阅读说明：本技术 调节皮肤细胞微环境的活性组合物及其制备方法与应用 (Active composition for regulating microenvironment of skin cells as well as preparation method and application thereof ) 是由 孙乐青 于 2019-11-15 设计创作，主要内容包括：本发明涉及一种调节皮肤细胞微环境的活性组合物及其制备方法与应用。本发明提供的调节皮肤细胞微环境的活性组合物的活性成分为β-葡聚糖、肌肽、棕榈酰寡肽、二棕榈酰羟脯氨酸和尿囊素,这五种活性组分通过超分子自组装技术处理组合后外用,各组分协同增效,从而能够更有效持续调节皮肤细胞微环境,疏通细胞间信号通路,增加细胞外基质的分泌,促进胶原蛋白的合成,捕获细胞间活性羰基,防止皮肤因羰基化而造成肤色加深,此外,还加速皮肤自我更新,启动抗老修护,加速细胞增殖代谢,抚平皱纹细纹,淡化色斑暗斑,改善皮肤的整体质感和外观。(The active components of the active composition for regulating the microenvironment of the skin cells comprise β -glucan, carnosine, palmitoyl oligopeptide, dipalmitoyl hydroxyproline and allantoin, the five active components are treated and combined by a supermolecule self-assembly technology and then are externally used, and the components have synergistic interaction, so that the microenvironment of the skin cells can be effectively and continuously regulated, intercellular signal pathways are dredged, the secretion of extracellular matrix is increased, the synthesis of collagen is promoted, intercellular active carbonyl groups are captured, the skin color deepening caused by carbonylation is prevented, in addition, the self renewal of the skin is accelerated, the anti-aging repair is started, the cell proliferation and metabolism are accelerated, wrinkles and fine lines are smoothed, color spots and dark spots are lightened, and the overall texture and appearance of the skin are improved.)

1. An active composition for regulating microenvironment of skin cells comprises β -dextran, carnosine, palmitoyl oligopeptide, dipalmitoyl hydroxyproline and allantoin.

2. Active composition according to claim 1, characterized in that its active components comprise:

3. active composition according to claim 1, characterized in that its active components comprise:

preferably, the active components thereof comprise:

4. a process for preparing an active composition with skin microenvironment promoting effect of any one of claims 1-3, which comprises using purified water as solvent, β -dextran, carnosine, palmitoyl oligopeptide, dipalmitoyl hydroxyproline and allantoin as active components, making a clear and transparent system, adjusting pH to 4.5-6.5, freezing, and thawing to allow intermolecular self-assembly of the active components to form a supramolecular structure composition.

5. The method of claim 4, wherein the pH is adjusted to 4.5-6.0, preferably 5.0 ± (0.2-0.5); and/or the presence of a gas in the gas,

repeatedly freezing and thawing for 1-10 times to allow the active ingredient to fully perform intermolecular self-assembly.

6. The method of claim 4 or 5, wherein the freezing is performed at 0 ℃ to-30 ℃, preferably for 1-20 hours per freezing; and/or the time for each thawing is 1-20 hours.

7. The method for producing according to any one of claims 4 to 6, further comprising a step of ultrasonic treatment before the freezing treatment; preferably, the conditions of the ultrasonic treatment are: ultrasonic frequency is 15-60Khz, and ultrasonic treatment time is 10-120 minutes.

8. An active composition prepared by the method of any one of claims 4-7.

9. Use of an active composition according to any one of claims 1 to 3, 7 for the preparation of a pharmaceutical, cosmetic or biological material.

10. A cosmetic comprising the active composition according to any one of claims 1 to 3 or 7;

preferably, the cosmetic comprises the following components in parts by weight:

Technical Field

The invention relates to an active composition for regulating microenvironment of skin cells, and also provides a preparation method and application of the active composition.

