Cationic carrier capable of loading cosmetic lipophilic active ingredients and its application

Abstract

The present invention relates to a cationic carrier and application thereof of a loadable cosmetic lipophilic active substance. The raw material of the cationic carrier includes an aqueous solution of a nonionic emulsifier, silk fibroin nanofiber and cocamidopropyl PG-dimethyl ammonium chloride phosphate, wherein the mass ratio of the nonionic emulsifier, the aqueous solution and the cocamidopropyl PG-dimethyl ammonium chloride phosphate is 1:(1.5~5):(0.7~2), and the content of β-folding in the silk fibroin nanofiber is 25%~45%. The cationic carrier provided by the present invention has a stronger lipophilic active substance loading capacity, and the cationic inclusion containing the cationic carrier has better permeability, stability and mildness simultaneously, and has broad application prospects.

Description

Technical Field

[0001] The present invention relates to the technical field of cosmetics, in particular to a cationic carrier capable of loading cosmetic lipophilic active substances and applications thereof. Background Art

[0002] In the cosmetics field, amphiphilic cationic lipid materials can be used as carriers to deliver lipophilic active ingredients, thereby improving their compatibility with the skin. However, existing cationic carriers, due to their strong cationic properties, strong skin affinity, and strong permeability, can cause skin irritation. Furthermore, when loaded with large amounts of lipophilic active ingredients, these carriers are prone to rupture, leading to precipitation of the lipophilic active ingredient and poor stability of the cationic inclusions.

[0003] Therefore, there is an urgent need for a cationic carrier that can increase the loading capacity of lipophilic active substances and whose cationic inclusions have good permeability, stability and mildness. Summary of the Invention

[0004] Therefore, it is necessary to provide a cationic carrier capable of loading cosmetic lipophilic active ingredients and its application to address the above-mentioned problems. The cationic carrier provided by the present invention has a strong loading capacity for lipophilic active ingredients, and the cationic inclusions containing the cationic carrier also have good permeability, stability, and mildness, and have broad application prospects.

[0005] A cationic carrier capable of loading cosmetic lipophilic active ingredients, wherein raw materials of the cationic carrier include a nonionic emulsifier, an aqueous solution of silk fibroin nanofibers, and cocamidopropyl PG-dimethylammonium chloride sodium phosphate, wherein the mass ratio of the nonionic emulsifier, the aqueous solution, and the cocamidopropyl PG-dimethylammonium chloride sodium phosphate is 1:(1.5-5):(0.7-2), and the content of β-sheets in the silk fibroin nanofibers is 25%-45%.

[0006] In one embodiment, the HLB value of the nonionic emulsifier is ≥10.

[0007] In one embodiment, the nonionic emulsifier is selected from at least one of polysorbate emulsifiers, polyglycerol ester emulsifiers and sucrose ester emulsifiers.

[0008] In one embodiment, the mass fraction of the silk fibroin nanofibers in the aqueous solution is 0.5% to 5%;

[0009] And / or, the length of the silk fibroin nanofiber is 20 nm to 4000 nm, and the diameter is 5 nm to 30 nm.

[0010] A cationic inclusion comprises the cationic carrier as described above, a lipophilic active substance and oil, wherein the cationic carrier is coated on the surface of a mixture of the lipophilic active substance and the oil.

[0011] In one embodiment, in the cationic inclusions, the mass ratio of the cationic carrier to the lipophilic active ingredient and the oil is 1:(0.02-1.32):(1.31-3.52);

[0012] and / or the lipophilic active ingredient is at least one selected from retinol and its derivatives, dimethylmethoxychromanol, astaxanthin, lycopene, β-carotene, lutein, anthocyanidins and tocopherol;

[0013] And / or, the oil is selected from at least one of caprylic / capric glyceride, phytosterol / octyldodecanol lauroyl glutamate, isopropyl lauroyl sarcosinate, hexyldecanol and meadowfoam seed oil.

[0014] In one embodiment, the surface Zeta potential of the cationic inclusion is ≥40 mV;

[0015] And / or, the particle size of the cationic inclusions is ≤150 nm.

