Core-shell structure for skin care composition, preparation method, skin care composition and skin care product

Abstract

The invention belongs to the technical field of skin care, and discloses a core-shell structure for a skin care composition, a preparation method, the skin care composition and a skincare .The core-shell structure for the skin care composition comprises a first coating layer, a second coating layer and a core layer; the first coating layer is a gel film formed by PVA, the second coating layer is a phospholipid film, and the core layer is a PLGA core layer; in the gel membrane, the phospholipid membrane and the PLGA core layer, the weight ratio of PVA to a phospholipid component in the phospholipid membrane to PLGA is (0.1-4): (1-20): (0.1-10). According to the core-shell structure for the skin care composition, a gel film formed by PVA serves as a first coating layer, a phospholipid film serves as a second coating layer, the skin care composition is loaded in combination with a PLGA core layer, and the effect of synergistically improving the slow release efficiency of the skin care composition can be achieved.

Description

TECHNICAL FIELD

[0001] The present application relates to the technical field of skin care, in particular to a core-shell structure for skin care composition, a preparation method, a skin care composition and a skin care product. BACKGROUND

[0002] With the development of society, people also pay more and more attention to their own skin management and facial lifting, and thus there are facial lifting methods such as radio frequency, laser, etc. Facial lifting by radio frequency, laser, etc. can effectively stimulate collagen regeneration, improve facial contour and aging problems, and has a relatively fast effect, and thus is welcomed by many consumers.

[0003] However, due to the damage to the skin barrier after laser and radio frequency, it has a certain impact on the subsequent further skin care, and thus most people do not dare to perform further skin care such as whitening and antioxidant after the operation, and can only choose skin barrier repair products such as prior art 1 and prior art 2 for skin care.

[0004] Prior art 1: Chinese patent 202210586188.7 discloses a skin barrier repair composition capable of resisting external stimulation, and the preparation raw materials include, by weight, 1-40 parts of an organic silicon compound, 5-50 parts of an isomeric alkane and its oil compound, 0.5-15 parts of a plant oil derivative, and 0.02-5 parts of a plant extract. The technology uses an organic silicon compound and an isomeric oil compound to form a breathable protective layer, which not only resists external stimulation, but also helps the plant extract to continuously act on sensitive skin, and under the synergistic action of the plant oil derivative, a better skin repair effect is achieved.

[0005] Prior art 2: Chinese patent application 201811590420.4 discloses a skin barrier repair cream composed of the following raw materials: water, a moisturizing agent, a skin conditioner, an emulsifier, a thickening agent, an antioxidant, a plant extract, and a skin repair agent; the skin repair agent is composed of palmitoyl tripeptide-5, acetyl tetrapeptide-2, acetyl hexapeptide-8, oligopeptide-1, ceramide 3, ceramide 6II, and ceramide 1. The ceramide-polypeptide skin repair agent with a network structure is prepared by combining ceramide and polypeptide, and can form a protective film on the skin surface during use, prolong the protection time of the skin, and play a role in skin barrier; the ceramide-polypeptide skin repair agent is prepared into a nano-gel microcapsule to protect the ceramide-polypeptide skin repair agent and enhance its stability, so that it can effectively act on skin cells and play a role in skin repair.

[0006] However, if the skin barrier repair products of prior art 1 and prior art 2 are used for skin care, it is difficult to further perform whitening, antioxidant care and the like due to the protective film formed on the skin surface and the resistance to external stimulation, and it is difficult to meet the further needs of consumers for facial lifting. SUMMARY

[0007] One of the purposes of the present application is to provide a core-shell structure for a skin care composition, which can enable the skin care composition to act on the skin and release the skin care composition for long-term skin care, and due to the presence of the core-shell structure, it can effectively penetrate the skin to release the skin care composition while reducing the stimulation to the skin, thereby meeting the further needs for facial lifting care after facial lifting by means of radio frequency, laser and the like.

[0008] Another purpose of the present application is to provide a preparation method of a core-shell structure for a skin care composition, which can be used to load the skin care composition and perform long-term skin care on the skin.

[0009] Meanwhile, the present application also provides a skin care composition, which can be used after laser and radio frequency surgery without further damaging the skin, and which can achieve long-term skin care by exerting excellent release effect.

[0010] Further, the present application provides a skin care product, which can be used for skin care after laser, radio frequency surgery and the like medical and beauty means, and which can avoid the initiation of stinging and erythema.

[0011] To achieve the above purposes, the present application provides a core-shell structure for a skin care composition, which comprises a first coating layer, a second coating layer and a core layer; the first coating layer is a gel film formed by PVA, the second coating layer is a phospholipid film, and the core layer is a PLGA core layer.

[0012] Further, the weight ratio of the gel film, the phospholipid film and the PLGA core layer is 0.1-4:1-20:0.1-10.

[0013] Further, the weight ratio of the gel film, the phospholipid film and the PLGA core layer is 0.1-4:1-20:0.1-10.

[0014] It should be noted that the weight ratio of the gel film, the phospholipid film and the PLGA core layer refers to the weight ratio of PVA, phospholipid components in the phospholipid film and PLGA; that is, the weight ratio of PVA, phospholipid components in the phospholipid film and PLGA in the gel film, the phospholipid film and the PLGA core layer is 0.1-4:4-14.5:0.1-10.

[0015] More preferably, in order to form a better embedding effect, the weight ratio of the PLGA in the PLGA core layer to the phospholipid component in the phospholipid film is 1:1-15.

[0016] Preferably, the PVA is 16000-200000 Da.