Background

With the age, the skin will gradually show aging symptoms, mainly manifested by the symptoms of deepening wrinkles, dark yellow skin color, dryness, desquamation, deepening color spots and pigments, and the like. The skin care product has the advantages of seriously affecting the quality of life of people, causing a series of uncertain skin diseases and seriously troubling the skin health of people. The prior art mainly solves the problem of dark yellow skin by inhibiting the activity of neuraminidase or promoting cutin shedding through the whitening agents, but the whitening agents such as arbutin, kojic acid, nicotinamide, salicylic acid and the like are poor in stability and have strong irritation to the skin. For fine wrinkles, the fine wrinkles are mainly solved by facial filling and other surgical methods at the present stage, and the fine wrinkles are high in cost and have large side effects.

Disclosure of Invention

The invention provides an active composition for regulating the microenvironment of skin cells, which has the dual effects of whitening and brightening the skin and smoothing wrinkles and fine lines based on a system biological mechanism.

The inventor researches and discovers that β -glucan, carnosine, palmitoyl oligopeptide, dipalmitoyl hydroxyproline and allantoin are taken as active ingredients and are combined for external use, and the active ingredients are synergistic, so that the microenvironment of skin cells can be effectively and continuously regulated, intercellular signal pathways are dredged, the secretion of extracellular matrix is increased, the synthesis of collagen is promoted, intercellular active carbonyl groups are captured, the skin color deepening caused by carbonylation of the skin is prevented, in addition, the self renewal of the skin is accelerated, the anti-aging repair is started, the cell proliferation metabolism is accelerated, wrinkles and fine lines are smoothed, color spots and dark spots are lightened, and the overall texture and appearance of the skin are improved.

The invention provides an active composition for regulating microenvironment of skin cells, which comprises β -glucan, carnosine, palmitoyl oligopeptide, dipalmitoyl hydroxyproline and allantoin as active components.

Further, the active composition with the effect of promoting the microenvironment of the skin comprises the following active components:

still further, the active composition having the effect of promoting the microenvironment of the skin comprises the following active components:

in some preferred embodiments of the present invention, the active ingredients in the active composition having the effect of promoting the microenvironment of the skin comprise:

in some embodiments of the present invention, the active composition for promoting the skin microenvironment is composed of or prepared from β -dextran, carnosine, palmitoyl oligopeptide, dipalmitoyl hydroxyproline, and allantoin as active ingredients.

The brief introduction of the five active components is as follows:

β -glucan is a flat spiral structure and is an accelerant and an activator of skin macrophage, so β -glucan can be used for healing wounds and resisting inflammation, and improving the immunity and the tumor of the skin, β -glucan has good compatibility, does not reduce the efficacy of other active additives, has a considerable penetration assisting effect, and is widely used as a humectant, a sun-screening agent, a soap-free detergent and a conditioner.

Carnosine is a dipeptide composed of two amino acids, namely β -alanine and L-histidine, can protect cells against oxidative stress, is used as an anti-inflammatory and anti-aging ingredient in cosmetics, can be used for cosmetics such as creams, gels, body milks, sun screens and the like, and hair care products such as shampoos, hair conditioners, hair gels, hair tonic, hair dyes and the like.

Palmitoyl oligopeptide is synthetic peptide composed of 3 amino acids such as glycine, histidine, lysine and the like, acts on the dermis, can promote the synthesis of extracellular matrixes such as type I and III collagen, elastin and structural glycoprotein such as laminin and fibronectin, strengthens the dermis, enables the skin to be thicker and firmer, relieves wrinkles and has stronger capacity of resisting ultraviolet irradiation. In some embodiments of the invention, the palmitoyl oligopeptide is more than or equal to 95% pure.

