Bionic sebum film lipid nanoparticle with repairing function, preparation method, application and product

By developing a bionic sebum membrane lipid nanoparticles with a specific component ratio, the problem of poor stability of existing bionic sebum membrane compositions is solved, and a high stability and strong permeability skin barrier repair system is achieved, which significantly improves the moisturizing and repairing effect of skin care products.

CN120131489AActive Publication Date: 2025-06-13BEIJING YANZHISHAN TECH CO LTD
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Patent Information

Application Number
CN202510601269.3
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-05-12
Publication Date
2025-06-13
Estimated Expiration
2045-05-12

AI Technical Summary

Technical Problem

The existing bionic sebum film compositions have poor stability, which can easily lead to loss of active ingredients and unstable physical characterization, limiting their application in skin care products.

Method used

A bionic sebum membrane lipid nanoparticles are developed to form a high stability and low irritation skin barrier repair system through specific proportions of ingredients such as wax esters, triglycerides, squalanes, sterols, ceramides, lecithin, antioxidants and polyols.

Benefits of technology

It achieves high stability, strong permeability and significant moisturizing effects, significantly repair and prevent damage to the skin's stratum corneum and sebum film, and promotes the effective absorption of active ingredients in skin care products.

✦ Generated by Eureka AI based on patent content.

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Abstract

The invention relates to the technical field of skin care products, and provides bionic sebum film lipid nanoparticles with a repairing function, a preparation method, application and a product. The bionic sebum film lipid nanoparticles are prepared from the following components in percentage by weight: 8%-10% of wax ester, 15%-20% of triglyceride, 3%-6% of squalane, 0.1%-2% of sterol, 0.05%-0.25% of ceramide, 1%-5% of lecithin, 0.1%-1% of an antioxidant, 5%-22.5% of polyol and the balance of water. The weight content of phosphatidylcholine in the lecithin is greater than or equal to 45%, and the particle size of the bionic sebum membrane lipid nanoparticles is less than or equal to 200nm. The added sterol and lecithin have a synergistic effect, so that the bionic sebum lipid membrane lipid nanoparticles have a better repairing effect, and transdermal permeation and absorption of water-soluble active matters in a formula can be more effectively promoted when the bionic sebum lipid membrane lipid nanoparticles are added into cosmetics.
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Description

Technical Field

[0001] The present invention relates to the technical field of skin care products, and particularly relates to a biomimetic sebum film lipid nanoparticle with a repair function, a preparation method, an application and a product. Background Art

[0002] The sebum film is an important part of the skin barrier and plays a key role in maintaining the skin's moisture balance and protecting the skin from external stimuli. In daily life, factors such as dryness, ultraviolet rays, and pollution can damage the sebum film, thus causing various skin problems. Therefore, protecting and reconstructing the damaged sebum film is the key to daily skin care for maintaining a healthy skin state. Moreover, the skin's barrier function limits the penetration of some substances, making it difficult for key active ingredients in skin care products to be absorbed and utilized. Therefore, the promoting penetration effect on active ingredients is of great significance in the field of skin care products.

[0003] Human sebum is composed of 40%-60% triglycerides, 25%-30% wax esters, 12%-15% squalene, 1.5% cholesterol, and 1% ceramide. Adding sebum-like components to skin care products can fill the gaps between stratum corneum cells, make the skin barrier more complete, and reduce transepidermal water loss. And it creates a good environment for the skin to self-repair, giving the skin time and conditions to restore its own barrier function. On the other hand, sebum-like components can interact with the lipids of the skin stratum corneum, making the stratum corneum relatively loose, so that the active ingredients in skin care products can penetrate the stratum corneum more smoothly and thus play a role. However, traditional biomimetic sebum film compositions generally have poor stability, which easily leads to the loss of active ingredients and unstable physical characteristics.

