Multi-capsule system for promoting residence and stable release of active components as well as preparation method and application of multi-capsule system

By combining the outer oil film and capsule shell in the multi-capsule system with the loricrin in the skin's stratum corneum, the problem of short residence time of cosmetic active ingredients on the skin surface is solved, and the stable release and deep penetration of active ingredients are achieved, achieving long-lasting moisturizing, whitening and anti-wrinkle effects.

CN120694906APending Publication Date: 2025-09-26MESOMIANS DIVIDE LIFE SCIENCE RESEARCH (GUANGZHOU) CO LTD +1
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Patent Information

Application Number
CN202510624768.4
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-05-15
Publication Date
2025-09-26

AI Technical Summary

Technical Problem

Existing cosmetic penetration enhancement systems can easily cause irreversible damage to the skin's stratum corneum barrier system when promoting active ingredients to penetrate deep into the skin. In addition, the active ingredients have a short residence time on the skin surface and cannot be slowly released for a long time, thus failing to achieve the expected moisturizing, whitening, anti-wrinkle and other effects.

Method used

A multi-capsule system is adopted, including an outer oil film and an inner capsule shell. The capsule shell encapsulates the active ingredient and combines with the loricrin in the skin stratum corneum through ionic bonds and covalent bonds, thereby increasing its water content and allowing the active ingredient to reside on the skin surface for a long time and be slowly released, thus avoiding reaction with other base materials and causing failure.

Benefits of technology

The active ingredients can stay on the skin surface for a long time and be released slowly, thus avoiding skin damage. The concentration is gradually increased during daily use, and the active ingredients enter the subcutaneous tissue to achieve moisturizing, whitening, anti-wrinkle and other effects, thus avoiding local burst release and adverse effects on the skin microenvironment.

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Abstract

The invention relates to a multi-capsule system for promoting residence and stable release of an active component as well as a preparation method and application of the multi-capsule system. The multi-capsule system for promoting residence and stable release of the active component comprises an outer-layer oil film, a component 1 and a plurality of inner capsule bodies, wherein the component 1 is wrapped in the outer-layer oil film, and the inner capsule bodies are dispersed in the component 1; the inner capsule body comprises a capsule shell and a component 2 wrapped in the capsule shell; the outer-layer oil film and the capsule shell are both skin absorbable substances; the component 1 is used for improving the water content of skin cuticle paphiopedilum A protein to enable the skin cuticle paphiopedilum A protein to be in a swelling state; the component 2 comprises an active component, and the active component is bonded to the ceilomethrin through an ionic bond and / or a covalent bond when the ceilomethrin is swelled in the cuticle of the skin. According to the multi-capsule system for promoting the residence and stable release of the active components, provided by the invention, the active components in cosmetics can stay on the skin surface for a long time and are slowly released into subcutaneous tissues to realize the effects of moisturizing, whitening, resisting wrinkles, resisting oxidation and the like.
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Description

Technical Field

[0001] The present invention relates to the field of cosmetics, and in particular to a multi-capsule system for promoting the retention and stable release of active components, and a preparation method and application thereof. Background Art

[0002] The cosmetic penetration enhancement system refers to the use of various technical means and ingredients to enhance the ability of the active ingredients in cosmetics to penetrate the skin surface into the deep layers of the skin, thereby improving the efficacy of the cosmetics.

[0003] The existing cosmetic penetration enhancement systems mainly include the following:

[0004] 1. Chemical penetration enhancement technology: This technology uses chemical penetration enhancers to change the structural arrangement of stratum corneum lipids, thereby enhancing permeability. Chemical penetration enhancers can be further divided into chemical penetration enhancers and traditional Chinese medicine penetration enhancers. For example, ethanol, the most widely used short-chain alcohol, can enhance the transdermal delivery of polar molecules by increasing the fluidity of intercellular lipids and interacting with intracellular proteins. Menthol, another natural penetration enhancer commonly used in traditional Chinese medicine preparations in recent years, has a significant effect on the transdermal absorption of both hydrophilic and lipophilic compounds, and its effect is particularly pronounced on fat-soluble drugs.