[0017] Preferably, the phospholipid component of the phospholipid film comprises at least one of hydrogenated lecithin, lecithin, phosphatidylcholine, sphingosine, acetylcholine.

[0018] As a preferred technical solution, the application further provides a preparation method of the core-shell structure for the skin care composition, comprising the following steps:

[0019] Step 1: coating the PLGA core layer with the phospholipid film;

[0020] Step 2: coating the phospholipid film with PVA.

[0021] Preferably, the specific operation of step 1 comprises the following steps:

[0022] Step 11: dissolving the PLGA dispersion with an organic solvent to obtain a PLGA solution;

[0023] Step 12: slowly injecting the PLGA solution into a buffer solution, and then volatilizing the organic solvent to obtain a nanoparticle suspension;

[0024] Step 13: centrifuging the nanoparticle suspension to retain the precipitate, washing the precipitate with a PBS phosphate buffer solution and resuspending to obtain a PLGA core layer solution;

[0025] Step 14: dissolving the phospholipid component with a phospholipid solvent to obtain a phospholipid film solution, adding Tween-80 to the phospholipid film solution for mixing, and spin-drying to obtain a dry phospholipid film;

[0026] Step 15: dissolving the dry phospholipid film with the PLGA core layer solution, and placing for 3h for sufficient hydration to obtain the phospholipid film coated PLGA core layer.

[0027] Preferably, the buffer solution is one of a PBS phosphate buffer solution, pure water, a Tris-HCl buffer, an acetate buffer, and a sodium chloride solution; in the technical solution of the application, the PBS phosphate buffer solution is preferred.

[0028] The phospholipid solvent is at least one of chloroform, dichloromethane, anhydrous methanol, and anhydrous ethanol; in the technical solution of the application, the anhydrous ethanol is preferred.

[0029] The organic solvent is at least one of ethyl lactate chlorinated solvent, tetrahydrofuran, acetone, ethyl lactate, ethyl acetate, anhydrous ethanol, and methanol.

[0030] Preferably, the specific operation of step 2 comprises the following steps:

[0031] Step 21: preparing a PVA aqueous solution;

[0032] Step 22: putting the phospholipid membrane-coated PLGA core layer into the PVA aqueous solution to obtain the core-shell structure for the skin care composition by dispersion or homogenization ultrasonic microjet technology.

[0033] As a more preferred technical solution, the core-shell structure for the skin care composition needs to coat water-soluble skin care active ingredients and oil-soluble skin care active ingredients, specifically, the following steps are used to prepare, by weight:

[0034] Step a: dispersing 0.1-10 parts of PLGA in 0.1-50 parts of an organic solvent to obtain a PLGA solution;

[0035] Step b: dissolving 0.1-1 part of a water-soluble active ingredient in 0.1-10 parts of pure water to obtain an active ingredient solution, or dissolving 0.1-1 part of a non-water-soluble active ingredient in 0.1-10 parts of an organic solvent to obtain an active ingredient solution;

[0036] Step c: mixing the PLGA solution and the active ingredient solution, slowly injecting into 10-50 parts of PBS phosphate buffer solution, and then volatilizing the organic solvent to obtain a nanoparticle suspension;

[0037] Step d: centrifuging the nanoparticle suspension to retain the precipitate, washing and resuspending with 10-50 parts of PBS phosphate buffer solution to obtain a PLGA core layer solution;

[0038] Step e: dissolving 0.1-20 parts of phospholipid components in 1-500 parts of anhydrous ethanol to obtain a phospholipid membrane solution, adding 0.01-1 parts of Tween-80 to the phospholipid membrane solution for mixing and spin-drying to obtain a phospholipid membrane dry film;

[0039] Step f: dissolving the phospholipid membrane dry film with the PLGA core layer solution and placing for 3 hours for sufficient hydration to obtain a phospholipid membrane-coated PLGA core layer;

[0040] Step g: weighing 1-600 parts of water, heating to 80-90°C, then adding 0.1-10 parts of PVA for stirring and dispersing, and cooling to 60°C to obtain a PVA aqueous solution;

[0041] Step h: putting the phospholipid membrane-coated PLGA core layer into the PVA aqueous solution to obtain the core-shell structure for the skin care composition by dispersion or homogenization ultrasonic microjet technology.

[0042] As an optional technical solution, the non-water-soluble active ingredient can be at least one of resveratrol, ceramide, bisabolol, and pterostilbene.

[0043] As an optional technical solution, the water-soluble active ingredient can be at least one of dipotassium glycyrrhizinate, gentian extract, centella asiatica extract, and tannic acid.

[0044] The application further discloses a skin care composition loaded with a skin care ingredient by using the core-shell structure for the skin care composition.

[0045] Preferably, the skin care ingredient comprises at least one of a whitening ingredient, a soothing ingredient, a moisturizing ingredient, an anti-wrinkle ingredient, an antioxidant ingredient, a repairing ingredient, a firming ingredient, and a redness-reducing ingredient.

[0046] Further preferably, the whitening ingredient comprises at least one of niacinamide, dipotassium glycyrrhizinate, sodium phosphate dibasic buffer, ascorbyl tetraisopalmitate, glabridin, tranexamic acid, ceramide, nonapeptide-1, resveratrol, and tannic acid.

[0047] Further preferably, the soothing ingredient comprises at least one of dipotassium glycyrrhizinate, tranexamic acid, ceramide, nonapeptide-1 and glabridin.

[0048] Further preferably, the moisturizing ingredient comprises at least one of ceramide, glabridin, tranexamic acid, niacinamide and bisabolol.

[0049] Further preferably, the anti-wrinkle ingredient comprises at least one of nonapeptide-1, glabridin, niacinamide and ascorbyl tetraisopalmitate.