[0004] Chinese Patent CN119053316A provides a cosmetic composition containing a vesicle concentrate, which is composed of an aqueous solution of plant or plant-derived lipid vesicles, and its wall includes phospholipids, phytosphingosine, phytosterols, β-phytosterol sulfate, and optionally other derivatives of phytosterols, as well as ceramides and / or ceramide-like substances, for preparing cosmetic products for skin and hair care and for decorating the face, eyes, eyelashes, lips, and body. The vesicle concentrate may also include lysophospholipids, esters of phytosterols, fatty acids, humectants, emollients, active lipophilic molecules, active hydrophilic molecules, thickeners, and film-forming molecules. The cosmetic product contains the vesicle concentrate cosmetic composition and any other cosmetically acceptable ingredients.

[0005] Phytosterols, mainly present in the cell membranes of plants, can flexibly regulate the interactions between phospholipid molecules, enabling the liposome membrane to maintain appropriate fluidity at different temperatures, preventing the membrane from being too loose or too tight, and ensuring the structural stability of the bionic sebum film composition. Moreover, due to its extremely similar structure to cholesterol, the main component of the sebum membrane, it can also directly participate in protecting and reconstructing the damaged sebum membrane. At the same time, phytosterols also have a certain anti-inflammatory effect, which can soothe the inflammation caused by damaged sebum membranes, thereby promoting the recovery of the sebum membrane. Therefore, phytosterols enhance the repair and penetration-promoting effects while stabilizing the structure of the bionic sebum film composition. When it coexists with cholesterol, it has a synergistic effect to better stabilize the liposome structure and resist the damage of external factors such as temperature changes and mechanical pressure to the liposome. Zhao Guozhi et al. pointed out in the article "Phytosterols and Their Product Development and Utilization (Part II)" (Cereals & Oils, 2006, Issue 3, pp. 3-8) that phytosterols such as stigmasterol have extensive applications in cosmetic preparations such as shaving creams, moisturizers, skin cleansers, and hair styling products.

[0006] Therefore, to overcome the problem of poor stability of existing bionic sebum film compositions and provide a highly stable and low-irritation sebum-like lipid carrier system with skin barrier repair and promoting the penetration of active ingredients is a current research hotspot in skin care product development. Summary of the Invention

[0007] In view of the above deficiencies, the present invention aims to provide a bionic sebum film lipid nanoparticle with repair and penetration-promoting effects, a preparation method, an application, and a product. The bionic sebum film lipid nanoparticle has high high-temperature accelerated stability, does not undergo physical appearance changes, and has strong permeability and moisturizing effects, and has a significant effect on repairing and / or preventing damage to the skin stratum corneum and sebum membrane.

[0008] To achieve the above invention object, on the one hand, the present invention provides a bionic sebum film lipid nanoparticle with a repair function, which is composed of the following components by weight percentage: wax ester 8%-10%, triglyceride 15%-20%, squalane 3%-6%, sterol 0.1%-2%, ceramide 0.05%-0.25%, lecithin 1%-5%, antioxidant 0.1%-1%, polyol 5%-22.5%, and the balance of water; the weight content of phosphatidylcholine in the lecithin ≥ 45%, and the particle size of the bionic sebum film lipid nanoparticle ≤ 200 nm.

[0009] The water includes but is not limited to purified water, deionized water, ultrapure water, distilled water, double-distilled water, sterile water, purified water, tap water, etc., and deionized water and / or double-distilled water are preferred.

[0010] Preferably, the wax ester is selected from one or more of jojoba seed oil, beeswax, and coconut alcohol octanoate / decanoate.

[0011] As an example of the present invention, the wax ester is jojoba seed oil.

[0012] As an example of the present invention, the wax ester is coco-caprylate / caprate.

[0013] Preferably, the triglyceride is selected from one or more of Prinsepia utilis Royle oil, caprylic / capric triglyceride, Limnanthes alba seed oil, soybean oil, corn germ oil, sunflower seed oil, perilla oil, linseed oil, tomato seed oil, macadamia nut oil, grape seed oil.

[0014] More preferably, the triglyceride is selected from one or more of Prinsepia utilis Royle oil, caprylic / capric triglyceride, Limnanthes alba seed oil, macadamia nut oil.

[0015] As an example of the present invention, the triglyceride is a mixture of Prinsepia utilis Royle oil and caprylic / capric triglyceride.

[0016] As an example of the present invention, the triglyceride is a mixture of Prinsepia utilis Royle oil, Limnanthes alba seed oil and caprylic / capric triglyceride.

