Skin barrier repairing and whitening composition, vesicle and preparation method and application thereof
By utilizing the synergistic mechanism of camellia seed oil, palm fruit oil, oxidized resveratrol, and palmate kelp extract, nanovesicles were prepared, solving the problem of poor efficacy when simply combining whitening ingredients and barrier repair ingredients. This achieved the dual effects of whitening and barrier repair, with improved transdermal penetration rate and good stability.
Patent Information
- Application Number
- CN202511697334.3
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-11-19
- Publication Date
- 2026-02-24
AI Technical Summary
Existing whitening and barrier repair ingredients are simply combined, which cannot effectively achieve both whitening and skin barrier repair effects. Furthermore, traditional transdermal absorption has low absorption rate, poor stability, and potential irritation.
By utilizing the synergistic mechanism of camellia seed oil, palm fruit oil, oxidized resveratrol and palmate seaweed extract, and through lipid dual-track synergy and dual antioxidant barrier, the transdermal rate and barrier function recovery are optimized, and nanovesicles are prepared to achieve non-irritating permeation promotion.
It achieves the dual effects of whitening and barrier repair, improves the transdermal penetration rate, has a long-lasting and stable effect, does not cause hyperpigmentation, and the vesicle structure avoids the barrier damage caused by traditional chemical penetration enhancers.
Smart Images

Figure CN121550089A_ABST
Abstract
Description
Technical Field
[0001] This invention relates to the field of cosmetic technology, and in particular to a skin barrier repair and whitening composition, vesicles, preparation method and application thereof. Background Technology
[0002] With increasing environmental pollution, enhanced ultraviolet radiation, and rising life stress, modern people's skin faces multiple problems, including pigmentation, impaired barrier function, and sensitivity to external stimuli. Among these, skin whitening, as an important skincare need to improve uneven skin tone, fade dark spots, and enhance skin texture, has long received widespread attention. Traditional whitening ingredients such as vitamin C and its derivatives, arbutin, and kojic acid, while having some effect, generally suffer from poor stability, low transdermal absorption, single target, or potential irritation. These limitations make it difficult to achieve highly effective whitening while maintaining a healthy skin barrier, which is fundamental to maintaining healthy skin.
[0003] Therefore, developing a composition with excellent transdermal penetration, high-efficiency whitening, and synergistic skin barrier repair capabilities has become a technical challenge. In existing technologies, whitening and barrier repair ingredients are often simply combined, failing to achieve both whitening and skin barrier repair effects effectively. Summary of the Invention
[0004] Based on this, the purpose of the present invention is to overcome the shortcomings of the prior art and provide a skin barrier repair and whitening composition, vesicles, preparation method and application thereof.
[0005] To achieve the above objectives, the technical solution adopted by the present invention is as follows: a skin barrier repair and whitening composition, comprising the following components in parts by weight: 0.1-8 parts of camellia seed oil, 0.1-5 parts of mulberry fruit oil, 0.5-5 parts of oxidized resveratrol, and 0.1-8 parts of palmate kelp extract.
[0006] This application provides a skin barrier repair and whitening composition, in which four active ingredients achieve multiple effects through a synergistic mechanism. Camellia seed oil and morrhagic palm fruit oil form a lipid dual-track synergy: the oleic acid in camellia seed oil rapidly fills the lipid defects in the stratum corneum, repairing the stratum corneum structure, while the ω-7 palmitoleic acid in morrhagic palm fruit oil, through its monounsaturated fatty acid chain highly matched with the lipids of the stratum corneum, significantly enhances the fluidity of the lipid bilayer. Together, they form a lipid membrane with optimized permeability in the stratum corneum, increasing the transdermal penetration rate of oxidized resveratrol and palmate seaweed extract in the composition. Simultaneously, the stratum corneum repaired by camellia seed oil provides a stable microenvironment for the activation of FLG expression by palmate seaweed extract, significantly promoting the recovery of barrier function. Morrhagic palm fruit oil and oxidized resveratrol form a surface-deep dual antioxidant barrier: morrhagic palm fruit oil rapidly scavenge surface free radicals, while oxidized resveratrol penetrates into the dermis to inhibit ROS generation. Together, they synergistically inhibit lipid oxidation and enhance the whitening effect. This sophisticated synergistic mechanism enables the combination of four ingredients to achieve synergistic effects, resulting in the dual benefits of whitening and barrier repair, with long-lasting and stable effects without causing post-inflammatory hyperpigmentation.
[0007] Optionally, the camellia seed oil is in the range of 0.1 parts, 0.5 parts, 1 part, 2 parts, 3 parts, 5 parts, 6 parts, and 8 parts by weight, or any two of these values; the morrhagic palm fruit oil is in the range of 0.1 parts, 0.5 parts, 1 part, 2 parts, 3 parts, and 5 parts by weight, or any two of these values; the resveratrol oxide is in the range of 0.1 parts, 0.5 parts, 1 part, 2 parts, 3 parts, and 5 parts by weight, or any two of these values; and the kelp extract is in the range of 0.1 parts, 0.5 parts, 1 part, 2 parts, 3 parts, 5 parts, 6 parts, and 8 parts by weight, or any two of these values.
[0008] Preferably, the skin barrier repair and whitening composition comprises the following components in parts by weight: 1-4 parts camellia seed oil, 0.5-2 parts morrhagic palm fruit oil, 0.8-1.5 parts oxidized resveratrol, and 1-4 parts palmate kelp extract.
[0009] The present invention has found that the weight proportions of the components in the skin barrier repair and whitening composition have a significant impact on the performance of the product. When the weight proportions of the components are further selected within the above range, the resulting product has better whitening and barrier repair effects, and the product has better durability.
[0010] Preferably, in the skin barrier repair and whitening composition, the weight ratio of camellia seed oil to mahogany fruit oil is (2-3):1. Optionally, the weight ratio of camellia seed oil to mahogany fruit oil is one or any two of the following: 2:1, 2.2:1, 2.5:1, 2.8:1, and 3:1.
[0011] This invention has found that when the weight ratio of camellia seed oil and morrhagic palm fruit oil in the skin barrier repair and whitening composition is within the above-mentioned range, the two work together to construct an intelligent lipid membrane in the stratum corneum that combines integrity and permeability. The oleic acid in camellia seed oil quickly fills lipid defects, repairs the barrier, and reduces moisture loss; while the ω-7 palmitoleic acid in morrhagic palm fruit oil moderately enhances the fluidity of the lipid bilayer, promotes the efficient penetration of oxidized resveratrol and palmate seaweed extract, resulting in a product with better whitening and barrier repair effects, and better long-lasting effects.