Dipalmitoyl hydroxyproline is an amino acid peculiar to skin collagen, the content of the collagen is generally represented by 7.46 times of dipalmitoyl hydroxyproline, allantoin and allantoin, and the reduction of the content of the dipalmitoyl hydroxyproline in a skin layer can be used as an index of the skin aging degree. Under the irradiation of ultraviolet rays or strong sunlight, the quantity of L-dipalmitoyl hydroxyproline in stratum corneum protein is greatly changed, and the reduction of the L-dipalmitoyl hydroxyproline is in direct proportion to the degree of wrinkles and aging of the skin, so that the dipalmitoyl hydroxyproline can be used as an exogenous nutritional additive and has the effects of skin moisture preservation, anti-aging, sun protection and the like; dipalmitoyl hydroxyproline has effect in inhibiting melanin generation, has inhibition rate of 18% at concentration of 0.1mmol/L, and can be used as whitening auxiliary agent. In the invention, dipalmitoyl hydroxyproline and glycine contained in palmitoyl oligopeptide enter the skin and then are bonded with the skin to consume proline in the cell microenvironment, so that collagen is generated, the skin color deepening caused by the absorption of ultraviolet rays by the proline is reduced, and in addition, the formed collagen can effectively fill and smooth fine wrinkles. In some embodiments of the invention, dipalmitoyl hydroxyproline is greater than or equal to 98% pure.

Allantoin is a substance which softens the stratum corneum of the skin, helps dead skin cells to drop off, helps the skin to keep more water and makes the skin smooth, easily reaches the deep layer of the skin, and promotes fibroblasts to generate more collagen, elastin and mucopolysaccharide, so that the formation of wrinkles can be effectively reduced and prevented.

Generally, the active composition with the effect of promoting the skin microenvironment can be prepared by taking β -glucan, carnosine, palmitoyl oligopeptide, dipalmitoyl hydroxyproline and allantoin as active components and adopting a conventional method in the field, for example, the components are taken according to a ratio, mixed and then added with purified water, stirred until the system is clear and transparent, or further freeze-dried, and then crushed into particles of 50-200 meshes for storage.

Surprisingly, it has been found that the active components of the active composition can be subjected to a supramolecular recognition self-assembly treatment, so as to play a sustained release role and significantly reduce skin irritation.

Specifically, the present invention also provides a preparation method of the above active composition, comprising:

preparing a clear and transparent system by using purified water as a solvent and β -glucan, carnosine, palmitoyl oligopeptide, dipalmitoyl hydroxyproline and allantoin as active components, adjusting the pH to 4.5-6.5, freezing, and then thawing to perform intermolecular self-assembly on the active components to form the composition with the supermolecular structure.

Among them, a clear and transparent system can be prepared by, for example, mixing β -dextran, carnosine, palmitoyl oligopeptide, dipalmitoyl hydroxyproline, and allantoin in the formulation amounts, slowly adding purified water, and continuously stirring until the system is clear and transparent.

Further, the pH of the clear and transparent system is adjusted to be between 4.5 and 6.0, more preferably between 5.0 ± (0.2 and 0.5). Researches show that the intermolecular force in the system is stronger in the pH range, and the intermolecular recognition and self-assembly are more facilitated.

In some embodiments of the invention, the pH of the clear transparent system is adjusted to 4.5, 4.8, 5.0, 5.2, or 5.5.

pH adjusting agents commonly used in the art, such as citric acid, salicylic acid, lactic acid, glycolic acid, and the like, may be used.

Further, the freezing treatment is preceded by an ultrasonic treatment step, under the promotion of ultrasonic cavitation, on one hand, molecular motion is intensified, collision opportunities among molecules are increased, and preliminary complexation or self-assembly is generated among the molecules, on the other hand, materials with larger polymerization degree, such as a small amount of β -glucan with molecular weight more than 50 ten thousand daltons, are broken, so that the polymerization degree is reduced, and the self-assembly among the molecules is facilitated, and in addition, small molecular materials are also beneficial to the permeation and absorption of skin.

In some embodiments of the present invention, the sonication conditions are: ultrasonic frequency is 15-60Khz, and ultrasonic treatment time is 10-120 minutes.

In some embodiments of the invention, the sonication is performed at room temperature (20-25 ℃).

In some embodiments of the present invention, the freezing is performed under a closed condition, which has an advantage of using a cyclic directional freezing-thawing (DFT) method, which is a biomimetic biosynthesis technique for inducing intermolecular self-assembly by changing external conditions, and has a main advantage of ensuring the biological activity of the base material, and after entering the skin, the base material slowly and spontaneously releases the self-assembly to release the active substance, thereby reducing the irritation of the active substance to the skin, and further, the active substance which is difficult to enter the skin can be complexed with the active substance with strong skin permeability by the self-assembly to promote the active substance to enter the deep layer of the skin to exert the biological activity.