[0005] 2. Physical penetration enhancement technology: usually involves the use of physical means, such as microneedles, ultrasound, etc., to directly or indirectly increase the permeability of the skin to cosmetic ingredients.

[0006] 3. Bio-permeation technology: Utilizes bioactive substances, such as enzymes and peptides, to improve the skin's absorption of cosmetic ingredients. These bioactive substances may improve the skin's physiological state and increase skin permeability.

[0007] 4. Pharmaceutical technology: including the use of pharmaceutical principles such as microemulsion, liposomes, nanotechnology, etc. to prepare cosmetics to improve their permeability and stability.

[0008] The first three methods will more or less cause irreversible damage to the skin's stratum corneum barrier system, and may also introduce viral mycoplasmas during the penetration process and after irreversible damage. Furthermore, after other active ingredients enter through these three systems, they are released at high concentrations in a short period of time, greatly disrupting the subcutaneous microenvironment. The fourth method, drawing on pharmaceutical principles and technologies, not only solves the problem of short-term burst release of active ingredients, but also reduces the inactivation of active ingredients during cosmetic production, transportation, and storage. However, as an oral or targeted injection drug, its application in the cosmetics field will face a residence time issue. That is, when used as a drug, it can be slowly released in the digestive system, peripheral blood, and targeted areas. However, as a cosmetic, due to consumers' sweating, oily skin, and periodic facial cleansing, the active ingredients in the cosmetics cannot remain on the skin surface for a long time to be slowly released, thus failing to achieve the desired effect. Summary of the Invention

[0009] Based on this, the purpose of the present invention is to provide a multi-capsule system and its preparation method and application that promotes the retention and stable release of active ingredients, so that the effective ingredients in cosmetics can stay on the skin surface for a long time and slowly release into the subcutaneous tissue to achieve moisturizing, whitening, anti-wrinkle, anti-oxidation and other effects.

[0010] A multi-capsule system for promoting the retention and stable release of active components comprises an outer oil film, a component 1 wrapped inside the outer oil film, and a plurality of inner capsules, wherein the inner capsules are dispersed in the component 1; the inner capsules comprise a capsule shell and a component 2 wrapped inside the capsule shell; the outer oil film and the capsule shell are both substances absorbable by the skin; the component 1 is used to increase the water content of the loricrin in the skin stratum corneum to put it in a swollen state; the component 2 comprises an active component, and when the loricrin in the skin stratum corneum swells, the active component is bound to the loricrin via ionic bonds and / or covalent bonds.

[0011] When the multi-capsule system for promoting the retention and stable release of active ingredients described in the present invention comes into contact with human skin, the outer oil film is absorbed by the human skin and then component 1 and component 2 wrapped by the capsule shell are released. At this time, component 1 increases the water content of loricrin in the skin's stratum corneum, causing it to swell slightly. Subsequently, the capsule shell is also absorbed by the human skin, and component 2 is released and combines with loricrin in a slightly swollen state through ionic and covalent bonds. Even if the water in the stratum corneum evaporates later, this bond remains stable in the stratum corneum, and the active ingredient is not easily lost during daily skin washing, sweating, and oil production. Moreover, its concentration can be gradually increased with daily use. When the multi-capsule system is used in a basic cosmetic formula, the outer oil film can avoid interference from other base materials, and the capsule shell can prevent components 1 and 2 from undergoing ionic adsorption and covalent bond reactions, which can cause the active ingredient to lose its effectiveness before being applied to the skin. As keratinocytes metabolize, the skin environment changes, and the ionic and covalent bonds bound to loricrin gradually dissociate. With daily use, the active components gradually accumulate in the stratum corneum to a certain concentration and can gradually enter the subcutaneous tissue with the help of solubility differences. This diffusion process will not cause local explosive release, and the residual active components will be eliminated with the metabolism of keratinocytes, which will not destroy the barrier function of the stratum corneum and avoid adverse effects on the overall microenvironment of the skin.

