Permeation promoting composition and application thereof in skin care products

Abstract

The invention discloses a permeation promoting composition and application thereof in skin care products, and particularly belongs to the field of cosmetics. The permeation enhancing composition is prepared by compounding hydroxyethyl chitosan and decapeptide-4, and the permeation enhancing composition is prepared by compounding the hydroxyethyl chitosan and the decapeptide-4; the penetration enhancing composition provided by the invention can improve the transdermal absorption rate of the target functional component, so that the target functional component can effectively act on deep skin, and the effective utilization rate of the functional component is improved; the permeation enhancing composition can be applied to skin care products with the effects of tightening, wrinkle resisting, moisturizing, repairing, oil controlling and relieving, and the requirements of consumers for efficient and safe skin care products are met.

Description

Technical Field

[0001] The invention belongs to the technical field of cosmetic preparations, and in particular relates to a penetration-promoting composition and application thereof in skin care products. Background Art

[0002] In the field of skin care products and drug delivery, improving the penetration efficiency of active ingredients has always been the focus and difficulty of research and development. As the largest organ of the human body, the skin's barrier function effectively blocks harmful substances from entering the body, but it also limits the transdermal absorption of many beneficial ingredients (such as nutrients and drugs in skin care products). Therefore, developing efficient and safe penetration enhancers to promote active ingredients to better penetrate the skin barrier and reach deep tissues is the key to achieving efficient skin care products and effective drug treatment.

[0003] As a natural biopolymer, hydroxyethyl chitosan has been widely used in skin care products due to its excellent moisturizing, biocompatibility and skin repair ability. Its unique molecular structure can form a protective film on the skin surface to lock in moisture, while promoting the metabolism of skin cells and enhancing the skin barrier function. More importantly, through chemical modification, hydroxyethyl chitosan can reduce the molecular weight and improve the transdermal absorption capacity, becoming an effective penetration enhancer ingredient.

[0004] As a signal peptide, decapeptide-4 has shown remarkable effects in promoting penetration, anti-aging, repairing damaged skin and improving skin quality in recent years. It can stimulate the synthesis of collagen, elastin and hyaluronic acid in the skin, thereby increasing skin elasticity and reducing wrinkles and fine lines. However, although the molecular weight of decapeptide-4 is moderate, its ability to improve transdermal absorption efficiency is still limited in unoptimized formulas, making it difficult to fully realize its skin care potential.

[0005] In summary, the main research direction of the present invention is to provide a penetration-enhancing composition that can solve the problem of low penetration efficiency of active ingredients in the prior art, and at the same time, the ingredients can promote each other and interact with each other, thereby achieving the efficient effect of the effective ingredients and meeting consumers' demand for efficient and safe skin care products. Summary of the invention

[0006] In view of the shortcomings of the prior art, the present invention provides a penetration-enhancing composition composed of hydroxyethyl deacetylated chitosan and decapeptide-4, aiming to solve the problem of low penetration efficiency of active ingredients in the prior art, and to achieve efficient transmission of effective ingredients in skin care products through scientific proportioning and process optimization, thereby meeting consumers' demand for efficient and safe skin care products.

[0007] To achieve the above object, the present invention discloses the following technical solutions:

[0008] In a first aspect, the present invention provides a penetration-enhancing composition, which is prepared by compounding hydroxyethyl deacetylated chitosan and decapeptide-4.

[0009] Preferably, the composition comprises the following components by weight:

[0010] Hydroxyethyl chitosan 0.015-0.15 parts;

[0011] Decapeptide-4 0.0001-0.0006 parts.

[0012] In a second aspect, the present invention provides an essence containing a penetration-enhancing composition, wherein the essence comprises the penetration-enhancing composition described in the first aspect and a target penetration-enhancing component.

[0013] Preferably, the target penetration-enhancing component is at least one of a polypeptide and a polysaccharide.

[0014] Preferably, the polypeptide is recombinant collagen; and the polysaccharide is sodium hyaluronate.

[0015] More preferably, it further comprises a pH adjuster, a thickener, a humectant, a preservative and a solvent.

[0016] More preferably, the pH regulator is arginine;

[0017] The thickener is carbomer;

[0018] The moisturizing agent is ethylhexylglycerin and / or 1,2-hexanediol;

[0019] The preservative is p-hydroxyacetophenone and / or 1,2-pentanediol;

[0020] The solvent is deionized water.