Further, in the above preparation method, freezing and thawing may be repeated 1 to 10 times (for example, 5 times) to allow the active ingredient to sufficiently undergo intermolecular self-assembly.

In some embodiments of the invention, the freezing is carried out at a temperature of from 0 ℃ to-30 ℃, for example-25 ℃, preferably for a time period of from 1 to 20 hours, for example 12 hours, per freezing.

In some embodiments of the invention, the time for each thaw is 1 to 20 hours.

The invention also comprises an active composition prepared by the supermolecule recognition self-assembly treatment.

The invention also comprises the application of the active composition with the function of promoting the microenvironment of the skin in the aspects of preparing medicines, cosmetics, biological materials and the like.

Specifically, the invention also provides a cosmetic which contains the active composition for regulating the microenvironment of skin cells or takes the active composition for regulating the microenvironment of skin cells as a main active ingredient. The cosmetic has skin brightening and wrinkle removing functions, and also has lasting moisturizing effect, and can be used as skin care product;

in some embodiments of the invention, the main active components in the cosmetic for promoting the skin microenvironment are β -glucan, carnosine, palmitoyl oligopeptide, dipalmitoyl hydroxyproline and allantoin, and the cosmetic comprises the following components in parts by weight:

the humectant and thickener can be selected conventionally in the art. For example, the humectant can be selected from glycerol xylitol, erythritol, betaine, ceramide, hyaluronic acid, Tremella polysaccharide, etc., and the thickener can be selected from xanthan gum, carbomer, hydroxyethyl cellulose, flaxseed gum, etc.

The basic principle of the invention is as follows: with the increase of age, intercellular signal pathways of skin are blocked, metabolism is slowed down, extracellular matrix secretion mainly comprising collagen is slowed down, collagen degradation speed is accelerated, and wrinkles and fine lines appear; the amount of proline generated by the degradation of collagen is increased, and the amount of dipalmitoyl hydroxyproline and glycine required by the synthesis of skin collagen by consuming proline is reduced, wherein the proline has the function of absorbing ultraviolet rays to deepen the color of the skin, so that the dark yellow degree of the skin is deeper; in addition, amino groups on protein molecules react with carbonyl groups on sugar molecules to generate glycosylated proteins (AGEs), the aging of tissue structures caused by the generation of the AGEs is difficult to repair, finally, collagen is crosslinked, the skin loses elasticity, lipofuscin is gradually accumulated, the skin color is gradually dark, and senile plaques are generated.

The invention combines the thought of 'integration, syndrome differentiation and unification' of the traditional Chinese medicine and the view of modern system biology, regulates the ecological balance of skin microenvironment, gets through skin cell signal channels, accelerates the proliferation and metabolism of skin cells, and stimulates the self-renewal of skin, thereby eliminating fine lines and wrinkles, improving the appearance of skin, lightening dark spots and spots, and improving the integral texture and appearance of skin.

Detailed Description

The following examples are intended to illustrate the invention but are not intended to limit the scope of the invention. The examples do not show the specific techniques or conditions, according to the technical or conditions described in the literature in the field, or according to the product specifications. The reagents or instruments used are conventional products available from regular distributors, not indicated by the manufacturer.

β -dextran is purchased from Sigma-Aldrich Sigma Aldrich trade company Limited and has a molecular weight of 5000-5 ten thousand, carnosine is purchased from Shanghai Merlin Biotechnology company Limited and has a purity of 98%, palmitoyl oligopeptide is purchased from Doudoshi chemical company Limited and has a purity of 95%, dipalmitoyl hydroxyproline is purchased from Sichuan Gingji biological medicine company Limited and has a purity of 98%, allantoin is purchased from Dissmann group of Switzerland has a purity of 99%, and Rosa damascena flower water is purchased from California Rose group.