[0012] Furthermore, the active components include but are not limited to one or more of blue copper peptide, recombinant collagen, glutathione, retinoids, carnosine, exosomes, biotin C, palmitoyl tripeptide-1, palmitoyl tetrapeptide-7, palmitoyl pentapeptide-4, palmitoyl hexapeptide-12, palmitoyl tripeptide-5, pentapeptide-3, hexapeptide-9, nonapeptide-1, undecapeptide-1, acetyl hexapeptide-8, acetyl dipeptide-1 spermaceti, acetyl octapeptide-3, acetyl tetrapeptide-5, glutathione, and corn peptide monomer TPM.

[0013] Furthermore, the mass ratio of the component 1 to the component 2 is (2-5):1.

[0014] Furthermore, the component 1 includes chitosan and its derivatives, sodium alginate, polyaspartic acid, and polyglutamic acid.

[0015] Furthermore, the mass ratio of chitosan and its derivatives, sodium alginate, polyaspartic acid and polyglutamic acid in component 1 is 1:3:2:4.

[0016] Furthermore, the component 1 further comprises one or more of transglutaminase, allantoin, hyaluronic acid, vitamin E, squalane, glycerin, sodium lactate, urea, seaweed extract, aloe extract, ceramide, and glycosaminoglycan.

[0017] Furthermore, the preparation method of component 2 comprises the following steps:

[0018] (1) dissolving the active component in a loricrin polypeptide and / or silk peptide solution, adding oligoarginine and / or lysine, and stirring to obtain a reaction solution;

[0019] (2) dialyzing and / or ultrafiltration the reaction solution to obtain a filtrate, adjusting the pH of the filtrate to alkaline, and adding zinc lactate;

[0020] (3) Freeze-dry for later use.

[0021] Furthermore, the outer oil film and the capsule shell both include one or more of cyclopentasiloxane, isononyl isononanoate and cetyl PEG / PPG-10 / 1 polydimethylsiloxane.

[0022] A method for preparing the multi-capsule system for promoting the retention and stable release of active ingredients comprises the following steps:

[0023] (1) Add component 2 to deionized water, heat and dissolve to obtain a component 2 solution, keep the solution warm for a certain period of time, then cool it down for later use;

[0024] (2) stirring the solution of component 2 and slowly adding the components of the capsule shell, controlling the stirring speed to prepare oil droplets of a desired size, and obtaining a water-in-oil system;

[0025] (3) Add component 1 to deionized water, heat and stir to dissolve uniformly to obtain a component 1 solution, and cool it for later use;

[0026] (4) adding the water-in-oil system to the solution of component 1, stirring and gradually adding the outer oil film component, and finally forming the multi-capsule system that promotes the retention and stable release of the active component.

[0027] An application of the multi-capsule system for promoting the retention and stable release of active ingredients in cosmetics; the cosmetics include but are not limited to the following forms: face cream, hand cream, hand mask, foot mask, and essence.

[0028] For better understanding and implementation, the present invention is described in detail below with reference to the accompanying drawings. BRIEF DESCRIPTION OF THE DRAWINGS

[0029] Figure 1 Schematic diagram of the structure of the multi-capsule system for promoting the retention and stable release of active ingredients in Examples 1 to 3. DETAILED DESCRIPTION

[0030] The terms used in the embodiments of this application are only for the purpose of describing specific embodiments and are not intended to limit the embodiments of this application. It should be made clear in this application that the embodiments described are only some embodiments of the embodiments of this application, not all embodiments. Based on the embodiments in the embodiments of this application, all other embodiments obtained by ordinary technicians in this field without making creative work are within the scope of protection of the embodiments of this application.

[0031] The terms used in the embodiments of the present application are only for the purpose of describing specific embodiments and are not intended to limit the embodiments of the present application. The singular forms of "a", "said" and "the" used in the embodiments of the present application and the appended claims are also intended to include plural forms, unless the context clearly indicates otherwise. It should be understood that the embodiments of the present application are not limited to the precise structures described above and shown in the accompanying drawings, and various modifications and changes can be made without departing from the scope thereof. The scope of the embodiments of the present application is limited only by the appended claims.

