Permeation-blocking compositions that reduce the transdermal penetration of sunscreen agents

Abstract

This invention discloses a barrier composition for reducing the transdermal penetration of sunscreens, belonging to the field of cosmetic technology. The barrier composition comprises a film-forming agent and plant extracts. The film-forming agent is composed of trimethylsiloxysilicate, polydimethylsiloxane, and acrylate / polytrimethylsiloxane methacrylate copolymer. The plant extracts are a mixture of Kappa longifolia extract and Astragalus membranaceus fruit extract. This composition achieves excellent barrier film-forming effect through the synergistic effect of its components. Furthermore, the raw materials are widely available, the preparation method is simple, and it exhibits high safety and stability, facilitating storage and transportation, thus demonstrating promising application prospects.

Description

Technical Field

[0001] This application relates to the field of cosmetic technology, and more specifically to a barrier composition for reducing the transdermal penetration of sunscreen agents. Background Technology

[0002] In the 21st century, rapid economic development has spurred industrial growth, leading to increasingly greater human impact on the natural environment. The ozone layer's protective function has weakened, and the intensity of ultraviolet (UV) radiation from sunlight poses a threat to human health, manifesting as short-term sunburn or long-term effects such as skin erythema, photoaging, tissue damage, and skin cancer. Therefore, sunscreen cosmetics have gradually become an essential part of daily life, and developing and promoting a sunscreen product to prevent UV damage to human health has become a new research hotspot in the cosmetics industry.

[0003] Common sunscreens include physical sunscreens (physical shielding agents) and chemical absorbers. Among physical sunscreens, titanium dioxide and zinc oxide have strong UV reflection effects, but they also have certain drawbacks, such as some physical sunscreens being difficult to apply evenly. Among chemical sunscreens, ethylhexyl methoxycinnamate and ethylhexyl salicylate have strong UV absorption, but they have a certain degree of skin penetration. Therefore, how to prevent sunscreens from penetrating the skin is currently a hot research topic.

[0004] Therefore, based on the above problems, there is an urgent need to provide a sunscreen and waterproofing composition that is safe to use, has good sun protection and waterproofing effects, and is highly stable for the market to choose from. Summary of the Invention

[0005] The purpose of this invention is to provide a barrier composition that reduces the transdermal penetration of sunscreen agents. It uses a combination of plant extracts and film-forming agents, which is highly safe, has good product stability, and provides excellent sun protection and barrier effects.

[0006] To achieve the above objectives, the present invention adopts the following technical solution:

[0007] In a first aspect, the present invention provides a barrier composition for reducing the transdermal penetration of sunscreen agents, the barrier composition comprising 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 / polytrimethylsiloxane methacrylate in a mass ratio of 1:0.1-0.2; the plant extract is a mixture of long-hearted Kappa algae extract and spiny aralia fruit extract.

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

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

[0013] Film-forming agent 11.5 parts;

[0014] 0.2 parts of plant extract;

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

[0016] Secondly, the present invention provides the use of the barrier composition described in the first aspect in the preparation of a sunscreen composition.

[0017] Thirdly, the present invention provides a sunscreen composition comprising the barrier composition described in the first aspect.

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

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

[0020] Preferably, the sunscreen composition further comprises one or more of the following: sunscreen agent, moisturizer, skin conditioner, thickener, antioxidant, chelating agent, skin feel modifier, pH adjuster, emulsifier, and solvent.

[0021] More preferably, the sunscreen agent is selected from at least one of the following: disodium phenyl dibenzimidazole tetrasulfonate, a mixture of ethylhexyl p-methoxycinnamate and butylated hydroxytoluene, a mixture of titanium dioxide and isododecane and polyhydroxystearic acid and stearic acid and aluminum hydroxide, ethylhexyl salicylate, diethylaminobenzoyl benzoate, bis-ethylhexyloxyphenol methoxyphenyl triazine, ethylhexyl triazine ketone, a mixture of zinc oxide and diethylhexyl carbonate and polyhydroxystearic acid and triethoxyoctylsilane, diethylhexylbutamidotriazine ketone, and homosalate.

