Bionic sebum membrane lipid nanoparticles with repairing function, preparation method, application and product

Abstract

The present invention relates to the technical field of skin care products, and provides a biomimetic sebum membrane lipid nanoparticle with a repairing function, a preparation method, an application, and a product. The biomimetic sebum membrane lipid nanoparticle is composed of the following ingredients by weight: 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 water; the weight content of phosphatidylcholine in the lecithin is ≥45%, and the particle size of the biomimetic sebum membrane lipid nanoparticle is ≤200nm. The sterol added in the present invention has a synergistic effect with the lecithin, so that the biomimetic sebum membrane lipid nanoparticle has a better repairing effect, and adding it to cosmetics can more effectively promote the transdermal penetration and absorption of water-soluble active substances in the formula.

Description

Technical Field

[0001] The present invention relates to the technical field of skin care products, and in particular to bionic sebum membrane lipid nanoparticles with a repairing function, a preparation method, an application and a product. Background Art

[0002] The sebum membrane is a crucial component of the skin barrier, playing a key role in maintaining the skin's moisture balance and protecting it from external stimuli. In daily life, factors such as dryness, ultraviolet rays, and pollution can damage the sebum membrane, leading to various skin problems. Therefore, protecting and rebuilding damaged sebum membranes is crucial for maintaining healthy skin and is essential for daily skincare. Furthermore, the skin's barrier function limits the penetration of some substances, making it difficult for key active ingredients in skincare products to be absorbed and utilized. Therefore, enhancing the penetration of active ingredients is of great significance in the skincare industry.

[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 ingredients to skin care products can fill the gaps between stratum corneum cells, making the skin barrier more complete and reducing transepidermal water loss. It also creates a good environment for skin self-repair, allowing the skin time and conditions to restore its barrier function. On the other hand, sebum-like ingredients can interact with the lipids in the skin's stratum corneum, making the stratum corneum relatively loose, allowing the active ingredients in skin care products to penetrate the stratum corneum more smoothly and thus exert their effects. However, traditional biomimetic sebum film compositions generally have poor stability, easily leading to loss of active ingredients, and unstable physical characteristics.

[0004] Chinese invention patent CN119053316A provides a cosmetic composition comprising a vesicle concentrate, which is composed of an aqueous solution of lipid vesicles of plants or plant origin, whose walls include phospholipids, phytosphingosine, phytosterols, β-phytosterol sulfate and optional other derivatives of phytosterols and 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, moisturizers, emollients, active lipophilic molecules, active hydrophilic molecules, thickeners and film-forming molecules. The cosmetic product comprises the vesicle concentrate cosmetic composition and any other cosmetically acceptable ingredients.

[0005] Phytosterols, primarily found in plant cell membranes, can flexibly regulate interactions between phospholipid molecules, maintaining appropriate fluidity in liposome membranes at varying temperatures, preventing the membrane from becoming too loose or too tight, and ensuring the structural stability of biomimetic sebum membrane compositions. Furthermore, due to their structural similarity to cholesterol, a key component of sebum membranes, phytosterols can directly participate in protecting and rebuilding damaged sebum membranes. Phytosterols also possess anti-inflammatory properties, alleviating inflammation caused by damaged sebum membranes and promoting their recovery. Therefore, phytosterols stabilize the structure of biomimetic sebum membrane compositions while enhancing their repair and penetration-enhancing properties. When present together with cholesterol, phytosterols exhibit a synergistic effect, further stabilizing the liposome structure and resisting damage from external factors such as temperature fluctuations and mechanical stress. Zhao Guozhi et al., in "Development and Utilization of Phytosterols and Their Products (Part 2)" (Grain and Oils, 2006, Vol. 3, pp. 3-8), noted that phytosterols, such as soybean sterols, are widely used in cosmetic formulations such as shaving creams, moisturizers, skin cleansers, and hair sprays.

[0006] Therefore, overcoming the poor stability of existing bionic sebum membrane compositions and providing a highly stable, low-irritation sebum-like lipid carrier system with the functions of repairing the skin barrier and promoting the penetration of active ingredients is a hot topic in current skin care product research and development. Summary of the Invention

[0007] To address these shortcomings, the present invention provides biomimetic sebum membrane lipid nanoparticles with repairing and penetration-enhancing properties, as well as a preparation method, applications, and products. These biomimetic sebum membrane lipid nanoparticles exhibit high high-temperature accelerated stability, exhibit no physical changes, and possess strong permeability and moisturizing properties, significantly repairing and / or preventing damage to the stratum corneum and sebum membrane.

