Composition for red fading repair

Abstract

The invention provides a composition for red fading repair, which comprises an excipient, a polysaccharide polymer, a freshener, a humectant, a preservative and a liposome, and the liposome is a liposome formed by wrapping mussel mucin with phospholipid. The phospholipid-coated mussel mucin liposome in the composition can effectively promote skin barrier repair, significantly reduce erythema and inflammatory response, and achieve the effect of efficient red fading and repair.

Description

Technical Field

[0001] This application relates to a composition for repairing redness. Background Technology

[0002] With the fast pace of life and increasing environmental pressure, skin barrier damage is becoming increasingly common, and its incidence has been gradually rising in recent years. In the modern environment, a variety of internal and external factors contribute to the high incidence of skin barrier damage: 1) External stimuli: Air pollution (PM2.5, heavy metals), excessive cleansing (soap-based, frequent exfoliation), post-medical aesthetic procedures such as acid peels / phototherapy, ultraviolet radiation, and inappropriate cosmetics (alcohol, irritating ingredients) directly damage the stratum corneum structure. 2) Internal factors: Stress, lack of sleep, and unbalanced diets (high sugar, high fat) trigger oxidative stress and chronic inflammation, weakening the skin's self-repair ability. 3) Disease-related: Atopic dermatitis, rosacea, hormone-dependent dermatitis, and other diseases are accompanied by barrier dysfunction and inflammatory responses.

[0003] Especially now, with the improvement of economic foundation, people's demand for beauty is increasing day by day. Choosing medical aesthetic phototherapy treatments (such as lasers, intense pulsed light (IPL), radiofrequency (RF), and ultrasound) to improve skin problems (pigmentation, wrinkles, acne, sagging, etc.) through photothermal or mechanical effects has become quite common. However, postoperative symptoms such as burning, stinging, erythema, edema, and temporary damage are common. Improper care may lead to persistent problems. Therefore, the interaction between skin barrier damage and inflammation has become a key issue in modern skin health. Repair and anti-inflammation are not only necessary for symptom relief, but also a scientific strategy to break the vicious cycle and achieve long-term skin stability. Currently available dressing products are not ideal for reducing redness and repairing damaged skin barriers and wounds, and they cannot achieve the safety of immediate postoperative use, easily causing sensitivity, barrier damage, post-inflammatory hyperpigmentation, and scarring. Summary of the Invention

[0004] The technical solution of this application is as follows:

[0005] 1. A composition for redness repair, comprising an excipient, a polysaccharide polymer, a cooling agent, a humectant, a preservative, and liposomes, wherein the liposomes are liposomes of mussel adhesive protein encapsulated by phospholipids.

[0006] 2. The composition according to claim 1, wherein,

[0007] The phospholipid is selected from one or more of egg yolk lecithin, sphingomyelin, hydrogenated soybean lecithin, lecithin, glycerophospholipid, and soybean lecithin; preferably, it is selected from one or more of hydrogenated soybean lecithin, lecithin, and soybean lecithin.

[0008] 3. The composition according to claim 1, wherein,

[0009] The molecular weight of the mussel adhesive protein is 3kDa-10kDa, preferably 8kDa-10kDa.

[0010] 4. The composition according to claim 1, wherein,

[0011] The mass ratio of the liposomes to the polysaccharide polymer is 120:(1-15).

[0012] 5. The composition according to claim 1, wherein,

[0013] The liposomes are 10wt%-15wt% by weight of the composition.

[0014] 6. The composition according to claim 1, wherein,

[0015] The mass ratio of the phospholipid to the mussel adhesive protein is (0.5-10):1, preferably (1-10):1.

[0016] 7. The composition according to claim 1, wherein,

[0017] The excipient is one or both of xanthan gum and carbomer; preferably carbomer.

[0018] Preferably, the excipient is 0.3 wt% to 1.5 wt% of the composition by mass.

[0019] 8. The composition according to claim 1, wherein,

[0020] The polysaccharide polymer is one or more of the following: carboxymethyl chitosan, carboxymethyl chitin, trehalose, cellulose and its derivatives, hyaluronic acid and its salts; preferably one or two of carboxymethyl chitosan and trehalose.