[0017] As an example of the present invention, the triglyceride is a mixture of Prinsepia utilis Royle oil, Limnanthes alba seed oil and macadamia nut oil.

[0018] As an example of the present invention, the triglyceride is caprylic / capric triglyceride.

[0019] Preferably, the sterol is selected from one or more of phytosterol and cholesterol.

[0020] More preferably, the sterol is selected from one or more of cholesterol, brassinolide, stigmasterol, avenasterol.

[0021] As an example of the present invention, the sterol is cholesterol.

[0022] As an example of the present invention, the sterol is stigmasterol.

[0023] As an example of the present invention, the sterol is brassinolide.

[0024] As an example of the present invention, the sterol is avenasterol.

[0025] As an example of the present invention, the sterol is cholesterol and brassinolide.

[0026] As an example of the present invention, the sterol is cholesterol and stigmasterol.

[0027] Preferably, the ceramide is selected from one or more of ceramide NP, ceramide NS, ceramide NG, ceramide AS, ceramide AP, ceramide EOP.

[0028] More preferably, the ceramide is selected from ceramide AP and / or ceramide NP.

[0029] As an example of the present invention, the ceramide is ceramide AP.

[0030] As an example of the present invention, the ceramide is ceramide NP.

[0031] Preferably, the lecithin is selected from one or more of soybean lecithin, egg yolk lecithin, and sunflower lecithin.

[0032] More preferably, and as an example of the present invention, the lecithin is soybean lecithin.

[0033] Preferably, the content of phosphatidylcholine (PC) in the lecithin is ≥70%.

[0034] Preferably, the antioxidant is selected from one or more of tocopherol, tocopheryl acetate, butylated hydroxyanisole, butylated hydroxytoluene, 2,6-di-tert-butyl-p-cresol, idebenone, coenzyme Q10, astaxanthin, ferulic acid, pentaerythrityl tetraester, dimethylmethoxy chromanol, phenoxyethanol, p-hydroxyacetophenone, and octanoyl hydroxamic acid.

[0035] More preferably, and as an example of the present invention, the antioxidant is tocopherol.

[0036] Preferably, the polyol is selected from one or more of 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, ethylhexylglycerin, or glycerol.

[0037] More preferably, the polyol is selected from one or more of 1,2-pentanediol, 1,2-hexanediol, or glycerol.

[0038] As an example of the present invention, the polyol is a mixture of 1,2-pentanediol, 1,2-hexanediol, and glycerol.

[0039] As some examples of the present invention, the wax ester is jojoba seed oil; the triglyceride is one or more of pittosporum oil and caprylic / capric triglyceride; the antioxidant is tocopherol; the sterol is one or more of cholesterol, brassinolide, stigmasterol, avenasterol; the ceramide is ceramide AP or ceramide NP; the lecithin is soybean lecithin with a PC content of ≥70%; the polyol is a mixture of 1,2-pentanediol, 1,2-hexanediol, and glycerol; the water is deionized water.

[0040] As some examples of the present invention, the wax ester is coco-caprylic / capric alcohol; the triglyceride is one or more of Prinsepia utilis Royle seed oil, Limnanthes alba seed oil, Macadamia ternifolia seed oil, and caprylic / capric triglyceride; the antioxidant is tocopherol; the sterol is cholesterol; the ceramide is ceramide AP; the lecithin is soy lecithin with a PC content of ≥70%; the polyol is a mixture of 1,2-pentanediol, 1,2-hexanediol, and glycerol; and the water is deionized water.

[0041] More preferably, the bionic sebum film lipid nanoparticles are composed of the following components by weight percentage: 8%-10% wax ester, 15%-20% triglyceride, 3%-6% squalane, 0.1%-2% sterol, 0.05%-0.25% ceramide, 1%-5% lecithin, 0.1%-1% antioxidant, 7.5%-22.5% polyol, and the balance water Even more preferably, the bionic sebum film lipid nanoparticles are composed of the following components by weight percentage: 9%-10% wax ester, 16.5%-20% triglyceride, 4.5%-6% squalane, 0.5%-2% sterol, 0.1%-0.25% ceramide, 2.5%-5% lecithin, 0.1%-1% antioxidant, 10.5%-22.5% polyol, and the balance water.