[0032] Example 1

[0033] A multi-capsule system for promoting the retention and stable release of active components comprises an outer oil film and components 1 and 2 wrapped inside the outer oil film, wherein component 2 is wrapped by a capsule shell and dispersed in component 1, and the mass ratio of component 1 to component 2 is 2:1.

[0034] The outer oil film and the capsule shell both include cyclopentasiloxane, isononyl isononanoate and cetyl PEG / PPG-10 / 1 polydimethylsiloxane.

[0035] Component 1 includes transglutaminase, chitosan and its derivatives, sodium alginate, polyaspartic acid, polyglutamic acid, and one or more of allantoin, hyaluronic acid, vitamin E, squalane, glycerin, sodium lactate, urea, seaweed extract, aloe extract, ceramide, and glycosaminoglycans. The chitosan and its derivatives, sodium alginate, polyaspartic acid, and polyglutamic acid in Component 1 have a mass ratio of 1:3:2:4. Component 1 is used to increase the water content of loricrin in the stratum corneum of the skin.

[0036] The component 2 includes an active component, and when the water content of the loricrin in the skin stratum corneum is high, the active component is bound to the loricrin through an ionic bond and / or a covalent bond; the active component includes but is not limited to one or more of blue copper peptide, recombinant collagen, glutathione, retinoid, carnosine, exosomes, biotin C, palmitoyl tripeptide-1, palmitoyl tetrapeptide-7, palmitoyl pentapeptide-4, palmitoyl hexapeptide-12, palmitoyl tripeptide-5, pentapeptide-3, hexapeptide-9, nonapeptide-1, undecapeptide-1, acetyl hexapeptide-8, acetyl dipeptide-1 spermaceti, acetyl octapeptide-3, acetyl tetrapeptide-5, glutathione, and corn peptide monomer TPM. The preparation method of the component 2 includes the following steps:

[0037] (1) dissolving the active component in a loricrin polypeptide and / or silk peptide solution, adding oligoarginine and / or lysine, and stirring to obtain a reaction solution;

[0038] (2) dialyzing and / or ultrafiltration the reaction solution to obtain a filtrate, adjusting the pH of the filtrate to alkaline, and adding zinc lactate;

[0039] (3) Freeze-dry for later use.

[0040] The method for preparing the multi-capsule system for promoting the retention and stable release of active components comprises the following steps:

[0041] (1) Add component 2 to deionized water, heat to 80-85°C to dissolve to obtain component 2 solution, keep warm for 20 minutes, and cool to below 50°C for later use;

[0042] (2) stirring the solution of component 2 and slowly adding the components of the capsule shell, controlling the stirring speed to prepare oil droplets of a desired size, and obtaining a water-in-oil system;

[0043] (3) Add component 1 to deionized water, heat to 80-85°C, and stir homogenously to dissolve to obtain a component 1 solution, and cool to below 60°C for later use;

[0044] (4) adding the water-in-oil system to the solution of component 1, stirring and gradually adding the outer oil film component, and finally forming the multi-capsule system that promotes the retention and stable release of the active component.

[0045] Example 2

[0046] A multi-capsule system for promoting the retention and stable release of active components comprises an outer oil film and components 1 and 2 wrapped inside the outer oil film, wherein component 2 is wrapped by a capsule shell and dispersed in component 1, and the mass ratio of component 1 to component 2 is 5:1.

[0047] The outer oil film and the capsule shell both include cyclopentasiloxane, isononyl isononanoate and cetyl PEG / PPG-10 / 1 polydimethylsiloxane.

[0048] The component 1 includes transglutaminase, chitosan and its derivatives, sodium alginate, polyaspartic acid, polyglutamic acid, allantoin, glycerol, and glycosaminoglycans; wherein the mass ratio of chitosan and its derivatives, sodium alginate, polyaspartic acid, and polyglutamic acid in the component 1 is 1:3:2:4; the component 1 is used to increase the water content of loricrin in the skin stratum corneum.

