Dark eye composition based on microcirculation regulation-melanin metabolism double targeting and application and cosmetics thereof

Abstract

The invention belongs to the technical field of cosmetic production, and discloses a black eye composition based on microcirculation regulation-melanin metabolism double targeting and application thereof, and cosmetics, the black eye composition comprises aminobutyric acid, nicotinamide, acetyl tetrapeptide-5 and a synergist in a mass ratio of (15-25): (5-15): (0.01-0.2): (0.01-0.2); the synergist is selected from at least one of hesperidin methyl chalcone and glucosyl hesperidin, the composition can inhibit generation of dark circles from the perspective of reducing generation of melanin and relieving angiotension, and then the composition is suitable for the dark circle problem caused by multiple action mechanisms; in addition, after the synergist is added, the action effect of an action pathway for inhibiting melanogenesis or relieving angiotensin is further improved, and the dark circle removing capacity of the composition is further enhanced.

Description

Technical Field

[0001] The present application relates to the technical field of cosmetic production, and in particular to a dark circle composition based on dual targeting of microcirculation regulation and melanin metabolism, and its application and cosmetics. Background Art

[0002] Dark circles are caused by various factors. Excessive late nights, irregular sleep patterns, and sleep deprivation can lead to slow blood flow in the eye area, resulting in stagnation. This leads to insufficient oxygen supply to the tissues and an accumulation of metabolic waste in the blood vessels, causing pigmentation. As melanin accumulates, dark circles appear around the eyes. Furthermore, with aging, the epidermis around the eyes dries and thins, collagen and elastin are gradually lost, and the eye metabolism slows, leading to wrinkles, dark circles, and eye bags. There are two types of dark circles: cyan dark circles, caused by venous blood stagnation in the microvasculature and slowed venous waste removal; and brown dark circles, primarily due to incomplete melanin production and metabolism.

[0003] In order to remove dark circles and delay the aging of the skin around the eyes, in addition to ensuring adequate sleep and developing good living habits and eye habits in daily life, a common method is to use eye cosmetics. There are many eye cosmetics on the market, but most of them have the problem of not obvious effects or single effects.

[0004] Chinese patent application 202310922820.5 discloses a composition containing γ-aminobutyric acid and a natural small molecule compound and its use in the preparation of products with anti-aging effects. The proposal points out that γ-aminobutyric acid has certain anti-aging, whitening, and melanin and brown pigment inhibition effects. At the same time, the proposal also believes that γ-aminobutyric acid also has antioxidant, anti-inflammatory, collagen synthesis promotion and skin relaxation effects, and has excellent skin anti-aging effects;

[0005] Chinese patent application 201510733280.1 discloses a complex for removing eye bags and dark circles and its preparation method. The scheme points out that acetyl tetrapeptide-5 can inhibit the activity of angiotensin-converting enzyme, relax capillary tension to promote blood circulation, and thus alleviate the formation of dark circles. In addition, the scheme also records that hesperidin methyl chalcone can reduce the permeability of blood vessels, prevent blood, lymph and water from entering the tissue space, and further inhibit eye bags and dark circles.

[0006] It can be seen that in the prior art, there are corresponding compositions for inhibiting dark circles caused by pigment deposition or vascular tension in the eyes, but there is still room for optimization in the exploration of the dark circle-inhibiting ability of cosmetics.

[0007] The problem to be solved by this solution is: how to provide a composition with multi-channel effects and good dark circle removal effect. Summary of the Invention

[0008] The purpose of the present application is to provide a composition with multi-pathway effects and good dark circle removal effect, wherein the aminobutyric acid, niacinamide, and acetyl tetrapeptide-5 contained in the composition inhibit the formation of dark circles through multiple pathways such as inhibiting pigment deposition and relieving vascular tension in the eyes, and at the same time, a synergist is added to further enhance the effects of the above pathways.