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

[0023] More preferably, the skin conditioning agent is selected from at least one of nicotinamide, polydimethylsiloxane, diisopropyl sebacate, isododecane, and octyl polymethylsiloxane.

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

[0025] More preferably, the antioxidant is selected from p-hydroxyacetophenone.

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

[0027] More preferably, the skin feel modifier is selected from methyl methacrylate crosspolymer and / or silica.

[0028] More preferably, the pH adjuster is selected from tromethamine.

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

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

[0031] Fourthly, the present invention provides a method for preparing the sunscreen composition described in the third aspect, the method comprising the following steps:

[0032] (1) Mix deionized water, dipropylene glycol, nicotinamide, sodium chloride, 1,2-hexanediol, tromethamine, disodium phenyl dibenzimidazole tetrasulfonate, p-hydroxyacetophenone, disodium EDTA, and plant extracts and heat to 70-75°C. Stir until completely dissolved and cool to 40-45°C to obtain phase A.

[0033] (2) A mixture of polydimethylsiloxane, ethylhexyl p-methoxycinnamate and butylated hydroxytoluene, titanium dioxide and isododecane and a mixture of polyhydroxystearic acid and stearic acid and aluminum hydroxide, ethylhexyl salicylate, diethylamino hydroxybenzoyl hexyl benzoate, diisopropyl sebacate, isododecane, bis-ethylhexyloxyphenol methoxyphenyl triazine, octyl polymethylsiloxane, ethylhexyl triazine ketone, PEG-10 polydimethylsiloxane, lithium distearate dimethylammonium montmorillonite, cetyl PEG / PPG-10 / 1 polydimethylsiloxane, zinc oxide and a mixture of diethylhexyl carbonate and polyhydroxystearic acid and triethoxyoctylsilane, and dextrin palmitate are mixed and heated to 80-85°C, stirred evenly, and then cooled to 40-45°C to obtain phase B;

[0034] (3) Mix polydimethylsiloxane and the copolymer of acrylate / polytrimethylsiloxane methacrylate, the remaining polydimethylsiloxane, trimethylsiloxysilicate, methyl methacrylate crosspolymer, and silica evenly to obtain phase C;

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

[0036] (5) Add phase A to phase E, stir evenly, cool 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 comprising a barrier composition that reduces the transdermal penetration of sunscreen agents. This barrier composition includes a film-forming agent and plant extracts. The film-forming agent is composed of trimethylsiloxysilicate, polydimethylsiloxane, and a copolymer of acrylates / polytrimethylsiloxane methacrylate. The plant extract is a mixture of Kappa longifolia extract and Astragalus membranaceus fruit extract. The copolymer formed by the cross-linking of polydimethylsiloxane, acrylates / polytrimethylsiloxane methacrylate possesses properties such as comfort and breathability. The mixture of Kappa longifolia extract and Astragalus membranaceus fruit extract, through the cross-linking of natural polysaccharides, can spontaneously form a firming film, achieving better skin-firming effects and reducing the risk of irritation. Through the synergistic effect of the film-forming agent and plant extracts, the present invention enables this barrier composition to have excellent barrier film-forming effects, with fast film-forming speed, low irritation, good breathability, and good makeup adherence.

[0038] Instruction manual illustrations:

[0039] Figure 1 HPLC chromatogram of 35wt% sunscreen agent A homosalyl ester standard;

[0040] Figure 2 HPLC chromatogram of the permeability of barrier composition 1, homosalate;

[0041] Figure 3 HPLC chromatogram of the permeability of barrier composition ⑥ Homosalate. Detailed Implementation

[0042] To better understand the present invention, the present invention will be further described below with reference to specific embodiments. The terminology used in the embodiments is for describing specific implementation schemes and does not constitute a limitation on the scope of protection of the present invention.

[0043] Unless otherwise specified, experimental methods in the following examples are generally performed under standard conditions or as recommended by the manufacturer. Unless otherwise stated, all measurements are by weight in percentages and parts.

