

[0059] In the mixture of zinc oxide, diethylhexyl carbonate, polyhydroxystearic acid and triethoxysilane octyl, the mass ratio of zinc oxide, diethylhexyl carbonate, polyhydroxystearic acid to triethoxysilane octyl is 5.7:3.5:0.5:0.3;

[0060] The preparation method of the above sunscreen composition 1 comprises the following steps:

[0061] (1) Mix deionized water, dipropylene glycol, niacinamide, sodium chloride, 1,2 - hexanediol, tromethamine, disodium phenyl dibenzimidazole tetrasulfonate, p - hydroxyacetophenone, disodium EDTA, and plant extract, heat the mixture to 70 °C, stir until completely dissolved, and then cool down to 45 °C to obtain Phase A;

[0062] (2) Mix 3 / 8 of the amount of polydimethylsiloxane with a mixture of ethylhexyl methoxycinnamate and butylated hydroxytoluene, titanium dioxide and a mixture of isododecane, polyhydroxystearic acid, stearic acid, and aluminum hydroxide, ethylhexyl salicylate, diethylamino hydroxybenzoyl hexyl benzoate, diisopropyl sebacate, isododecane, bis - ethylhexyloxyphenol methoxyphenyl triazine, octyl polymethylsiloxane, ethylhexyl triazone, PEG - 10 polydimethylsiloxane, dimethyldistearylammonium lithium montmorillonite, cetyl PEG / PPG - 10 / 1 polydimethylsiloxane, zinc oxide and a mixture of diethylhexyl carbonate, polyhydroxystearic acid, and triethoxysilane octyl, dextrin palmitate, heat the mixture to 80 °C, stir evenly, and then cool down to 40 °C to obtain Phase B;

[0063] (3) Stir evenly polydimethylsiloxane and a copolymer of acrylate / polymethyltrimethoxysiloxysilane methacrylate, the remaining polydimethylsiloxane, trimethylsilanol silicate, methyl methacrylate cross - polymer, and silica to obtain Phase C;

[0064] (4) Add Phase C to Phase B, disperse evenly to obtain Phase E;

[0065] (5) Add Phase A to Phase E, stir evenly, cool down to 38 °C, and discharge to obtain the said sunscreen composition.

[0066] Compared with the preparation method of sunscreen composition 1, in the preparation of the comparative sunscreen composition, the plant extract, polydimethylsiloxane, and copolymer of acrylate / polymethyltrimethoxysiloxysilane methacrylate, and trimethylsilanol silicate are replaced with deionized water of equal mass, and the remaining steps are the same as those of sunscreen composition 1.

[0067] Test 1 Human safety test

[0068] 1. Human skin patch test

[0069] Test substances: The sunscreen composition 1 of the present invention and the comparative sunscreen composition.

[0070] Subject selection: Select healthy volunteers aged 21 - 44 years old, who are willing to participate and sign an informed consent form, and can complete the test as required during the test period. 10 subjects are set in each group.

[0071] Experimental method: Select qualified patch test equipment. Using the occlusive patch test method, place approximately 0.020 mL - 0.025 mL (liquid) of the test substance in the patch test device, and apply a low-sensitization tape externally to the back or the flexor side of the forearm of the subject. Remove the test substance after 24 hours, and observe and record the skin reaction at 0.5, 24, and 48 hours after removal respectively.

[0072] Evaluation criteria: The classification of skin adverse reactions is judged according to the classification of skin adverse reactions in the human trial test stipulated in the "Technical Specifications for Cosmetics Safety" (2015 Edition) issued by the National Medical Products Administration. The classification criteria are shown in Table 3.

[0073] Table 3 Classification criteria for skin adverse reactions

[0074] Grade Classification Phenomenon Grade 0 No skin reaction Grade 1 Faint erythema appears on the skin Grade 2 Erythema, infiltration and papules appear on the skin Grade 3 Erythema, edema, papules and blisters appear on the skin Grade 4 Erythema, edema and large blisters appear on the skin

[0075] Experimental results: The skin reactions of the subjects in each group were all grade 0, indicating that the sunscreen composition 1 of the present invention and the comparative sunscreen composition are safe to use.

[0076] 2. Human trial for sensitive skin

[0077] Test substance: The same as the human patch test.

[0078] Subject selection: Select healthy volunteers aged 21 - 44 years old, who meet the positive result of the lactic acid sting test, voluntarily participate and sign the informed consent form, and can complete the test as required during the test period. Each group has 10 subjects.