[0050] Further preferably, the antioxidant ingredient comprises at least one of glabridin, ascorbyl tetraisopalmitate, niacinamide and tranexamic acid.

[0051] Further preferably, the repairing ingredient comprises at least one of ceramide, glabridin, niacinamide and dipotassium glycyrrhizinate.

[0052] The application further discloses a skin care product containing 0.01-99.9% of the skin care composition.

[0053] Advantages

[0054] Compared with the prior art, the application has at least the following advantages:

[0055] (1) The application discloses a core-shell structure for a skin care composition, which can produce a synergistic effect of improving the sustained-release efficiency of the skin care composition by using a PVA-formed gel film as a first coating layer, a phospholipid film as a second coating layer, and a PLGA core layer to load the skin care composition.

[0056] (2) The core-shell structure, the gel film formed by PVA and the phospholipid film used in the skin care composition of the present application can produce a synergistic transdermal effect, can deliver a large amount of active substances to the dermis for sustained release, and can improve the skin care effect of the skin care composition on the skin.

[0057] (3) The present application finds that the PLGA core layer coated with a phospholipid layer can produce a synergistic effect of improving the whitening effect of whitening ingredients after loading the whitening ingredients. BRIEF DESCRIPTION OF DRAWINGS

[0058] The present application will be further described below in conjunction with the drawings and examples.

[0059] Figure 1 is a 500 times microscope image of Example 2 of the present application.

[0060] Figure 2 is a Raman imaging image of Example 2 of the present application. DETAILED DESCRIPTION

[0061] The present application will be further described below in conjunction with the drawings and examples.

[0062] In order to explain the technical content of the present application in detail, the following further describes the embodiments.

[0063] It should be noted that the technical solution of the present application is not limited to the above-mentioned raw materials provided by the suppliers, and all commercially available products can achieve the technical solution of the present application.

[0064] In the following examples and comparative examples, the PVA was purchased from Sanwei in China, the model number was L088-35 (type 20-88); the PLGA was purchased from Evonik in Germany, the model number was RG 752H; the PVP was purchased from BASF, the model number was Kollidon®30; the hydrogenated lecithin was purchased from Lipoid Kosmetik, the model number was Lipoid®90H; the ascorbyl tetraisopalmitate was purchased from NIKKO CHEMICALS; the ethyl acetate was purchased from Shanghai Lingfeng Chemical Reagent Co., Ltd.; and the PBS phosphate buffer solution was purchased from Solarbio.

[0065] As common knowledge of those skilled in the art, the Chinese name of the PLGA is lactic acid / glycolic acid copolymer, the Chinese name of the PVP is polyvinylpyrrolidone, and the Chinese name of the PVA is polyvinyl alcohol.

[0066] ​​​It should be noted that the technical scheme of the present application is not limited to the above-mentioned raw materials provided by the supplier, and all commercially available products can realize the technical scheme of the present application.

[0067] In the following examples and comparative examples, the parts and % are weight parts and weight percentages, respectively, unless otherwise specified.

[0068] Example 1

[0069] A core-shell structure for a skin care composition is prepared by the following steps:

[0070] Step 1: 70 parts of ethyl acetate are used to dissolve 2.1 parts of PLGA to obtain a PLGA solution;

[0071] Step 2: The PLGA solution is slowly injected into 30 parts of PBS phosphate buffer solution, and the organic solvent is volatilized at room temperature to obtain a nanoparticle suspension;

[0072] Step 3: The nanoparticle suspension is centrifuged to retain the precipitate, and the precipitate is washed with 30 parts of PBS phosphate buffer solution and resuspended to obtain a PLGA core layer solution;

[0073] Step 4: 210 parts of anhydrous ethanol are used to dissolve 21 parts of hydrogenated lecithin to obtain a phospholipid film solution, 1.05 parts of Tween-80 is added to the phospholipid film solution and mixed, and the phospholipid film is dried to obtain a phospholipid film dry film;

[0074] Step 5: The phospholipid film dry film is dissolved with the PLGA core layer solution and placed for 3 hours for sufficient hydration to obtain a phospholipid film coated PLGA core layer;

[0075] Step 6: 250 parts of water are weighed, heated to 85±5℃, and then 2.5 parts of PVA is added and stirred to disperse, and the temperature is lowered to 60℃ to obtain a PVA aqueous solution;

[0076] Step 7: The phospholipid film coated PLGA core layer is added to the PVA aqueous solution to obtain the core-shell structure for the skin care composition.

[0077] Example 2

[0078] A whitening composition is prepared by the following steps:

[0079] Step 1: 70 parts of ethyl acetate are used to dissolve 2.1 parts of PLGA to obtain a PLGA solution;

[0080] Step 2: 10 parts of pure water are used to dissolve 0.2 parts of ascorbic acid to obtain an active ingredient solution;

[0081] Step 3: After mixing the PLGA solution and the active ingredient solution, slowly inject into 30 parts of PBS phosphate buffer solution, and then stir at room temperature to evaporate the organic solvent to obtain a nanoparticle suspension; Step 4: Centrifuge the nanoparticle suspension to retain the precipitate, wash the precipitate with 30 parts of PBS phosphate buffer solution and resuspend to obtain a PLGA core layer solution;

[0082] Step 5: Dissolve 21 parts of hydrogenated lecithin in 210 parts of anhydrous ethanol to obtain a phospholipid film solution, add 1.05 parts of Tween-80 to the phospholipid film solution, mix, and spin dry to obtain a phospholipid film dry film;

[0083] Step 6: Dissolve the phospholipid film dry film with the PLGA core layer solution, and place for 3 hours for sufficient hydration to obtain a phospholipid film coated PLGA core layer;

[0084] Step 7: Weigh 250 parts of water, heat to 85±5℃, then add 2.5 parts of PVA and stir to disperse, and then cool to 60℃ to obtain a PVA aqueous solution;

[0085] Step 8: Put the phospholipid film coated PLGA core layer into the PVA aqueous solution to disperse to obtain a core-shell structure for the skin care composition.

