阅读说明：本技术 一种用于提升角质层含水量的组合物 (composition for increasing water content of stratum corneum ) 是由 胡嘉奂 顾红健 贺来健 于 2019-10-17 设计创作，主要内容包括：本发明提供一种用于提升角质层含水量的组合物,所述组合物包含二十二碳六烯酸、蛋白质和作为活性物载体的卵磷脂。本发明还提供所述用于提升角质层含水量的组合物的用途。(The invention provides compositions for increasing the hydration of the stratum corneum, the compositions comprising docosahexaenoic acid, a protein and lecithin as an active carrier.)

A composition for increasing the moisture content of the stratum corneum, said composition comprising docosahexaenoic acid, a protein and lecithin as an active carrier.

2. The composition of claim 1, wherein the lecithin is present in an amount of 0.01% to 10% (W/W), the docosahexaenoic acid is present in an amount of 0.0001% to 10% (W/W), and wherein the protein is present in an amount of 0.0001% to 10% (W/W).

3. The composition of claim 2, wherein the lecithin is present in an amount of 0.1% to 8% (W/W), the docosahexaenoic acid is present in an amount of 0.001% to 5% (W/W), and wherein the protein is present in an amount of 0.001% to 5% (W/W).

4. The composition according to claim 3, wherein the lecithin is present in an amount of 0.2% to 5% (W/W), the docosahexaenoic acid is present in an amount of 0.005% to 1% (W/W), and wherein the protein is present in an amount of 0.005% to 1% (W/W).

5. The composition according to claim 4, wherein the lecithin is present in an amount of 0.5% to 3% (W/W), the docosahexaenoic acid is present in an amount of 0.01% to 0.1% (W/W), and wherein the protein is present in an amount of 0.005% to 0.1% (W/W).

6. The composition of any of claims 1-5, wherein the lecithin is hydrogenated phosphatidylcholine.

7. The composition of any of , wherein the protein is selected from the group consisting of mussel mucin extract.

8. The composition of any of , wherein the composition further comprises at least of a moisturizer, a vegetable oil, an anti-inflammatory soothing agent, an antioxidant, and a pH modifying agent.

9. The composition of claim 8, wherein the humectant is at least selected from glycerin, glycol, sucrose laurate, hydrolyzed sodium hyaluronate, and sodium hyaluronate, the vegetable oil is selected from squalane, the anti-inflammatory soothing agent is selected from dipotassium glycyrrhizinate, the antioxidant is selected from tocopherol or tocopherol acetate, and the pH adjusting agent is at least selected from sodium citrate and citric acid.

10. The composition of claim 9, wherein the glycol is selected from 1, 3-propanediol.

11. Use of a composition comprising lecithin, docosahexaenoic acid and a protein for improving the skin barrier.

12. Use of a composition comprising lecithin, docosahexaenoic acid and a protein for increasing the content of natural moisturizing factors.

13. Use of a composition comprising lecithin, docosahexaenoic acid and a protein for moisturizing skin.

Technical Field

The present invention relates to a composition comprising docosahexaenoic acid and protein and lecithin as an active carrier, which can promote the production of natural moisturizing factors, increase the content of the natural moisturizing factors, and thus improve the skin barrier.

Background

The normal healthy stratum corneum contains 10% -20% water to maintain the skin's moisture and elasticity. When the moisture content in the stratum corneum is reduced to below 10% due to changes in climatic conditions such as age, cold and dryness, the skin will appear dry, wrinkled and gradually age. Modern cosmetic development has focused on protecting skin and delaying skin aging. Therefore, it is of great significance to study the reason why the water in the stratum corneum of the skin can be maintained.

