Peptide composition for skin care product and preparation method thereof

Abstract

The invention provides a peptide composition for skin care products and a preparation method of the peptide composition, and belongs to the technical field of cosmetics. The composition includes liposome-resin hybrid particles, a competitive cationic compound, and a gelling agent. The hybrid particle is formed by cation exchange resin and peptide-loaded cationic liposome through electrostatic interaction, a competitive cationic compound (such as choline chloride) can prevent competitive adsorption of other cations, and a gelling agent (such as ammonium acryloyldimethyl taurate / VP copolymer) forms a three-dimensional network structure to prevent particle sedimentation. According to the system, the physical and chemical stability of peptide components in a liquid formula is remarkably improved, transdermal absorption is promoted by utilizing lipidosome, and the system is suitable for anti-aging, barrier repairing and moisturizing skin care products.

Description

TECHNICAL FIELD

[0001] The present application belongs to the technical field of cosmetics, and relates to a stable peptide composition based on a liposome-resin hybrid structure, a preparation method thereof, and application thereof in skin care products. BACKGROUND

[0002] Peptide components are increasingly widely used in anti-aging, skin barrier repair and moisturizing skin care products due to their excellent biocompatibility and clear physiological activity. Small molecule active peptides such as pentapeptide have become a research hotspot in recent years due to their outstanding effects of promoting collagen synthesis and regulating cell metabolism. However, peptide components in skin care product formulations face two major challenges: first, the low transdermal absorption efficiency, the lipid barrier of the stratum corneum and the polar characteristics of peptides themselves result in a transdermal rate of most active peptides of less than 5%, making it difficult to reach the dermis to play a role; second, the poor stability, which is easily affected by the pH value, temperature and enzymatic action of the system, seriously restricting the manifestation of its efficacy.

[0003] Although the existing technology has a general concept of using ion exchange resin to load active ingredients to improve stability, when this technology is applied to liquid skin care products of peptide active ingredients (especially pentapeptide), there are inherent defects that cannot be overcome: first, the resin particles are prone to sedimentation and caking, affecting the sensory of the product; second, and most importantly, the existing technology ignores the competitive adsorption of common cationic components (such as preservatives) in liquid formulations to resin sites, which will cause peptides to be displaced and rapidly degraded during storage, resulting in product failure.

[0004] In addition, there is a bottleneck in the transdermal absorption efficiency. Therefore, there is an urgent need in the art for a new technology and new formulation system that can systematically improve the physical stability, chemical stability and transdermal efficiency of peptides in liquid skin care products. SUMMARY

[0005] The purpose of the present application is to provide a peptide composition for skin care products and a preparation method thereof, which effectively improves the stability and absorption of peptide components in liquid formulations.

[0006] The purpose of the present application can be achieved by the following technical solutions: In a first aspect, the present application provides a peptide composition for skin care products, comprising the following components: a) liposome-resin hybrid particles, the liposome-resin hybrid particles being composed of a cation exchange resin and a peptide-loaded cationic liposome adsorbed on the surface thereof by electrostatic action; b) a competitive cationic compound; c) a gelling agent; The dry weight ratio of the peptide-carrying cationic liposomes to the cation exchange resin is 1:3 to 1:1.

[0007] As used in this text, the term "liposome-resin hybrid particle" refers to a composite functional particle constructed through electrostatic interactions: a cation exchange resin serves as the core framework, while peptide-carrying cationic liposomes are adsorbed onto the resin surface through electrostatic forces.

[0008] The "electrostatic adsorption" mentioned in the text refers to the electrostatic attraction between the negatively charged cation exchange resin surface and the positively charged peptide-carrying cationic liposomes. The positive charge of these liposomes originates from the cationic lipids modified on their surface and the positively charged peptides encapsulated within them.

[0009] As used in this text, "peptide-carrying cationic liposomes" refers to a type of functionalized nanovesicle constructed by integrating cationic lipids into a phospholipid bilayer. The internal water core encapsulates peptide active ingredients (such as pentapeptides), and the surface exhibits a net positive charge. This structure not only effectively protects peptides from degradation by the formulation environment through physical encapsulation, but also utilizes the positive charge on its surface to generate electrostatic interactions with the negatively charged resin and the stratum corneum of the skin, thereby simultaneously achieving stable adsorption with the resin carrier and synergistic improvement in transdermal efficiency.

[0010] Preferably, the cationic lipid content in the peptide-loaded cationic liposomes is 3% to 6% of the total lipid weight of the liposomes. This content range ensures that the liposomes are effectively adsorbed by the resin in the formulation and can be effectively released when in contact with the skin in a high ionic strength environment.

[0011] Preferably, the cationic lipid is stearamide propyl dimethylamine.

