Skin care compositions and uses thereof

Abstract

The present application provides a skin care composition with antioxidant effect, comprising baicalin and a hyaluronic acid substance, the hyaluronic acid substance of the present application has synergistic antioxidant effect with baicalin, which helps to obtain excellent antioxidant effect with less amount of baicalin.

Description

Technical Field

[0001] This application relates to the field of cosmetics, specifically to a skincare composition and its use. Background Technology

[0002] Skin is a highly metabolically active tissue, and its frequent exposure to external environmental factors, including UV radiation and air pollution, can induce the production of harmful reactive oxygen species (ROS). These ROS can cause oxidative damage to various biomolecules, including cell membranes, lipids, proteins, RNA, and DNA, damaging vital cells and increasing DNA damage and mutations. Antioxidants can terminate the oxidative chain by binding to free radicals and donating their electrons to them, thus preventing free radicals from attacking intracellular biomolecules.

[0003] Although many studies have reported that baicalin has antioxidant effects, how to more effectively achieve these antioxidant effects remains a goal pursued in this field. Summary of the Invention

[0004] This application was completed through an unexpected discovery during research that combining hyaluronic acid-like substances, which do not have antioxidant activity, with baicalin can enhance antioxidant effects.

[0005] The specific plan is as follows:

[0006] 1. A skin care composition comprising baicalin and hyaluronic acid-like substances.

[0007] 2. The composition according to claim 1, wherein,

[0008] The mass ratio of baicalin to hyaluronic acid is 1:(0.001-100);

[0009] Preferably, the mass ratio of baicalin to hyaluronic acid is 1:(0.01-70).

[0010] 3. The composition according to item 1 or 2, wherein,

[0011] The hyaluronic acid-like substance is selected from one or more of acetylated hyaluronic acid or its salts, or hyaluronic acid or its salts.

[0012] 4. The composition according to item 1 or 2, wherein,

[0013] The hyaluronic acid or its salts include hydrolyzed hyaluronic acid or its salts.

[0014] 5. The composition according to any one of items 1 to 4, wherein,

[0015] The baicalin is 0.03wt%-2wt%, preferably 0.03wt%-1wt%, based on a mass percentage of the total mass of the composition.

[0016] 6. The composition according to any one of items 1 to 5, wherein,

[0017] The hyaluronic acid substance is 0.001 wt% to 10 wt%, preferably 0.001 wt% to 5 wt%, based on the mass percentage of the total mass of the composition.

[0018] 7. Use of the composition described in any one of items 1 to 6 in cosmetics.

[0019] 8. Use of the composition of any one of items 1 to 6 in antioxidant applications.

[0020] 9. Uses of hyaluronic acid-like substances in enhancing the antioxidant effect of baicalin.

[0021] 10. According to the use described in item 9, the hyaluronic acid substance is selected from one or more of acetylated hyaluronic acid or its salt, hyaluronic acid or its salt, preferably, the hyaluronic acid or its salt includes hydrolyzed hyaluronic acid or its salt.

[0022] Technical effect

[0023] The hyaluronic acid-like substances in this application have a synergistic antioxidant effect with baicalin, which helps to achieve excellent antioxidant effects with a smaller amount of baicalin. Detailed Implementation

[0024] 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.

[0025] 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 used 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.

[0026] Composition

[0027] One subject matter of this application relates to compositions, which are defined as long as they achieve the effects of this application. The "composition" includes, but is not limited to, the simultaneous or sequential use of the components. "Simultaneous use" includes using them together in the same formulation or separately in different formulations. "Sequential use" includes using them sequentially in different formulations, with no restriction on the order of sequential use.

[0028] In this application, the baicalin is a pale yellow powder obtained by extraction and drying.

[0029] In some embodiments, the baicalin can be purchased commercially, for example, baicalin can be purchased directly, or other raw materials containing baicalin can be purchased, such as Scutellaria baicalensis root extract.

[0030] In some embodiments, the baicalin can be prepared, for example by crushing the whole Scutellaria baicalensis plant or Scutellaria baicalensis root, extracting with solvent, concentrating and drying to obtain baicalin.

[0031] This application provides a skincare composition comprising baicalin and hyaluronic acid, wherein the mass ratio of baicalin to hyaluronic acid is 1:(0.001-100); preferably, the mass ratio of baicalin to hyaluronic acid is 1:(0.01-70); for example, the mass ratio of baicalin to hyaluronic acid can be 1:0.001, 1:0.005, 1:0.01, etc. 1:0.05, 1:0.1, 1:0.2, 1:0.3, 1:0.4, 1:0.5, 1:0.6, 1:0.7, 1:0.8, 1:0.9, 1:1, 1:2, 1:3, 1:4, 1:5, 1:6, 1:7, 1:8, 1:9, 1:10, 1:11, 1:12, 1:13, 1:14, 1:15, 1:16, 1:17, 1:18, 1:19 1:20, 1:21, 1:22, 1:23, 1:24, 1:25, 1:26, 1:27, 1:28, 1:29, 1:30, 1:31, 1:32, 1:33, 1:34, 1:35, 1:36, 1:37, 1:38, 1:39, 1:40, 1:41, 1:42, 1:43, 1:44, 1:45, 1:46, 1:47, 1:48, 1: 49, 1:50, 1:51, 1:52, 1:53, 1:54, 1:55, 1:56, 1:57, 1:58, 1:59, 1:60, 1:61, 1:62, 1:63, 1:64, 1:65, 1:66, 1:67, 1:68, 1:69, 1:70, 1:75, 1:80, 1:85, 1:90, 1:95, 1:100 or any range thereof.