[0079] Experimental method: The volunteers randomly divide both sides of the face into the test side and the control side. After cleansing the skin, apply the product evenly on the facial skin of the test side according to the product usage method, and do not use any product on the control side. After 28 days of trial, the volunteers report the local skin reaction, and then a dermatologist evaluates the adverse reaction situation.

[0080] Evaluation criteria: The classification of skin adverse reactions is judged according to the classification of skin adverse reactions in the human trial test stipulated in the "Technical Specifications for Cosmetics Safety" (2015 Edition). The classification criteria are shown in Table 3.

[0081] Experimental results: The skin reactions of the sensitive skin subjects in each group were all grade 0, indicating that the sunscreen composition 1 of the present invention and the comparative sunscreen composition are safe and non-irritating, and are suitable for people with sensitive skin.

[0082] Combined with the results of the human skin patch test and the test for sensitive skin suitability, no subject had skin adverse reactions for both the sunscreen composition 1 and the comparative sunscreen composition, indicating that the sunscreen and permeation-blocking composition 1 and the comparative sunscreen composition have good safety, are mild and non-irritating, and are suitable for people with sensitive skin.

[0083] Test 2: Film-forming and barrier effect test

[0084] Test substance: A mixture composed of a barrier composition, a sunscreen agent, and a 65 v / v% ethanol-PBS solution, where the dosage of the barrier composition is 1 wt%, the dosage of the sunscreen agent is 35 wt%, and the balance is the 65 v / v% ethanol-PBS solution.

[0085] Selection of sunscreen agent:

[0086] A: Homosalate (CAS: 118-56-9);

[0087] B: Ethylhexyl methoxycinnamate (CAS: 5466-77-3);

[0088] C: Disodium phenyl dibenzimidazole tetrasulfonate (CAS: 180898-37-7);

[0089] D: Bis-ethylhexyloxyphenol methoxyphenyl triazine (CAS: 187393-00-6);

[0090] Experimental method: Refer to GB / T 27818-2011.

[0091] The test skin is selected from the abdominal skin of 1.5-month-old Bama miniature pigs, with a thickness of 1000 μm;

[0092] Experimental time: 6 h;

[0093] Accepting solution: 65 v / v% ethanol-PBS solution;

[0094] Dosage of test substance: 500 μg / cm 2 ;

[0095] The residual amount or content determination of the above sunscreen agent is quantitatively determined by HPLC.

[0096] Table 4 Film-forming and barrier effect test

[0097]

[0098]

[0099] It was determined that the recovery rates of this test were all within 100 ± 10%, meeting the requirements.

[0100] According to the results in Table 4, the anti-permeation compositions 1-4 can effectively prevent the percutaneous penetration of the sunscreen agent. Even at an ultra-high dose of 35 wt% of the sunscreen agent, its penetration rate is still less than 15%. In particular, the anti-permeation composition 1 can effectively prevent the penetration of the sunscreen agent. By comparing the anti-permeation composition 1 with the anti-permeation compositions ①-③, it can be seen that the dosage ratio of each component in the anti-permeation composition within the range defined in the present invention can improve the film-forming anti-permeation efficacy of the composition. By comparing the anti-permeation composition 1 with the anti-permeation compositions ④-⑥, it can be seen that there is a certain synergistic effect between trimethylsiloxysilicate, polydimethylsiloxane and the copolymer of acrylate / polymethyltrimethoxysiloxysilane methacrylate and the plant extract in the anti-permeation composition.

[0101] The embodiments described above are some, but not all, of the embodiments of the present application. The detailed description of the embodiments of the present application is not intended to limit the scope of the present application claimed, but merely represents the selected embodiments of the present application. All other embodiments obtained by those skilled in the art based on the embodiments in the present application without creative efforts fall within the scope of protection of the present application.

Claims

1. An occlusive composition for reducing percutaneous penetration of a sunscreen agent, characterized in that, Comprising the following components in parts by weight: Film former 5.5 - 22 parts; Plant extract 0.1 - 1 part; The film former is composed of trimethylsiloxysilicate, polydimethylsiloxane and a copolymer of acrylate / polytrimethylsiloxane methacrylate in a mass ratio of 1:0.1 - 0.2, and the plant extract is a mixture of Kappaphycus alvarezii extract and Caesalpinia spinosa fruit extract.

2. The barrier composition according to claim 1, wherein The copolymer of polydimethylsiloxane and acrylate / polymethyltrimethoxysiloxysilane methacrylate is purchased from Dow (Zhangjiagang) Investment Co., Ltd., trade name: DOWSIL TM FA4003 DM Silicone Acrylate; the plant extract is purchased from SILAB company, product model: FILMEXEL.