[0016] A method for preparing the cationic inclusions as described above comprises the following steps:

[0017] mixing the lipophilic active substance and the oil to obtain an oil phase solution;

[0018] Mixing the cationic carrier described above with water to obtain an aqueous solution;

[0019] The oil phase solution and the water phase solution are mixed and then subjected to nano-processing, and then cooled to obtain the cationic inclusions dispersed in water.

[0020] In one embodiment, the pressure of the nano-processing is 100 MPa to 150 MPa and the temperature is 40° C. to 70° C.;

[0021] And / or, the number of cycles of the nano-processing is 2 to 5 times;

[0022] And / or, the cooling temperature is ≤25°C.

[0023] A use of the above-mentioned cationic carrier or the above-mentioned cationic inclusion in cosmetics.

[0024] The above-mentioned cationic carrier capable of loading cosmetic lipophilic active ingredients, on the one hand, cocamidopropyl PG-dimethyl ammonium chloride phosphate sodium is cationic, and at the same time, the β-pleated structure of silk fibroin nanofibers and the non-ionic emulsifier effectively improve the surface tension of the cationic inclusions, thereby not only increasing the zeta potential of the cationic inclusions, preventing agglomeration between the cationic inclusions, effectively improving the stability of the cationic inclusions, but also reducing the particle size of the cationic inclusions, effectively improving the permeability of the cationic inclusions; on the other hand, the bionic phospholipid structure of cocamidopropyl PG-dimethyl ammonium chloride phosphate sodium and the β-pleated structure of silk fibroin nanofibers not only improve the lipophilic active ingredient loading capacity of the cationic carrier, which is beneficial to preventing the cationic carrier from breaking and the active ingredient from precipitating, but also have good skin affinity, thereby improving the stability and mildness of the cationic inclusions.

[0025] Therefore, the cationic inclusions containing the above cationic carriers have good permeability, stability and mildness, and have broad application prospects. DETAILED DESCRIPTION

[0026] To facilitate understanding of the present invention, the present invention will be described in more detail below. However, it should be understood that the present invention can be implemented in many different forms and is not limited to the embodiments or examples described herein. On the contrary, the purpose of providing these embodiments or examples is to make the understanding of the disclosure of the present invention more thorough and comprehensive.

[0027] Unless otherwise defined, all technical and scientific terms used herein have the same meaning as those generally understood by those skilled in the art of the technical field of the present invention. The terms used herein in the specification of the present invention are only for the purpose of describing specific embodiments or embodiments and are not intended to limit the present invention. The optional scope of the term "and / or" used herein includes any one of two or more related listed items, and also includes any and all combinations of related listed items, including any two related listed items, any more related listed items, or the combination of all related listed items.

[0028] The present invention provides a cationic carrier capable of loading cosmetic lipophilic active ingredients. The raw materials include a nonionic emulsifier, an aqueous solution of silk fibroin nanofibers, and cocamidopropyl PG-dimethylammonium chloride sodium phosphate. The mass ratio of the nonionic emulsifier, the aqueous solution, and the cocamidopropyl PG-dimethylammonium chloride sodium phosphate is 1:(1.5-5):(0.7-2), and the content of β-sheets in the silk fibroin nanofibers is 25%-45%.

[0029] The above-mentioned cationic carrier capable of loading cosmetic lipophilic active ingredients, on the one hand, cocamidopropyl PG-dimethyl ammonium chloride phosphate sodium is cationic, and at the same time, the β-pleated structure of silk fibroin nanofibers and the non-ionic emulsifier effectively improve the surface tension of the cationic inclusions, thereby not only increasing the zeta potential of the cationic inclusions, preventing agglomeration between the cationic inclusions, effectively improving the stability of the cationic inclusions, but also reducing the particle size of the cationic inclusions, effectively improving the permeability of the cationic inclusions; on the other hand, the bionic phospholipid structure of cocamidopropyl PG-dimethyl ammonium chloride phosphate sodium and the β-pleated structure of silk fibroin nanofibers not only improve the lipophilic active ingredient loading capacity of the cationic carrier, which is beneficial to preventing the cationic carrier from breaking and the active ingredient from precipitating, but also have good skin affinity, thereby improving the stability and mildness of the cationic inclusions.