[0012] Preferably, the preparation method of the palmate kelp extract includes the following steps: (1) After crushing the palmate kelp, add it to deionized water, and add cellulase and alginate lyase to perform enzymatic hydrolysis to obtain the hydrolysate. (2) Add activated EM bacteria and nitrogen source to the enzymatic hydrolysate, ferment and culture, centrifuge, collect the supernatant, concentrate and dry to obtain the palmate kelp extract.
[0013] Preferably, the weight ratio of cellulase to alginate lyase is 1:(1-2). Optionally, the weight ratio of cellulase to alginate lyase is one of 1:1, 1:5, 1:2, or any combination thereof.
[0014] Preferably, the total amount of enzyme added is 0.2%-0.8% of the total mass of palmate kelp and deionized water.
[0015] Preferably, the enzymatic hydrolysis temperature is 35-45℃, and the enzymatic hydrolysis time is 4-8h; the enzymatic hydrolysis temperature is one or any two of 35℃, 38℃, 40℃, and 45℃; and the enzymatic hydrolysis time is one or any two of 4h, 5h, 6h, 7h, and 8h.
[0016] Preferably, the pH value of the enzymatic hydrolysis is 6.5-7.5; the pH value of the enzymatic hydrolysis is a range of one or any two of 6.5, 6.8, 6.9, 7.0, and 7.5.
[0017] Preferably, in the preparation method of the skin barrier repair and whitening composition, the weight ratio of the palmate kelp to deionized water is 1:(8-12). Optionally, the weight ratio of the palmate kelp to deionized water is one or any two of the following: 1:8, 1:9, 1:10, 1:11, 1:12.
[0018] Preferably, in the preparation method of the skin barrier repair and whitening composition, the nitrogen source includes at least one selected from soy milk, beef extract, peptone, ammonium sulfate, ammonium chloride, and urea. Preferably, in the preparation method of the skin barrier repair and whitening composition, the weight ratio of the enzymatic hydrolysate, EM agent, and nitrogen source is enzymatic hydrolysate:EM agent:nitrogen source = 100:(0.5-5):(0.1-1). Optionally, the weight ratio of the enzymatic hydrolysate, EM agent, and nitrogen source is one or any two of the following: 100:0.5:0.1, 100:1:0.5, 100:2:0.8, 100:3:0.5, 100:4:1, and 100:5:0.1.
[0019] Preferably, in the preparation method of the skin barrier repair and whitening composition, the fermentation temperature is 35-45℃, and the fermentation time is 24-48h. Optionally, the fermentation temperature is a range of 35℃, 38℃, 40℃, 45℃, or any two of these values; and the fermentation time is a range of 24h, 30h, 35h, 40h, 48h, or any two of these values.
[0020] This invention reveals that kelp extract, prepared using enzymatic hydrolysis and EM (Effective Microorganisms) fermentation, yields an extract with unique biological activity that exhibits synergistic effects with camellia seed oil, palmetto fruit oil, and oxidized resveratrol. On one hand, the addition of cellulase and alginate lyase effectively disrupts the cell wall structure of kelp, releasing more active ingredients such as fucoidan and sulfated polysaccharides. EM agents, a complex microbial community, can transform large-molecule active substances into smaller, more permeable molecules, such as oligosaccharides and organic acid metabolites. These significantly reduced molecular weight active ingredients possess stronger hydrophilicity and membrane permeability. On the other hand, the organic acids (such as lactic acid and acetic acid) and microbial metabolites produced during EM fermentation have a slight "physiological permeation-enhancing" effect. These components can moderately regulate the pH of the stratum corneum, loosen the lipid arrangement between keratinocytes, increase the fluidity of the lipid bilayer, and work synergistically with ω-7 palmitoleic acid in morrhagic palm fruit oil and oleic acid in camellia seed oil to further reduce the barrier resistance of the stratum corneum, creating favorable conditions for the penetration of active ingredients such as oxidized resveratrol.
[0021] This invention uses an enzymatic hydrolysis + EM bacteria fermentation method to prepare palmate kelp extract, which, in synergy with camellia seed oil, palm fruit oil and oxidized resveratrol, results in a product with superior whitening and barrier repair effects.
[0022] In addition, the present invention provides a vesicle containing the aforementioned skin barrier repair and whitening composition.
[0023] Preferably, the vesicles further contain amphiphilic nonionic surfactants, phytosterols, polyols, and stabilizers; Furthermore, the camellia seed oil, morrhagic palm fruit oil, amphiphilic nonionic surfactant, and phytosterols form the oil phase of vesicles; The palmate kelp extract, oxidized resveratrol, polyols and stabilizers form the aqueous phase of vesicles; The oil phase has a mass percentage of 5-15% in the vesicles, and the aqueous phase has a mass percentage of 85-95% in the vesicles.
[0024] Optionally, the mass percentage of the oil phase in the vesicle is a range of 5%, 8%, 10%, 12%, 15%, or any two of these values.
[0025] Optionally, the mass percentage of the aqueous phase in the vesicle is one or any two of 85%, 88%, 90%, 92%, and 95%.
[0026] This invention provides a non-irritating transdermal nanovesicle. The fluid lipid bilayer membrane of the vesicle adopts a liquid crystal structure. Its semi-solid-liquid equilibrium characteristic allows the membrane to temporarily lower the melting point of intercellular lipids in the stratum corneum upon contact with the skin, softening the stratum corneum without damaging its structural integrity. The water activity within the membrane is higher than that of dry skin, creating an osmotic pressure difference that drives the passive diffusion of active ingredients into the depths of the stratum corneum, avoiding barrier damage caused by traditional chemical penetration enhancers that dissolve lipids or dilate pores. The vesicles provided by this invention can achieve stable, zero-irritation penetration enhancement at room temperature, significantly improving the delivery efficiency of functional ingredients, and simultaneously achieving the triple effects of anti-oxidation, whitening, and barrier repair, with long-lasting and stable efficacy.