3. The barrier composition according to claim 1, wherein Comprising the following components in parts by weight: Film former 11.5 parts; Plant extract 0.2 part; The film former is composed of trimethylsiloxysilicate, polydimethylsiloxane and a copolymer of acrylate / polytrimethylsiloxane methacrylate in a mass ratio of 10:1.

5.

4. Use of the barrier - permeation - preventing composition according to any one of claims 1 - 3 in the preparation of a sunscreen composition.

5. A sunscreen composition, characterized in that, The sunscreen composition contains the barrier - permeation - preventing composition according to any one of claims 1 - 3, and the addition amount of the barrier - permeation - preventing composition is 1 - 1.5 wt%.

6. The sunscreen composition according to claim 5, characterized in that, The sunscreen composition is any one of sunscreen, sunscreen lotion, and sunscreen spray.

7. The sunscreen composition according to claim 5, characterized in that, The sunscreen composition further contains one or more of sunscreen agents, humectants, skin conditioners, thickeners, antioxidants, chelating agents, skin - feel regulators, pH regulators, emulsifiers, solvents.

8. The sunscreen composition according to claim 7, characterized in that, The sunscreen agent is selected from at least one of disodium phenyl dibenzimidazole tetrasulfonate, a mixture of ethylhexyl methoxycinnamate and butylated hydroxytoluene, a mixture of titanium dioxide, isododecane, polyhydroxystearic acid, stearic acid and aluminum hydroxide, ethylhexyl salicylate, diethylamino hydroxybenzoyl hexyl benzoate, bis - ethylhexyloxyphenol methoxyphenyl triazine, ethylhexyl triazone, a mixture of zinc oxide, diethylhexyl carbonate, polyhydroxystearic acid and triethoxysilane octane, diethylhexyl butamido triazone, homosalate; The humectant is selected from dipropylene glycol and / or 1,2 - hexanediol; The skin conditioner is selected from at least one of niacinamide, polydimethylsiloxane, diisopropyl sebacate, isododecane, octyl polymethylsiloxane; The thickener is selected from at least one of sodium chloride, lithium magnesium stearate smectite, dextrin palmitate; The antioxidant is selected from p - hydroxyacetophenone; The chelating agent is selected from disodium EDTA; The skin - feel regulator is selected from poly(methyl methacrylate) cross - polymer and / or silica; The pH regulator is selected from tromethamine; The emulsifier is selected from PEG - 10 polydimethylsiloxane and / or cetyl PEG / PPG - 10 / 1 polydimethylsiloxane; The solvent is selected from deionized water.

9. A method for preparing a sunscreen composition according to claim 8, characterized in that, The preparation method of the sunscreen composition comprises the following steps: (1) Mix deionized water, dipropylene glycol, niacinamide, sodium chloride, 1,2 - hexanediol, tromethamine, disodium phenyl dibenzimidazole tetrasulfonate, p - hydroxyacetophenone, disodium EDTA, and plant extract, heat to 70 - 75 °C, stir until completely dissolved, and cool to 40 - 45 °C to obtain Phase A; (2) Heat a mixture of a portion of polydimethylsiloxane, ethylhexyl methoxycinnamate and butylated hydroxytoluene, titanium dioxide and a mixture of isododecane, polyhydroxystearic acid, stearic acid and aluminum hydroxide, ethylhexyl salicylate, diethylamino hydroxybenzoyl hexyl benzoate, diisopropyl sebacate, isododecane, bis-ethylhexyloxyphenol methoxyphenyl triazine, octyl polymethylsiloxane, ethylhexyl triazone, PEG-10 polydimethylsiloxane, distearyldimonium hectorite, cetyl PEG / PPG-10 / 1 polydimethylsiloxane, zinc oxide and a mixture of diethylhexyl carbonate, polyhydroxystearic acid and triethoxysilane octyl, dextrin palmitate to 80 - 85 °C, stir evenly, and cool down to 40 - 45 °C to obtain Phase B; (3) Stir evenly a copolymer of polydimethylsiloxane and acrylate / polymethyltrimethoxysiloxysilane methacrylate, the remaining polydimethylsiloxane, trimethylsiloxysilicate, methyl methacrylate cross-linked polymer, and silica to obtain Phase C; (4) Add Phase C to Phase B and disperse evenly to obtain Phase E; (5) Add Phase A to Phase E, stir evenly, cool down to below 38 °C, and discharge to obtain the sunscreen composition.

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