[0030] The hydrophobicity of silk fibroin nanofibers can be distributed at the oil-water interface, which is beneficial to promoting emulsification and reducing the surface tension of cationic inclusions. At the same time, the silk fibroin nanofibers can be entangled with each other to form a stable coating layer, which is beneficial to improving the loading capacity of lipophilic active substances. Preferably, the β-folding content in the silk fibroin nanofibers is 30% to 40%, which is beneficial to further improve the loading capacity of lipophilic active substances, prevent the cationic carrier from breaking and the active substance from precipitating, thereby further improving the stability and mildness of the cationic inclusions.

[0031] It can be understood that the above-mentioned β-sheet content is represented by the ratio of the silk fibroin nanofibers having the β-sheet protein structure to the total amount of the silk fibroin nanofibers in the silk fibroin nanofibers.

[0032] In one embodiment, the mass fraction of the silk fibroin nanofibers in the aqueous solution is 0.5% to 5%.

[0033] In one embodiment, the silk fibroin nanofibers have a length of 20 nm to 4000 nm and a diameter of 5 nm to 30 nm.

[0034] It should be noted that the present invention has no particular limitation on the source of the aqueous solution of silk fibroin nanofibers. A commercially available aqueous solution of silk fibroin nanofibers can be used, or the aqueous solution can be prepared homemade.

[0035] In one embodiment, the HLB value of the nonionic emulsifier is ≥10, which is conducive to further promoting emulsification, reducing the interfacial tension of the cationic inclusions, thereby reducing the particle size of the cationic inclusions, making the cationic inclusions have better permeability, and effectively improving the utilization rate of lipophilic active substances. In addition, it is conducive to further improving the stability of the surface charge of the cationic inclusions, promoting the electrostatic balance between the cationic inclusions, preventing the cationic inclusions from agglomerating, effectively improving the stability of the cationic inclusions, and reducing the problems of cationic inclusion aggregation and phase separation that may occur during long-term storage.

[0036] Specifically, the nonionic emulsifier is at least one selected from polysorbate emulsifiers, polyglycerol ester emulsifiers and sucrose ester emulsifiers.

[0037] The present invention also provides a cationic inclusion comprising the cationic carrier described above, a lipophilic active ingredient, and an oil, wherein the cationic carrier is coated on the surface of a mixture of the lipophilic active ingredient and the oil. The cationic inclusion of the present invention effectively increases the amount of lipophilic active ingredient encapsulated by the cationic carrier, and also exhibits good permeability, stability, and mildness, thus promising broad application prospects.

[0038] It can be understood that in the cationic inclusions, the lipophilic active substance is dispersed in the oil, and the cations are coated on the surface of the mixture consisting of the oil and the lipophilic active substance.

[0039] In one embodiment, in the cationic inclusions, the mass ratio of the cationic carrier to the lipophilic active ingredient and the oil is 1:(0.02-1.32):(1.31-3.52).

[0040] Specifically, the lipophilic active ingredient is at least one selected from retinol and its derivatives, dimethylmethoxychromanol, astaxanthin, lycopene, β-carotene, lutein, anthocyanidin and tocopherol.

[0041] Specifically, the oil is selected from at least one of caprylic / capric glyceride, phytosterol / octyldodecanol lauroyl glutamate, lauroyl sarcosinate isopropyl ester, hexyldecanol and meadowfoam seed oil.

[0042] In one embodiment, the cationic inclusions further include at least one of a polyol and a regulator.

[0043] In one embodiment, the polyol is at least one selected from glycerol, butylene glycol and dipropylene glycol.

[0044] In one embodiment, the conditioning agent includes at least one of a water-soluble conditioning agent and an oil-soluble conditioning agent.

[0045] It should be noted that the aforementioned modifiers are commonly used adjuvants in the art and are not particularly limited thereto in the present invention. Those skilled in the art may select them according to actual needs. For example, water-soluble modifiers include pH modifiers, chelating agents, preservatives, and water-soluble antioxidants, while oil-soluble modifiers include oil-soluble antioxidants.

[0046] It should be noted that the cationic inclusions are usually dispersed in a solvent when used, that is, a dispersion of cationic inclusions, and the solvent is selected from water.