[0009] To achieve the above-mentioned purpose, the present application discloses a dark circle composition based on microcirculation regulation-melanin metabolism dual targeting, comprising aminobutyric acid, nicotinamide, acetyl tetrapeptide-5 and a synergist in a mass ratio of 15-25:5-15:0.01-0.2:0.01-0.2;

[0010] The synergist is selected from at least one of hesperidin methyl chalcone and glucosyl hesperidin;

[0011] Preferably, the synergist is a mixture of hesperidin methyl chalcone and glucosyl hesperidin, and the mass ratio of hesperidin methyl chalcone to glucosyl hesperidin is 0.0001-0.002:0.01-0.2.

[0012] In addition, the present application also discloses the use of the above-mentioned dark circle composition based on dual targeting of microcirculation regulation and melanin metabolism to prepare cosmetics.

[0013] In addition, the present application also discloses a cosmetic containing 5 to 10 wt % of the above-mentioned dark circle composition based on dual targeting of microcirculation regulation and melanin metabolism.

[0014] Preferably, the cosmetic is in the form of a patch, ointment, liquid, spray, gel, emulsion or cream.

[0015] Preferably, the cosmetic is an essence, toner, facial mask, cleanser, lotion or spray

[0016] The beneficial effects of this application are:

[0017] The composition of the present application uses aminobutyric acid, niacinamide, and acetyl tetrapeptide-5 as main ingredients. The composition can inhibit the formation of dark circles from the perspective of reducing the production of melanin and relieving vascular tension, and is therefore suitable for dark circle problems caused by various mechanisms of action. In addition, after adding a synergist, the effect of the action pathway of inhibiting melanin production or relieving vascular tension is further enhanced, thereby further enhancing the composition's ability to remove dark circles. DETAILED DESCRIPTION

[0018] The present invention will be described clearly and completely below in conjunction with the examples of the present invention. In the description of the present invention, it should be noted that if specific conditions are not specified in the examples, the experiments were carried out according to conventional conditions or the conditions recommended by the manufacturer. The reagents or instruments used, if the manufacturer is not specified, are all conventional products that can be purchased commercially.

[0019] Before presenting the examples, the following necessary explanations are given on the preparation and acquisition of the raw materials involved in the examples:

[0020] GABA: purchased from Bloomage Biotechnology Co., Ltd., with an active substance content of 100%;

[0021] Nicotinamide: purchased from Shanghai Xuntian Biotechnology Co., Ltd., with an active substance content of 100%;

[0022] Acetyl tetrapeptide-5: purchased from Shenzhen Readlin Biotechnology Co., Ltd., with an active substance content of 100%;

[0023] Hesperidin methyl chalcone: purchased from AXIALYS INNOVATIONS, with an active substance content of 100%;

[0024] Glucosyl hesperidin: purchased from INNOVATION LABO, with an active substance content of 100%.

[0025] Preparation method of a dark circle composition based on dual targeting of microcirculation regulation and melanin metabolism (unless otherwise specified, the dark circle compositions based on dual targeting of microcirculation regulation and melanin metabolism in the following examples and comparative examples are all prepared by this method): water, butylene glycol, 1,2-hexanediol, and parahydroxyacetophenone are heated to 80°C and stirred to dissolve, then cooled to 60°C, and aminobutyric acid, niacinamide, acetyl tetrapeptide-5, hesperidin methyl chalcone and / or glucosyl hesperidin are added and stirred to dissolve to obtain a dark circle composition based on dual targeting of microcirculation regulation and melanin metabolism. It should be noted that water, butylene glycol, 1,2-hexanediol, and parahydroxyacetophenone in this application are all used as solvents.

[0026] Examples 1-5

[0027] A dark circle treatment composition based on dual targeting of microcirculation regulation and melanin metabolism, the formula of which is shown in Table 1:

[0028] Table 1

[0029]

[0030] Example 6

[0031] The invention is basically the same as Example 1, except that the invention is specifically composed of aminobutyric acid, nicotinamide, acetyl tetrapeptide-5, hesperidin methyl chalcone, and glucosyl hesperidin in a mass ratio of 18:12:0.05:0.00015:0.09985.