[0044] Some of the raw materials and their sources are as follows:

[0045] Trimethylsiloxane silicate: Purchased from Wacker Chemie (China) Co., Ltd., item number: TMS 803

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

[0047] Plant extracts: A mixture of extracts from Kappa longifolia and fruit of Astragalus membranaceus, purchased from SILAB, product model FILMEXEL.

[0048] Unless otherwise specified above, all chemical reagents used in this invention were purchased from Shanghai Aladdin Biochemical Technology Co., Ltd.

[0049] A barrier composition for reducing the transdermal penetration of sunscreen agents, the specific components and mass fractions of which are shown in Table 1.

[0050] Table 1. Components and mass fractions of the barrier composition

[0051]

[0052]

[0053] A sunscreen composition, the specific components of which 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 p-methoxycinnamate and butylated hydroxytoluene, the mass ratio of ethylhexyl p-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 triethoxyoctylsilane, the mass ratio of zinc oxide, diethylhexyl carbonate, polyhydroxystearic acid, and triethoxyoctylsilane is 5.7:3.5:0.5:0.3.

[0060] The preparation method of the above-mentioned sunscreen composition 1 includes the following steps:

[0061] (1) Deionized water, dipropylene glycol, nicotinamide, sodium chloride, 1,2-hexanediol, tromethamine, disodium phenyl dibenzimidazole tetrasulfonate, p-hydroxyacetophenone, disodium EDTA and plant extract were mixed and heated to 70°C, stirred until completely dissolved, and then cooled to 45°C to obtain phase A.

[0062] (2) Mix 3 / 8 of the amount of polydimethylsiloxane with a mixture of ethylhexyl p-methoxycinnamate and butylated hydroxytoluene, a mixture of titanium dioxide and isododecane and polyhydroxystearic acid and stearic acid and aluminum hydroxide, ethylhexyl salicylate, diethylamino hydroxybenzoyl hexyl benzoate, diisopropyl sebacate, isododecane, bis-ethylhexyloxyphenol methoxyphenyl triazine, octyl polymethylsiloxane, ethylhexyl triazine ketone, PEG-10 polydimethylsiloxane, lithium distearate dimethylammonium montmorillonite, cetyl PEG / PPG-10 / 1 polydimethylsiloxane, a mixture of zinc oxide and diethylhexyl carbonate and polyhydroxystearic acid and triethoxyoctylsilane, and dextrin palmitate. Heat the mixture to 80°C, stir until homogeneous, and then cool to 40°C to obtain phase B.

[0063] (3) The copolymer of polydimethylsiloxane and acrylate / polytrimethylsiloxane methacrylate, the remaining polydimethylsiloxane, trimethylsiloxysilicate, methyl methacrylate crosspolymer, and silica are stirred evenly to obtain phase C;

[0064] (4) Add phase C to phase B and disperse it evenly to obtain phase E;

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

[0066] Compared with the preparation method of sunscreen composition 1, the comparative sunscreen composition replaces the plant extract, polydimethylsiloxane and copolymer of acrylate / polytrimethylsiloxane methacrylate, and trimethylsiloxysilicate with an equal mass of deionized water during preparation, while the remaining steps are the same as those of sunscreen composition 1.

[0067] Experiment 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] Participant selection: Healthy volunteers aged 21-44 years were selected who voluntarily participated, signed informed consent forms, and were able to complete the trial as required during the testing period. Each group consisted of 10 participants.

[0071] Experimental method: Using qualified patch testing equipment, the test substance (approximately 0.020 mL - 0.025 mL) was placed in the patch testing device using the closed patch test method. The sample was then applied to the back or flexor side of the forearm of the subject with hypoallergenic adhesive tape. The test substance was removed after 24 hours. Skin reactions were observed and recorded at 0.5, 24, and 48 hours after removal.

[0072] Evaluation criteria: Adverse skin reactions are graded according to the classification of adverse skin reactions in human trials as specified in the "Cosmetic Safety Technical Specifications" (2015 edition) issued by the National Medical Products Administration. The grading criteria are shown in Table 3.