[0027] This invention prepares nanovesicles using amphiphilic nonionic surfactants, phytosterols, and stabilizers. The amphiphilic nonionic surfactants promote nanostructure formation by reducing interfacial tension; the ethyl groups on the side chains of phytosterols enhance membrane fluidity regulation; and the stabilizers form a hydration layer, increasing vesicle stability and reducing irritation. The formation of the vesicle structure further improves delivery efficiency, thereby better achieving the triple effects of anti-oxidation, whitening, and barrier repair, with long-lasting and stable efficacy.
[0028] Preferably, the amphiphilic nonionic surfactant is at least one of lauryl ether-23, polysorbate-80, polysorbate-20, Span-80, poloxamer 188, and alkyl glycoside; and / or, the polyol is at least one of propylene glycol, butylene glycol, glycerol, polyethylene glycol, and polyglycerol; and / or, the stabilizer is at least one of trehalose, chitosan, hyaluronic acid, and hydroxypropyl-β-cyclodextrin.
[0029] Furthermore, the present invention provides a method for preparing the aforementioned vesicles, comprising the following steps: S1, Camellia seed oil, palm fruit oil, amphiphilic nonionic surfactant and phytosterol are dissolved in a solvent to obtain the oil phase; S2, after dissolving oxidized resveratrol and polyol, a mixture is obtained; palmate kelp extract and stabilizer are dissolved in deionized water, and the mixture is added at the same time. After mixing, an aqueous phase is obtained. S3, evaporate the oil phase to form a thin film, add the aqueous phase, sonicate to form a vesicle suspension, homogenize and cool to obtain the vesicle.
[0030] Preferably, in step S1, the weight ratio of camellia seed oil, morrhagic palm fruit oil, amphiphilic nonionic surfactant, and phytosterol is camellia seed oil: morrhagic palm fruit oil: amphiphilic nonionic surfactant: phytosterol = (5-10): (1-5): (5-15): 1. Optionally, the weight ratio of camellia seed oil, morrhagic palm fruit oil, amphiphilic nonionic surfactant, and phytosterol is one or any two of the following: 5:1:5:1, 10:5:10:1, 8:3:15:1.
[0031] Preferably, the solvent is a chloroform-methanol mixture, with a volume ratio of chloroform to methanol of 2:1, and the weight ratio of the mixture of camellia seed oil, morrhagic palm fruit oil, amphiphilic nonionic surfactant, and phytosterols to the solvent is 1:(10-20). Optionally, the weight ratio of the mixture to the solvent is one or any two of the following: 1:10, 1:12, 1:15, 1:18, and 1:20.
[0032] Preferably, in step S2, the weight ratio of resveratrol oxide to polyol is resveratrol oxide:polyol = 1:(3-8). Optionally, the weight ratio of resveratrol oxide to polyol is one or any two of the following: 1:3, 1:4, 1:5, 1:6, 1:8.
[0033] Preferably, the weight ratio of the palmate kelp extract, stabilizer, and deionized water is palmate kelp extract: stabilizer: deionized water = (2-8):1:(60-120). Optionally, the weight ratio of the palmate kelp extract, stabilizer, and deionized water is one or any combination of 2:1:60, 5:1:80, and 8:1:120.
[0034] Preferably, the weight percentage of the mixture is 5-20% based on the weight percentage of the aqueous phase. Optionally, the weight percentage of the mixture is a range of one or any two of 5%, 7%, 8%, 10%, 15%, 17%, 18%, and 20%.
[0035] Preferably, in step S3, the oil phase is transferred to a rotary evaporator and evaporated under reduced pressure in a water bath at 40-50°C to form a uniform thin film, wherein the vacuum degree is ≤0.1MPa and the rotation speed is 100-150 rpm.
[0036] Preferably, the ultrasonic treatment power is 150-250W and the ultrasonic treatment time is 5-15min.
[0037] Preferably, the homogenization pressure is 500-800 bar, and the temperature is reduced to 20-30°C.
[0038] The vesicles prepared by this invention have an average particle size of 180-210 nm and an encapsulation efficiency >85%. The average particle size and encapsulation efficiency of the vesicles prepared using the above method both meet the aforementioned requirements. Optionally, the average particle size of the vesicles is a range of 180 nm, 190 nm, 200 nm, 205 nm, and 210 nm, or any two of these values; the encapsulation efficiency is a range of 86%, 88%, 89%, and 90%, or any two of these values.
[0039] The average particle size of the vesicles was determined by dynamic light scattering (DLS), and the encapsulation efficiency of the vesicles was determined by ultrafiltration tube centrifugation.
[0040] Furthermore, the present invention provides the use of the skin barrier repair and whitening composition or the vesicles in the preparation of skin products.
[0041] In addition, the present invention provides a skin product comprising the skin barrier repair and whitening composition or the vesicles. Preferably, the skin product comprises any one of toner, lotion, cream, mask, serum, and spray.
[0042] This invention provides an emulsion comprising the following components in weight percentage: 3-10% skin barrier repair and whitening composition or vesicles, 0.05-0.8% thickener, 0.5-10% moisturizer, 0.5-20% oil, 0.5-5% emulsifier, 0.5-3% preservative, 0.01-0.3% pH adjuster, and the balance being water.
[0043] Preferably, it includes at least one of the following (a)-(f): (a) The thickener comprises at least one of xanthan gum, carbomer, polyacrylamide taurate, ammonium acryloyl dimethyl taurate / VP copolymer, and sclerotium gum; (b) The moisturizer comprises at least one of allantoin, propylene glycol, panthenol, β-glucan, trehalose, caprylyl glycol, dipropylene glycol, sodium hyaluronate, 1,3-butanediol, glycerin, budding cleavage enzyme polysaccharide, and ceramide; (c) The oils include at least one of squalane, isononyl isononanoate, caprylic / capric triglyceride, polydimethylsiloxane, jojoba oil, grape seed oil, shea butter, sunflower seed oil, and vitamin E.
[0044] (d) The emulsifier comprises at least one of cetearyl alcohol, glyceryl stearate, polyglycerol-10 diisostearate, cetearyl alcohol polyether-20, C12-20 alkyl glucoside, cetearyl glucoside, polysorbate-80, pentaerythritol tetraester, and sucrose stearate. (e) The preservative comprises at least one of 1,2-propanediol, 1,2-hexanediol, ethylhexylglycerin, p-hydroxyacetophenone, capryloyl hydroxamic acid, and phenoxyethanol; (f) The pH adjuster includes at least one of arginine and tromethamine.