[0049] The component 2 and its preparation method are the same as those in Example 1.

[0050] The preparation method of the multi-capsule system for promoting the retention and stable release of active ingredients is the same as that in Example 1.

[0051] Example 3

[0052] A serum containing the multi-capsule system for promoting the retention and steady release of active components comprises the following ingredients: 86 wt% of water, 0.02 wt% of sodium EDTA-2, 7 wt% of 1,3-butylene glycol, 4 wt% of propylene glycol, 0.15 wt% of arginine, 0.2 wt% of cinnamone, 0.4 wt% of hyaluronic acid, 0.2 wt% of glycerol and 2.03 wt% of the multi-capsule system for promoting the retention and steady release of active components.

[0053] Comparative Example 1

[0054] A permeation-enhancing system comprises an outer oil film and components 1 and 2 wrapped inside the outer oil film, wherein component 2 is dispersed in component 1; the outer oil film, component 1, component 2 and their preparation method are the same as those in Example 1.

[0055] The penetration-enhancing system comprises the following steps:

[0056] (1) Add component 2 to deionized water, heat and dissolve to obtain a component 2 solution, keep the solution warm for a certain period of time, then cool it down for later use;

[0057] (2) adding component 1 to deionized water, heating and homogenizing and stirring to dissolve to obtain a component 1 solution, and cooling for later use;

[0058] (3) adding the solution of component 2 to the solution of component 1, stirring and gradually adding the outer oil film components to finally form the penetration-enhancing system.

[0059] Comparative Example 2

[0060] A permeation enhancement system comprises an outer oil film, a deionized water component encapsulated within the outer oil film, and a component 2, wherein the component 2 is encapsulated by a capsule shell and dispersed within the deionized water component. The component 2 and its preparation method are the same as those in Example 1; the outer oil film and the capsule shell are the same as those in Example 1.

[0061] The preparation method of the penetration-enhancing system comprises the following steps:

[0062] (1) adding the component 2 to deionized water, heating to 80-85°C to dissolve the component 2 solution, keeping the temperature for 20 minutes, and cooling to below 50°C for later use;

[0063] (2) stirring the solution of component 2 and slowly adding the components of the capsule shell, controlling the stirring speed to prepare oil droplets of a desired size, and obtaining a water-in-oil system;

[0064] (3) heating the deionized water component to 80-85° C. and stirring to dissolve the mixture, then cooling the mixture to below 60° C. for later use;

[0065] (4) adding the water-in-oil system to the ionized water component, stirring and gradually adding the outer oil film component to finally form a permeation-enhancing system.

[0066] The multicapsule systems for promoting the retention and stable release of active ingredients in Examples 1 and 2 were labeled as Sample A and Sample B, respectively, and the penetration-enhancing systems obtained in Comparative Examples 1 and 2 were labeled as Sample C and Sample D, respectively, and the following tests were performed:

[0067] 1. Transepidermal water loss test (refer to QB / T 4256-2011 Guidelines for Evaluation of Cosmetic Moisturizing Efficacy):

[0068] In order to verify the barrier repair performance of the present invention, the samples prepared in the examples and comparative examples were subjected to a moisturizing efficacy test.

[0069] Experimental Principle: Based on the fact that water has the highest dielectric constant, measuring skin capacitance reflects skin moisture content. Transepodermal water loss (TWEL) measures changes in water vapor pressure near the skin surface. TEWL indicates water loss from the stratum corneum and is an important criterion for evaluating the stratum corneum's barrier function. Lower TWEL values ​​indicate better barrier function, and vice versa. The Corneometer CM 825 and Tewameter™ 300 were used to measure the hydration level and transepodermal water loss of the skin's stratum corneum before and after application of the sample. These indicators reflect the sample's moisturizing properties.