[0032] Comparative Examples 1-6

[0033] A dark circle treatment composition based on dual targeting of microcirculation regulation and melanin metabolism, the formula of which is shown in Table 2:

[0034] Table 2

[0035]

[0036] Performance testing:

[0037] 1. Melanin inhibition rate test

[0038] Select healthy zebrafish embryos that are 6 to 8 hours old after fertilization.

[0039] 1.1 Test Grouping

[0040] The test requires setting up a blank / solvent control group (fish embryo culture medium / solvent solution. It should be noted that the fish embryo culture medium is prepared by dissolving 2940 mg of anhydrous calcium chloride, 1233 mg of magnesium sulfate heptahydrate, 630 mg of sodium bicarbonate, and 55 mg of potassium chloride in 10 L of water), a 100% melanin inhibition model group (phenylthiourea working solution), a positive control group (kojic acid solution), and a test substance group (test substance).

[0041] 1.1.1 Blank control group setting

[0042] Five fish embryos were randomly selected and placed in a 96-well plate, with each well containing one fish embryo and 0.2 mL of fish embryo culture medium / solvent solution.

[0043] 1.1.2 100% melanin inhibition model group settings

[0044] Five fish embryos were randomly selected and placed in a 96-well plate, with each well containing one fish embryo and 0.2 mL of phenylthiourea working solution.

[0045] 1.1.3 Positive control group setting

[0046] Five fish embryos were randomly selected and placed in a 96-well plate, with each well containing one fish embryo and 0.2 mL of kojic acid solution.

[0047] 1.1.4 Test substance treatment

[0048] 60 fish embryos were randomly selected and placed in a 96-well plate, with each well containing one fish embryo and 0.2 mL of the test solution (the compositions of the Examples and Comparative Examples were diluted with pure water to a composition mass fraction of 5%, with 5 fish per group, for a total of 12 groups). The embryos were placed in an incubator at 28°C ± 1°C until 48 h ± 1 h after fertilization.

[0049] 1.2 Microscopic analysis of samples

[0050] Under a microscope (e.g., a 2x eyepiece), carefully peel the embryonic shell from the unhatched fish embryo using forceps, taking care not to damage the fish. Cover the embryo with 2% to 4% methylcellulose and position it with its back facing upwards. Then, place it under a stereomicroscope and photograph it. Use the same imaging parameters for all embryos.

[0051] 1.3 Data and result calculation

[0052] Open the photo with analysis software such as Image J, mark the head and yolk dorsal area of ​​each fish embryo, then select "Measure average intensity" in the "Measurement" column, and select the "average signal intensity" in the test results as the melanin content index.

[0053] Calculate the melanin inhibition rate:

[0054]

[0055] In formula 1:

[0056] S is the average value of the “mean signal intensity” of fish embryos in the test substance-treated groups;

[0057] B is the average value of “average signal intensity” of fish embryos in the blank control group;

[0058] P is the average value of the “mean signal intensity” of fish embryos in the 100% melanin inhibition model group.

[0059] The average value of each test group was calculated, and P < 0.05 indicated a significant difference. The specific test results are shown in Table 3:

[0060] Table 3

[0061]

[0062]

[0063] Result analysis:

[0064] 1. As can be seen from Examples 1-4, when the amount of raw materials added to the composition is slightly adjusted, the melanin inhibition rate of Examples 1-4 shows a certain degree of fluctuation trend, but the overall amplitude is relatively small;

[0065] Further observation of Example 5 shows that when hesperidin methyl chalcone is used instead of glucosyl hesperidin as a synergist, the melanin inhibition ability of Example 5 shows a relatively obvious downward trend compared to Example 2. It can be seen that glucosyl hesperidin can produce a stronger inhibitory ability on melanin than hesperidin methyl chalcone. However, further observation of Example 6 shows that the melanin inhibition rate of Example 6 is higher than that of Example 2. It is speculated that the reason for this phenomenon may be that Example 6 accelerates pigment metabolism to a certain extent through the ability of hesperidin methyl chalcone to promote blood circulation. Further combined with the inhibitory ability of glucosyl hesperidin on melanin, the two synergistically enhance the ability of the composition to inhibit melanin with aminobutyric acid, niacinamide, and acetyl tetrapeptide-5, thereby unexpectedly improving the melanin inhibition rate of Example 6.