[0042] Further preferably, the bionic sebum film lipid nanoparticles are composed of the following components by weight percentage: 9% wax ester, 16.5% triglyceride, 4.5% squalane, 0.5% sterol, 0.1% ceramide, 2.5% lecithin, 0.1% antioxidant, 10.5% polyol, and the balance water.

[0043] Preferably, the particle size of the bionic sebum film lipid nanoparticles is ≤200 nm.

[0044] More preferably, the particle size of the bionic sebum film lipid nanoparticles is ≤150 nm.

[0045] Even more preferably, the particle size of the bionic sebum film lipid nanoparticles is 80-150 nm.

[0046] On the other hand, the present invention provides a method for preparing the above bionic sebum film lipid nanoparticles, comprising the following steps: S1. Mix the wax ester, triglyceride, lecithin, antioxidant, squalane, ceramide, and sterol, and dissolve them into an oil solution at 55-80 °C; S2. Mix the polyol and water to form an aqueous phase; S3. Mix and emulsify the oil phase obtained in step S1 and the aqueous phase obtained in step S2, and perform homogenization treatment to obtain bionic sebum film lipid nanoparticles.

[0047] Preferably, in step S1, the mixing is stirring and dissolving, the temperature of the stirring and dissolving is 55 - 80°C, more preferably 65 - 75°C, and still more preferably 70°C; the speed of the stirring and dissolving is 50 - 400 rpm, more preferably 200 - 400 rpm; the time of the stirring and dissolving is 10 - 120 min, more preferably 15 - 30 min.

[0048] Preferably, in step S2, the mixing is stirring and dissolving, the temperature of the stirring and dissolving is 55 - 80°C, more preferably 70°C; the speed of the stirring and dissolving is 50 - 400 rpm, more preferably 200 - 400 rpm; the time of the stirring and dissolving is 5 - 30 min, more preferably 10 - 15 min.

[0049] Preferably, in step S3, the mixing is stirring and dissolving, the temperature of the stirring and dissolving is 55 - 80°C, more preferably 70°C, the speed of the stirring and dissolving is 50 - 400 rpm, more preferably 100 - 200 rpm; the time of the stirring and dissolving is 10 - 30 min, more preferably 10 - 15 min.

[0050] Preferably, in step S3, the conditions for emulsification are emulsifying at 55 - 80°C and 1000 - 8000 rpm for 5 - 30 min.

[0051] More preferably, in step S3, the conditions for emulsification are emulsifying at 70°C and 3000 - 6000 rpm for 5 - 15 min.

[0052] Preferably, in step S3, the homogenization is carried out using a high-pressure homogenizer or microfluidic homogenization.

[0053] More preferably, in step S3, the homogenization is carried out using a high-pressure homogenizer, and the homogenization conditions are homogenizing at 700 - 1500 bar for 3 - 8 cycles.

[0054] On the other hand, the present invention provides the use of the above-mentioned biomimetic sebum film lipid nanoparticles or the biomimetic sebum film lipid nanoparticles prepared by the above method in the production of cosmetics.

[0055] Finally, the present invention provides a cosmetic, which contains the above-mentioned biomimetic sebum film lipid nanoparticles or the biomimetic sebum film lipid nanoparticles prepared by the above method.

[0056] The dosage forms of the cosmetic include but are not limited to emulsions, ointments, etc.

[0057] The beneficial effects of the present invention are as follows: (1)The present invention simulates the types and relative proportions of lipid components in the skin to form a biomimetic sebum composition, which has extremely high biocompatibility, is safe and non-irritating, and can maximize the moisturizing, soothing and repairing effects of lipids on the skin.

[0058] (2)The sterols and lecithin added in the present invention have a synergistic effect, making the lipid nanoparticles of the biomimetic sebum film more stable and having a more effective repair effect.

[0059] (3)The lipid nanoparticles of the biomimetic sebum film provided by the present invention can more effectively promote the skin penetration and absorption of other water-soluble active substances in cosmetics. BRIEF DESCRIPTION OF THE DRAWINGS

[0060] Figure 1 is a photograph of a cell scratch experiment; wherein, the dashed line indicates the boundary between the cells and the scratch.