[0086] Example 3

[0087] A whitening composition is prepared by the following steps:

[0088] Step 1: Dissolve 4 parts of PLGA in 70 parts of ethyl acetate to obtain a PLGA solution;

[0089] Step 2: Dissolve 0.2 parts of ascorbic acid in 10 parts of pure water to obtain an active ingredient solution;

[0090] Step: After mixing the PLGA solution and the active ingredient solution, slowly inject into 30 parts of PBS phosphate buffer solution, and then stir at room temperature to evaporate the organic solvent to obtain a nanoparticle suspension;

[0091] Step: Centrifuge the nanoparticle suspension to retain the precipitate, wash the precipitate with 30 parts of PBS phosphate buffer solution and resuspend to obtain a PLGA core layer solution;

[0092] Step: Dissolve 3 parts of hydrogenated lecithin in 210 parts of anhydrous ethanol to obtain a phospholipid film solution, add 1.05 parts of Tween-80 to the phospholipid film solution, mix, and spin dry to obtain a phospholipid film dry film;

[0093] Step: Dissolve the phospholipid film dry film with the PLGA core layer solution, and place for 3 hours for sufficient hydration to obtain a phospholipid film coated PLGA core layer;

[0094] Step 7: 250 parts of water was weighed and heated to 85±5℃, then 2.5 parts of PVA was added to stir and disperse, and cooled to 60℃ to obtain a PVA aqueous solution;

[0095] Step 8: The PLGA core layer coated with phospholipid film was put into the PVA aqueous solution to obtain a core-shell structure for the skin care composition.

[0096] Example 4

[0097] The same as Example 2, except that the step 5 was changed to use 500 parts of anhydrous ethanol to dissolve 50 parts of hydrogenated lecithin to obtain a phospholipid film solution, 2.50 parts of Tween-80 was added to the phospholipid film solution to mix and spin dry to obtain a phospholipid film dry film.

[0098] Example 5

[0099] The same as Example 2, except that the amount of PVA was 0.05 parts.

[0100] Example 6

[0101] The same as Example 2, except that the amount of PVA was 25 parts.

[0102] Comparative Example 1

[0103] The same as Example 2, except that PVA was changed to PVP.

[0104] Comparative Example 2

[0105] The same as Example 2, except that PVA was changed to PLGA.

[0106] Comparative Example 3

[0107] A whitening composition was prepared by the following steps:

[0108] Step 1: 70 parts of ethyl acetate was used to dissolve 2.1 parts of PLGA to obtain a PLGA solution;

[0109] Step 2: 10 parts of pure water was used to dissolve 0.2 parts of ascorbic acid to obtain an active ingredient solution;

[0110] Step 3: 210 parts of anhydrous ethanol was used to dissolve 21 parts of hydrogenated lecithin to obtain a phospholipid film solution, 1.05 parts of Tween-80 was added to the phospholipid film solution to mix, and then the active ingredient solution was mixed with the phospholipid film mixed solution to spin dry to obtain a dry film of the mixture;

[0111] Step 4: 10 parts of pure water was used to dissolve 0.2 parts of ascorbic acid to obtain an active ingredient solution;

[0112] Step 5: dissolve the dry film by mixing 30 parts of PBS phosphate buffer solution with the active ingredient solution of tympanic acid, and place it for 3 hours for complete hydration to obtain a phospholipid film-coated active ingredient solution;

[0113] Step 6: mix the PLGA solution with the phospholipid film-coated active ingredient solution, then stir at room temperature to evaporate the organic solvent, to obtain a PLGA-coated phospholipid layer nanoparticle suspension;

[0114] Step 7: weigh 250 parts of water, heat to 85±5°C, then add 2.5 parts of PVA for stirring and dispersion, and cool to 60°C to obtain a PVA aqueous solution;

[0115] Step 8: pour the PLGA-coated phospholipid layer nanoparticle suspension into the PVA aqueous solution, and disperse to obtain a whitening composition;

[0116] The film layer structure of the whitening composition is: the first coating layer is a PVA coating layer, the second coating layer is a PLGA coating layer, and the core layer is a phospholipid film.

[0117] Performance test

[0118] I. Sustained-release effect

[0119] 1. Purpose of the experiment

[0120] Through in vitro release experiment, the speed of tympanic acid release from the sample into the surrounding environment is understood, and the release efficiency is judged.

[0121] 2. Materials and reagents

[0122] 2.1 Materials: dialysis bag MD77-3500, 0.22 μm microporous filter membrane, centrifuge tube 2.2 Reagents: sodium chloride (NaCl), potassium chloride (KCl), sodium phosphate dibasic (Na2HPO4), potassium phosphate monobasic (KH2PO4), sodium dodecyl sulfate (SDS), triethylamine, phosphoric acid, methanol.

[0123] 3. Main instruments

[0124] Analytical balance (Mettler, MS205DU / A), pipette (Eppendorf), Dingxin Yi DXY-MS-5L magnetic stirrer, Shimadzu high-performance liquid chromatograph LC-2040C 3D.