[0070] Testing instruments: Corneometer CM 825 (CK electronic GmbH, Germany); Tewameter™ 300 (CK electronic GmbH, Germany).

[0071] Test Subjects: Each test sample was selected from volunteers with healthy skin, no history of skin diseases or allergies. Because the limbs are relatively uniform among individuals, they are suitable test areas. An appropriate area of ​​the flexor lateral area of ​​the volunteers' forearms was selected as the test area.

[0072] Test population: 60 healthy volunteers with no skin diseases and no significant differences in skin quality were selected, 15 people per group.

[0073] Test conditions: Let the volunteers calm down in an environment with a room temperature below 25℃±2℃ and a relative humidity (RH) below 50%±2%. Expose the test area 10 minutes before the test, and measure the stratum corneum hydration and transepidermal water loss (recorded as the control value).

[0074] Test Method: When determining the moisturizing effect of a sample, a single application test, typically completed within a short period of time, is appropriate. Apply 0.5 mL of the test sample to the area being tested and massage until fully absorbed. Measure the moisture content of the stratum corneum after application of the test sample and the transepidermal water loss (TEWL) of the epidermis before and after application (recorded as the test value).

[0075] The calculation formulas for the change rate of skin hydration and TEWL are as follows:

[0076]

[0077] The test results are averaged, see Table 1 below:

[0078] Table 1

[0079]

[0080] 2. Transdermal absorption test (using Franz diffusion cell method, refer to national standard GBT 27818-2011)

[0081] Experimental method: The suckling pig skin-Franz cell osmotic diffusion cell test was used for the test, with glutathione as the target substance.

[0082] Reagents: PBS buffer solution (Solyb), methanol (Sigma).

[0083] Equipment: TK-12D transdermal absorption diffusion instrument (Shanghai Kaikai), Franz cell (Shanghai Kaikai), high performance liquid chromatography (Agilent), KQ3200E ultrasonic cleaner (Kunshan Shumei), low temperature high speed centrifuge (Hunan Xiangyi).

[0084] Test steps:

[0085] (1) Preparation of ex vivo suckling pig skin: The dorsal skin of one-month-old suckling pig stored at -20°C was used as an ex vivo diffusion model, thawed with deionized water at room temperature, and repeatedly rinsed with PBS buffer.

[0086] (2) The suckling pig skin was fixed between the donor chamber and the receiving chamber of the Franz diffusion cell, with the stratum corneum facing the donor chamber and the dermis facing the receiving chamber.

[0087] (3) Fill the receiving chamber with receiving solution, tighten and fix the suckling pig skin, and then add 1.0 mL of receiving solution (PBS, pH 7.0-7.4) into the receiving chamber through the sampler. Expel the air to ensure that the dermis layer of the skin is in close contact with the receiving solution.

[0088] (4) Add the sample to the skin surface in the supply chamber. The effective penetration area S is about 3.14 cm 2 Add the sample to the pigskin surface and spread evenly from the center of the skin to the edge; repeat 3 times for each sample in parallel.

[0089] (5) Infiltration: The receiving cell was placed in a constant temperature water bath, the water bath temperature was set to (32±1)°C, and the electromagnetic stirrer was turned on and stirred at a speed of 300 rpm to ensure that there were no bubbles in the water bath interlayer.

[0090] (6) Monitoring the total cumulative permeability of the target substance at different time points: 2.0 mL of receiving solution was extracted from the receiving chamber at 24 h, 48 h, and 96 h through a sampling tube using a sampler, and then placed in a 2 mL EP tube. The glutathione concentration in the receiving solution was analyzed by liquid chromatography-mass spectrometry to obtain the total cumulative permeability of the target substance. In addition, an equal amount of receiving solution was added after each sampling.

[0091] (7) Testing of the supply chamber and skin cleansing fluid samples: After 96 hours, the residual sample in the supply chamber was aspirated and the skin surface and the inner wall of the supply chamber were rinsed multiple times with PBS buffer. The cleansing fluid and residual sample were combined and fixed to volume. The glutathione content was then analyzed by liquid chromatography-mass spectrometry under the same chromatographic and mass spectrometric conditions to obtain the content of the target substance that had not penetrated. A blank piglet back skin sample that was not used for the transdermal absorption test was processed in the same manner and used as a blank control for the skin surface sample to eliminate the influence of inherent components on the skin surface.