[0008] To achieve the above-mentioned purpose of the invention, on the one hand, the present invention provides a bionic sebum membrane lipid nanoparticle with a repair function, which is composed of the following ingredients by weight: 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 remainder water; the weight content of phosphatidylcholine in the lecithin is ≥45%, and the particle size of the bionic sebum membrane lipid nanoparticle is ≤200nm.

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

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

[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 coconut oil alcohol caprylate / caprate.

[0013] Preferably, the triglyceride is selected from one or more of sedge 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, and grape seed oil.

[0014] More preferably, the triglyceride is selected from one or more of sedge oil, caprylic / capric triglyceride, meadowfoam seed oil, and macadamia nut oil.

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

[0016] As an example of the present invention, the triglyceride is a mixture of scutellaria baicalensis oil, meadowfoam seed oil and caprylic / capric triglyceride.

[0017] As an example of the present invention, the triglyceride is a mixture of scutellaria baicalensis oil, meadowfoam 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, campesterol, soya sterol and avenasterol.

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

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

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

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

[0025] As an example of the present invention, the sterols are cholesterol and campesterol.

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

[0027] Preferably, the ceramide is selected from one or more of ceramide NP, ceramide NS, ceramide NG, ceramide AS, ceramide AP, and 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 phosphatidylcholine (PC) content in the lecithin is ≥70%.

[0034] Preferably, 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, and octanoylhydroxamic 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, ethylhexylglycerol 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 jojoba oil and caprylic / capric triglyceride; the antioxidant is tocopherol; the sterol is one or more of cholesterol, rape sterol, soybean sterol, and 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; and the water is deionized water.

[0040] As some examples of the present invention, the wax ester is coconut oil caprylate / caprate; the triglyceride is one or more of smilax china oil, meadowfoam seed oil, macadamia nut oil, and caprylic / capric triglyceride; the antioxidant is tocopherol; the sterol is cholesterol; the ceramide is ceramide AP; 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; and the water is deionized water.

[0041] More preferably, the biomimetic sebum membrane lipid nanoparticles are composed of the following ingredients by weight: 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 7.5%-22.5% and the balance water

[0042] More preferably, the biomimetic sebum membrane lipid nanoparticles are composed of the following ingredients by weight: wax ester 9%-10%, triglyceride 16.5%-20%, squalane 4.5%-6%, sterol 0.5%-2%, ceramide 0.1%-0.25%, lecithin 2.5%-5%, antioxidant 0.1%-1%, polyol 10.5%-22.5% and the balance water.

[0043] Further preferably, the biomimetic sebum membrane lipid nanoparticles are composed of the following ingredients by weight: 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.

[0044] Preferably, the particle size of the biomimetic sebum membrane lipid nanoparticles is ≤200 nm.

[0045] More preferably, the particle size of the biomimetic sebum membrane lipid nanoparticles is ≤150 nm.

[0046] More preferably, the particle size of the biomimetic sebum membrane lipid nanoparticles is 80-150 nm.

[0047] In another aspect, the present invention provides a method for preparing the biomimetic sebum membrane lipid nanoparticles, comprising the following steps:

[0048] S1. Mix wax esters, triglycerides, lecithin, antioxidants, squalane, ceramides, and sterols and dissolve them into an oil solution at 55-80°C;

[0049] S2, mixing the polyol with water to form an aqueous phase;

[0050] S3. Mixing, emulsifying, and homogenizing the oil phase obtained in step S1 and the water phase obtained in step S2 to obtain biomimetic sebum membrane lipid nanoparticles.

[0051] Preferably, in step S1, the mixing is stirring and dissolving, and the temperature of the stirring and dissolving is 55-80°C, more preferably 65-75°C, and even more preferably 70°C; the speed of the stirring and dissolving is 50-400rpm, more preferably 200-400rpm; the time of the stirring and dissolving is 10-120min, more preferably 15-30min.