[0125] 4. Experimental method

[0126] Take the sample containing 567 mg of tympanic acid and place it in a dialysis bag in 200 mL of dissolution medium at 37°C, and perform in vitro release experiment at 100 r / min. Take 1 mL of release liquid at 0.5, 2.0, 6.0, 12.0, and 24.0 h, and supplement 1 mL of dissolution medium at the same temperature.

[0127] The release solution was filtered with a 0.22 μm microporous filter and subjected to HPLC determination. A standard curve of rutin peak area was established, and the rutin content in the release solution at different time points was calculated according to the standard curve, and the cumulative release rate was calculated.

[0128] Liquid chromatography conditions: chromatographic column 5 μm C18 (2) 100A, LC Column 250 mm x 4.6 mm, mobile phase: pH 2.5 phosphate buffer-methanol (60:40), volume flow rate 0.5 mL / min, detection wavelength 220 nm, column temperature 30°C, injection volume 50 μL, isocratic elution.

[0129] The standard curve is shown in Table 1;

[0130] Table 1 Linear equation, linear range, correlation coefficient, etc.

[0131]

[0132] According to the above method, examples 2-6 and comparative examples 1-3 were detected, and the results are shown in Table 2;

[0133] Table 2 Release effect test results of whitening composition of examples 2-6 and comparative examples 1-3

[0134]

[0135]

[0136] According to the results in Table 2, it can be seen that:

[0137] According to the data of examples 1-6, it can be seen that the core-shell structure formed by the present application has good release effect, which can avoid the large amount of active substance released in a short time, thereby reducing the skin irritation.

[0138] Among them, the release effect of example 3 is the worst, which shows a high release rate at 0.5 h, 2 h, 6 h and 12 h. It is speculated that it is because the mass of PLGA is higher than that of phospholipid, which leads to poor coating effect of phospholipid membrane, affecting the stability of the membrane structure, and disrupting the kinetics of the active substance.

[0139] According to the comparison of the data of example 2 and example 4, it can be seen that the release rate of example 4 at 0.5 h and 2 h is lower than that of example 2, but the release rate at 6 h and 12 h is greatly improved than that of example 2, especially between 2 h and 6 h, which is the rapid release stage. That is, the technical solution of example 4 deviates to a certain extent in the process of transition to long-acting sustained release. It is speculated that the following may be the reason:

[0140] (1) Excessive phospholipid dosage destroys the stability of the membrane structure, leading to the release kinetics of the active substance being disrupted;

[0141] (2) Excessive phospholipid dosage leads to unstable aggregate structure, thereby accelerating the leakage of the active substance at 2h-6h.

[0142] According to the comparison of the data of Example 2 and Example 5, Example 5 reduces the amount of PVA compared to Example 2, resulting in a certain degree of decline in the overall sustained-release effect. It is speculated that this is because PVA cannot completely coat the phospholipid, and the surface of the phospholipid is exposed to the outside world, which is easily affected by external factors such as temperature, pH value, and enzymes, leading to phenomena such as rupture and fusion. This will cause the internal encapsulated pantothenic acid to be released prematurely, reducing the efficiency and purpose of encapsulation.

[0143] In view of the insufficient PVA dosage of Example 5, Example 6 increases the dosage of PVA, but the sustained-release effect appears a problem: Example 6 has little change in release rate at 0.5h and 2h, that is, excessive PVA dosage makes it difficult for the active substance to be released in a short time, and it can only play a good skin care effect in the process of 2h-6h. It is speculated that excessive PVA film wrapping may cause particles to adhere to each other, making it difficult for the particles to exert their sustained-release effect in a short time.

[0144] According to the comparison of the data of Example 2 and Comparative Example 1, using PVP instead of PVA as the outermost coating layer will cause the active substance in the core-shell structure to have a significant decline in sustained-release effect, with a release rate of more than 80% at 6h, failing to achieve a good long-acting sustained-release effect.

[0145] According to the comparison of the data of Example 2 and Comparative Example 2, if PLGA is used instead of PVA as the outermost coating layer to improve the sustained-release effect, the release rate at 0.5h is similar to that of Example 2, but the release rates at 2h, 6h, 12h, and 24h are significantly higher, even lower than that of Comparative Example 1. It is speculated that this may be due to the following reasons:

[0146] (1) The hydrophobic nature of the outer PLGA may damage the integrity of the phospholipid bilayer, affecting the stability of the drug loading;

[0147] (2) The degradation rate of the outer PLGA, the degradation rate of the second coating phospholipid film, and the degradation rate of the PLGA in the core layer form a large mismatch, causing a burst effect.

[0148] According to the comparison of the data of Example 2 and Comparative Example 3, if a core-shell structure of PVA-coated PLGA and phospholipid film is used to encapsulate the active substance, its sustained-release effect is significantly worse than that of Example 2. The possible reasons for this difference are:

[0149] (1) The hydrophilicity of PVA and the hydrophobicity of PLGA can cause interfacial delamination or drug leakage;

[0150] (2) The weak interaction between the hydroxyl group of PVA and the ester group of PLGA forms a physical barrier layer, affecting drug diffusion.

[0151] II. Film structure

[0152] Preparation before experiment

[0153] 1. Sample preparation:

[0154] Take the cross-section sample stage specially for Fei, paste conductive glue on the cross-section of the sample stage, take a small amount of sample, slowly spread it on the sample stage, and blow the sample surface to ensure that the sample does not flow.

[0155] 2. Check the equipment status:

[0156] 3. Check whether the power light on the main panel of the Fei electron microscope is normal.

[0157] Operation method

[0158] 1. Sample loading:

[0159] - Put the finished sample into the sample cup with a special tweezer.