Natural Moisturizing Factor (NMF) is an important component of the stratum corneum, and is an important factor for maintaining the health of the stratum corneum and controlling the moisture content of the stratum corneum, so that the stratum corneum can keep moisture to resist the dryness of the environment. NMF is also important to maintain the physical properties of the stratum corneum, which can be rendered plastic by the water retained by NMF, and to maintain skin elasticity against cracking and flaking due to external mechanical stress. The main source of NMF is a derivative of Filaggrin (FLG). Cysteine proteinase 14(Caspase-14) acts on filaggrin to hydrolyze into free amino acids and form moisturizing factors during the terminal differentiation process of keratinocytes, thereby regulating the hydration function of stratum corneum, so that the relative expression level of cysteine proteinase 14 is closely related to the permeation barrier of skin.

Keratinocytes are the main cells of the epithelium, and the stratum corneum, the last stage of keratinocyte differentiation, is the main barrier to prevent foreign substances from entering the human body and water loss in the body. During the differentiation process, filaggrin, Loricrin (LOR), incrustation protein (IVL) and the like can be expressed, and the proteins are crossed and connected to form a keratinization envelope and play an important role in maintaining the epithelial barrier of the cell skin.

In recent years, with the continuous and intensive research on a silk polymerization protein gene (FLG), more and more evidences show that the mutation of the gene is related to the occurrence of various skin diseases.

fatty acids, which are PPAR agonists, stimulate the metabolism of cellular lipids, and filaggrin, which is proteins activated by PPAR agonists and expresses upregulated proteins, plays a major role in the integrity of the skin barrier, the regulation of skin pH, UV resistance and the onset of atopic dermatitis, it has been reported in the literature that the disruption of skin barrier function caused by abnormal expression of Filaggrin (FLG) protein may be , which causes the pathogenesis of skin diseases in infants, and fatty acids may promote the expression of barrier protein at the gene level, which may play an important role in improving abnormal skin barrier function.

However, there is still a need to provide a composition for promoting the production of natural moisturizing factors, increasing the content of natural moisturizing factors, and thus improving the skin barrier.

Disclosure of Invention

Without wishing to be bound by any theory, it is believed that lecithin, when applied in cosmetics, can improve skin hydration as a penetration enhancer, effectively promoting transdermal absorption of active ingredients in cosmetics, thereby achieving highly effective delivery of active ingredients in cosmetics.

In 1844, Gohley, a french person, finds lecithin from egg yolk and is named Lecithos (lecithin) in Greek, belongs to mixtures, is groups of yellow brown greasy substances existing in animal and plant tissues and egg yolk, and comprises phosphoric acid, choline, fatty acid, glycerol, glycolipid, triglyceride and phospholipid, the lecithin is known as a third nutrient juxtaposed to protein and vitamin, and is also a synonym of lecithin and pure phosphatidylcholine, the lecithin is mixtures, mainly comprises Phosphatidylcholine (PC), Phosphatidylethanolamine (PE), Phosphatidylinositol (PI), Phosphatidylserine (PS) and the like, and the lecithin has a tail with a double hydrophobic structure, can form vesicles by directly dispersing in water, has an ordered bilayer structure of the phospholipid, meets the conditions in a surfactant, and can serve as an emulsifier to the extent of .

However, when phospholipid is used as an emulsifier to emulsify oil, phosphatidylcholine in a lecithin mixture is beneficial to promoting the formation of O/W type emulsion, phosphatidylethanolamine is beneficial to promoting the formation of W/O type emulsion, and the phosphatidylcholine and the phosphatidylethanolamine are mutually inhibited, so that the hydrophilic-lipophilic balance (HLB) value of lecithin is low, the emulsifying capacity is not strong, and the application of lecithin in cosmetics is greatly limited.

The inventors have surprisingly found that the composition of the present invention comprising docosahexaenoic acid and protein as active ingredients can better maintain the stability of the composition by a relay emulsification method using lecithin as a carrier without compounding other emulsifiers.

The mussel mucin is secreted byssus of marine mussels, also called mussel byssus protein, is special proteins secreted by marine mussels, namely purple mussels, thick-shell mussels, emerald mussels and the like, has high strength, high toughness and high water resistance.