[0047] In one embodiment, in the dispersion of the cationic inclusions, the mass fraction of the cationic carrier is 0.01% to 10%, the mass fraction of the lipophilic active substance is 0.01% to 10%, the mass fraction of the oil is 10% to 26%, and the balance is water.

[0048] In one embodiment, the mass fraction of the polyol in the dispersion of the cationic inclusions is 10% to 30%.

[0049] In one embodiment, the mass fraction of the regulator in the dispersion of the cationic inclusions is 0.01% to 0.05%.

[0050] In one embodiment, the surface Zeta potential of the cationic inclusions is ≥40 mV, which effectively prevents the cationic inclusions from agglomerating, effectively improves the stability of the cationic inclusions, and reduces the problems of cationic inclusion aggregation and phase separation that may occur during long-term storage. In addition, there is a charge attraction between the positively charged cationic inclusions and the negative charges of skin cells, which is conducive to promoting the adsorption of cationic inclusions to the skin surface, and promotes the penetration and retention of lipophilic active substances by enhancing the interaction with the cell membrane, thereby improving the utilization rate of lipophilic active substances.

[0051] In one embodiment, the particle size of the cationic inclusions is ≤150 nm, which is beneficial to improving the permeability of the cationic inclusions. At the same time, it is beneficial to increase the surface area and interfacial energy of the cationic inclusions, enhance the interaction between the dispersed phase and the continuous phase, reduce the sedimentation and aggregation of the cationic inclusions, and thus improve the dispersibility and stability of the cationic inclusions in water.

[0052] The present invention also provides a method for preparing the cationic inclusions as described above, comprising the following steps:

[0053] mixing the lipophilic active substance and the oil to obtain an oil phase solution;

[0054] Mixing the cationic carrier described above with water to obtain an aqueous solution;

[0055] The oil phase solution and the water phase solution are mixed and then subjected to nano-processing, and then cooled to obtain the cationic inclusions dispersed in water.

[0056] In one embodiment, the nano-processing is performed under a pressure of 100 MPa to 150 MPa and a temperature of 40° C. to 70° C.

[0057] In one embodiment, the number of cycles of the nano-processing is 2 to 5 times, which is beneficial to reducing the particle size of the cationic inclusions and improving the dispersibility and stability of the cationic inclusions in water.

[0058] In one embodiment, the cooling temperature is ≤ 25°C.

[0059] It should be noted that when preparing the oil phase solution and the aqueous phase solution, the mixing uniformity can be improved by heating and stirring. For example, the temperature when preparing the oil phase solution is 60°C to 80°C, and the temperature when preparing the aqueous phase solution is 50°C to 70°C. The nano-processing of the present invention adopts existing methods in the art, such as high-pressure microfluidization method, high-pressure homogenization method, etc.

[0060] It can be understood that when the cationic inclusions also include polyols, the polyols are mixed with cationic carriers and water to prepare an aqueous phase solution; when the cationic inclusions also include a regulator, the water-soluble regulator is mixed with the cationic carrier and water to prepare an aqueous phase solution, and the oil-soluble regulator lipophilic active ingredient is mixed with oil to prepare an oil phase solution.

[0061] The present invention also provides a use of the above-mentioned cationic carrier or the above-mentioned cationic inclusion in cosmetics.

[0062] It should be noted that the cationic carrier of the present invention has a strong lipophilic active substance loading capacity, and the prepared cationic inclusions release the lipophilic active substance therein when used to exert the efficacy of the active substance; the nanoemulsion composition of the present invention is generally applicable to different types of cosmetic systems, and can be used in skin care products such as creams, essences or lotions, and can also be used in makeup products. It is understood that when the nanoemulsion composition is used in different types of cosmetic systems, the cosmetic system also includes other excipients, and the present invention is not limited to this.

[0063] Hereinafter, the cationic carrier capable of loading cosmetic lipophilic active ingredients and its application will be further described through the following specific examples.

[0064] The present invention provides general and / or specific descriptions of the materials and experimental methods used in all embodiments and comparative examples. Reagents or instruments used in all embodiments and comparative examples without indicating the manufacturer are conventional reagents or instruments that can be obtained commercially.