[0073] Table 3. Grading Standards for Adverse Skin Reactions

[0074] Classification Phenomenon Level 0 No skin reaction Level 1 Light red spots appeared on the skin Level 2 Skin shows erythema, infiltration and papules Level 3 Skin erythema, edema, papules and vesicles Level 4 Skin erythema, edema and blisters

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

[0076] 2. Suitable for sensitive skin (human trials conducted).

[0077] Test substance: Same as human patch test.

[0078] Subject selection: Healthy volunteers aged 21-44 years who tested positive for lactic acid stinging were selected, voluntarily participated and signed informed consent forms, and were able to complete the test as required during the testing period. Each group consisted of 10 subjects.

[0079] Experimental Methods: Volunteers randomly divided their faces into test and control sides. After cleansing, the product was applied evenly to the test side according to the instructions, while no product was used on the control side. After 28 days of use, volunteers reported local skin reactions, and dermatologists evaluated any adverse reactions.

[0080] Evaluation criteria: Adverse skin reactions are graded according to the classification of adverse skin reactions in human trials as specified in the "Cosmetic Safety Technical Specifications" (2015 edition) issued by the National Medical Products Administration. The grading criteria are shown in Table 3.

[0081] Experimental results: The skin reaction of all sensitive skin subjects was 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] Based on the results of human skin patch tests and sensitive skin suitability tests, no adverse skin reactions were observed in any subjects using either sunscreen composition 1 or the control sunscreen composition. This indicates that both sunscreen composition 1 and the control sunscreen composition are safe, gentle, and non-irritating, and are suitable for people with sensitive skin.

[0083] Experiment 2 Film-forming barrier effect test

[0084] Test substance: A mixture of an antipermeation composition, a sunscreen agent, and a 65v / v% ethanol-PBS solution, wherein the antipermeation composition is used in an amount of 1 wt%, the sunscreen agent in an amount of 35 wt%, and the balance is the 65v / v% ethanol-PBS solution.

[0085] Sunscreen selection:

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

[0087] B: Ethylhexyl p-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 experimental skin was selected from the abdomen of 1.5-month-old Bama miniature pigs, with a thickness of 1000 μm;

[0092] Experiment duration: 6 hours;

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

[0094] Test substance dosage: 500 μg / cm³ 2 ;

[0095] The residual amount or content of the above sunscreen agents was determined quantitatively using HPLC.

[0096] Table 4. Test of Barrier Film Formation Efficacy

[0097]

[0098]

[0099] The recovery rates of this experiment were all within 100±10%, which meets the requirements.

[0100] As shown in Table 4, barrier compositions 1-4 effectively prevent the transdermal penetration of sunscreen agents. Even at an ultra-high dosage of 35 wt% sunscreen agent, the penetration rate is still less than 15%, especially barrier composition 1, which effectively prevents the penetration of sunscreen agents. Comparing barrier composition 1 with barrier compositions ①-③, it can be seen that the proportions of each component in the barrier compositions within the range defined by this invention can improve the film-forming barrier effect of the compositions. Comparing barrier composition 1 with barrier compositions ④-⑥, it can be seen that the copolymers of trimethylsiloxysilicate, polydimethylsiloxane, and acrylate / polytrimethylsiloxane methacrylate in the barrier compositions have a certain synergistic effect with the plant extracts.

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

Claims

1. A barrier composition for reducing the transdermal penetration of sunscreen agents, characterized in that, Includes the following components by weight: Film-forming agent: 5.5-22 parts; Plant extract 0.1-1 part; The film-forming agent is composed of trimethylsiloxane, polydimethylsiloxane, and a copolymer of acrylates / polytrimethylsiloxane methacrylate in a mass ratio of 1:0.1-0.

2. The plant extract is a mixture of extracts from *Kappa longifolia* and *Solanum lyratum*. The copolymer of polydimethylsiloxane and acrylates / polytrimethylsiloxane methacrylate was purchased from Dow (Zhangjiagang) Investment Co., Ltd., trade name: DOWSIL™ FA 4003 DMSilicone Acrylate. The plant extract was purchased from SILAB, product model: FILMEXEL. The trimethylsiloxane was purchased from Wacker Chemie (China) Co., Ltd., product model: TMS 803.