[0021] Preferably, the polysaccharide polymer is 0.15 wt% to 1.4 wt% of the composition by mass.

[0022] 9. The composition according to claim 1, wherein,

[0023] The cooling agent is LP-MT30; the cooling agent accounts for 0.3wt%-1.5wt% of the composition by mass.

[0024] The moisturizer is two or more of the following: glycerin, propylene glycol, butylene glycol, betaine, polyethylene glycol, and glyceryl glucoside; the moisturizer accounts for 3wt%-10wt% of the composition by mass percentage.

[0025] The preservative is selected from at least two of p-hydroxyacetophenone, 1,2-pentanediol, and 1,2-hexanediol; the preservative is 0.8 wt% to 2 wt% of the composition by mass.

[0026] 10. A method for preparing the composition according to any one of claims 1 to 9, wherein,

[0027] The excipient is dissolved in water and swollen; the resulting solution is denoted as phase A.

[0028] The solution obtained by mixing the polysaccharide polymer, the cooling agent, the humectant, and the preservative is designated as phase B.

[0029] Phase A is added to Phase B, then an alkaline substance is added and stirred until fully dissolved to obtain the dressing;

[0030] Liposomes were added to the dressing to obtain a composition.

[0031] 11. The method for preparing the composition according to claim 10, wherein,

[0032] The liposomes are prepared as follows:

[0033] Phospholipids and cholesterol are dissolved to obtain a lipid solution;

[0034] An aqueous solution containing mussel adhesive protein was added to the lipid solution to obtain a mixed solution;

[0035] The mixed solution is ultrasonicated to form a W / O type emulsion;

[0036] The solvent was removed by evaporation, yielding mussel adhesive protein encapsulated in phospholipids.

[0037] 12. The method for preparing the composition according to claim 11, wherein,

[0038] In the lipid phase, the mass fraction of phospholipids is 50%-70%, the mass fraction of cholesterol is 10%-30%, and the mass fraction of mussel adhesive protein is 10%-30%.

[0039] Beneficial effects:

[0040] The phospholipids in the composition of this application encapsulate mussel adhesive protein liposomes, which can effectively promote skin barrier repair, significantly reduce erythema and inflammatory response, and achieve a highly effective effect of redness reduction and repair.

[0041] After being stored at 4°C for 28 days, the encapsulation efficiency of the liposomes remained at a high level, ensuring the long-term effectiveness of the product and demonstrating good stability.

[0042] The composition contains no irritating ingredients, making it suitable for use after cosmetic procedures and for sensitive skin, with high safety and compatibility.

[0043] This application optimizes the formulation ratio to achieve a mass ratio of liposomes to polysaccharide polymers of 120:(1-15) and a mass ratio of phospholipids to mussel adhesive protein of (1-10):1, ensuring optimal encapsulation rate and efficacy.

[0044] The composition of this application promotes wound healing. According to four-dimensional quantitative scoring, the composition can significantly improve scarring, redness and pain scores, and accelerate wound repair. Attached Figure Description

[0045] Figure 1 The efficacy results of this application are shown in the diagram. Detailed Implementation

[0046] The present application is further illustrated below with reference to embodiments. It should be understood that the embodiments are only used to further illustrate and explain the present application and are not intended to limit the present application.

[0047] Unless otherwise defined, technical and scientific terms used in this specification have the same meaning as commonly understood by one of ordinary skill in the art. While similar or identical methods and materials may be applied in experimental or practical applications, materials and methods are described herein. In case of conflict, the definitions included herein shall prevail. Furthermore, materials, methods, and examples are for illustrative purposes only and are not intended to be limiting. The present application is further described below with reference to specific embodiments, but is not intended to limit the scope of the application.

[0048] This application provides a composition for repairing redness, comprising an excipient, a polysaccharide polymer, a cooling agent, a moisturizer, a preservative, and liposomes, wherein the liposomes are liposomes of mussel adhesive protein encapsulated by phospholipids.