[0021] In a third aspect, the present invention provides a method for preparing the essence containing the penetration-enhancing composition according to the second aspect, the preparation method comprising the following steps:

[0022] S1. Preparation of hydroxyethyl chitosan solution: hydroxyethyl chitosan, 1,2-pentanediol and p-hydroxyacetophenone were added to deionized water in sequence, mixed and stirred at 50°C and 200 r / min for 30 minutes, cooled to 25°C, and passed through a 200-mesh sieve to obtain a hydroxyethyl chitosan solution;

[0023] S2. Preparation of decapeptide-4 solution: decapeptide-4 and arginine were added to deionized water, mixed and stirred at 25°C and 200 r / min for 30 min, and passed through a 200 mesh sieve to obtain a decapeptide-4 solution;

[0024] S3. The hydroxyethyl deacetylated chitosan solution and the decapeptide-4 solution were mixed and stirred at 25° C. and 200 r / min to obtain component A;

[0025] S4. Ethylhexylglycerol and 1,2-hexanediol were mixed and stirred at 25° C. and 200 r / min to obtain component B;

[0026] S5. Mix the target penetration-enhancing component with deionized water, and stir evenly at 25° C. and 200 r / min to obtain component C;

[0027] S6. Heat the deionized water to 85° C. and keep the temperature, add carbomer and stir evenly to obtain component D;

[0028] S7. Cool component D to 60°C, add component B, stir evenly, then cool to 25°C, add component A and component C, stir evenly, discharge, and obtain essence.

[0029] Preferably, the stirring speed of step S6 is 600 r / min; the stirring speed of step S7 is 200 r / min.

[0030] In a fourth aspect, the present invention provides the use of the penetration-enhancing composition described in the first aspect in the preparation of a skin care product with firming, anti-wrinkle, moisturizing, repairing, oil-controlling and / or soothing effects.

[0031] In the present invention:

[0032] Hydroxyethyl chitosan has a significant effect in transdermal effect. It can be used as a permeation enhancer to form nanoparticles through self-assembly. These nanoparticles have the characteristics of small particle size and easy transdermal penetration. They can stably encapsulate the effective ingredients of various skin care products and achieve efficient transdermal delivery and absorption of these ingredients.

[0033] Decapeptide-4 has multiple effects, including promoting transdermal absorption, anti-aging and anti-wrinkle, and eliminating fat. It promotes transdermal absorption by regulating ATP1B1 protein and enhances the recovery of the skin barrier. Decapeptide-4 can also mimic the growth factor involved in skin growth, healing and wound repair, promote the production of collagen and elastin, improve skin elasticity and firmness, support the active generation of new skin cells, and reduce fine lines and wrinkles. In addition, it acts as an anabolic peptide in adipose tissue, blocking the production of new triglycerides and restructuring subcutaneous adipose tissue.

[0034] Hydroxyethyl chitosan is used in combination with decapeptide-4, wherein hydroxyethyl chitosan can be used as a carrier to carry decapeptide-4 into the skin by utilizing its transdermal absorption enhancement properties, thereby improving the utilization efficiency of decapeptide-4. The two promote each other and synergistically improve the skin's absorption rate of the active ingredients.

[0035] Beneficial effects of the present invention:

[0036] The penetration-enhancing composition provided by the present invention can improve the transdermal absorption rate of the target functional component, so that the target functional component can effectively act on the deep skin layer, thereby improving the effective utilization rate of the functional component. DETAILED DESCRIPTION

[0037] The following will be combined with the embodiments of the present invention to clearly and completely describe the technical solutions in the present invention. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of the embodiments. Based on the embodiments of the present invention, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of the present invention.

[0038] The technical solution of the present invention is further described in detail below in conjunction with specific embodiments. It should be understood that the following embodiments are only used to explain the present invention and are not used to limit the present invention.

[0039] In the present invention:

[0040] Hydroxyethyl deacetylated chitosan: purchased from Zhongke Houpu (Guangzhou) Technology Development Co., Ltd., specification: ≥98%;

[0041] Decapeptide-4: purchased from Shandong Jipeptide Biotechnology Co., Ltd., specification: ≥98%, amino acid sequence: Cys-Asp-Leu-Arg-Arg-Leu-Glu-Met-Tyr-Cys;

[0042] Transdermal short peptide: Chengdu Yunxi Chemical Co., Ltd., amino acid sequence: Ala-Cys-Ser-Ser-Ser-Pro-Ser-Lys-His-Cys-Gly;

[0043] Sodium hyaluronate: purchased from Jiangsu Chuangjian Medical Technology Co., Ltd.;

[0044] Collagen: Recombinant collagen type I was purchased from Jiangsu Chuangjian Medical Technology Co., Ltd.