2. The barrier composition according to claim 1, characterized in that, Includes the following components by weight: Film-forming agent 11.5 parts; 0.2 parts of plant extract; The film-forming agent is composed of a copolymer of trimethylsiloxysilicate, polydimethylsiloxane, and acrylate / polytrimethylsiloxane methacrylate in a mass ratio of 10:1.

5.

3. The use of a barrier composition according to any one of claims 1-2 in the preparation of a sunscreen composition.

4. A sunscreen composition, characterized in that, The sunscreen composition comprises the barrier composition according to any one of claims 1-2, wherein the amount of the barrier composition added is 1-1.5 wt%.

5. The sunscreen composition according to claim 4, characterized in that, The sun protection composition is any one of sunscreen cream, sunscreen lotion, or sunscreen spray.

6. The sunscreen composition according to claim 4, characterized in that, The sunscreen composition further comprises one or more of the following: sunscreen agent, moisturizer, skin conditioner, thickener, antioxidant, chelating agent, skin feel modifier, pH adjuster, emulsifier, and solvent.

7. The sunscreen composition according to claim 6, characterized in that, The sunscreen agent is selected from at least one of the following: disodium phenyl dibenzimidazole tetrasulfonate, a mixture of ethylhexyl p-methoxycinnamate and butylated hydroxytoluene, a mixture of titanium dioxide and isododecane and polyhydroxystearic acid and stearic acid and aluminum hydroxide, ethylhexyl salicylate, diethylaminobenzoyl benzoate, bis-ethylhexyloxyphenol methoxyphenyl triazine, ethylhexyl triazine ketone, a mixture of zinc oxide and diethylhexyl carbonate and polyhydroxystearic acid and triethoxyoctylsilane, diethylhexylbutamidotriazine ketone, and homosalate. The humectant is selected from dipropylene glycol and / or 1,2-hexanediol; The skin conditioning agent is selected from at least one of niacinamide, polydimethylsiloxane, diisopropyl sebacate, isododecane, and octyl polymethylsiloxane; The thickener is selected from at least one of sodium chloride, distearate dimethylammonium lithium montmorillonite, and dextrin palmitate. The antioxidant is selected from p-hydroxyacetophenone; The chelating agent is selected from disodium EDTA; The skin feel modifier is selected from methyl methacrylate crosspolymer and / or silica; The pH adjuster 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.

8. A method for preparing the sunscreen composition according to claim 7, characterized in that, The method for preparing the sunscreen composition includes the following steps: (1) Mix deionized water, dipropylene glycol, nicotinamide, sodium chloride, 1,2-hexanediol, tromethamine, disodium phenyl dibenzimidazole tetrasulfonate, p-hydroxyacetophenone, disodium EDTA, and plant extracts and heat to 70-75°C. Stir until completely dissolved and cool to 40-45°C to obtain phase A. (2) Mix a portion of polydimethylsiloxane with a mixture of ethylhexyl p-methoxycinnamate and butylated hydroxytoluene, a mixture of titanium dioxide and isododecane and polyhydroxystearic acid and stearic acid and aluminum hydroxide, ethylhexyl salicylate, diethylamino hydroxybenzoyl hexyl benzoate, diisopropyl sebacate, isododecane, bis-ethylhexyloxyphenol methoxyphenyl triazine, octyl polymethylsiloxane, ethylhexyl triazine ketone, PEG-10 polydimethylsiloxane, lithium distearate dimethylammonium montmorillonite, cetyl PEG / PPG-10 / 1 polydimethylsiloxane, a mixture of zinc oxide and diethylhexyl carbonate and polyhydroxystearic acid and triethoxyoctylsilane, and dextrin palmitate. Heat the mixture to 80-85°C, stir until homogeneous, and then cool to 40-45°C to obtain phase B. (3) The copolymer of polydimethylsiloxane and acrylate / polytrimethylsiloxane methacrylate, the remaining polydimethylsiloxane, trimethylsiloxysilicate, methyl methacrylate crosspolymer, and silica are stirred evenly 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 to below 38°C, and discharge to obtain the sunscreen composition.

Images