[0061] Figure 2 is a fluorescence photograph of a fluorescence-labeled transdermal effect evaluation experiment. DETAILED DESCRIPTION OF THE INVENTION

[0062] Terms and statements of the present invention: 1. Articles "a", "an" and "the": Unless otherwise explicitly limited to one (kind) of object, it includes plural objects.

[0063] 2. Numerical ranges: Unless otherwise explicitly indicated, all ranges or ratios disclosed herein will be understood to include any and all sub-ranges or sub-ratios contained therein. For example, the stated range or ratio of 1 to 30 should be considered to include between the minimum value of 1 and the maximum value of 30, and any sub-range or sub-ratio, integer, decimal or sub-range or sub-ratio composed of integers or decimals including the end points.

[0064] The following non-limiting examples can enable those of ordinary skill in the art to more comprehensively understand the present invention, but do not limit the present invention in any way. The following content is only an exemplary illustration of the scope claimed by the present invention. Those skilled in the art can make various changes and modifications to the present invention based on the disclosed content, and they should also fall within the scope claimed by the present invention.

[0065] The present invention will be further described below in the form of specific examples. All chemical reagents used in the examples of the present invention are obtained through conventional commercial channels unless otherwise specified. Unless otherwise specified, the contents described below are mass contents. Unless otherwise specified, it is understood to be carried out at room temperature.

[0066] In the following examples, the sources of some reagents are as follows: Soybean lecithin (PC content 70%) was purchased from Shenyang Tianfeng Biopharmaceutical Co., Ltd., and the product number is SD-240501.

[0067] Examples 1-11 provide biomimetic sebum film lipid nanoparticles with repair and penetration-enhancing effects. Their formulations are shown in Table 1 and Table 2. The content unit of each raw material in the formulation table (including Table 1 and Table 2) is g ("-" indicates that the component is not contained).

[0068] Table 1

[0069] Table 2

[0070] The components in Table 1 and Table 2 are used to obtain biomimetic sebum film lipid nanoparticles according to the following steps: S1. Wax esters, triglycerides, lecithin, antioxidants, and squalane, ceramides, and sterols are mixed and stirred at 200 rpm for 30 min at 70 °C to dissolve, forming an oil solution; S2. Glycerol and polyols are added to deionized water and stirred at 200 rpm for 15 min at 70 °C to dissolve, forming an aqueous phase; S3. The oil phase formed in step S1 is mixed with the aqueous phase formed in step S2, emulsified at 4000 rpm for 5 min at 70 °C, and then homogenized under high pressure at 800 bar 4 times to obtain biomimetic sebum film lipid nanoparticles, and their particle sizes are measured using a laser particle size analyzer.

[0071] The average particle sizes of the biomimetic sebum film lipid nanoparticles obtained from each group in Table 1 and Table 2 are shown in Table 3.

[0072] Table 3

[0073] Comparative Example 1 Compared with Example 1, the difference is only that sterols are not used, and 3 g of soybean lecithin is used instead, and the rest are the same.

[0074] Biomimetic sebum film lipid nanoparticles are obtained according to the following steps: S1. Wax esters, triglycerides, lecithin, antioxidants, and squalane, ceramides are mixed and stirred at 200 rpm for 30 min at 70 °C to dissolve, forming an oil solution; S2. Glycerol and polyols are added to deionized water and stirred at 200 rpm for 15 min at 70 °C to dissolve, forming an aqueous phase; S3. Mix the oil phase formed in step S1 with the water phase formed in step S2, emulsify at 4000 rpm for 5 min at 70 °C, and then perform high-pressure homogenization 4 times at 800 bar to obtain lipid nanoparticles of the bionic sebum film. Measure their particle size using a laser particle size analyzer.

[0075] Tested by a laser particle size analyzer, the average particle size of the obtained lipid nanoparticles of the bionic sebum film was 134 nm.

[0076] Comparative Example 2 Compared with Example 1, the difference is only that soy lecithin is not used, and the amount of phytosterol is changed to 3 g, and the rest are the same.