[0045] Compared to existing technologies, the beneficial effects of this invention are as follows: This application provides a skin barrier repair and whitening composition, in which four active ingredients achieve multiple effects through a synergistic mechanism. Camellia seed oil and morrhagic palm fruit oil form a lipid dual-track synergy: the oleic acid in camellia seed oil rapidly fills the lipid defects in the stratum corneum, repairing the stratum corneum structure, while the ω-7 palmitoleic acid in morrhagic palm fruit oil, through its monounsaturated fatty acid chain highly matched with the lipids of the stratum corneum, significantly enhances the fluidity of the lipid bilayer. Together, they form a lipid membrane with optimized permeability in the stratum corneum, increasing the transdermal penetration rate of oxidized resveratrol and palmate seaweed extract in the composition. Simultaneously, the stratum corneum repaired by camellia seed oil provides a stable microenvironment for the activation of FLG expression by palmate seaweed extract, significantly promoting the recovery of barrier function. Morrhagic palm fruit oil and oxidized resveratrol form a surface-deep dual antioxidant barrier: morrhagic palm fruit oil rapidly scavenge surface free radicals, while oxidized resveratrol penetrates into the dermis to inhibit ROS generation. Together, they synergistically inhibit lipid oxidation and enhance the whitening effect. This sophisticated synergistic mechanism enables the combination of four ingredients to achieve synergistic effects, resulting in the dual benefits of whitening and barrier repair, with long-lasting and stable effects without causing post-inflammatory hyperpigmentation. Attached Figure Description
[0046] Figure 1 The image shows the skin whitening effect of the lotion in Example 1. Detailed Implementation
[0047] To better illustrate the purpose, technical solution, and advantages of this invention, the invention will be further described below in conjunction with the accompanying drawings and specific embodiments. The purpose is to provide a detailed understanding of the invention, not to limit it. All other embodiments obtained by those skilled in the art without inventive effort are within the scope of protection of this invention. Unless otherwise specified, the experimental reagents and instruments designed in the embodiments and comparative examples of this invention are commonly used reagents and instruments, all of which are commercially available. Unless otherwise specified, the experimental methods used in the embodiments and comparative examples are conventional methods; and unless otherwise specified, the raw materials used in parallel experiments are from the same batch.
[0048] The raw materials of this invention will now be further described, but are not limited to the following raw materials: Camellia seed oil: Ji'an Hairui Natural Plant Co., Ltd., purity: ≥99%; Palmyra fruit oil: Guangzhou Yanfu Biotechnology Co., Ltd., purity: ≥99%; Oxidized resveratrol: Shanghai Yuanye Biotechnology Co., Ltd., purity: ≥98%; Lauryl alcohol polyether-23: Shanghai Hengchen Industrial Co., Ltd., item number: TEGO Alkanol L 23 P; Phytosterols: Shanghai Yuanye Biotechnology Co., Ltd., Product No.: B61374; Trehalose: Hebei Kelongduo Biotechnology Co., Ltd.; Purity: ≥99%; Sunflower seed oil: Shanghai Yuanye Biotechnology Co., Ltd., product number: S24927; Jojoba oil: Shanghai Yuanye Biotechnology Co., Ltd., Product No.: S25041; Resveratrol: Shanghai Yuanye Biotechnology Co., Ltd., purity: ≥98%; Chlorella extract: Xi'an Tianguangyuan Biotechnology Co., Ltd., Product No.: Chlorella powder; EM stock solution: Zhengzhou Baiyibao Biotechnology Co., Ltd., Product No.: EM stock solution; Lactic acid bacteria: purchased from Jiangsu Xinshengao Biotechnology Co., Ltd., preservation number: CCTCC NO: M 2013511; Cellulase: Huazhong Haiwei (Beijing) Gene Technology Co., Ltd., enzyme activity: 50000U / g; Pectinase: Shanghai Yuanye Biotechnology Co., Ltd., enzyme activity: 50000U / g; Alginate lyase: Shanghai Huashang Xiangyang Biotechnology Co., Ltd., Product No.: alginate lyase, yellow powder, enzyme activity: 250,000 U / ml; Palmate kelp extract-1: self-made, the preparation method is as follows: (1) Palmate kelp is crushed and passed through a 100-mesh sieve and then added to deionized water. The weight ratio of palmate kelp to deionized water is 1:10. Cellulase and alginate lyase are added for enzymatic hydrolysis. The weight ratio of cellulase to alginate lyase is 1:1.5. Based on the total mass of palmate kelp and deionized water, the total amount of enzyme added accounts for 0.45% of the base. The hydrolysis temperature is 40℃ and the hydrolysis time is 6h. The pH value of the hydrolysis is 7.0, and the hydrolysate is obtained. (2) Activated EM bacteria and soy milk are added to the hydrolysate. The weight ratio of the hydrolysate, EM bacteria and nitrogen source is hydrolysate:EM bacteria:nitrogen source = 100:2:0.5. After fermentation at 40℃ for 24h, the mixture is centrifuged, the supernatant is collected, concentrated and dried to obtain the palmate kelp extract.
[0049] The activation method is as follows: Prepare a sterile culture medium with 10 g / L brown sugar, 5 g / L peptone and 2 g / L potassium dihydrogen phosphate, inoculate with EM bacterial stock solution at 1% inoculation amount (volume ratio), and culture on a shaker until OD600 reaches 0.4-0.6 as the termination mark.
[0050] Palmate kelp extract-2: self-made, the preparation method is as follows: (1) Palmate kelp is crushed and passed through a 120-mesh sieve and then added to deionized water. The weight ratio of palmate kelp to deionized water is 1:12. Cellulase and alginate lyase are added for enzymatic hydrolysis. The weight ratio of cellulase to alginate lyase is 1:2. Based on the total mass of palmate kelp and deionized water, the total amount of enzyme added accounts for 0.55% of the base. The hydrolysis temperature is 45℃ and the hydrolysis time is 8h. The pH value of the hydrolysis is 7.0, and the hydrolysate is obtained. (2) Activated EM agent (activation method is the same) and soy milk are added to the hydrolysate. The weight ratio of the hydrolysate, EM agent and nitrogen source is hydrolysate:EM agent:nitrogen source = 100:4:0.8. After fermentation at 45℃ for 48h, the mixture is centrifuged, the supernatant is collected, concentrated and dried to obtain the palmate kelp extract.