[0066] 2. From Example 2 and Comparative Examples 1 and 5, it can be seen that the three main components (aminobutyric acid, niacinamide, and acetyl tetrapeptide-5) and the synergist (glucosyl hesperidin) have a synergistic effect in inhibiting melanin deposition. The reason is that, as can be seen from the data in Table 3, the melanin inhibition rate of Example 2 is 50.83%, while the melanin inhibition rate of Comparative Example 1 is only 42.73%, and the melanin inhibition rate of Comparative Example 5 is only 25.44%.

[0067] Theoretically, the melanin inhibition rate of Example 2 should be Comparative Example 1 × 30.05 / 30.15 + Comparative Example 5 × 0.1 / 30.15 ≈ 42.81%;

[0068] However, the actual melanin inhibition rate of Example 2 reached 50.83%, indicating that Example 2 achieved a melanin inhibition ability that exceeded its theoretical value. It is speculated that this phenomenon may be due to the fact that the addition of glucosyl hesperidin enriched the melanin inhibition pathways, thereby enhancing the melanin inhibition ability of the composition through the interaction between multiple pathways.

[0069] 3. Comparative Examples 1-5 show that when any of the main ingredients (aminobutyric acid, nicotinamide, and acetyl tetrapeptide-5) in Comparative Examples 2-4 are used in combination with the synergist (glucosyl hesperidin), the melanin inhibition rates of Comparative Examples 2-4 are only 40.50%, 38.45%, and 36.57%, respectively.

[0070] Further combined with the data of Comparative Example 5, it can be calculated that the melanin inhibition rates of the main components are at most 40.42%, 38.37%, and 36.49%; in contrast, the melanin inhibition rate of Comparative Example 1 reaches 42.73%. It can be seen that there is a certain synergistic effect between the three main components, which makes the melanin inhibition ability of Comparative Example 1 significantly better than any of the melanin inhibition rates of the three main components.

[0071] 2. Blood circulation promotion test

[0072] Select healthy 3-day-post-fertilization (DPF) zebrafish embryos.

[0073] 2.1 Test Grouping

[0074] The test requires setting up a blank control group (fish embryo culture medium / solvent solution, the preparation method is the same as the melanin inhibition rate test), a positive control group (caffeine solution) and a test substance group (test substance).

[0075] 2.1.1 Blank control group setting

[0076] Randomly select 5 fish embryos and place them in a 6 cm culture dish, and add 8 mL of fish embryo culture medium.

[0077] 2.1.2 Positive control group setting

[0078] Five fish embryos were randomly selected and placed in a 6 cm culture dish, and 8 mL of 0.05 g / L caffeine solution was added.

[0079] 2.1.3 Test substance treatment

[0080] Randomly select 60 fish embryos and culture them in 12 6cm culture dishes. Add 8mL of the test solution (preparation method is the same as the melanin inhibition rate test) and culture them in a 28℃±1℃ incubator for 2h±0.5h.

[0081] 2.2 Microscopic analysis of samples

[0082] The fish embryos were anesthetized with tricaine working solution for 2 minutes, and the aorta at the tail of the fish embryos was photographed under a microscope for 20 seconds.

[0083] 2.3 Data and result calculation

[0084] Use software such as DanioScope to measure the relative blood flow velocity of the tail aorta of each fish embryo and take the average value.

[0085] Calculate the blood circulation promotion rate:

[0086]

[0087] In formula 2, S is the average relative velocity of blood flow in the caudal aorta of fish embryos in the test substance treatment group; B is the average relative velocity of blood flow in the caudal aorta of fish embryos in the blank control group.