[0049] In some embodiments of this application, the phospholipid is selected from one or more of egg yolk lecithin, sphingomyelin, hydrogenated soybean lecithin, lecithin, glycerophospholipid, and soybean lecithin.

[0050] In some embodiments of this application, the phospholipid is one or more of hydrogenated soybean lecithin, lecithin, and soybean lecithin.

[0051] In some embodiments of this application, the molecular weight of the mussel adhesive protein is 3kDa-10kDa, preferably 8kDa-10kDa. For example, the molecular weight of the mussel adhesive protein can be 3kDa, 4kDa, 5kDa, 6kDa, 7kDa, 8kDa, 9kDa, 10kDa, or any range thereof.

[0052] As used in this article, the term "molecular weight" refers to the weight-average molecular weight (Mw) of a sample population composed of polymer species with various molecular weights. This quantity is defined by the following formula:

[0053]

[0054] Where n i M represents the number of molecules of substance i. i This represents the molecular weight of the i-th substance. Unless otherwise stated, the term "molecular weight" as used herein refers to weight-average molecular weight.

[0055] In some embodiments of this application, the mass ratio of the liposomes to the polysaccharide polymer is 120:(1-15). For example, the mass ratio of the liposomes to the polysaccharide polymer can be 120:1, 120:2, 120:3, 120:4, 120:5, 120:6, 120:7, 120:8, 120:9, 120:10, 120:11, 120:12, 120:13, 120:14, 120:15, or any range thereof.

[0056] In some embodiments of this application, the liposomes are 10wt%-15wt% by weight of the composition. For example, the liposomes may be 10wt%, 11wt%, 12wt%, 13wt%, 14wt%, 15wt%, or any range thereof.

[0057] In some embodiments of this application, the mass ratio of the phospholipid to the mussel adhesive protein is (0.5-10):1. For example, the mass ratio of the phospholipid to the mussel adhesive protein can be 0.5:1, 1:1, 1.5:1, 2:1, 2.5:1, 3:1, 3.5:1, 4:1, 4.5:1, 5:1, 5.5:1, 6:1, 6.5:1, 7:1, 7.5:1, 8:1, 8.5:1, 9:1, 9.5:1, 10:1, or any range thereof.

[0058] In some embodiments of this application, the excipient is one or both of xanthan gum and carbomer; preferably carbomer.

[0059] In some embodiments of this application, the excipient is 0.3 wt% to 1.5 wt% of the composition by mass. For example, the excipient may be 0.3 wt%, 0.4 wt%, 0.5 wt%, 0.6 wt%, 0.7 wt%, 0.8 wt%, 0.9 wt%, 1.0 wt%, 1.1 wt%, 1.2 wt%, 1.3 wt%, 1.4 wt%, 1.5 wt%, or any range thereof.

[0060] In some embodiments of this application, the polysaccharide polymer is one or more of the following: carboxymethyl chitosan, carboxymethyl chitin, trehalose, cellulose and its derivatives, hyaluronic acid and its salts; preferably one or two of carboxymethyl chitosan and trehalose.

[0061] In some embodiments of this application, the polysaccharide polymer is 0.15 wt% to 1.4 wt% of the composition by mass. For example, the polysaccharide polymer can be 0.15 wt%, 0.3 wt%, 0.4 wt%, 0.5 wt%, 0.6 wt%, 0.7 wt%, 0.8 wt%, 0.9 wt%, 1.0 wt%, 1.1 wt%, 1.2 wt%, 1.3 wt%, 1.4 wt%, or any range thereof.

[0062] In some embodiments of this application, the cooling agent is LP-MT30.

[0063] In some embodiments of this application, the cooling agent is 0.3wt%-1.5wt% by mass percentage of the composition; for example, the cooling agent can be 0.3wt%, 0.4wt%, 0.5wt%, 0.6wt%, 0.7wt%, 0.8wt%, 0.9wt%, 1.0wt%, 1.1wt%, 1.2wt%, 1.3wt%, 1.4wt%, 1.5wt%, or any range thereof.