[0012] The “competitive cationic compounds” mentioned in the text refer to a class of harmless cations (such as choline chloride) that are added in excess. By preferentially occupying the unused adsorption sites of cation exchange resins, they form a dynamic protective layer during storage, effectively blocking the competitive replacement of the resin-liposome complex structure by other cationic components (such as preservatives) in the formulation, thereby avoiding the premature release and degradation of peptide active ingredients and ensuring the chemical stability of the product.

[0013] Preferably, the competitive cationic compound is choline chloride.

[0014] As used in this text, the term "gelling agent" refers to a functional material that can spontaneously construct a three-dimensional network structure in an aqueous phase through intermolecular interactions (such as ammonium acryloyl dimethyl taurate / VP copolymer). The thixotropic gel network formed by it can generate significant yield stress, effectively suspend solid particles to prevent sedimentation when left to stand, and quickly restore fluidity when shear force is applied, thereby simultaneously achieving the unity of long-term physical stability and excellent skin feel of the system.

[0015] Preferably, the gelling agent is an ammonium acryloyldimethyl taurate / VP copolymer. This type of resin can remain fully ionized within the pH range commonly used in cosmetics, providing a stable and strong negatively charged surface, making it an ideal choice for forming robust electrostatic adsorption.

[0016] Preferably, the cation exchange resin is a polystyrene-divinylbenzenesulfonic acid type resin.

[0017] Preferably, the peptide is a pentapeptide.

[0018] Preferably, the peptide-loaded cationic liposomes further include a penetration enhancer, which is azone or phytosphingosine. The introduction of the penetration enhancer can further enhance the membrane fluidity of the liposomes and disturb the lipid structure of the stratum corneum of the skin, thereby providing additional synergistic effects in the transdermal process.

[0019] The composition of this invention achieves excellent storage stability while also possessing intelligent release characteristics during use: when applied to the skin, the high concentration of physiological cations such as sodium and potassium in the interstitial fluid of the stratum corneum can competitively exchange ions with choline chloride and peptide-carrying cationic liposomes that pre-occupy resin sites in the system, effectively disrupting the electrostatic adsorption between the liposomes and the resin, promoting the dissociation of the peptide-carrying liposomes and further interacting with the negatively charged stratum corneum of the skin. Through lipid fusion and electrostatic adsorption, the encapsulated active peptides are efficiently delivered to the deep layers of the skin.

[0020] Secondly, the present invention provides a method for preparing a peptide composition for skincare products, comprising the following steps: (1) Preparation of peptide-loaded cationic liposomes; (2) The peptide-loaded cationic liposomes obtained in step (1) are mixed with cation exchange resin to form liposome-resin hybrid particles; (3) Add a competitive cationic compound to the liposome-resin hybrid particles obtained in step (2) and premix to obtain premixed hybrid particles; (4) Dissolve the rheology modifier in the aqueous phase to form a matrix; (5) Disperse the premixed hybrid particles obtained in step (3) into the matrix obtained in step (4).

[0021] The beneficial effects of this invention are: This invention improves the stability of peptide active ingredients in a liquid environment through a dual protection mechanism of liposome encapsulation and resin adsorption. Secondly, the introduction of competitive cationic compounds effectively blocks the competitive substitution of the active ingredient by other components in the formulation, enhancing the product's efficacy stability throughout its shelf life. Finally, this system not only improves the problem of sedimentation and clumping in traditional resin complexes but also enhances the bioavailability of the active ingredient through the permeation-enhancing properties of liposomes. Detailed Implementation

[0022] To further illustrate the technical means and effects of the present invention in achieving its intended purpose, the following detailed description of the specific implementation methods, structures, features, and effects of the present invention, in conjunction with embodiments, is provided below.

[0023] While peptide active ingredients (such as pentapeptides) are highly effective in anti-aging and other fields, they face the dual challenges of stability and transdermal efficiency in liquid skincare formulations. Through systematic research, the inventors discovered that the root cause of peptide failure in liquid skincare products lies in their lack of a stable structure to resist the corrosive effects of the formulation environment and the lack of an efficient delivery pathway to the site of action. Traditional technologies only perform localized optimization through single methods, failing to construct an integrated system of synergistic protection and delivery. To overcome this limitation, the inventors innovatively proposed a synergistic mechanism of "liposome-resin hybrid structure," "competitive cation protection," and "three-dimensional network suspension," achieving multiple protections and intelligent release of peptides through structural design, thereby simultaneously improving their stability and absorption efficiency. This led to the creation of this invention.