[0065] Example 1

[0066] 5 parts of retinol, 0.5 parts of tocopherol, 21 parts of phytosterol / octyldodecanol lauroyl glutamate and 2.5 parts of caprylic / capric triglyceride were heated and mixed at 70° C. to form a homogeneous phase to obtain an oil phase solution.

[0067] 6.4 parts of a cationic carrier (the mass ratio of polysorbate 80, an aqueous solution of silk fibroin nanofibers and cocamidopropyl PG-dimethylammonium chloride phosphate is 1:1.5:0.7, and the HLB value of polysorbate 80 is 15), 20 parts of glycerin, 0.1 parts of lauroyl arginine ethyl ester hydrochloride and 44.5 parts of water are heated and mixed at 60°C until a homogeneous phase is obtained to obtain an aqueous phase solution; wherein the β-folding content in the silk fibroin nanofibers is 30%, the mass fraction of the silk fibroin nanofibers in the aqueous solution of the silk fibroin nanofibers is 0.5%, and the length of the silk fibroin nanofibers is 20nm to 4000nm, and the diameter is 5nm to 30nm.

[0068] Under continuous stirring, the oil phase solution was slowly injected into the aqueous phase solution, and then nano-treated by a high-pressure microfluidizer. The solution was circulated three times at 40°C and 100 MPa. During the last cycle, the cooling temperature of the discharge port was 20°C to obtain cationic inclusions. The particle size of the cationic inclusions was 115.37 nm and the surface Zeta potential was +51.2 mV.

[0069] Example 2

[0070] 5 parts of retinol, 0.5 parts of tocopherol, 2.5 parts of phytosterol / octyldodecanol lauroyl glutamate and 21 parts of caprylic / capric triglyceride were heated and mixed at 60° C. to form a homogeneous phase to obtain an oil phase solution.

[0071] 8 parts of cationic carrier (polysorbate-80, an aqueous solution of silk fibroin nanofibers and cocamidopropyl PG-dimethylammonium chloride phosphate in a mass ratio of 1:5:2), 25 parts of glycerol, 0.02 parts of EDTA-2Na and 37.98 parts of water are heated and mixed at 70°C until a homogeneous phase is obtained to obtain an aqueous phase solution; wherein the β-folding content in the silk fibroin nanofibers is 30%, the mass fraction of the silk fibroin nanofibers in the aqueous solution of the silk fibroin nanofibers is 0.5%, and the length of the silk fibroin nanofibers is 20nm~4000nm, and the diameter is 5nm~30nm.

[0072] Under continuous stirring, the oil phase solution was slowly injected into the aqueous phase solution, and then nano-treated by a high-pressure microfluidizer. The solution was circulated twice at 65°C and 140 MPa. During the last cycle, the cooling temperature of the discharge port was 15°C to obtain cationic inclusions. The particle size of the cationic inclusions was 98.87 nm and the surface Zeta potential was +48.0 mV.

[0073] Example 3

[0074] 1 part of dimethylmethoxychromanol, 5 parts of hexyldecanol and 21 parts of caprylic / capric triglyceride were heated and mixed at 80° C. to form a homogeneous phase to obtain an oil phase solution.

[0075] 8 parts of a cationic carrier (polysorbate 80, an aqueous solution of silk fibroin nanofibers and sodium cocamidopropyl PG-dimethylammonium chloride phosphate in a mass ratio of 1:5:2), 25 parts of glycerol, 0.5 parts of hydroxyethylpiperazineethane sulfonic acid and 39.5 parts of water are heated and mixed at 65°C until a homogeneous phase is obtained to obtain an aqueous phase solution; wherein the β-folding content in the silk fibroin nanofibers is 45%, the mass fraction of the silk fibroin nanofibers in the aqueous solution of the silk fibroin nanofibers is 1%, and the length of the silk fibroin nanofibers is 20nm to 4000nm, and the diameter is 5nm to 30nm.