[0052] 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 50-400rpm, more preferably 200-400rpm; the time of the stirring and dissolving is 5-30min, more preferably 10-15min.

[0053] 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 50-400rpm, more preferably 100-200rpm; the time of the stirring and dissolving is 10-30min, more preferably 10-15min.

[0054] Preferably, in step S3, the emulsification conditions are 55-80° C., 1000-8000 rpm, and emulsification for 5-30 min.

[0055] More preferably, in step S3, the emulsification conditions are 70° C., 3000-6000 rpm, and emulsification for 5-15 min.

[0056] Preferably, in step S3, the homogenization is performed by a high-pressure homogenizer or microfluidizer.

[0057] More preferably, in step S3, the homogenization is performed by a high-pressure homogenizer, and the homogenization conditions are 700-1500 bar and 3-8 homogenization cycles.

[0058] In another aspect, the present invention provides use of the bionic sebum membrane lipid nanoparticles or the bionic sebum membrane lipid nanoparticles prepared by the above method in the production of cosmetics.

[0059] In a final aspect, the present invention provides a cosmetic comprising the biomimetic sebum membrane lipid nanoparticles or the biomimetic sebum membrane lipid nanoparticles prepared by the above method.

[0060] The dosage form of the cosmetic includes but is not limited to emulsion, ointment and the like.

[0061] The beneficial effects of the present invention are:

[0062] (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.

[0063] (2) The sterols and lecithin added in the present invention have a synergistic effect, making the bionic sebum membrane lipid nanoparticles more stable and having a more effective repair effect.

[0064] (3) The biomimetic sebum membrane lipid nanoparticles provided by the present invention can more effectively promote the skin penetration and absorption of other water-soluble active ingredients in cosmetics. BRIEF DESCRIPTION OF THE DRAWINGS

[0065] Figure 1 A photograph of a cell scratch experiment; the dotted line indicates the boundary between the cell and the scratch.

[0066] Figure 2 Fluorescent photos of the experiment to evaluate the transdermal effect of fluorescent labeling. DETAILED DESCRIPTION

[0067] Terms and Claims of the Present Invention:

[0068] 1. The articles "a", "an" and "the" include plural referents unless expressly limited to one or more referents otherwise.

[0069] 2. Numerical ranges: Unless expressly stated otherwise, all ranges or ratios disclosed herein are to be understood to include any and all subranges or subratios contained therein. For example, a range or ratio stated as 1 to 30 is to be considered inclusive of any and all subranges or subratios, integers, decimals, or subranges or subratios comprised therein, between a minimum of 1 and a maximum of 30, including any subranges or subratios, integers, decimals, or subranges or subratios comprised therein.

[0070] The following non-limiting examples are provided to enable those skilled in the art to more fully understand the present invention, but are not intended to limit the present invention in any way. The following are merely illustrative of the scope of the present invention, and those skilled in the art may make various changes and modifications to the present invention based on the disclosed content, which should also fall within the scope of the present invention.

[0071] The present invention will be further described below by way of specific examples. The various chemical reagents used in the examples of the present invention were obtained through conventional commercial channels unless otherwise specified. Unless otherwise specified, the contents described below are all by weight. Unless otherwise specified, it is understood that the experiments were conducted at room temperature.

[0072] In the following examples, some reagents are from the following sources:

[0073] Soybean lecithin (PC content 70%) was purchased from Shenyang Tianfeng Biopharmaceutical Co., Ltd. with the product number SD-240501.

[0074] Examples 1 to 11 provide biomimetic sebum membrane lipid nanoparticles with repairing and penetration-promoting effects. The formulas thereof are shown in Tables 1 and 2. The content of each raw material in the formula table (including Tables 1 and 2) is in g (“ / ” indicates that the ingredient is not contained).

[0075] Table 1

[0076]

[0077] Table 2

[0078]

[0079] The components in Table 1 and Table 2 were used to obtain biomimetic sebum membrane lipid nanoparticles according to the following steps:

[0080] S1. Mix wax esters, triglycerides, lecithin, antioxidants, squalane, ceramide, and sterols, and dissolve them by stirring at 200 rpm for 30 min at 70°C to form an oil solution;

[0081] S2. Add glycerol and polyol to deionized water, stir at 200 rpm for 15 min at 70°C to dissolve and form an aqueous phase;

[0082] S3. The oil phase formed in step S1 was mixed with the aqueous phase formed in step S2, and the mixture was emulsified at 4000 rpm for 5 min at 70° C., and then homogenized at 800 bar for 4 times to obtain biomimetic sebum membrane lipid nanoparticles. The particle size of the biomimetic sebum membrane lipid nanoparticles was measured using a laser particle size analyzer.