[0092] (8) Testing of dermal samples: Remove the cleaned skin and dry the surface liquid with filter paper. Cut the effective contact area of ​​the piglet back skin with the stratum corneum removed, cut it into pieces with surgical scissors, and then place it in 10 mL of receiving solution. Ultrasonicate for 60 minutes, grind it with an adjustable speed homogenizer, centrifuge, take about 1 mL of the supernatant, freeze it and store it for testing. Then, liquid chromatography-mass spectrometry is used to analyze the stratum corneum glutathione content that penetrates the dermis under the same chromatographic and mass spectrometry conditions, and finally obtain the stratum corneum cumulative retention rate. Take another blank pig back skin that is not used for transdermal absorption testing and treat it in the same way as above. Use it as a blank control for the dermal sample to eliminate the influence of the inherent components of the dermis.

[0093] Statistics and Analysis:

[0094] Cumulative permeability (%): P = Qn / Po × 100% = [Cn × V + ∑Ci × V0 (i = 1…n-1)] / Po × 100%;

[0095] Where: Qn: cumulative permeation amount measured at the nth sampling point in the receiving chamber (mg); V: volume of receiving liquid in the receiving chamber (mL); V0: volume of each sampling (mL); Ci: sample concentration in the receiving liquid at the i-th sampling; Cn: sample concentration measured at the n-th sampling point; P: diffusion percentage (%); Po: theoretical content of the sample in the receiving chamber (mg).

[0096] Cumulative retention rate (%) = total retention amount in the skin / theoretical content of the sample in the receptor compartment * 100%.

[0097] The test results are shown in Table 2 and Table 3 below:

[0098] Table 2 Total cumulative transmittance

[0099]

[0100] Table 3 Cumulative retention rate of stratum corneum

[0101]

[0102] It can be seen from Table 1, Table 2 and Table 3 that the stability of sample C of comparative example 1 is low because component 2 is not wrapped with a capsule shell, and it is easy to react with component 1 or other component materials and become ineffective, resulting in its transdermal effect being far inferior to sample A of Example 1 and sample B of Example 2; the moisturizing effect and water-locking ability of sample D of comparative example 2 that does not contain component 1 on the stratum corneum of the skin are obviously inferior to sample A of Example 1 and sample B of Example 2. Sample D cannot significantly increase the water content of loricrin in the skin and it is difficult to make it reach a swollen state, thereby affecting the binding of the active component to loricrin.

[0103] The present invention provides a multi-capsule system for promoting the retention and stable release of active components, comprising an outer oil film, a component 1 wrapped inside the outer oil film, and a plurality of inner capsules, wherein the inner capsules are dispersed in the component 1; the inner capsules comprise a capsule shell and a component 2 wrapped inside the capsule shell; the outer oil film and the capsule shell are both substances absorbable by the skin; the component 1 is used to increase the water content of the loricrin in the stratum corneum of the skin to put it in a swollen state; the component 2 comprises an active component, and when the loricrin in the stratum corneum of the skin swells, the active component is bound to the loricrin through ionic bonds and / or covalent bonds, so that the effective components in the cosmetics stay on the skin surface for a long time and are slowly released into the subcutaneous tissue to achieve moisturizing, whitening, anti-wrinkle, anti-oxidation and other effects.

[0104] The above-described embodiments merely represent several implementations of the present invention. While the descriptions are relatively specific and detailed, they should not be construed as limiting the scope of the present invention. It should be noted that a person skilled in the art would be able to make numerous variations and modifications without departing from the spirit of the present invention, and the present invention is intended to encompass such modifications and variations.