[0076] Under continuous stirring, the oil phase solution was slowly injected into the aqueous phase solution, and then nano-treated by a high-pressure microfluidizer. The solution was circulated three times at 70°C and 120 MPa. During the last cycle, the cooling temperature of the discharge port was 25°C to obtain cationic inclusions. The particle size of the cationic inclusions was 105.34 nm and the surface Zeta potential was +53.2 mV.

[0077] Example 4

[0078] 0.2 parts of pentaerythritol tetra(di-tert-butyl hydroxyhydrocinnamate) ester and 10 parts of caprylic / capric triglyceride were mixed and heated to 75° C. for complete dissolution, then cooled to 65° C., and 10 parts of retinol propionate were added and stirred until a uniform phase was obtained to obtain an oil phase solution.

[0079] 7.6 parts of a cationic carrier (the mass ratio of polysorbate-20, an aqueous solution of silk fibroin nanofibers and cocamidopropyl PG-dimethylammonium chloride phosphate is 1:2:0.8, and the HLB value of polysorbate-20 is 16.7), 30 parts of glycerol, 0.01 parts of EDTA-2Na and 42.19 parts of water are heated and mixed at 65°C until a homogeneous phase is obtained to obtain an aqueous phase solution; wherein the β-folding content in the silk fibroin nanofibers is 25%, the mass fraction of the silk fibroin nanofibers in the aqueous solution of the silk fibroin nanofibers is 3%, and the length of the silk fibroin nanofibers is 20nm~4000nm, and the diameter is 5nm~30nm.

[0080] Under continuous stirring, the oil phase solution was slowly injected into the aqueous phase solution, and then nano-treated by a high-pressure microfluidizer. The solution was circulated three times at 65°C and 130 MPa. During the last cycle, the cooling temperature of the discharge port was 20°C to obtain cationic inclusions. The particle size of the cationic inclusions was 118.3 nm and the surface Zeta potential was +54.7 mV.

[0081] Example 5

[0082] 0.1 parts of pentaerythritol tetra(di-tert-butyl hydroxyhydrocinnamate) ester and 18 parts of caprylic / capric triglyceride were mixed and heated to 75° C. and completely dissolved, and then 2 parts of astaxanthin were added and stirred until a uniform phase was obtained to obtain an oil phase solution.

[0083] 5.7 parts of a cationic carrier (the mass ratio of polyglycerol-10 laurate, an aqueous solution of silk fibroin nanofibers and cocamidopropyl PG-dimethylammonium chloride phosphate is 1:2:0.8, and the HLB value of polyglycerol-10 laurate is 15.5), 20 parts of glycerol and 54.2 parts of water are heated and mixed at 60°C until a homogeneous phase is obtained to obtain an aqueous phase solution; wherein the β-folding content in the silk fibroin nanofibers is 40%, the mass fraction of the silk fibroin nanofibers in the aqueous solution of the silk fibroin nanofibers is 0.8%, and the length of the silk fibroin nanofibers is 20nm to 4000nm, and the diameter is 5nm to 30nm.

[0084] Under continuous stirring, the oil phase solution was slowly injected into the aqueous phase solution, and then nano-treated by a high-pressure microfluidizer. The mixture was circulated five times at 70°C and 150 MPa. During the last cycle, the cooling temperature of the discharge port was 20°C to obtain cationic inclusions. The particle size of the cationic inclusions was 117.36 nm, and the surface Zeta potential was +54.2 mV.

[0085] Example 6

[0086] 0.01 parts of lycopene, 5 parts of isopropyl lauroyl sarcosinate and 10 parts of caprylic / capric triglyceride were heated and mixed at 75° C. until a uniform phase was obtained to obtain an oil phase solution.

[0087] 4.6 parts of a cationic carrier (polysorbate-20, an aqueous solution of silk fibroin nanofibers and cocamidopropyl PG-dimethylammonium chloride phosphate in a mass ratio of 1:2.4:1.2), 10 parts of glycerol, 0.02 parts of EDTA-2Na and 70.37 parts of water were heated and mixed at 65°C until a homogeneous phase was obtained to obtain an aqueous phase solution; wherein the β-folding content in the silk fibroin nanofibers was 35%, the mass fraction of the silk fibroin nanofibers in the aqueous solution of the silk fibroin nanofibers was 1%, and the length of the silk fibroin nanofibers was 20nm to 4000nm, and the diameter was 5nm to 30nm.