[0051] Palmate kelp extract-3: Compared with the preparation method of palmate kelp extract-1, the only difference is the type of enzyme used. Pectinase and alginate lyase are used, with a weight ratio of 1:1.5. The rest of the preparation method and dosage are exactly the same.
[0052] Palmate kelp extract-4: Prepared in-house. Compared with the preparation method of palmate kelp extract-1, the only difference is the type of enzyme used. Only cellulase is used. The amount of cellulase used is the same as the total amount of cellulase and alginate lyase used in palmate kelp extract-1. The rest of the preparation method and dosage are exactly the same.
[0053] Palmate kelp extract-5: Prepared in-house. Compared with the preparation method of palmate kelp extract-1, the only difference is the type of enzyme used. Only alginate lyase is used. The amount of alginate lyase used is the same as the total amount of cellulase and alginate lyase used in palmate kelp extract-1. The rest of the preparation method and dosage are exactly the same.
[0054] Laminaria japonica extract-6: prepared in-house. The preparation method is the same as Laminaria japonica extract-1, except for the bacteria used, which is lactic acid bacteria. The other preparation methods and dosages are exactly the same. The lactic acid bacteria activation method is as follows: the freeze-dried bacteria are washed with sterile sodium phosphate buffer (pH 6.0-6.5) and resuspended. They are then inoculated into MRS liquid medium at a 1% inoculation rate (volume ratio) and cultured on a shaker until the OD600 reaches 0.4-0.6.
[0055] Palmate kelp extract-7: self-made, extracted by hot water extraction method. (1) After crushing palmate kelp through a 100-mesh sieve, add it to deionized water to obtain a mixture. The weight ratio of palmate kelp to deionized water is 1:10. Control the extraction temperature at 60°C and the extraction time at 15 hours. Stir once every 1 hour to ensure that the kelp fragments are fully rolled. (2) Filter the mixture, centrifuge, take the supernatant, concentrate and dry to obtain the palmate kelp extract.
[0056] Examples and Comparative Examples Examples 1-11 and Comparative Examples 1-12 of this invention provide a skin barrier repair and whitening composition. The components and their weight parts in the skin barrier repair and whitening composition are shown in Tables 1-2 below. The preparation method of the skin barrier repair and whitening composition of Examples 1-11 and Comparative Examples 1-12 is as follows: the substances are thoroughly mixed evenly to obtain the skin barrier repair and whitening composition.
[0057] Table 1 Table 2 Example 12 A vesicle is prepared from the skin barrier repair and whitening composition corresponding to Example 1, comprising the following steps: S1, 2g of camellia seed oil, 0.8g of palm fruit oil, 2.5g of amphiphilic nonionic surfactant (lauryl alcohol polyether-23) and 0.3g of phytosterol were dissolved in 94.4mL of chloroform-methanol mixed solvent (volume ratio 2:1) to obtain the oil phase; S2, after dissolving 1g of oxidized resveratrol and 5g of polyol (propylene glycol), a mixture was obtained; 3g of palmate kelp extract and 1g of stabilizer (trehalose) were dissolved in 84.4mL of deionized water, and the mixture was added at the same time. After mixing, an aqueous phase was obtained. S3. The oil phase is transferred to a rotary evaporator and evaporated under reduced pressure in a 45°C water bath to form a uniform thin film (vacuum degree ≤0.1MPa, rotation speed 150 rpm). The aqueous phase is added, and the mixture is sonicated (power 200 W, time 10 minutes) to form a vesicle suspension. The suspension is then homogenized and cooled to 25°C at 600 bar to obtain the vesicles.
[0058] Example 13 A vesicle was prepared from the skin barrier repair and whitening composition corresponding to Example 1. The only difference was the choice of the amphiphilic nonionic surfactant used in the preparation process, which was Span 80. The other dosages and preparation methods were exactly the same.
[0059] Example 14 A vesicle was prepared from the skin barrier repair and whitening composition corresponding to Example 1. The only difference was the choice of amphiphilic polyol in the preparation process, which was glycerol. The other dosages and preparation methods were exactly the same.
[0060] Example 15 A vesicle was prepared from the skin barrier repair and whitening composition corresponding to Example 1. The only difference was the choice of stabilizer in the preparation process, which was chitosan (Aladdin, catalog number: C105799, degree of deacetylation ≥95%). The other dosages and preparation methods were exactly the same.
[0061] Example 16 A vesicle is prepared from the skin barrier repair and whitening composition corresponding to Example 2, comprising the following steps: S1, 3g of camellia seed oil, 1g of palm fruit oil, 4g of amphiphilic nonionic surfactant (lauryl alcohol polyether-23) and 0.5g of phytosterol were dissolved in 91.5mL of chloroform-methanol mixed solvent (volume ratio 2:1) to obtain the oil phase; S2, after dissolving 1.5g of oxidized resveratrol and 7g of polyol (propylene glycol), a mixture was obtained; 1g of palmate kelp extract and 0.4g of stabilizer (trehalose) were dissolved in 40.1mL of deionized water, and the mixture was added at the same time. After mixing, an aqueous phase was obtained. S3. The oil phase is transferred to a rotary evaporator and evaporated under reduced pressure in a 50°C water bath to form a uniform thin film (vacuum degree ≤0.1MPa, rotation speed 100 rpm). The aqueous phase is added, and the mixture is sonicated (power 180 W, time 15 minutes) to form a vesicle suspension. The suspension is then homogenized and cooled to 25°C at 550 bar to obtain the vesicles.
[0062] Application examples The present invention provides an emulsion in application examples, comparative application examples and blank application examples, the components (mass percentage) of the emulsion being shown in Table 3; In Application Examples 1-11, the skin barrier repair and whitening compositions used were those prepared in Examples 1-11, and in Application Examples 12-16, the vesicles used were those prepared in Examples 12-16. In Comparative Application Examples 1-12, the skin barrier repair and whitening compositions used were those prepared in Comparative Examples 1-12. For example, in Application Example 1, the skin barrier repair and whitening composition used was the one prepared in Example 1; in Application Example 2, the skin barrier repair and whitening composition used was the one prepared in Example 2; in Application Example 12, the vesicles used were those prepared in Example 12; in Comparative Application Example 1, the skin barrier repair and whitening composition used was the one prepared in Comparative Example 1, and so on.