[0083] The average particle size of the biomimetic sebum membrane lipid nanoparticles obtained in each group in Table 1 and Table 2 is shown in Table 3.

[0084] Table 3

[0085]

[0086] Comparative Example 1

[0087] Compared with Example 1, the only difference is that sterol is not used and 3 g of soybean lecithin is used instead, and the rest are the same.

[0088] The biomimetic sebum membrane lipid nanoparticles were obtained by the following steps:

[0089] S1. Mix wax esters, triglycerides, lecithin, antioxidants, squalane, and ceramide, and dissolve them by stirring at 200 rpm at 70°C for 30 min to form an oil solution;

[0090] S2. Add glycerol and polyol to deionized water, stir at 200 rpm for 15 min at 70°C to dissolve and form an aqueous phase;

[0091] S3. The oil phase formed in step S1 was mixed with the aqueous phase formed in step S2, and the mixture was emulsified at 4000 rpm for 5 min at 70° C., and then homogenized at 800 bar for 4 times to obtain biomimetic sebum membrane lipid nanoparticles. The particle size of the biomimetic sebum membrane lipid nanoparticles was measured using a laser particle size analyzer.

[0092] The laser particle size analyzer test showed that the average particle size of the bionic sebum membrane lipid nanoparticles was 134 nm.

[0093] Comparative Example 2

[0094] Compared with Example 1, the only difference is that soybean lecithin is not used and 3 g of soybean sterol is used instead, and the rest are the same.

[0095] Prepare as follows:

[0096] S1. Mix wax esters, triglycerides, antioxidants, squalane, sterols, and ceramide, and dissolve them by stirring at 200 rpm for 30 min at 70°C to form an oil solution;

[0097] S2. Add glycerol and polyol to deionized water, stir at 200 rpm for 15 min at 70°C to dissolve and form an aqueous phase;

[0098] S3. The oil phase formed in step S1 was mixed with the aqueous phase formed in step S2, and the mixture was emulsified at 4000 rpm for 5 min at 70° C., and then homogenized at 800 bar for 4 times to obtain biomimetic sebum membrane lipid nanoparticles. The particle size of the biomimetic sebum membrane lipid nanoparticles was measured using a laser particle size analyzer.

[0099] After testing, this method was unable to emulsify and form a uniform emulsion.

[0100] Comparative Example 3

[0101] Compared with Example 1, the only difference is that lecithin is not used and 2.5 g of sucrose stearate is added, and the rest are the same.

[0102] The biomimetic sebum membrane lipid nanoparticles were obtained by the following steps:

[0103] S1. Mix wax esters, triglycerides, sucrose stearate, antioxidants, squalane, ceramide, and sterols, and dissolve them by stirring at 200 rpm for 30 min at 70°C to form an oil solution;

[0104] S2. Add glycerol and polyol to deionized water, stir at 200 rpm for 15 min at 70°C to dissolve and form an aqueous phase;

[0105] S3. The oil phase formed in step S1 was mixed with the aqueous phase formed in step S2, and the mixture was emulsified at 4000 rpm for 5 min at 70° C., and then homogenized at 800 bar for 4 times to obtain biomimetic sebum membrane lipid nanoparticles. The particle size of the biomimetic sebum membrane lipid nanoparticles was measured using a laser particle size analyzer.

[0106] The laser particle size analyzer test showed that the average particle size of the bionic sebum membrane lipid nanoparticles was 112 nm.

[0107] Comparative Example 4

[0108] Compared with Example 1, the only difference is that lecithin is not used and 2.5 g of polyglyceryl-10 laurate is added, and the rest are the same.