[0045] Preparation of penetration enhancing composition:

[0046] Step 1-1, preparation of hydroxyethyl chitosan solution: hydroxyethyl chitosan, 1,2-pentanediol and p-hydroxyacetophenone are sequentially added into deionized water, mixed and stirred at 50° C. and 200 r / min for 30 min, cooled to 25° C., and passed through a 200-mesh sieve to obtain a hydroxyethyl chitosan solution;

[0047] Step 1-2, preparation of decapeptide-4 solution: add decapeptide-4 and arginine to deionized water, mix and stir at 25° C. and 200 r / min for 30 min, and pass through a 200 mesh sieve to obtain a decapeptide-4 solution;

[0048] Step 1-3, the hydroxyethyl deacetylated chitosan solution and the decapeptide-4 solution are mixed and stirred at 25° C. and 200 r / min to obtain component A.

[0049] Preparation of application examples:

[0050] Step 2-1, ethylhexylglycerol and 1,2-hexanediol are mixed, and stirred at 25° C. and 200 r / min to obtain component B;

[0051] Step 2-2, mixing sodium hyaluronate, collagen and deionized water, and stirring at 25° C. and 200 r / min to obtain component C;

[0052] Step 2-3, heating deionized water to 85° C. and then keeping the temperature, adding carbomer and stirring at 600 r / min until completely dispersed, to obtain component D;

[0053] Step 2-4, cool component D to 60°C, add component B and stir evenly at 200r / min, then cool to 25°C, add component A and component C and stir evenly at 200r / min, discharge and obtain essence.

[0054] Table 1 Mass percentage of raw materials in application examples

[0055]

[0056] Note: “-” in the table means no addition.

[0057] Performance experiment:

[0058] Experimental animals: 40 male ICR mice (20±2 g) were purchased from Beijing Weitonglihua Experimental Animal Technology Co., Ltd.

[0059] This test example evaluates the in vitro transdermal effects of Application Examples 1-5 and Comparative Examples 1-5 by using a transdermal diffusion tester.

[0060] Healthy male ICR mice with intact skin were selected, and their abdominal hair was removed after anesthesia with 2% chloral hydrate, and they were killed by dislocating the neck, peeling the skin of the lower abdomen, and carefully removing excess fat, and stored at -20°C for use. Seven experimental groups (Application Example 1, Application Example 2, Application Example 3, Application Example 4, Application Example 5, Comparative Example 1, Comparative Example 2 and Comparative Example 4) and two control groups (the blank control group was Comparative Example 3, and the positive control group was Comparative Example 5) were set up, with 4 mice in each group.

[0061] After thawing at room temperature, the ex vivo mouse skin was fixed in a Franz diffusion cell with the stratum corneum facing upwards. PBS was used as the receiving solution. 0.5 g of each group of preparations was added to the supply chamber. The in vitro transdermal experiment was carried out at 37°C and 300 rpm. 0.2 mL of the sample was taken every 1 h for 1-12 h, and the sample was immediately supplemented with an equal volume of fresh blank receiving solution at the same temperature. The cumulative permeation per unit area (Q 12 ).

[0062] The calculation formula is as follows:

[0063]

[0064] In the formula, C n is the drug (collagen and sodium hyaluronate) concentration (μg / mL) at the nth sampling point, Ci is the drug (collagen and sodium hyaluronate) concentration (μg / mL) at the ith sampling point, A is the effective drug administration area (3.14 cm 2 ), V is the volume of the receiving solution (mL). The specific results are shown in Table 2.