[0024] Example 1 A method for preparing liposome-resin hybrid particles in a peptide composition for use in skincare products, specifically comprising the following steps: (1) Preparation of peptide-loaded cationic liposomes: 450 mg of hydrogenated lecithin, 160 mg of cholesterol, 32 mg of stearamide propyl dimethylamine (5% of the total lipid weight), and 10 mg of phytosphoin were weighed and dissolved in an appropriate amount of ethanol. The organic solvent was removed by rotary evaporation in a 50°C water bath to form a uniform lipid film. Then, 10 mL of phosphate buffer (pH 6.5, 0.01 M) containing 50 mg of pentapeptide was added, and the mixture was hydrated by rotary evaporation for 30 minutes at the same temperature. The resulting liposome suspension was extruded five times each through 400 nm and 200 nm polycarbonate membranes to obtain peptide-loaded cationic liposomes with uniform particle size distribution. The average particle size was 185 nm and the Zeta potential was +35 mV, as determined by dynamic light scattering. (2) Formation of liposome-resin hybrid particles: Weigh 1.0 g of sulfonic acid type polystyrene-divinylbenzene cation exchange resin (such as Amberlite™ IRP69) into a beaker and add 10 mL of deionized water to swell. Under stirring conditions, slowly add the peptide-loaded cationic liposome dispersion obtained in step (1) to the resin suspension, wherein the dry weight ratio of cationic liposomes to cation exchange resin is 1:1.5. Continue stirring for 2 hours to form liposome-resin hybrid particles; (3) Premixing protection: 0.3 g of choline chloride was slowly added to the liposome-resin hybrid particle mixture obtained in step (2) under stirring conditions, and stirring was continued at room temperature for 30 minutes to obtain premixed hybrid particles. After the reaction was completed, the mixture was filtered and the filter cake was rinsed slightly with deionized water to finally obtain wet premixed hybrid particles.

[0025] Example 2 A method for preparing a peptide composition for use in skincare products includes the following steps: (1) Preparation of peptide-loaded cationic liposomes: Peptide-loaded cationic liposomes were prepared according to the method in step (1) of Example 1; (2) Formation of liposome-resin hybrid particles: Liposome-resin hybrid particles were prepared according to step (2) in Example 1; (3) Premixing protection: Following the method in step (3) of Example 1, choline chloride was added to obtain premixed hybrid particles; (4) Dissolve the gelling agent in the aqueous phase to form a matrix: In 200 mL of deionized water, 0.8 g of ammonium acryloyl dimethyl taurate / VP copolymer (such as Aristoflex AVC) was slowly added under stirring (800 rpm) and stirred until completely dispersed. Then, the pH of the matrix system was adjusted to 6.0 with triethanolamine to form a clear and transparent gel matrix. (5) Disperse the liposome-resin hybrid particles in the matrix: The wet liposome-resin hybrid particles obtained in Example 1 (with a dry weight of approximately 1.0 g) were added to the matrix obtained in step (4), followed by the addition of 3.0 g glycerol, 1.0 g phenoxyethanol and 0.2 g ethylhexylglycerol. Finally, the mixture was homogenized at 2000 rpm for 5 minutes and degassed under vacuum to obtain the peptide composition essence of the present invention.

[0026] Example 3 A method for preparing a peptide composition for use in skincare products includes the following steps: The difference between this embodiment and Example 2 is that the amount of stearamide propyl dimethylamine used in the preparation of peptide-loaded cationic liposomes is adjusted to 19 mg (accounting for 3% of the total weight of lipids), while the remaining steps and raw material amounts are exactly the same as in Example 2.

[0027] Example 4 A method for preparing a peptide composition for use in skincare products includes the following steps: The difference between this embodiment and Example 2 is that the amount of stearamide propyl dimethylamine used in the preparation of peptide-loaded cationic liposomes is adjusted to 50 mg (accounting for 7.5% of the total weight of lipids), while the remaining steps and raw material amounts are exactly the same as in Example 2.

[0028] Comparative Example 1 The pentapeptide-resin complex was prepared using a conventional process: 1.0 g of sulfonic acid-type polystyrene-divinylbenzene cation exchange resin was swollen and then mixed with a solution of 50 mg of pentapeptide at pH 4.5 for 2 hours. After filtration, a wet conventional pentapeptide-resin complex was obtained. This wet complex was dispersed in the same matrix as in Example 2 (but without competing cations) at the same addition amount (based on the dry weight of the resin), and homogenized to obtain a comparative sample.

[0029] Comparative Example 2 The preparation process is exactly the same as in Example 2, but without the addition of choline chloride.

[0030] Comparative Example 3 The liposome-resin hybrid particles in Example 2 were directly replaced with the pentapeptide-resin complex prepared in Comparative Example 1, and the remaining steps and raw material amounts were exactly the same as in Example 2.