[0063] The skin barrier repair and whitening composition used in Application Example 17 is the skin barrier repair and whitening composition prepared in Example 1.
[0064] The method for preparing the emulsion according to the present invention includes the following steps: (1) Mix the humectant and thickener with water and stir. Heat to 75±2℃ and homogenize at 1200 rpm for 4 min. After homogenization, keep warm for later use to obtain pre-prepared component A. (2) Mix the emulsifier with the oil and heat to 75±2℃ to obtain the pre-prepared component B; (3) Mix the preservatives and heat to 60±2℃ to melt them, to obtain the pre-prepared component C; (4) Heat the pre-prepared component A to 80±2℃, add the pre-prepared component B heated to 80±2℃ at 1200 rpm, homogenize, then cool to 60±2℃, add the pre-prepared component C at 250 rpm and stir to mix, then cool to 40℃ and add the skin barrier repair and whitening composition or vesicles and continue stirring for 8 min, finally add the remaining pH adjuster to adjust the pH to 6.0, then stop stirring, discharge the material, and obtain the emulsion.
[0065] The preparation methods of the emulsions provided in the other application examples, comparative application examples, and blank application examples are consistent with those in application example 1. If the relevant components are not available, they can be omitted.
[0066] Table 3 Performance Testing - 1 Transdermal Permeation Experiment Test samples: Skin barrier repair and whitening compositions or vesicles prepared in Examples 1-16 and Comparative Examples 1-12.
[0067] Experimental method: Ex vivo pig skin was used for testing, and the exposed skin area in the diffusion cell was 1.5 cm². 2 The receiving chamber volume was 5.0 mL. A 50:50 volume ratio of phosphate buffer solution (pH 5.8) to anhydrous ethanol was used as the receiving solution. 500 μL of sample was evenly applied to the skin and covered with a thin film to prevent evaporation. The transdermal absorption of oxidized resveratrol at different time points was measured by HPLC, and the cumulative permeation after 48 hours (in μg / cm³) was recorded. 2 The greater the cumulative amount of penetration, the better the skin permeability. The results are shown in Table 4 below.
[0068] Table 4 As can be seen from the table above, the skin barrier repair and whitening compositions or vesicles prepared in the examples and comparative examples all have good permeability. When the skin barrier repair and whitening compositions are prepared into vesicles, the permeability is even better.
[0069] As can be seen from the comparison of Examples 1-5, the weight percentage of the components in the skin barrier repair and whitening composition has a significant impact on the product's performance. When the weight percentage of the components is further selected within the range of "1-4 parts camellia seed oil, 0.5-2 parts mulberry fruit oil, 0.8-1.5 parts oxidized resveratrol, and 1-4 parts palmate kelp extract", the resulting products exhibit better penetration effects. Although the oxidized resveratrol content was high in Example 4, the amount of palmate kelp extract was too small, and the difference in the ratio of camellia seed oil and mulberry fruit oil was too large, resulting in poor penetration effects.
[0070] As can be seen from the comparison of Examples 1 and 6-11, the preparation method of palmate kelp extract will further affect the product penetration effect. When a specific enzymatic hydrolysis + EM bacteria fermentation method is used to prepare palmate kelp extract, the product penetration effect is better.
[0071] As can be seen from the comparison of Example 1 and Comparative Examples 1-12, the effects of the present invention cannot be achieved when one of the components is not added, or when other components are used to make up the difference while the component is not added; and when other similar ingredients are used as substitutes, or when the weight proportions of the components in the composition are not within the scope of this application, a good synergistic effect cannot be achieved. Among them, Comparative Example 8 does not contain palmate seaweed extract and is made up with oxidized resveratrol. Although the amount of oxidized resveratrol is extremely high, the penetration effect is poor, and the final maximum penetration accumulation is low.
[0072] Performance Testing - 2 In Vitro Stratum Corneum Inflammation Test to Verify Irritation Test samples: Skin barrier repair and whitening compositions or vesicles prepared in Examples 1-16 and Comparative Examples 1-12.
[0073] RHE model pretreatment: Place the RHE model in a 6-well plate, add complete culture medium (RPMI-1640 + 10% FBS + 1% antibiotic), and incubate at 37℃ and 5% CO2 for 24 hours to ensure model stability.
[0074] Test substance determination: Capsaicin preparation: First, dissolve in 5 mL of ethanol, then add 94.97 mL of pure water to obtain 0.03% capsaicin. Sample group: Apply 0.5 mL of 0.03% capsaicin to the surface of the RHE model, then apply the sample (0.5 mL) evenly to the surface of the RHE model. Set up a blank control (no test substance added) and a positive control (0.5 mL of 0.03% capsaicin). Exposure time: 45 minutes.
[0075] Post-culture stage: Remove residual material from the surface of the RHE model. Continue culturing the RHE model in the culture medium for 24 hours to simulate the in vivo environment.
[0076] Sample collection: The supernatant of the RHE model cultured for 24 hours after collection was used for the quantitative determination of IL-1α.
[0077] IL-1α ELISA assay: Determine the IL-1α level according to the operating procedures of the ELISA kit. Calculate the IL-1α inhibition rate (%) using the following formula: IL-1α inhibition rate (%) = (IL-1α content in positive control group - IL-1α content in sample group) / IL-1α content in positive control group × 100%.
[0078] The results are shown in Table 5.
[0079] Table 5 As can be seen from the table above, the skin barrier repair and whitening compositions or vesicles prepared in the examples and comparative examples have low irritation. When the skin barrier repair and whitening compositions are prepared into vesicles, the irritation is even lower.
[0080] As can be seen from the comparison of Examples 1-5, the weight parts of the components in the skin barrier repair and whitening composition have a significant impact on the performance of the product. When the weight parts of the components are further selected within the range of "1-4 parts of camellia seed oil, 0.5-2 parts of mulberry fruit oil, 0.8-1.5 parts of oxidized resveratrol, and 1-4 parts of palmate kelp extract", the resulting product has lower irritation.