[0065] Table 2 Transdermal penetration parameters of different groups

[0066] Group <![CDATA[Collagen / Q 12 (μg / cm 2 )]]> <![CDATA[Sodium hyaluronate / Q 12 (μg / cm 2 ) <!-- 4 -->]]> Blank (Comparative Example 3) 0.36 1.15 Positive (Comparative Example 5) 8.32 15.72 Application Example 1 10.11 17.16 Application Example 2 12.28 23.08 Application Example 3 13.89 24.05 Application Example 4 12.94 23.24 Application Example 5 12.53 21.39 Comparative Example 1 5.06 8.94 Comparative Example 2 4.10 7.92 Comparative Example 4 9.14 16.27

[0067] Result analysis:

[0068] According to the results, the penetration-enhancing composition provided by the present invention has an obvious effect of promoting transdermal penetration on collagen and sodium hyaluronate. The use of hydroxyethyl deacetylated chitosan alone or decapeptide-4 alone also has a transdermal penetration-enhancing effect compared with the blank group. However, the penetration-enhancing effect of the effective ingredients when hydroxyethyl deacetylated chitosan and decapeptide-4 are used in combination is more obvious than when the two are used alone, which proves that the hydroxyethyl deacetylated chitosan and decapeptide-4 in the penetration-enhancing composition provided by the present invention have a mutually promoting effect on the penetration-enhancing effect.

[0069] Finally, it should be noted that the above embodiments and comparative examples are only used to illustrate the technical solution of the present invention rather than to limit the protection scope of the present invention. Although the present invention has been described in detail with reference to the preferred embodiments, those skilled in the art should understand that the technical solution of the present invention can be modified or replaced by equivalents without departing from the essence and scope of the technical solution of the present invention.

Claims

1. A penetration-enhancing composition, characterized in that The composition is prepared by compounding hydroxyethyl deacetylated chitosan and decapeptide-4.

2. The penetration-enhancing composition according to claim 1, characterized in that The composition comprises the following components by weight: Hydroxyethyl chitosan 0.015-0.15 parts; Decapeptide-4 0.0001-0.0006 parts.

3. An essence containing a penetration-enhancing composition, characterized in that: The essence contains the penetration-enhancing composition according to claim 1 or 2, and a target penetration-enhancing component.

4. The essence containing the penetration-enhancing composition according to claim 3, characterized in that: The target penetration-enhancing component is at least one of a polypeptide and a polysaccharide.

5. The essence containing the penetration-enhancing composition according to claim 4, characterized in that: The polypeptide is recombinant collagen, and the polysaccharide is sodium hyaluronate.

6. The essence containing the penetration-enhancing composition according to any one of claims 3 to 5, characterized in that: It also contains pH adjusters, thickeners, humectants, preservatives, and solvents.

7. The essence containing the penetration-enhancing composition according to claim 6, characterized in that: The pH regulator is arginine; The thickener is carbomer; The moisturizing agent is ethylhexylglycerin and / or 1,2-hexanediol; The preservative is p-hydroxyacetophenone and / or 1,2-pentanediol; The solvent is deionized water.

8. The method for preparing the essence containing the penetration-enhancing composition according to claim 7, characterized in that: The preparation method comprises the following steps: S1. Preparation of hydroxyethyl chitosan solution: hydroxyethyl chitosan, 1,2-pentanediol and p-hydroxyacetophenone were added to deionized water in sequence, mixed and stirred at 50°C and 200 r / min for 30 minutes, cooled to 25°C, and passed through a 200-mesh sieve to obtain a hydroxyethyl chitosan solution; S2. Preparation of decapeptide-4 solution: decapeptide-4 and arginine were added to deionized water, mixed and stirred at 25°C and 200 r / min for 30 min, and passed through a 200 mesh sieve to obtain a decapeptide-4 solution; S3. The hydroxyethyl chitosan solution and the decapeptide-4 solution were mixed and stirred at 25° C. and 200 r / min to obtain component A; S4. Ethylhexylglycerol and 1,2-hexanediol were mixed and stirred at 25° C. and 200 r / min to obtain component B; S5. Mix the target penetration-enhancing component with deionized water, and stir evenly at 25° C. and 200 r / min to obtain component C; S6. Heat the deionized water to 85° C. and keep the temperature, add carbomer and stir evenly to obtain component D; S7. Cool component D to 60°C, add component B, stir evenly, then cool to 25°C, add component A and component C, stir evenly, discharge, and obtain essence.

9. The method for preparing the essence containing the penetration-enhancing composition according to claim 8, characterized in that: The stirring speed of step S6 is 600 r / min; the stirring speed of step S7 is 200 r / min.

10. Use of the penetration-enhancing composition according to claim 1 or 2 in the preparation of skin care products with firming, anti-wrinkle, moisturizing, repairing, oil-controlling and / or soothing effects.

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