[0077] Prepare according to the following steps: S1. Mix wax esters, triglycerides, antioxidants, squalane, sterols, and ceramides, and stir at 200 rpm for 30 min at 70 °C to dissolve, forming an oil solution; S2. Add glycerol and polyols to deionized water, and stir at 200 rpm for 15 min at 70 °C to dissolve, forming a water phase; S3. Mix the oil phase formed in step S1 with the water phase formed in step S2, emulsify at 4000 rpm for 5 min at 70 °C, and then perform high-pressure homogenization 4 times at 800 bar to obtain lipid nanoparticles of the bionic sebum film. Measure their particle size using a laser particle size analyzer.

[0078] After testing, this method cannot emulsify to form a uniform emulsion.

[0079] Comparative Example 3 Compared with Example 1, the difference is only that lecithin is not used, and 2.5 g of sucrose stearate is added, and the rest are the same.

[0080] Obtain lipid nanoparticles of the bionic sebum film according to the following steps: S1. Mix wax esters, triglycerides, sucrose stearate, antioxidants, squalane, ceramides, and sterols, and stir at 200 rpm for 30 min at 70 °C to dissolve, forming an oil solution; S2. Add glycerol and polyols to deionized water, and stir at 200 rpm for 15 min at 70 °C to dissolve, forming a water phase; S3. Mix the oil phase formed in step S1 with the water phase formed in step S2, emulsify at 4000 rpm for 5 min at 70 °C, and then perform high-pressure homogenization 4 times at 800 bar to obtain lipid nanoparticles of the bionic sebum film. Measure their particle size using a laser particle size analyzer.

[0081] Tested by a laser particle size analyzer, the average particle size of the obtained lipid nanoparticles of the bionic sebum film was 112 nm.

[0082] Comparative Example 4 Compared with Example 1, the difference is only that lecithin is not used, and 2.5 g of polyglyceryl-10 laurate is added, and the rest are the same.

[0083] The biomimetic sebum film lipid nanoparticles were obtained according to the following steps: S1. Mix wax esters, triglycerides, polyglyceryl-10 laurate, antioxidants, squalane, ceramides, and sterols, and stir at 200 rpm for 30 min at 70 °C to dissolve, forming an oil solution; S2. Add glycerol and polyhydric alcohols to deionized water, and stir at 200 rpm for 15 min at 70 °C to dissolve, forming an aqueous phase; S3. Mix the oil phase formed in step S1 with the aqueous phase formed in step S2, emulsify at 4000 rpm for 5 min at 70 °C, and then perform high-pressure homogenization 4 times at 800 bar to obtain the biomimetic sebum film lipid nanoparticles, and measure their particle size using a laser particle size analyzer.

[0084] The average particle size of the obtained biomimetic sebum film lipid nanoparticles was 105 nm as measured by a laser particle size analyzer.

[0085] Effect evaluation 1. Cell scratch repair test.

[0086] By creating a scratch on a monolayer of cells, the cells at the scratch edge gradually fill the blank area, causing the scratch to "heal", which to a certain extent simulates the migration process of cells in vivo. Treating cells with different substances can study the effects of these substances on cell migration ability. Cell migration includes the function of healing minor wounds in physiological activities in vivo, which is similar to the purpose of the repair effect of cosmetics in lightening skin texture and promoting skin damage healing. At the same time, human keratinocytes are the core constituent cells of the stratified epithelial tissue in the epidermis, and the results of its model can reflect the physiological characteristics of the skin barrier function and repair mechanism. Selecting human keratinocytes for cell migration experiments can evaluate the efficacy of cosmetics in enhancing epidermal repair by assessing the cell re-epithelialization ability.

[0087] The specific experimental method is as follows: Prepare a 6-well plate and mark it with a horizontal straight line on the back using a marker pen. Select well-grown human keratinocytes (HaCaT, Beina Chuanglian Biotechnology Co., Ltd.), digest them and dilute to an appropriate concentration, add them to the well plate, and incubate in an incubator for about 24 h. Dilute the sample with the culture medium. For the sample groups (Example 1, Comparative Example 1, Comparative Example 3, and Comparative Example 4 are diluted 500 times respectively) and add the culture medium with 2% serum, the positive control group adds the culture medium with 10% serum, and the blank control group adds the culture medium with 2% serum. Place the cell culture plate in the incubator and incubate for about 24 h. Observe when the cells grow confluent, and use a 200 µL pipette tip to make scratches. After making the scratches, gently wash 3 times with PBS to remove the floating cells. Take a photo immediately after making the scratches. After taking the photo, aspirate the PBS.