[0081] A comparison of Examples 1 and 6-11 shows that the preparation method of *Kelpia palmata* extract further affects the product's irritation. When a specific enzymatic hydrolysis + EM fermentation method is used to prepare *Kelpia palmata* extract, the resulting product has lower irritation. *Kelpia palmata* extract-3 uses pectinase and alginate lyase. Pectinase acts differently from cellulase; it mainly decomposes pectin substances, thus reducing the release of the target component. Simultaneously, the release of new components may have some irritant properties, increasing the overall irritation. *Kelpia palmata* extracts-4 and 5 use only cellulase or alginate lyase, respectively. Compared to using both enzymes simultaneously, the action of a single enzyme may not completely destroy the cell wall, but it leads to the large release of certain specific components and a significant reduction in the target component. *Kelpia palmata* extract-6 differs only in the bacteria used, employing lactic acid bacteria. Lactic acid bacteria fermentation produces metabolites such as lactic acid. These metabolites may alter the chemical composition of the extract, introducing irritating substances or transforming some originally less irritating components into more irritating ones, resulting in higher irritation. Kelp extract-7 is produced using hot water extraction. During hot water extraction, the high temperature and prolonged extraction cause a large amount of various components in the kelp to dissolve, including some components that were not fully released or transformed during enzymatic hydrolysis and microbial fermentation. Furthermore, hot water extraction lacks selectivity, extracting components of various properties from the kelp, which may include a significant amount of irritating macromolecules and impurities. This mixture of components makes Kelp extract-7 significantly more irritating than other extracts obtained through enzymatic hydrolysis and microbial fermentation.
[0082] As can be seen from the comparison of Example 1 and Comparative Examples 1-12, the effect of the present invention cannot be achieved when one of the components is not added, or when other components are added to make up the difference while not adding the component; and when other similar components are substituted, or when the weight of the components in the composition is not within the scope of this application, the synergistic effect cannot be achieved.
[0083] Performance Test - 3 Melanin Production Inhibition Test Experimental methods: The cell line used was mouse melanoma cell line B16F10 (Wuhan Saiss Biotechnology Co., Ltd.). The test conditions were: incubator temperature 37±1℃, saturated humidity, and carbon dioxide 5±1%. Cells were cultured and treated according to groups, followed by testing. The specific test was the determination of melanin content in the cells, and the test method is as follows: (1) Seed the cell suspension into 6-well plates at a density of 1×10⁶ cells / well. 6 Cells / mL, cultured in DMEM medium (Gibco) for 24 hours; (2) Add 0.5 mL of pure water and 1.5 mL of DMEM culture medium to the blank control group, and add 0.5 mL of the skin barrier repair and whitening composition or vesicles prepared in Examples 1-16 and Comparative Examples 1-12 and 1.5 mL of DMEM culture medium to the sample group respectively. Collect the cells after culturing for 24 hours. (3) Determination of melanin content in cells: Cells were lysed at 80°C, and the total melanin content of each lysate was measured at a wavelength of 405 nm using an ELISA reader. The total protein concentration was calculated and the melanin content (OD value) was adjusted. The melanin content of the blank group (solvent control) was normalized and compared with that of the sample group. The melanin content of each example and comparative example was calculated using the following formula; Content inhibition rate: Melanin content inhibition rate (%) = (OD value of blank group - OD value of sample) / OD value of blank group × 100%; The test results are shown in Table 6 below.
[0084] Table 6 As can be seen from the table above, the skin barrier repair and whitening compositions or vesicles prepared in the examples and comparative examples all have good whitening effects. The whitening effect is even better when the skin barrier repair and whitening compositions are prepared into vesicles.
[0085] As can be seen from the comparison of Examples 1-5, the weight parts of the components in the skin barrier repair and whitening composition have a significant impact on the performance of the product. When the weight parts of the components are further selected within the range of "1-4 parts of camellia seed oil, 0.5-2 parts of palm fruit oil, 0.8-1.5 parts of oxidized resveratrol, and 1-4 parts of palmate kelp extract", the whitening effect of the product is better.
[0086] As can be seen from the comparison of Examples 1 and 6-11, the preparation method of palmate kelp extract will further affect the whitening effect of the product. When a specific enzymatic hydrolysis + EM bacteria fermentation method is used to prepare palmate kelp extract, the whitening effect of the product is better.
[0087] As can be seen from the comparison of Example 1 and Comparative Examples 1-12, the effect of the present invention cannot be achieved when one of the components is not added, or when other components are added to make up the difference while not adding the component; and when other similar components are substituted, or when the weight of the components in the composition is not within the scope of this application, the synergistic effect cannot be achieved.
[0088] Performance Testing - 4 Human Skin Patch Test In accordance with the "Cosmetic Safety Technical Specifications" (2015) for human skin patch testing, 33 volunteers aged 20-50 years were recruited. The test environment was a temperature of (21±1)℃ and a humidity of (50±10)%. Volunteers washed their forearms with water. After 10 minutes, when the moisture had evaporated, the testers applied 0.020-0.025mL of each sample emulsion (Application Examples 1-17, Control Application Examples 1-12, and Blank Application Examples) to each chamber of a 10-well patch applicator. The inner sides of both forearms of the volunteers were selected, avoiding the skin at the joints of the front and back of the hands. Each arm was covered with a patch applicator and marked accordingly. The patch application lasted for 24 hours. The patch applicators were removed, and any remaining sample was wiped off. Skin reactions were observed at 0.5h, 24h, and 48h, and the results were recorded according to the skin reaction grading standards in the "Cosmetic Safety Technical Specifications" (2015). Table 7 shows that skin reactions are divided into four rating levels. The higher the rating, the more severe the skin irritation reaction.
[0089] The test results are as follows: 0 cases of withdrawal and 0 cases of adhesive tape allergy were observed in the technical solution provided by this invention. No adverse reactions occurred in the application case, control application case, and blank application case.
[0090] Table 7 Performance Test 5: Composition's Barrier Repair Efficacy and Whitening Human Testing Test samples: emulsions prepared in Application Examples 1-17, Comparative Application Examples 1-12, and Blank Application Examples.
[0091] One hundred and fifty Asian adults aged 28-40 with sensitive skin and uniform facial pigmentation (such as melasma and sunspots) were selected and randomly divided into 30 groups of five. Volunteers applied the sample to their faces twice daily, morning and evening. Data was collected on day 0 (T0), day 14 (T14), and day 28 (T28). After 28 days of use, the sample was discontinued for 15 days, during which time basic moisturizing products were used. Data was collected again after 15 days of discontinuation.
[0092] After arriving, volunteers washed their faces with facial cleanser and sat quietly for 2 hours in an air-conditioned room with a temperature of 21±1℃ and a humidity of 50±10%. The melanin content of the face was measured using the Mexameter skin analyzer, and the initial value of TEWL was determined using the Tewameter®TMHex transepidermal water loss probe.