[0160] - Leveling: rotate the sample cup counterclockwise to ensure that the highest point of the sample is level with the plane of the sample cup opening.

[0161] - Lowering: continue to rotate the sample cup counterclockwise to make the highest surface of the sample at least 2 mm lower than the upper surface of the sample cup.

[0162] 2. Image adjustment:

[0163] - Click the corresponding button on the operation window of the scanning electron microscope software to appear a new window, and enlarge the image to 500 times.

[0164] - Adjust the brightness and contrast on the operation platform, as well as the focusing button, to the appropriate position to get a clear image.

[0165] 3. Observation and shooting: after adjusting the image, you can observe and shoot, mark the size, and record the required image information.

[0166] The above method is used to detect Example 2, and the results are shown in Figure 1 .

[0167] It can be seen that the technical scheme of the present application can form a three-layer core-shell structure.

[0168] III. Embedding rate

[0169] The whitening composition of Example 2 was detected by Raman spectrum test, and it was found that the encapsulation rate of the core-shell structure active material of Example 2 was 56.2%, which can be seen from Figure 2 .

[0170] Application Example

[0171] A dual-carrier whitening essence was prepared according to the formulation table of Table 3, and the preparation method was as follows:

[0172] (1) Accurately weigh the water into the clean and disinfected production tank, open the homogenizer, add the first process material, homogenize until completely dissolved without fine particles, open the stirring and heat to 40℃, and homogenize several times during the period to ensure complete dissolution of the material.

[0173] (2) Add the second process material to the oil phase pot, start heating, open the stirring, and stir to 85℃ until completely dissolved, and standby.

[0174] (3) Open the vacuum of the production tank, open the homogenizer, and draw the second process material into the production tank, homogenize for 15 min, stir and keep warm for 30 min, and start cooling.

[0175] (4) When the temperature is reduced to 45℃, open the stirring, use a clean container to stir the third process material until completely dissolved and transparent, add it to the production tank, stir for 10 min, and continue to cool;

[0176] (5) Add the fourth process material to the production tank, stir for 20 min, stir evenly, take samples for detection, and filter the material after the detection is qualified.

[0177] Table 3 Whitening Essence Formulation Table

[0178]

[0179]

[0180] Efficacy Detection

[0181] The application example of the present application entrusts Kangzheng Detection Service Co., Ltd. to conduct human efficacy detection and issue a detection report, and the report number is K25E02061-01S1.

[0182] The following is the efficacy detection content of the detection report:

[0183] 1.1 Purpose

[0184] A certain number of subjects were used as objects, and the non-registered record efficacy of the dual-carrier whitening essence product, such as repair, moisturizing, soothing, instant redness reduction (15 minutes), brightening, tightening, and anti-wrinkle efficacy, were comprehensively evaluated through continuous trial of the test product and instrument detection and clinical evaluation.

[0185] 1.2 Test instruments

[0186] Facial imaging analysis system VISIA7 (CANFIELD, USA);

[0187] Skin three-dimensional imaging system Primos CR (CANFIELD, USA);

[0188] Skin color test probe Colorimeter (Courage-Khazaka, Germany);

[0189] Skin elasticity test probe Cutometer (Courage-Khazaka, Germany);

[0190] Skin moisture test probe Corneometer (Courage-Khazaka, Germany);

[0191] Skin glossiness test probe Glossymeter (Courage-Khazaka, Germany);

[0192] Transdermal water loss probe Tewameter (Courage-Khazaka, Germany);

[0193] Skin hemoglobin and melanin tester Mexamete (Courage-Khazaka, Germany);

[0194] Skin texture test system (VC 20plus).

[0195] 1.3 Number of subjects

[0196] The effective number of subjects is not less than 10.

[0197] 1.4 Inclusion criteria

[0198] The subjects are required to be between 18 and 60 years old, in good health, and of either sex;

[0199] Volunteers who can strictly follow the requirements and time arrangement of the research scheme and have obtained informed consent;

[0200] Those who have one of the symptoms of impaired skin barrier function such as dry skin, desquamation, and redness;

[0201] Those who have dry skin and have obvious forehead lines, frown lines, and crow's feet;

[0202] Those who have passed the lactic acid stinging test and have been identified by a dermatologist as having sensitive skin.

[0203] 1.5 Exclusion criteria

[0204] oral or topical tretinoin and antibiotics within the last month;

[0205] Acute inflammation or other skin diseases (such as rosacea, eczema, lupus erythematosus, seborrheic dermatitis, psoriasis, severe exfoliation, etc.) on the face;

[0206] Use of antihistamines within the last week or use of hormones and immunosuppressants within the last month;

[0207] Chemical peeling (fruit acid treatment), microdermabrasion, laser resurfacing, etc. within the last three months;

[0208] Use of any topical medication on the test site within the last two months;

[0209] Subjects with inflammatory skin diseases that have not been clinically cured;

[0210] Insulin-dependent diabetics;

[0211] Patients with asthma or other chronic respiratory diseases who are receiving treatment;

[0212] Patients who have received anticancer chemotherapy within the last six months;

[0213] Patients with immunodeficiency or autoimmune diseases;

[0214] Lactating or pregnant women or female patients who plan to become pregnant during the test period;

[0215] Patients who have undergone bilateral mastectomy and bilateral axillary lymph node dissection;

[0216] Patients with obvious sunburn on the test site or other defects that affect the determination of test results due to scarring, pigmentation, atrophy, port-wine stains, or other defects;

[0217] Patients who have participated in other clinical trials on the test site within the last month;

[0218] Patients with highly sensitive constitutions or those who are allergic to cosmetics;

[0219] Non-volunteers or those who cannot complete the required content according to the requirements of the test.