[0064] In some embodiments of this application, the moisturizer is two or more of glycerin, propylene glycol, butylene glycol, betaine, polyethylene glycol, and glyceryl glucoside.

[0065] In some embodiments of this application, the humectant is 3wt%-10wt% by mass percentage of the composition; for example, the humectant can be 3wt%, 4wt%, 5wt%, 6wt%, 7wt%, 8wt%, 9wt%, 10wt%, or any range thereof.

[0066] In some embodiments of this application, the preservative is selected from at least two of p-hydroxyacetophenone, 1,2-pentanediol, and 1,2-hexanediol.

[0067] In some embodiments of this application, the preservative is 0.8 wt% to 2 wt% of the composition by mass. For example, the preservative may be 0.8 wt%, 0.9 wt%, 1.0 wt%, 1.1 wt%, 1.2 wt%, 1.3 wt%, 1.4 wt%, 1.5 wt%, 1.6 wt%, 1.7 wt%, 1.8 wt%, 1.9 wt%, 2 wt%, or any range thereof.

[0068] This application provides a method for preparing the above composition, wherein the excipient is dissolved in water and swollen to obtain a solution denoted as phase A; the polysaccharide polymer, the cooling agent, the moisturizer, and the preservative are mixed to obtain a solution denoted as phase B; phase A is added to phase B, and then an alkaline substance is added and stirred until fully dissolved to obtain a dressing; liposomes are added to the dressing to obtain the composition.

[0069] In some embodiments of this application, the liposomes are prepared as follows: phospholipids and cholesterol are dissolved to obtain a lipid solution; an aqueous solution containing mussel adhesive protein is added to the lipid solution to obtain a mixed solution; the mixed solution is sonicated to form a W / O emulsion; the solvent is evaporated to remove the solvent, thereby obtaining phospholipid-encapsulated mussel adhesive protein.

[0070] In some embodiments of this application, the mass fraction of phospholipids in the lipid phase mixture is 50%-70%, the mass fraction of cholesterol is 10%-30%, and the mass fraction of mussel adhesive protein is 10%-30%.

[0071] In some embodiments of this application, the mass fraction of phospholipids in the lipid phase mixture solution can be 50%, 51%, 52%, 53%, 54%, 55%, 56%, 57%, 58%, 59%, 60%, 61%, 62%, 63%, 64%, 65%, 66%, 67%, 68%, 69%, 70%, or any range thereof.

[0072] In some embodiments of this application, the mass fraction of cholesterol in the lipid phase mixture solution can be 10%, 11%, 12%, 13%, 14%, 15%, 16%, 17%, 18%, 19%, 20%, 21%, 22%, 23%, 24%, 25%, 26%, 27%, 28%, 29%, 30%, or any range thereof.

[0073] In some embodiments of this application, the mass fraction of mussel adhesive protein in the lipid phase mixed solution can be 10%, 11%, 12%, 13%, 14%, 15%, 16%, 17%, 18%, 19%, 20%, 21%, 22%, 23%, 24%, 25%, 26%, 27%, 28%, 29%, 30%, or any range thereof.

[0074] Preparation Example

[0075] Preparation Example 1: Preparation method of liposomes encapsulating mussel adhesive protein:

[0076] (1) Dissolve lecithin and cholesterol in chloroform; wherein the mass fraction of lecithin is 60 wt% and the mass fraction of cholesterol is 20 wt%.

[0077] (2) Add an aqueous solution containing mussel adhesive protein to the solution obtained in step (1) to form a two-phase system; the mass fraction of mussel adhesive protein is 20%.

[0078] (3) Ultrasonicate the mixture on a water bath ultrasonic instrument until a uniform W / O emulsion is formed, which can be left to stand for 30 minutes without separation.

[0079] (4) The W / O type emulsion is evaporated under reduced pressure in a rotary evaporator to remove chloroform. As the organic solvent is further evaporated, liposomes containing mussel adhesive protein can be obtained.