[0109] The biomimetic sebum membrane lipid nanoparticles were obtained by the following steps:

[0110] S1. Mix wax esters, triglycerides, polyglyceryl-10 laurate, antioxidants, squalane, ceramide, and sterols, and dissolve them by stirring at 200 rpm for 30 min at 70°C to form an oil solution;

[0111] S2. Add glycerol and polyol to deionized water, stir at 200 rpm for 15 min at 70°C to dissolve and form an aqueous phase;

[0112] S3. The oil phase formed in step S1 was mixed with the aqueous phase formed in step S2, and the mixture was emulsified at 4000 rpm for 5 min at 70° C., and then homogenized at 800 bar for 4 times to obtain biomimetic sebum membrane lipid nanoparticles. The particle size of the biomimetic sebum membrane lipid nanoparticles was measured using a laser particle size analyzer.

[0113] The laser particle size analyzer test showed that the average particle size of the bionic sebum membrane lipid nanoparticles obtained was 105 nm.

[0114] Effect evaluation

[0115] 1. Cell scratch repair test.

[0116] By creating a scratch on a monolayer of cells, the cells at the edge of the scratch gradually fill in the blank area, causing the scratch to "heal", simulating the migration process of cells in the body to a certain extent. By treating cells with different substances, the effects of these substances on cell migration ability can be studied. The physiological activities of cell migration in the body include the healing effect of tiny wounds, which is similar to the purpose of cosmetics to lighten skin texture and promote the healing of skin injuries. At the same time, human keratinocytes are the core constituent cells of the stratified epithelial tissue in the epidermis, and the results of their model can reflect the physiological characteristics of the skin barrier function and repair mechanism. By using human keratinocytes for cell migration experiments, the efficacy of cosmetics in enhancing epidermal repair can be evaluated by assessing the cell re-epithelialization ability.

[0117] The specific experimental methods are as follows:

[0118] Prepare a 6-well plate and mark the back with a horizontal line using a marker. Select well-grown human keratinocytes (HaCaT, Beina Biotech), digest them, dilute them to an appropriate concentration, add them to the plate, and incubate them in an incubator for approximately 24 hours. Dilute the samples with culture medium. For the sample groups (Example 1, Comparative Example 1, Comparative Example 3, and Comparative Example 4), dilute them 500-fold and add culture medium containing 2% serum. For the positive control group, add culture medium containing 10% serum. For the blank control group, add culture medium containing 2% serum. Incubate the cell culture plate in an incubator for approximately 24 hours. Once the cells are confluent, scratch them with a 200 µL pipette tip. After scratching, gently rinse three times with PBS to remove floating cells. Immediately after the scratch, take a photo. After taking the photo, aspirate the PBS.

[0119] The blank control group consisted of a culture medium supplemented with 2% serum. The positive control group consisted of a culture medium supplemented with 10% serum. Example 1, Comparative Example 1, Comparative Example 3, and Comparative Example 4 groups, respectively, consisted of a culture medium supplemented with 0.2% of the biomimetic sebum membrane lipid nanoparticles prepared in the corresponding group and 2% serum.

[0120] Place the cells back in the incubator and continue incubating for 24 h. After incubation, gently wash with PBS three times and use the same magnification objective lens to take pictures of the same position for 24 h.

[0121] Cell migration through scratch wounds Figure 1 As shown in the figure, the cell migration ability of the Example 1 group is close to that of the positive control group. The cell migration ability of the Comparative Example 1 group is significantly reduced due to the removal of sterols. The cell migration ability of the Comparative Examples 3 and 4 is significantly reduced by replacing lecithin with non-ionic emulsifiers sucrose stearate and polyglycerol-10 laurate, respectively. In summary, it can be seen that Example 1 of the present invention has a good repair effect.

[0122] 2. Promote the transdermal permeation and absorption test of water-soluble active ingredients

[0123] Using ex vivo Panamanian suckling pig skin as a carrier and a Franz diffusion cell, FITC-labeled cono peptide (purchased from Shanghai Chupeptide Biotechnology Co., Ltd., purity 98%) was used as a water-soluble active ingredient model to test the penetration-enhancing effect of biomimetic sebum membrane lipid nanoparticles on cono peptide.

[0124] The labeled cono peptides were administered to the surface of suckling pig skin according to the experimental groups. After 6 hours of penetration, the sections were fixed and the location of the penetration of the test substance into the skin was observed under a fluorescence microscope. The fluorescence accumulation below the stratum corneum in the sections was statistically analyzed using software, and the percentage of fluorescence intensity accumulation increase was processed.