Claims

1. A multi-capsule system for promoting the retention and stable release of active ingredients, characterized by: It includes an outer oil film, a component 1 wrapped inside the outer oil film, and several inner capsules, wherein the inner capsules are dispersed in the component 1; the inner capsules include a capsule shell and a component 2 wrapped inside the capsule shell; the outer oil film and the capsule shell are both substances that can be absorbed by the skin; the component 1 is used to increase the water content of the loricrin in the stratum corneum of the skin to make it in a swollen state; the component 2 includes an active component, and when the loricrin in the stratum corneum of the skin swells, the active component is bound to the loricrin through ionic bonds and / or covalent bonds.

2. The multi-capsule system for promoting the retention and stable release of active ingredients according to claim 1, characterized in that: The active ingredients include but are not limited to one or more of blue copper peptide, recombinant collagen, glutathione, retinoid, carnosine, exosomes, biotin C, palmitoyl tripeptide-1, palmitoyl tetrapeptide-7, palmitoyl pentapeptide-4, palmitoyl hexapeptide-12, palmitoyl tripeptide-5, pentapeptide-3, hexapeptide-9, nonapeptide-1, undecapeptide-1, acetyl hexapeptide-8, acetyl dipeptide-1 spermaceti, acetyl octapeptide-3, acetyl tetrapeptide-5, glutathione, and corn peptide monomer TPM.

3. The multi-capsule system for promoting the retention and stable release of active ingredients according to claim 1, characterized in that: The mass ratio of the component 1 to the component 2 is (2-5):

1.

4. The multi-capsule system for promoting the retention and stable release of active ingredients according to claim 1, characterized in that: The component 1 comprises chitosan and its derivatives, sodium alginate, polyaspartic acid and polyglutamic acid.

5. The multi-capsule system for promoting the retention and stable release of active ingredients according to claim 4, characterized in that: The mass ratio of chitosan and its derivatives, sodium alginate, polyaspartic acid and polyglutamic acid in the component 1 is 1:3:2:

4.

6. The multi-capsule system for promoting the retention and stable release of active ingredients according to claim 4, characterized in that: The component 1 further comprises one or more of transglutaminase, allantoin, hyaluronic acid, vitamin E, squalane, glycerin, sodium lactate, urea, seaweed extract, aloe extract, ceramide, and glycosaminoglycan.

7. The multi-capsule system for promoting the retention and stable release of active ingredients according to claim 1, characterized in that: The preparation method of the component 2 comprises the following steps: (1) dissolving the active component in a loricrin polypeptide and / or silk peptide solution, adding oligoarginine and / or lysine, and stirring to obtain a reaction solution; (2) dialyzing and / or ultrafiltration the reaction solution to obtain a filtrate, adjusting the pH of the filtrate to alkaline, and adding zinc lactate; (3) Freeze-dry for later use.

8. The multi-capsule system for promoting the retention and stable release of active ingredients according to claim 1, characterized in that: The outer oil film and the capsule shell both include one or more of cyclopentasiloxane, isononyl isononanoate and cetyl PEG / PPG-10 / 1 polydimethylsiloxane.

9. A method for preparing the multicapsule system for promoting the retention and stable release of active ingredients according to any one of claims 1 to 8, comprising the following steps: (1) Add component 2 to deionized water, heat and dissolve to obtain a component 2 solution, keep the solution warm for a certain period of time, then cool it down for later use; (2) stirring the solution of component 2 and slowly adding the components of the capsule shell, controlling the stirring speed to prepare oil droplets of a desired size, and obtaining a water-in-oil system; (3) Add component 1 to deionized water, heat and stir to dissolve uniformly to obtain a component 1 solution, and cool it for later use; (4) adding the water-in-oil system to the solution of component 1, stirring and gradually adding the outer oil film component, and finally forming the multi-capsule system that promotes the retention and stable release of the active component.

10. Use of the multi-capsule system for promoting the retention and stable release of active ingredients according to any one of claims 1 to 8 in cosmetics; the cosmetics include but are not limited to the following forms: face cream, hand cream, hand mask, foot mask, and essence.