[0220] 1.6 Subject Restrictions

[0221] Prohibition of oral or topical tretinoin and antibiotics or the use of similar claimed cosmetics;

[0222] Prohibition of medical and special skin care (beauty salon, etc.) treatment or other cosmetic methods on the test site during the test period;

[0223] Subjects who mainly engage in indoor activities to avoid long-term exposure to outdoor sunlight;

[0224] Keep the original work and rest schedule, do not change the original good habits, avoid emotional fluctuations;

[0225] Avoid excessive exercise, sleep deprivation, weight loss and overeating during the test period, which deviate greatly from daily life;

[0226] During the test period, unless necessary, no medical products should be used. If necessary, the name and amount of the product should be recorded in the log.

[0227] 1.7 Suspension criteria

[0228] During the test period, if the test site has adverse reactions and is attributed to the test sample, and the dermatologist determines that it is not a serious adverse reaction and does not require drug treatment, the use of the sample is stopped and the skin problem will be solved naturally.

[0229] After the skin problem is solved, the sample can be used again to continue the test. During the test period, if the test site has adverse reactions but is not attributed to the test sample, and the dermatologist determines that it is not a serious adverse reaction and does not require drug treatment, the use of the sample is stopped and the skin problem will be solved naturally. After the skin problem is solved, the sample can be used again to continue the test.

[0230] 1.8 Withdrawal criteria

[0231] In the following cases, the subject is considered to be withdrawn from the test:

[0232] During the test period, if the test site has serious adverse reactions, whether or not attributed to the test sample, and requires drug treatment;

[0233] Due to the personal arrangements of the subject, the subject cannot participate in the test at the expected follow-up time;

[0234] During the test period, the subject suddenly falls ill and needs drug treatment, which will affect the results of this test;

[0235] There are serious non-compliance in the use of the sample.

[0236] 1.9 Test procedure

[0237] 1.9.1 Recruit qualified subjects according to the requirements and sign the written informed consent form. Before enrollment, ask the subject a series of questions about disease history, health status, etc. according to the inclusion and exclusion criteria.

[0238] 1.9.2 Screening process of subjects: the dermatologist or qualified test personnel trained by the test personnel screen the face of the subject, and finally select subjects who meet the criteria according to the screening results according to the set number of subjects.

[0239] 1.9.3 The qualified subjects who enrolled in the group wait for more than 20 minutes in the environmental laboratory before using the product, and cannot drink water and beverages. The subjects remain relaxed, expose their faces, and avoid touching. After adaptation, the baseline values are evaluated, including VISIA 7 to take pictures of the red area and wrinkles on the front, left side, and right side of the subject's face, Primos CR to take pictures of the forehead wrinkles, crow's feet, and marionette lines, and to measure the skin stratum corneum water content, skin transepidermal water loss (TEWL) value, skin elasticity R2 value, skin hemoglobin content, skin ITA ° value, skin gloss, and skin roughness of the face as initial values.

[0240] 1.9.4 The product is used for 15 minutes and 14 days.

[0241] 1.9.3 The evaluations and tests are performed and recorded.

[0242] 1.10 Adverse reactions

[0243] Adverse reactions refer to any signs of discomfort (including abnormal clinical diagnostic data), symptoms, or conditions that occur during the trial of the sample, regardless of the causal relationship with the sample. However, if the observed symptoms occur before the use of the sample and do not worsen after the use of the sample, or if the reactions occur as predicted by the subject based on past daily experience and their own state before the start of the trial, such as a cold, chronic headache, etc., they are not considered adverse reactions. Measures to be taken when adverse reactions occur: If the subject experiences any subjective feelings of itching, stinging, burning, etc., and / or develops clinical symptoms (such as scaling, erythema, papules, blisters, etc.) during the trial, based on the subject's self-reporting, the content recorded in the log, inquiries, observations, etc. during the trial, the subject must report to the trial project leader within 24 hours, and the symptoms are checked by a dermatologist, the incident is inquired in detail, and the cause is recorded and analyzed. At the same time, the dermatologist should evaluate whether the subject is suitable for continuing the trial and treatment based on the severity of the subject's symptoms. When it is determined that there is a causal relationship between the adverse reactions and the trial, the subject should be compensated accordingly.

[0244] 1.11 Test site The test site is the face.

[0245] 1.12 Test environment requirements

[0246] The test results should be observed in a constant environment with a temperature of (21 ± 1) °C and a relative humidity of (50 ± 10) % RH, and real-time dynamic monitoring should be performed; the test conditions during the test should be consistent, such as the tester, the place, the instrument, etc.; all subjects should be adapted to this environmental condition for at least 20 minutes before evaluation and testing. 1.13.1 Descriptive statistics are performed on the measured values of each test index, including mean, standard deviation, minimum, median, and maximum.

[0247] 1.13.2 Percentage of change = (n-day value - initial value) / initial value.