[0125] The specific groups are:

[0126] The control group was given 0.01% conopeptide aqueous solution;

[0127] The Example group is an aqueous solution containing 0.01% cono peptide and 5% by weight concentration of biomimetic sebum membrane lipid nanoparticles prepared in the Example;

[0128] The comparative example group was an aqueous solution of 0.01% conopeptide + lipid nanoparticles prepared in the comparative example with a weight concentration of 5%.

[0129] Fluorescent photos of the experiment to evaluate the effect of fluorescent labeling on transdermal performance Figure 2 As shown. It can be seen that in the control group, the fluorescently labeled cono peptide basically stayed on the stratum corneum without adding biomimetic sebum membrane lipid nanoparticles, and it was difficult to overcome the stratum corneum barrier; in Example 1 group, due to the addition of biomimetic sebum membrane lipid nanoparticles, the fluorescently labeled cono peptide can more effectively overcome the stratum corneum barrier, penetrate below the stratum corneum, and can be evenly distributed, which can significantly improve the osmotic absorption of cono peptide; in the comparative example 1 group, the lipid nanoparticles for removing sterols were added, and although the fluorescently labeled cono peptide could also penetrate below the stratum corneum, the overall accumulated fluorescence intensity was much weaker; in the comparative example 3 group and the comparative example 4 group, lipid nanoparticles containing other emulsifiers that replaced lecithin were added, and the fluorescently labeled cono peptide basically stayed in the stratum corneum, and the fluorescence intensity below the stratum corneum was relatively weak. This shows that Example 1 of the present invention has a very significant effect of promoting the osmotic absorption of water-soluble active substances in cosmetic formulas.

[0130] Furthermore, the 6-hour transdermal fluorescence intensity was statistically analyzed using image processing software, and the percentage increase in transdermal penetration was calculated compared to the control group. The results are shown in Table 4 below.

[0131] Table 4

[0132]

[0133] It can be seen that the biomimetic sebum membrane lipid nanoparticles provided by each embodiment of the present invention, when added to the fluorescently labeled cono peptide aqueous solution, have a higher 6-hour transdermal penetration enhancement effect on the fluorescently labeled cono peptide. Compared with the control group, the transdermal penetration increase percentage of Example 1 is the highest, reaching 97.2%. The 6-hour transdermal penetration increase percentages of Comparative Examples 1, 3, and 4 are all lower than those of the embodiments.

[0134] Finally, it should be noted that the above content is only used to illustrate the technical solution of the present invention, rather than to limit the scope of protection of the present invention. Simple modifications or equivalent substitutions of the technical solution of the present invention by ordinary technicians in this field do not deviate from the essence and scope of the technical solution of the present invention.

Claims

1. A bionic sebum membrane lipid nanoparticle with a repairing function, characterized in that: The composition is composed of the following ingredients by weight: 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; the weight content of phosphatidylcholine in the lecithin is greater than 70%, and the particle size of the biomimetic sebum membrane lipid nanoparticles is ≤200nm; The triglyceride consists of 10% of jojoba oil and 6.5% of caprylic / capric triglyceride by weight, the wax ester is jojoba seed oil, the sterol is soybean sterol, the ceramide is ceramide NP, the lecithin is soybean lecithin, and the polyol consists of 2% of 1,2-pentanediol, 0.5% of 1,2-hexanediol and 8% of glycerol.

2. The method for preparing biomimetic sebum membrane lipid nanoparticles according to claim 1, wherein: The following steps are involved: S1. Mix wax esters, triglycerides, lecithin, antioxidants, squalane, ceramides, and sterols and dissolve 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 aqueous phase obtained in step S2 to obtain biomimetic sebum membrane lipid nanoparticles.

3. Use of the biomimetic sebum membrane lipid nanoparticles according to claim 1 or the biomimetic sebum membrane lipid nanoparticles obtained by the preparation method according to claim 2 in cosmetic production.

4. A cosmetic, characterized in that: The cosmetic contains the biomimetic sebum membrane lipid nanoparticles according to claim 1 or the biomimetic sebum membrane lipid nanoparticles obtained by the preparation method according to claim 2.

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