The mussel mucin for use in the invention is in the form of an extract thereof.

accordingly, the present invention provides compositions for increasing the hydration of the stratum corneum, said compositions comprising docosahexaenoic acid and protein as active ingredients and lecithin as an active carrier.

According to preferred embodiments, the lecithin is present in an amount of 0.01% to 10% (W/W), the docosahexaenoic acid is present in an amount of 0.0001% to 10% (W/W), and wherein the protein is present in an amount of 0.0001% to 10% (W/W).

According to another preferred embodiments, the lecithin is present in an amount of 0.1% to 8% (W/W), the docosahexaenoic acid is present in an amount of 0.001% to 5% (W/W), and wherein the protein is present in an amount of 0.001% to 5% (W/W).

According to preferred embodiments, the lecithin is present in an amount of 0.2% to 5% (W/W), the docosahexaenoic acid is present in an amount of 0.005% to 1% (W/W), and wherein the protein is present in an amount of 0.005% to 1% (W/W).

According to another preferred embodiments, the lecithin is present in an amount of 0.5% to 3% (W/W), the docosahexaenoic acid is present in an amount of 0.01% to 0.1% (W/W), and wherein the protein is present in an amount of 0.005% to 0.1% (W/W).

According to preferred embodiments, the lecithin is hydrogenated phosphatidylcholine.

According to another preferred embodiments, the protein is selected from the group consisting of mussel mucin extract.

According to preferred embodiments, the protein is selected from the group consisting of mussel mucin or mussel mucin extract, the mussel mucin extract comprising mussel mucin polypeptides and other hydrolysates.

According to preferred embodiments, the composition further comprises at least of a moisturizer, a vegetable oil, an anti-inflammatory soothing agent, an antioxidant, and a pH adjusting agent.

The moisturizer in the composition of the present invention can form film on the skin surface to seal the moisture in the skin to prevent the moisture from evaporating, and at the same time, does not interfere with the absorption of moisture in the air by the skin, thereby maintaining the proper moisture content of the skin.

The vegetable oil and fat in the composition can be retained on the surface of the skin, plays a role in lubrication in the stratum corneum, fills the space on the surface of the skin, replaces the lipid lost in the stratum corneum, keeps the skin soft, flexible and smooth, reduces the scaly skin and improves the appearance of the skin.

The anti-inflammatory and soothing agent in the composition has the effects of resisting inflammation, killing bacteria and soothing nerves.

The antioxidants of the compositions of the present invention can prevent the adverse effects of oxygen and thus can help to trap and neutralize free radicals, thereby removing free radical damage to human skin.

The pH adjusting agent in the composition of the present invention is capable of interacting with the acidic material in the composition to adjust the pH of the composition.

The humectant is at least selected from glycerol, 1, 3-propylene glycol, sucrose laurate, hydrolyzed sodium hyaluronate and sodium hyaluronate, the vegetable oil is squalane, the anti-inflammatory soothing agent is dipotassium glycyrrhizinate, the antioxidant is tocopherol or tocopherol acetate, and the pH regulator is at least selected from sodium citrate and citric acid.

According to a most preferred embodiment, the composition consists of:

composition (I)	Content (g)
		Water (W)	To 100
Glycerol	30.00
		Hydrolyzed sodium hyaluronate	0.001
Docosahexaenoic acid	0.05
		Tocopherol (vitamin E)	0.000115
Mussel mucin extract	1.00
		Citric acid	0.001
Squalane	4.00
		Sucrose laurate	1.00
Hydrogenated phosphatidylcholine	1.05
		1, 3-propanediol	1.20
Glycyrrhizic acid dipotassium salt	0.50

The composition of the present invention comprising docosahexaenoic acid and protein and lecithin as an active carrier can increase the expression level of cysteine protease 14, promote the production of the natural moisturizing factor PCA, increase the content of the natural moisturizing factor, and thus improve the skin barrier, wherein lecithin is used as an active carrier in the composition of the present invention, according to preferred embodiments, the lecithin is hydrogenated phosphatidylcholine, which is extracted from soybean and hydrogenated, which has high purity and good stability compared to other lecithins.