[0088] The blank control group is the culture medium with 2% serum. The positive control group is the culture medium with 10% serum. The Example 1 group, Comparative Example 1 group, Comparative Example 3 group, and Comparative Example 4 group are the culture medium with 2% serum added with the corresponding bionic sebum film lipid nanoparticles prepared at 0.2% of each group in turn.

[0089] Put it back into the incubator and continue to incubate for 24 h. After the incubation, gently wash 3 times with PBS, and take a photo at the same position for 24 h using the same magnification objective lens.

[0090] The cell scratch migration photos are as Figure 1 shown. It can be seen that the cell migration ability of the Example 1 group is close to that of the positive control group. In the Comparative Example 1 group, due to the removal of sterol, the cell migration ability significantly decreases. In Comparative Example 3 and Comparative Example 4, the lecithin is replaced with the non-ionic emulsifiers sucrose stearate and polyglyceryl-10 laurate respectively, and the cell migration ability significantly decreases. In summary, it shows that Example 1 of the present invention has a good repair effect.

[0091] 2. Promotion of transdermal penetration and absorption test of water-soluble active substances Using ex vivo Panama minipig skin as a carrier, based on a Franz diffusion cell, use FITC-labeled conotoxin (purchased from Shanghai Chutai Biotechnology Co., Ltd., purity 98%) as a water-soluble active substance model to test the permeation-enhancing effect of bionic sebum film lipid nanoparticles on conotoxin.

[0092] Administer the labeled conotoxin to the surface of the minipig skin according to the experimental grouping. After 6 h of permeation, fix the sections, and observe the position where the test substance penetrates into the skin under a fluorescence microscope. According to the software, statistically analyze the fluorescence accumulation under the stratum corneum in the sections, and perform data processing on the percentage increase in fluorescence intensity accumulation.

[0093] The specific groups are as follows: The drug administration in the control group is 0.01% conotoxin aqueous solution; The experimental group was an aqueous solution prepared by mixing 0.01% conotoxin peptide with the biomimetic sebum film lipid nanoparticles with a weight concentration of 5% prepared in the examples; The control group was an aqueous solution prepared by mixing 0.01% conotoxin peptide with the lipid nanoparticles with a weight concentration of 5% prepared in the comparative examples.

[0094] The fluorescence photographs of the fluorescence-labeled transdermal effect evaluation experiment are as Figure 2 shown. It can be seen that in the control group, without the addition of biomimetic sebum film lipid nanoparticles, the fluorescence-labeled conotoxin peptide basically remained on the stratum corneum and it was relatively difficult to overcome the stratum corneum barrier; in the experimental group 1, due to the addition of biomimetic sebum film lipid nanoparticles, the fluorescence-labeled conotoxin peptide could more effectively overcome the stratum corneum barrier, penetrate below the stratum corneum, and could be evenly distributed, which could significantly improve the penetration and absorption of conotoxin peptide; in the comparative example 1, the lipid nanoparticles with sterols removed were added, although the fluorescence-labeled conotoxin peptide could also penetrate below the stratum corneum, the overall accumulated fluorescence intensity was much weaker; in the comparative example 3 and the comparative example 4, the lipid nanoparticles containing other emulsifiers replacing lecithin were added, and the fluorescence-labeled conotoxin peptide basically remained on the stratum corneum, and the fluorescence intensity below the stratum corneum was relatively weak. It shows that the example 1 of the present invention has a very significant effect of promoting the penetration and absorption of water-soluble active substances in cosmetic formulations.

[0095] Furthermore, the 6-hour transdermal fluorescence intensity was statistically analyzed using image processing software, and the percentage increase in transdermal penetration was calculated compared with the control group. The results are shown in Table 4 below.