[0088] Under continuous stirring, the oil phase solution was slowly injected into the aqueous phase solution, and then nano-treated by a high-pressure microfluidizer. The solution was circulated twice at 70°C and 100 MPa. During the last cycle, the cooling temperature of the discharge port was 20°C to obtain cationic inclusions. The particle size of the cationic inclusions was 102.79 nm and the surface Zeta potential was +47.9 mV.

[0089] Comparative Example

[0090] Comparative Examples 1 to 8 were prepared according to the preparation method of Example 2. In the cationic inclusions, the mass fractions of the nonionic emulsifier, the aqueous solution of silk fibroin nanofibers, and sodium cocamidopropyl PG-dimethylammonium chloride phosphate were shown in Table 1. In Comparative Example 7, the β-folding content of the silk fibroin nanofibers was 15%, and the β-folding content of the silk fibroin nanofibers in Comparative Example 8 was 80%.

[0091] Table 1

[0092]

[0093]

[0094] The cationic inclusions prepared in the examples and comparative examples were subjected to performance tests, and the test indicators and methods were as follows:

[0095] (1) Particle size and surface zeta potential: Particle size was measured by dynamic light scattering (DLS) and surface zeta potential was measured by electrophoretic light scattering (ELS).

[0096] (2) Stability test: The cationic inclusions were kept away from light and placed at -10°C, 5°C and room temperature (25°C) respectively, and the changes in the appearance of the cationic inclusions, such as color change, phase separation or oil-water stratification, were observed over a time span of one week, two weeks and four weeks.

[0097] (3) Irritation test: The cationic inclusions of Example 2 and Comparative Example 2 (the mass fraction of retinol is 5%) were prepared into essence A, essence B and essence C according to the ratio in Table 2, wherein the mass fraction of retinol was 0.05%, 0.1% and 0.05%, respectively; 32 volunteers aged 18 to 60 were selected, and an irritation test was conducted with reference to the "Technical Specifications for Safety of Cosmetics 2015 Edition" - Human Skin Patch Test. Essence A, essence B and essence C were added to the patch tester, and then the patch tester with essence was applied to the back of the subject with non-irritating tape. The palm of the hand was gently pressed to evenly apply it to the skin. After 24 hours, the test patch tester was removed, and the test substance residue on the test site was gently wiped off with a moistened absorbent cotton ball. After 0.5 hours, the skin reaction was observed after the indentation disappeared, and the skin reaction was observed again 24 hours and 48 hours after the patch was removed. The reaction results were recorded according to the grading standard.

[0098] Table 2

[0099]

[0100]

[0101] The test results of the particle size and surface Zeta potential of the cationic inclusions of Example 2 and Comparative Examples 1 to 8 are shown in Table 3.

[0102] Table 3

[0103]

[0104] The results of the cationic encapsulation stability test of Example 2 and Comparative Examples 1 to 3 are shown in Table 3.

[0105] Table 4

[0106]

[0107]

[0108] The test results of cationic inclusions of Example 2 and Comparative Example 2 are shown in Table 5. Among them, when the number of people with grade 1 adverse skin reactions is less than 5 and there are no grade 2 to grade 4 adverse skin reactions, it can be determined that the product has no adverse reaction to the human body.

[0109] Table 5

[0110]

[0111] Note: 1 *(19) It means the number of adverse reactions is 1, and the corresponding subject number is 19.

[0112] Combined with the test results in Tables 3 to 5, it can be seen that under the same test conditions, the cationic inclusions prepared in Example 1 have a smaller particle size and a higher surface Zeta potential. At the same time, the ionic inclusions prepared in Example 2 remained unchanged after being placed at different temperatures for four weeks, and there was no oil production or stratification. Moreover, when the ionic inclusions prepared in Example 2 were used as an emulsion, when the mass fraction of the highly irritating retinol in the emulsion was 0.05% and 0.1%, the emulsion had no adverse skin reactions on the human body. However, the cationic inclusions prepared in Comparative Example 1 had a larger particle size and a smaller Zeta potential, and showed oil production and stratification after being placed at room temperature for two weeks. Although the cationic inclusions prepared in Comparative Examples 2 and 3 had smaller particle sizes and higher surface Zeta potentials, they showed oil production or stratification after being placed for two weeks. Moreover, when the ionic inclusions prepared in Comparative Example 2 were used as an emulsion, adverse skin reactions occurred on the human body. The ionic inclusions prepared in Comparative Examples 4 to 6 showed stratification and poor stability. In summary, the cationic carrier provided by the present invention has a strong lipophilic active substance loading capacity, and the cationic inclusions containing the cationic carrier also have good permeability, stability and mildness, and have broad application prospects.