The composition can be prepared into different dosage forms according to different requirements, and preferably skin external preparations, including liquid, gel, emulsion, cream, foam, patch and the like. However, it will be understood by those skilled in the art that the compositions of the present invention may be supplemented with various desired additives, including but not limited to, humectants, vegetable fats and oils, anti-inflammatory soothing agents, antioxidants, and pH adjusting agents, and the like, depending on the various dosage forms of the composition. The composition of the present invention may further comprise various excipients as required depending on various formulations of the composition. For example, when the composition of the present invention is prepared as a liquid, the excipient may be selected from water, physiological saline, etc.; when the composition of the present invention is prepared into a gel, the excipient may be selected from cellulose derivatives, starch, gelatin, agar, polysaccharides, and the like; when the composition of the present invention is prepared into a cream, the excipient may be selected from glycerin, vaseline, paraffin, etc.; when the composition of the present invention is prepared into a foaming agent, the excipient may be selected from hydroxypropyl methyl cellulose, sodium lauryl sulfate polyethylene glycol, sodium fatty alcohol-polyoxyethylene ether sulfonate, etc.; when the composition of the present invention is prepared as a patch, the excipient may be selected from cellulose derivatives, starch, gelatin, agar, polysaccharides, and the like.

The composition for increasing the water content of the stratum corneum and various dosage forms of the present invention can be prepared according to conventional methods known to those skilled in the art.

In a second aspect, the present invention provides the use of a composition comprising lecithin, docosahexaenoic acid and a protein for improving the skin barrier.

In a third aspect, the present invention provides the use of a composition comprising lecithin, docosahexaenoic acid and a protein for increasing the content of natural moisturizing factors.

In a fourth aspect, the present invention provides the use of a composition comprising lecithin, docosahexaenoic acid and protein for moisturizing skin.

In a fifth aspect, the present invention provides a composition for increasing the moisture content of the stratum corneum, obtained according to the manufacturing method of the present invention, comprising docosahexaenoic acid and protein as active ingredients, and lecithin as an active carrier.

Unexpectedly, the inventors have unexpectedly discovered that in compositions using lecithin as the active carrier, proteins, particularly mussel mucin extract, are able to synergize with docosahexaenoic acid, thereby increasing the expression of cysteine protease 14, promoting the production of the natural moisturizing factor PCA, increasing the natural moisturizing factor content, and thus increasing the stratum corneum moisture content.

The composition for increasing the water content of the horny layer has the advantages that:

lecithin has the effect of increasing the expression of cysteine protease 14 as an active carrier in cosmetic compositions. When the lecithin is applied in cosmetics, the lecithin can be used as a penetration enhancer to improve skin hydration and effectively promote the transdermal absorption of active ingredients in effective cosmetics, so that the highly effective delivery of the active ingredients in the cosmetics is realized.

The composition for increasing the water content of the stratum corneum of the present invention increases PCA levels by promoting the expression of cysteine protease 14, which cleaves FLG. The composition for improving the water content of the stratum corneum can improve the ability of skin to synthesize NMF, enhance the self-hydration ability of the skin and improve the barrier function of the skin.

Drawings

Figure 1 shows the effect of composition 1 of the present invention and composition 4 of comparative example 1 on the relative expression level of cysteine protease 14(caspase 14) in a 3D skin model. FIG. 1 shows that treatment with composition 1 of the present invention significantly increased the relative expression level of Caspase14 in the 3D skin model compared to composition 4 of comparative example 1.

Figure 2 shows the effect of composition 1 of the invention and composition 4 of comparative example 1 on PCA content of 3D skin models. FIG. 2 shows a significant increase in PCA content of 3D skin models treated with composition 1 of the present invention as compared to composition 4 of comparative example 1

Detailed Description