[0088] The average value of each test group was calculated, and P < 0.05 indicated a significant difference. The specific test results are shown in Table 4:

[0089] Table 4

[0090] Group Promotion rate / % P-value Group Promotion rate / % P-value Example 1 7.17 P＜0.05 Comparative Example 1 5.04 P＜0.05 Example 2 7.69 P＜0.05 Comparative Example 2 4.58 P＜0.05 Example 3 6.96 P＜0.05 Comparative Example 3 4.36 P＜0.05 Example 4 6.85 P＜0.05 Comparative Example 4 4.89 P＜0.05 Example 5 8.13 P＜0.05 Comparative Example 5 2.93 P＜0.05 Example 6 7.92 P＜0.05 Comparative Example 6 4.91 P＜0.05

[0091] Result analysis:

[0092] 1. As can be seen from Examples 1-4, when the amount of raw materials added to the composition is slightly adjusted, the blood circulation promotion rate of Examples 1-4 shows a certain degree of fluctuation trend, but the overall amplitude is relatively small;

[0093] Further observation of Example 5 shows that when hesperidin methyl chalcone is used instead of glucosyl hesperidin as a synergist, the blood circulation promoting ability of Example 5 shows a certain degree of improvement compared with Example 2. It can be seen that hesperidin methyl chalcone has a better blood circulation promoting ability than glucosyl hesperidin.

[0094] 2. As can be seen from Example 5 and Comparative Examples 1 and 6, the three main components (aminobutyric acid, nicotinamide, and acetyl tetrapeptide-5) and the synergist (hesperidin methyl chalcone) have a synergistic effect in inhibiting and promoting blood circulation. The reason is that, as can be seen from the data in Table 3, the promotion rate of Example 5 is 8.13%, while the promotion rate of Comparative Example 1 is only 5.04%, and the promotion rate of Comparative Example 6 is only 4.91%.

[0095] Theoretically, the promotion rate of Example 5 should be Comparative Example 1 + Comparative Example 5 × 0.1 / 30.15 ≈ 5.06%;

[0096] However, the actual promotion rate of Example 5 reached 8.13%, indicating that Example 5 achieved a blood circulation promotion ability that exceeded its theoretical value. It is speculated that this phenomenon may be due to the fact that the addition of hesperidin methyl chalcone enriched the pathways for promoting blood circulation, thereby enhancing the blood circulation promotion ability of the composition through the interaction between multiple pathways.

[0097] 3. Comparative Examples 1-6 show that when any of the main ingredients (aminobutyric acid, nicotinamide, and acetyl tetrapeptide-5) in Comparative Examples 2-4 are used in combination with the synergist (glucosyl hesperidin), the promotion rates of Comparative Examples 2-4 are only 4.58%, 4.36%, and 4.89%, respectively.

[0098] Further combined with the data of Comparative Example 5, it can be calculated that the blood circulation promotion rates of the main components are at most: 4.57%, 4.35%, and 4.88%; in contrast, the blood circulation promotion rate of Comparative Example 1 reaches 5.04%. It can be seen that there is a certain synergistic effect between the three main components, which makes the blood circulation promotion ability of Comparative Example 1 significantly better than any of the three main components.

Claims

1. A dark circle treatment composition based on dual targeting of microcirculation regulation and melanin metabolism, characterized in that: Containing aminobutyric acid, nicotinamide, acetyl tetrapeptide-5 and synergist in a mass ratio of 15-25:5-15:0.01-0.2:0.01-0.2; The synergist is selected from at least one of hesperidin methyl chalcone and glucosyl hesperidin.

2. The dark circle composition based on microcirculation regulation and melanin metabolism dual targeting according to claim 1, characterized in that: The synergist is a mixture of hesperidin methyl chalcone and glucosyl hesperidin, and the mass ratio of hesperidin methyl chalcone to glucosyl hesperidin is 0.0001-0.002:0.01-0.

2.

3. Use of the dark circle composition based on dual targeting of microcirculation regulation and melanin metabolism as described in any one of claims 1 to 2 in preparing cosmetics.

4. A cosmetic, characterized in that: The invention contains 5 to 10 wt % of the dark circle composition based on microcirculation regulation and melanin metabolism dual targeting according to any one of claims 1 to 2.

5. The cosmetic according to claim 4, characterized in that The dosage form of the cosmetic is a patch, ointment, liquid, spray, gel, emulsion or cream.

6. The cosmetic according to claim 4, characterized in that The cosmetics are essence, toner, facial mask, cleanser, lotion or spray.

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