[0248] The results are shown in Table 4;

[0249] Table 4 Statistical results of human detection

[0250]

[0251]

[0252] According to the results in Table 4, it can be seen that:

[0253] After 10 subjects used the double-carrier whitening essence multiple times, the cosmetic non-registered record efficacy test of repair, moisturizing, soothing, instant redness reduction (15 minutes), brightening, tightening, and anti-wrinkle efficacy was performed, and the results showed that:

[0254] 1. None of the subjects in this test had adverse reaction cases, and the test product had high safety;

[0255] 2. After the subjects used the product, the skin transepidermal water loss (TEWL) value test results at the revisit points (15 minutes) and (14 days) were significantly different from the initial value (0 days), indicating that the product helped to maintain the moisture content of the application site or reduce water loss, and maintained the normal state of the skin, indicating that the product had a repair effect; 3. After the subjects used the product, the skin stratum corneum water content and skin transepidermal water loss (TEWL) value test results at the revisit points (15 minutes) and (14 days) were significantly different from the initial value (0 days), indicating that the product helped to maintain the moisture content of the application site or reduce water loss, and maintained the normal state of the skin, indicating that the product had a moisturizing effect;

[0256] 4. After the subjects used the product, the skin hemoglobin content and facial red area characteristic count at the revisit points (15 minutes) and (14 days) were significantly different from the initial value (0 days), indicating that the product could alleviate the state of skin immune inflammation and other skin irritation, indicating that the product had an instant redness reduction (15 minutes) effect and a soothing effect;

[0257] 5. After the subjects used the product, the skin ITA° value test results at the follow-up point (15 minutes) and (day 14) showed a positive significant difference compared with the initial value (day 0). The skin roughness test results at the follow-up point (day 14) also showed a positive significant difference compared with the initial value (day 0). The skin radiance test results at the follow-up point (15 minutes) and (day 14) also showed a positive significant difference compared with the initial value (day 0). This indicates that the product has a skin brightening effect.

[0258] 6. After using the product, the R2 value of skin elasticity at the follow-up point (15 minutes) and (day 14) showed a significant positive difference compared to the initial value (day 0), indicating that the product has the effect of maintaining skin firmness and elasticity, and thus has a firming effect. 7. After using the product, the length of forehead wrinkles and crow's feet wrinkles at the follow-up point (15 minutes) and (day 14) showed a significant positive difference compared to the initial value (day 0), and the length of nasolabial folds at the follow-up point (day 14) showed a significant positive difference compared to the initial value (day 0), indicating that the product helps to slow down the formation of wrinkles or make wrinkles less noticeable, thus demonstrating an anti-wrinkle effect.

[0259] The embodiments presented herein are merely selected implementations based on combinations of all possible embodiments. The appended claims should not be limited to the embodiments described herein. Some numerical ranges used in the claims include sub-ranges within them, and variations within these ranges should also be covered by the appended claims.

Claims

1. A core-shell structure for use in skincare compositions, characterized in that, It includes a first coating layer, a second coating layer, and a core layer; the first coating layer is a gel membrane formed of PVA, the second coating layer is a phospholipid membrane, and the core layer is a PLGA core layer; in the gel membrane, phospholipid membrane, and PLGA core layer, the weight ratio of PVA, the phospholipid component in the phospholipid membrane, and PLGA is 0.1-4:1-20:0.1-10.

2. The core-shell structure for use in the skincare composition according to claim 1, characterized in that, In the gel membrane, phospholipid membrane, and PLGA core layer, the weight ratio of PVA, the phospholipid component in the phospholipid membrane, and PLGA is 0.1-4:4-14.5:0.1-10.

3. The core-shell structure for use in skincare compositions according to claim 1, characterized in that, The weight ratio of PLGA in the PLGA core layer to the phospholipid components in the phospholipid membrane is 1:1-15.

4. The core-shell structure for use in skincare compositions according to claim 1, characterized in that, The phospholipid components include at least one of hydrogenated lecithin, lecithin, phosphatidylcholine, sphingosine, and acetylcholine.

5. A method for preparing a core-shell structure for use in skincare compositions according to any one of claims 1-4, characterized in that, Includes the following steps: Step 1: Coat the PLGA core layer with a phospholipid membrane; Step 2: Coat PVA with a phospholipid membrane.

6. The method for preparing the core-shell structure for skincare composition according to claim 5, characterized in that, The specific operations of step 1 include the following steps: Step 11: Dissolve and disperse PLGA in an organic solvent to obtain a PLGA solution; Step 12: Slowly inject the PLGA solution into the PBS phosphate buffer solution, and then evaporate the organic solvent to obtain a nanoparticle suspension; Step 13: After centrifuging the nanoparticle suspension, retain the precipitate, wash the precipitate with PBS phosphate buffer solution and resuspend it to obtain PLGA core layer solution; Step 14: Dissolve the phospholipid components in a phospholipid solvent to obtain a phospholipid membrane solution, add Tween-80 to the phospholipid membrane solution, mix, and evaporate to dryness to obtain a dry phospholipid membrane. Step 15: Dissolve the dry phospholipid membrane with PLGA core layer solution and let it stand for 3 hours to fully hydrate, thus obtaining a PLGA core layer coated with phospholipid membrane.

7. The method for preparing the core-shell structure for skincare compositions according to claim 6, characterized in that, The specific operations of step 2 include the following steps: Step 21: Prepare PVA aqueous solution; Step 22: The PLGA core layer coated with phospholipid membrane is immersed in PVA aqueous solution, and the core-shell structure for the skin care composition is obtained by dispersion or homogenization ultrasonic micro-spinning technology.

8. A skincare composition, characterized in that, The skincare ingredients are loaded using a core-shell structure for skincare compositions as described in any one of claims 1-3; the skincare ingredients are loaded in the PLGA core layer and / or between the first coating layer and the second coating layer.

9. The skincare composition according to claim 8, characterized in that, The skincare ingredients include at least one of the following: whitening ingredients, soothing ingredients, moisturizing ingredients, anti-wrinkle ingredients, antioxidant ingredients, repairing ingredients, redness-reducing ingredients, and firming ingredients.

10. A skincare product, characterized in that, Contains 0.01-99.9% of the skin care composition as described in claim 8 or 9.

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