[0031] Comparative Example 4 The acrylamide dimethyl taurate ammonium / VP copolymer in Example 2 was replaced with the same amount of ordinary carbomer (such as Carbomer 940), neutralized to the same pH, and the remaining steps and raw material amounts were exactly the same as in Example 2.

[0032] Performance testing: 1. Stability Testing: The test was designed with reference to drug stability guidelines and common methods in the cosmetics industry to assess the stability of samples under accelerated conditions (40°C, 75% RH, 60 days) to predict their long-term storage stability. Physical stability was assessed by visual observation and centrifugation; chemical stability was determined by HPLC.

[0033] 2. Transdermal Performance Testing: Following the general principles of in vitro transdermal testing in the "Cosmetic Efficacy Evaluation Standards," freshly prepared samples were used. A Franz diffusion cell was employed, with fresh, excised porcine skin as the transdermal barrier. The receiving chamber was filled with a pH 7.4 phosphate buffer solution containing 30% ethanol as the receiving solution, and the temperature was maintained at a constant 37°C. Samples were taken at 2, 4, 8, 12, and 24 hours. After filtration through a 0.22 μm filter membrane, the pentapeptide content was determined by HPLC, and the cumulative permeation per unit area was calculated.

[0034] Table 1. Accelerated stability test results (60 days) Table 2 Transdermal performance test results Note: The cumulative permeation over 24 hours in Example 2 is calculated as 100%.

[0035] The above experimental results demonstrate that the peptide compositions provided by this invention exhibit significant advantages in terms of physical stability, chemical stability, and transdermal performance. In particular, Examples 2 and 3 maintained high active ingredient content and good physical stability even after a 60-day accelerated test, while also demonstrating excellent transdermal efficiency, fully validating the synergistic effect of the liposome-resin hybrid particles, competitive cation protection, and three-dimensional network suspension system.

[0036] The above description is merely a preferred embodiment of the present invention and is not intended to limit the present invention in any way. Although the present invention has been disclosed above with reference to preferred embodiments, it is not intended to limit the present invention. Any person skilled in the art can make some modifications or alterations to the above-disclosed technical content to create equivalent embodiments without departing from the scope of the present invention. Any simple modifications, equivalent changes and alterations made to the above embodiments based on the technical essence of the present invention without departing from the scope of the present invention shall still fall within the scope of the present invention.

Claims

1. A peptide composition for use in skincare products, characterized in that, Includes the following components: a) Liposome-resin hybrid particles, wherein the liposome-resin hybrid particles are composed of a cation exchange resin and peptide-carrying cationic liposomes adsorbed on its surface by electrostatic interaction. b) Competitive cationic compounds; c) Gelling agents; The dry weight ratio of the peptide-carrying cationic liposomes to the cation exchange resin is 1:3 to 1:

1.

2. The peptide composition for use in skincare products as described in claim 1, characterized in that, The cationic lipid content in the peptide-loaded cationic liposomes is 3% to 6% of the total lipid weight of the liposomes.

3. The peptide composition for skincare products as described in claim 2, characterized in that, The cationic lipid is stearamidopropyl dimethylamine.

4. The peptide composition for use in skincare products as described in claim 1, characterized in that, The competitive cationic compound is choline chloride.

5. The peptide composition for use in skincare products as described in claim 1, characterized in that, The gelling agent is an ammonium acryloyldimethyl taurate / VP copolymer.

6. The peptide composition for use in skincare products as described in claim 1, characterized in that, The cation exchange resin is a polystyrene-divinylbenzenesulfonic acid type resin.

7. The peptide composition for use in skincare products as described in claim 1, characterized in that, The peptide in question is a pentapeptide.

8. The peptide composition for use in skincare products as described in claim 1, characterized in that, The peptide-loaded cationic liposomes also include a penetration enhancer, which is azone or phytosphingosine.

9. A method for preparing a peptide composition for use in skincare products as described in any one of claims 1 to 8, characterized in that, Includes the following steps: (1) Preparation of peptide-loaded cationic liposomes; (2) The peptide-loaded cationic liposomes obtained in step (1) are mixed with cation exchange resin to form liposome-resin hybrid particles; (3) Add a competitive cationic compound to the liposome-resin hybrid particles obtained in step (2) and premix to obtain premixed hybrid particles; (4) Dissolve the rheology modifier in the aqueous phase to form a matrix; (5) Disperse the premixed hybrid particles obtained in step (3) into the matrix obtained in step (4).

10. Use of a peptide composition for skin care products as described in any one of claims 1 to 8 in the preparation of skin care products for anti-aging, skin barrier repair, or moisturizing.

Images