[0093] The improvement is represented by the improvement rate, which is calculated as follows: 14-day improvement rate = (T0-T14) / T0 × 100%; 28-day improvement rate = (T0-T28) / T0 × 100%; Improvement rate after discontinuation = (T0 - T_discontinuation) / T0 × 100%; The results are shown in the table: Table 8 As shown in the table above, the skin barrier repair and whitening compositions or vesicles prepared in the application examples and comparative application examples all have good repair and whitening effects after being made into emulsions. When the skin barrier repair and whitening compositions are prepared into vesicles and then into emulsions, the repair and whitening effects are even better. Figure 1 To illustrate the skin whitening effect of the lotion in Example 1, from... Figure 1 It can be seen that the emulsion prepared in Example 1 has a significant whitening effect, and the effect is long-lasting.
[0094] As can be seen from the comparison of application examples 1-5, the weight parts of the components in the skin barrier repair and whitening composition have a significant impact on the performance of the emulsion product. When the weight parts of the components are further selected within the range of "1-4 parts of camellia seed oil, 0.5-2 parts of palm fruit oil, 0.8-1.5 parts of oxidized resveratrol, and 1-4 parts of palmate kelp extract", the resulting emulsion has better repair and whitening effects.
[0095] As can be seen from the comparison of Application Examples 1 and 6-11, the preparation method of palmate kelp extract will further affect the product's repair and whitening effects. When a specific enzymatic hydrolysis + EM bacteria fermentation method is used to prepare palmate kelp extract, the product's repair and whitening effects are better.
[0096] As can be seen from the comparison of Application Example 1 and Comparative Application Examples 1-12, the effect of the present invention cannot be achieved when one of the components is not added, or when other components are added to make up the difference while not adding the component; and when other similar components are substituted, the synergistic effect cannot be achieved when the weight proportions of the components in the composition are not within the scope of this application.
[0097] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention and are not intended to limit the scope of protection of the present invention. Although the present invention has been described in detail with reference to preferred embodiments, those skilled in the art should understand that modifications or equivalent substitutions can be made to the technical solutions of the present invention without departing from the essence and scope of the technical solutions of the present invention.
Claims
1. A skin barrier repair and whitening composition, characterized in that, It includes the following components in parts by weight: 0.1-8 parts camellia seed oil, 0.1-5 parts morrhagic palm fruit oil, 0.5-5 parts oxidized resveratrol, and 0.1-8 parts palmate kelp extract.
2. The skin barrier repair and whitening composition as described in claim 1, characterized in that, It includes the following components in parts by weight: 1-4 parts camellia seed oil, 0.5-2 parts morrhagic palm fruit oil, 0.8-1.5 parts oxidized resveratrol, and 1-4 parts palmate kelp extract.
3. The skin barrier repair and whitening composition as described in claim 1, characterized in that, The weight ratio of camellia seed oil to morrhagic palm fruit oil is (2-3):
1.
4. The skin barrier repair and whitening composition as described in claim 1, characterized in that, The preparation method of the palmate kelp extract includes the following steps: (1) After crushing the palmate kelp, add it to deionized water, and add cellulase and alginate lyase to perform enzymatic hydrolysis to obtain the hydrolysate. (2) Add activated EM bacteria and nitrogen source to the enzymatic hydrolysate, ferment and culture, centrifuge, collect the supernatant, concentrate and dry to obtain the palmate kelp extract.
5. The skin barrier repair and whitening composition as described in claim 4, characterized in that, The weight ratio of cellulase to alginate lyase is 1:(1-2); and / or, the enzymatic hydrolysis temperature is 35-45℃, and the enzymatic hydrolysis time is 4-8h; and / or, the pH value of the enzymatic hydrolysis is 6.5-7.
5.
6. The skin barrier repair and whitening composition as described in claim 4, characterized in that, Includes at least one of the following (1)-(4): (1) The weight ratio of the palmate kelp to deionized water is 1:(8-12). (2) The nitrogen source includes at least one of soy milk, beef extract, peptone, ammonium sulfate, ammonium chloride, and urea; (3) The weight ratio of the enzymatic hydrolysate, EM agent and nitrogen source is enzymatic hydrolysate: EM agent: nitrogen source = 100: (0.5-5): (0.1-1); (4) The fermentation temperature is 35-45℃ and the fermentation time is 24-48h.
7. A vesicle, characterized in that, The vesicles contain the skin barrier repair and whitening composition as described in any one of claims 1-6.
8. The vesicle as described in claim 7, characterized in that, The vesicles also contain amphiphilic nonionic surfactants, phytosterols, polyols, and stabilizers; Furthermore, the camellia seed oil, morrhagic palm fruit oil, amphiphilic nonionic surfactant, and phytosterols form the oil phase of vesicles; The palmate kelp extract, oxidized resveratrol, polyols and stabilizers form the aqueous phase of vesicles; The oil phase has a mass percentage of 5-15% in the vesicles, and the aqueous phase has a mass percentage of 85-95% in the vesicles.
9. The vesicle as described in claim 8, characterized in that, The amphiphilic nonionic surfactant is at least one of lauryl ether-23, polysorbate-80, polysorbate-20, Span-80, poloxamer 188, and alkyl glycoside; and / or, the polyol is at least one of propylene glycol, butylene glycol, glycerol, polyethylene glycol, and polyglycerol; and / or, the stabilizer is at least one of trehalose, chitosan, hyaluronic acid, and hydroxypropyl-β-cyclodextrin.
10. A method for preparing vesicles as described in any one of claims 7-9, characterized in that, Includes the following steps: S1, Camellia seed oil, palm fruit oil, amphiphilic nonionic surfactant and phytosterol are dissolved in a solvent to obtain the oil phase; S2, after dissolving oxidized resveratrol and polyol, a mixture is obtained; palmate kelp extract and stabilizer are dissolved in deionized water, and the mixture is added at the same time. After mixing, an aqueous phase is obtained. S3, evaporate the oil phase to form a thin film, add the aqueous phase, sonicate to form a vesicle suspension, homogenize and cool to obtain the vesicle.
11. The use of a skin barrier repair and whitening composition as described in any one of claims 1-6 or a vesicle as described in any one of claims 7-9 in the preparation of skin products.