[0113] The technical features of the above-mentioned embodiments can be combined arbitrarily. In order to make the description concise, not all possible combinations of the technical features in the above-mentioned embodiments are described. However, as long as there is no contradiction in the combination of these technical features, they should be considered to be within the scope of this specification.

[0114] The above-described embodiments merely illustrate several implementations of the present invention, and while their descriptions are relatively specific and detailed, they should not be construed as limiting the scope of the patent. It should be noted that a person skilled in the art would be able to make numerous variations and improvements without departing from the spirit of the present invention, all of which fall within the scope of protection of the present invention. Therefore, the scope of protection of the patent for this invention shall be determined by the appended claims.

Claims

1. A cationic carrier capable of loading cosmetic lipophilic active ingredients, characterized in that: The raw materials of the cationic carrier include a nonionic emulsifier, an aqueous solution of silk fibroin nanofibers, and cocamidopropyl PG-dimethylammonium chloride phosphate, wherein the mass ratio of the nonionic emulsifier, the aqueous solution, and the cocamidopropyl PG-dimethylammonium chloride phosphate is 1:(1.5-5):(0.7-2), and the β-folding content in the silk fibroin nanofibers is 25%-45%, and the nonionic emulsifier is selected from polysorbate 80.

2. The cationic carrier capable of loading cosmetic lipophilic active ingredients according to claim 1, characterized in that: In the aqueous solution, the mass fraction of the silk fibroin nanofibers is 0.5% to 5%; And / or, the length of the silk fibroin nanofiber is 20 nm to 4000 nm, and the diameter is 5 nm to 30 nm.

3. A cationic inclusion, characterized in that: The invention comprises the cationic carrier according to any one of claims 1 to 2, a lipophilic active substance and an oil, wherein the cationic carrier is coated on the surface of the mixture consisting of the lipophilic active substance and the oil.

4. The cationic inclusion according to claim 3, characterized in that In the cationic inclusions, the mass ratio of the cationic carrier to the lipophilic active ingredient and the oil is 1:(0.02-1.32):(1.31-3.52); and / or the lipophilic active ingredient is at least one selected from retinol, dimethylmethoxychromanol, astaxanthin, lycopene, β-carotene, lutein, anthocyanidin and tocopherol; And / or, the oil is selected from at least one of caprylic / capric glyceride, phytosterol / octyldodecanol lauroyl glutamate, isopropyl lauroyl sarcosinate, hexyldecanol and meadowfoam seed oil.

5. The cationic inclusion according to claim 3, characterized in that The surface Zeta potential of the cationic inclusions is ≥40 mV; And / or, the particle size of the cationic inclusions is ≤150 nm.

6. A method for preparing a cationic inclusion according to any one of claims 3 to 5, characterized in that: The steps include: mixing the lipophilic active ingredient and the oil to obtain an oil phase solution; Mixing the cationic carrier according to any one of claims 1 to 2 with water to obtain an aqueous solution; The oil phase solution and the water phase solution are mixed and then subjected to nano-processing, and then cooled to obtain the cationic inclusions dispersed in water.

7. The method for preparing cationic inclusions according to claim 6, characterized in that: The pressure of the nano-processing is 100MPa~150MPa, and the temperature is 40℃~70℃; And / or, the number of cycles of the nano-processing is 2 to 5 times; And / or, the cooling temperature is ≤25°C.

8. Use of the cationic carrier according to any one of claims 1 to 2 or the cationic inclusion according to any one of claims 3 to 5 in the preparation of cosmetics.

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