[0080] The only difference between Preparation Examples 2-11, Comparative Examples 1-2 and Preparation Example 1 is Table 1; otherwise, they are the same as Preparation Example 1.

[0081] Table 1

[0082]

[0083] Example

[0084] Example 1

[0085] (1) Weigh an appropriate amount of purified water into a beaker, add carbomer to the beaker to swell, and denote it as phase A;

[0086] (2) Weigh out the cooling agent (LP-MT30), glycerin, carboxymethyl chitosan, trehalose, p-hydroxyacetophenone, and 1,2-hexanediol to form a well-dispersed solution, which is designated as phase B.

[0087] (3) Add phase A to phase B and stir until fully dissolved;

[0088] (4) Adding an appropriate amount of sodium hydroxide to the solution after mixing in (3) can form a liquid or gel dressing;

[0089] (5) Add the liposomes of Preparation Example 1 to the dressing obtained in step (4) and stir until homogeneous to obtain the composition.

[0090] The composition of the liposomes is as follows: carbomer 1%, LP-MT30 1%, glycerol 5%, carboxymethyl chitosan 0.2%, trehalose 0.5%, p-hydroxyacetophenone 0.5%, 1,2-hexanediol 0.5%, and liposomes 12%.

[0091] Examples 2-13 and Comparative Examples 3-7 differ from Example 1 only in Table 2; the rest are the same as Example 1.

[0092] Table 2

[0093]

[0094]

[0095] According to Table 2, the storage stability of the liposome-containing compositions was verified under room temperature (25℃), refrigeration at 4℃, and freezing at -20℃ for 28 days. The encapsulation rate of mussel adhesive protein in the samples was used as an indicator to investigate the storage stability of the mussel adhesive protein-containing liposome compositions at different temperatures.

[0096] Table 3

[0097]

[0098]

[0099] Table 3 shows that the encapsulation efficiency of mussel adhesive liposomes decreased with prolonged storage at room temperature. Morphological observation revealed precipitation in the composition containing mussel adhesive liposomes at room temperature, while the morphology of the mussel adhesive liposomes showed no significant changes after freezing at 20℃ and refrigeration at 4℃. In summary, these results indicate that mussel adhesive liposomes are best stored at 4℃, exhibiting minimal morphological changes, low leakage rate, and strong stability.

[0100] Composition efficacy data evaluation

[0101] Volunteers aged 18-60 who had undergone non-chronic wound repair procedures such as laser / photorejuvenation / chemical peels / minimally invasive cosmetic procedures were selected. Dressings prepared according to Examples 1, 7, 12, and 13 (which exhibited high encapsulation rates and good stability) were used as test products and applied to the volunteers. Each group consisted of 30 volunteers. The first group used the product from Example 1 on one half of their face and the product from Example 12 on the other half. The second group used the product from Example 7 on one half of their face and the product from Example 13 on the other half. Results were observed after two weeks of continuous product use. Red pigment, TEWL value, and stratum corneum moisture content were directly measured using a skin melanin and heme testing probe (Mexameter MX18), a transepidermal water loss and heat loss testing probe (Tewameter™ Hex), and a skin moisture testing probe (Corneometer CM825). Wound repair and healing efficacy was evaluated using a four-dimensional quantitative scoring method, with the scoring levels as follows:

[0102]

[0103] The criteria for judging the efficacy are as follows:

[0104] 1. Significant effect

[0105] All of the following conditions must be met simultaneously:

[0106] Pigmentation score: 0-3 points

[0107] Scarring score: 0-3 points

[0108] Redness and swelling rating: 0-3 points

[0109] Pain rating: 0-3 points

[0110] 2. Effective

[0111] Satisfy any of the following combinations:

[0112] Low scarring (0-3 points) + Medium pigmentation (4-6 points) + Low redness and swelling (0-3 points) + Low pain (0-3 points) Medium scarring (4-6 points) + Low pigmentation (0-3 points) + Low redness and swelling (0-3 points) + Low pain (0-3 points) Medium scarring (4-6 points) + Medium pigmentation (4-6 points) + Low redness and swelling (0-3 points) + Low pain (0-3 points)

[0113] 3. Invalid

[0114] Healing status that does not meet the above criteria of "significant effect" or "effectiveness"

[0115]

[0116] The results are shown in Table 4-8 and Figure 1 As shown.