[0096] Table 4

[0097] It can be seen that the biomimetic sebum film lipid nanoparticles provided in each example of the present invention were added to the aqueous solution of fluorescence-labeled conotoxin peptide, and had a higher 6-hour transdermal penetration promoting effect on the fluorescence-labeled conotoxin peptide. Compared with the control group, the percentage increase in transdermal penetration of example 1 was the highest, reaching 97.2%. The percentage increases in 6-hour transdermal penetration of comparative example 1, comparative example 3 and comparative example 4 were all less than those of each example.

[0098] Finally, it should be noted that the above content is only used to illustrate the technical solution of the present invention, rather than a limitation on the protection scope of the present invention. Any simple modification or equivalent replacement of the technical solution of the present invention by those of ordinary skill in the art shall not depart from the essence and scope of the technical solution of the present invention.

Claims

1. A bionic sebum membrane lipid nanoparticle with repairing function, characterized in that: The invention is composed of the following ingredients by weight percentage: 8%-10% wax ester, 15%-20% triglyceride, 3%-6% squalane, 0.1%-2% sterol, 0.05%-0.25% ceramide, 1%-5% lecithin, 0.1%-1% antioxidant, 5%-22.5% polyol and the balance water; the weight content of phosphatidylcholine in the lecithin is ≥45%, and the particle size of the bionic sebum membrane lipid nanoparticles is ≤200nm.

2. The biomimetic sebum membrane lipid nanoparticle according to claim 1, characterized in that: The wax ester is selected from one or more of jojoba seed oil, beeswax or coconut oil alcohol caprylate / caprate.

3. The biomimetic sebum membrane lipid nanoparticle according to claim 1, characterized in that: The triglyceride is selected from one or more of linalool oil, caprylic / capric triglyceride, meadowfoam seed oil, soybean oil, corn germ oil, sunflower seed oil, perilla oil, linseed oil, tomato seed oil, macadamia nut oil or grape seed oil.

4. The bionic sebum membrane lipid nanoparticle according to claim 1, characterized in that: The sterol is selected from one or more of cholesterol, campesterol, soya sterol or avenasterol.

5. The biomimetic sebum membrane lipid nanoparticle according to claim 1, characterized in that: The ceramide is selected from one or more of ceramide NP, ceramide NS, ceramide NG, ceramide AS, ceramide AP or ceramide EOP; the lecithin is selected from one or more of soybean lecithin, egg yolk lecithin or sunflower lecithin.

6. The biomimetic sebum membrane lipid nanoparticle according to claim 1, characterized in that: The antioxidant is selected from one or more of tocopherol, tocopherol acetate, butylated hydroxyanisole, butylated hydroxytoluene, 2,6-di-tert-butyl-p-cresol, idebenone, coenzyme Q10, astaxanthin, ferulic acid, pentaerythritol tetraester, dimethylmethoxychromanol, phenoxyethanol, p-hydroxyacetophenone or caprylhydroxamic acid.

7. The biomimetic sebum membrane lipid nanoparticle according to claim 1, characterized in that: The polyol is selected from one or more of 1,2-pentanediol, 1,2-hexanediol, 1,2-octanediol, ethylhexylglycerol or glycerol.

8. The method for preparing biomimetic sebum membrane lipid nanoparticles according to any one of claims 1 to 7, characterized in that: The following steps are involved: S1, mixing wax esters, triglycerides, lecithin, antioxidants, squalane, ceramide and sterols, and dissolving them into an oil solution at 55-80°C; S2, mixing the polyol with water to form an aqueous phase; S3, mixing, emulsifying, and homogenizing the oil solution obtained in step S1 and the water phase obtained in step S2 to obtain bionic sebum membrane lipid nanoparticles.

9. Use of the bionic sebum membrane lipid nanoparticles according to any one of claims 1 to 7 or the bionic sebum membrane lipid nanoparticles obtained by the preparation method according to claim 8 in the production of cosmetics.

10. A cosmetic, characterized in that: The cosmetic contains the biomimetic sebum membrane lipid nanoparticles according to any one of claims 1 to 7 or the biomimetic sebum membrane lipid nanoparticles obtained by the preparation method according to claim 8.

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