[0117] Table 4

[0118]

[0119]

[0120] Table 5

[0121]

[0122]

[0123] Table 6

[0124]

[0125]

[0126] Table 7

[0127]

[0128] Table 8 Comparison of efficacy values ​​before and after treatment

[0129]

[0130] Although the present invention has been disclosed above with reference to embodiments, it is not intended to limit the present invention. Anyone skilled in the art may make some modifications and refinements without departing from the spirit and scope of the present invention. Therefore, the scope of protection of the present invention shall be determined by the scope of the appended patent application.

Claims

1. A composition for redness repair, comprising an excipient, a polysaccharide polymer, a cooling agent, a humectant, a preservative, and liposomes, wherein the liposomes are liposomes of mussel adhesive protein encapsulated by phospholipids.

2. The composition according to claim 1, wherein, The phospholipid is selected from one or more of egg yolk lecithin, sphingomyelin, hydrogenated soybean lecithin, lecithin, glycerophospholipid, and soybean lecithin; preferably, it is selected from one or more of hydrogenated soybean lecithin, lecithin, and soybean lecithin.

3. The composition according to claim 1, wherein, The molecular weight of the mussel adhesive protein is 3kDa-10kDa, preferably 8kDa-10kDa.

4. The composition according to claim 1, wherein, The mass ratio of the liposomes to the polysaccharide polymer is 120:(1-15).

5. The composition according to claim 1, wherein, The liposomes are 10wt%-15wt% by weight of the composition.

6. The composition according to claim 1, wherein, The mass ratio of the phospholipid to the mussel adhesive protein is (0.5-10):1, preferably (1-10):

1.

7. The composition according to claim 1, wherein, The excipient is one or both of xanthan gum and carbomer; preferably carbomer. Preferably, the excipient is 0.3 wt% to 1.5 wt% of the composition by mass.

8. The composition according to claim 1, wherein, The polysaccharide polymer is one or more of the following: carboxymethyl chitosan, carboxymethyl chitin, trehalose, cellulose and its derivatives, hyaluronic acid and its salts; preferably one or two of carboxymethyl chitosan and trehalose. Preferably, the polysaccharide polymer is 0.15 wt% to 1.4 wt% of the composition by mass.

9. The composition according to claim 1, wherein, The cooling agent is LP-MT30; the cooling agent accounts for 0.3wt%-1.5wt% of the composition by mass. The moisturizer is two or more of the following: glycerin, propylene glycol, butylene glycol, betaine, polyethylene glycol, and glyceryl glucoside; the moisturizer accounts for 3wt%-10wt% of the composition by mass percentage. The preservative is selected from at least two of p-hydroxyacetophenone, 1,2-pentanediol, and 1,2-hexanediol; the preservative is 0.8 wt% to 2 wt% of the composition by mass.

10. A method for preparing the composition according to any one of claims 1 to 9, wherein, The excipient is dissolved in water and swollen; the resulting solution is denoted as phase A. The solution obtained by mixing the polysaccharide polymer, the cooling agent, the humectant, and the preservative is designated as phase B. Phase A is added to Phase B, then an alkaline substance is added and stirred until fully dissolved to obtain the dressing; Liposomes were added to the dressing to obtain a composition; Preferably, The liposomes are prepared as follows: Phospholipids and cholesterol are dissolved to obtain a lipid solution; An aqueous solution containing mussel adhesive protein was added to the lipid solution to obtain a mixed solution; The mixed solution is ultrasonicated to form a W / O type emulsion; The solvent was removed by evaporation to obtain phospholipid-encapsulated mussel adhesive protein; More preferably, In the lipid phase, the mass fraction of phospholipids is 50%-70%, the mass fraction of cholesterol is 10%-30%, and the mass fraction of mussel adhesive protein is 10%-30%.

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