[0032] In this application, hyaluronic acid-based substances refer to hyaluronic acid or its salts, hyaluronic acid derivatives or their salts. For example, the hyaluronic acid-based substances are selected from one or more of acetylated hyaluronic acid or its salts, hyaluronic acid or its salts.

[0033] The intrinsic viscosity of acetylated hyaluronic acid is 0.1-10.0 dl / g. For example, the intrinsic viscosity of acetylated hyaluronic acid can be 0.1 dl / g, 0.2 dl / g, 0.3 dl / g, 0.4 dl / g, 0.5 dl / g, 0.6 dl / g, 0.7 dl / g, 0.8 dl / g, 0.9 dl / g, 1.0 dl / g, 2.0 dl / g, 3.0 dl / g, 4.0 dl / g, 5.0 dl / g, 6.0 dl / g, 7.0 dl / g, 8.0 dl / g, 9.0 dl / g, 10.0 dl / g, or any range thereof.

[0034] In this application, intrinsic viscosity is the most commonly used method for expressing the viscosity of polymer solutions. Intrinsic viscosity, also known as logarithmic viscosity, is defined as the "specific viscosity" (ηspc) or specific logarithmic viscosity ((lnηr) / c) when the concentration of the polymer solution approaches zero. It is obtained by measuring with an Ubbelohde viscometer.

[0035] In this application, the hyaluronic acid or its salt includes hydrolyzed hyaluronic acid or its salt, wherein the molecular weight of the hydrolyzed hyaluronic acid or its salt can be 5000 Da-10 wDa; for example, the molecular weight of the hydrolyzed hyaluronic acid or its salt can be 5000 Da, 6000 Da, 7000 Da, 8000 Da, 9000 Da, 1 wDa, 2 wDa, 3 wDa, 4 wDa, 5 wDa, 6 wDa, 7 wDa, 8 wDa, 9 wDa, 10 wDa or any range therefrom, preferably 3 wDa-5 wDa.

[0036] In some embodiments of this application, the baicalin is 0.03wt%-2wt% by mass percentage of the total composition; for example, the baicalin is 0.03wt%, 0.04wt%, 0.05wt%, 0.06wt%, 0.07wt%, 0.08wt%, 0.09wt%, 0.1wt%, 0.2wt%, 0.3wt%, 0.4wt%, 0.5wt%, 0.6wt%, 0.7wt%, 0.8wt%, 0.9wt%, 1wt%, 1.1wt%, 1.2wt%, 1.3wt%, 1.4wt%, 1.5wt%, 1.6wt%, 1.7wt%, 1.8wt%, 1.9wt%, 2wt%, or any range thereof, preferably 0.03wt%-1wt%, by mass percentage of the total composition.

[0037] In some embodiments of this application, the hyaluronic acid substance is 0.001 wt% to 10 wt% of the total mass of the composition; for example, the hyaluronic acid substance is 0.001 wt%, 0.002 wt%, 0.003 wt%, 0.004 wt%, 0.005 wt%, 0.006 wt%, 0.007 wt%, 0.008 wt%, 0.009 wt%, 0.01 wt%, 0.02 wt%, or 0.03 wt% of the total mass of the composition. %, 0.04wt%, 0.05wt%, 0.06wt%, 0.07wt%, 0.08wt%, 0.09wt%, 0.1wt%, 0.2wt%, 0.3wt%, 0.4wt%, 0.5wt%, 0.6wt%, 0.7wt%, 0.8wt%, 0.9wt%, 1wt%, 2wt%, 3wt%, 4wt%, 5wt%, 6wt%, 7wt%, 8wt%, 9wt%, 10wt%, or any range between these, preferably 0.001wt%-5wt%.

[0038] In some embodiments, the composition also includes cosmetic excipients and / or active ingredients.

[0039] In this application, the excipients are commonly used by those skilled in the art, such as solvents, pH adjusters, preservatives, fragrances, etc. The solvents include monohydric alcohols, polyhydric alcohols, etc., and the pH adjusters include triethanolamine, arginine, or citric acid, etc.

[0040] In this application, the active ingredient is a commonly used active ingredient by those skilled in the art, such as a water-soluble active ingredient, such as hyaluronic acid, ectoine, ergothioneine, carnosine, etc.

[0041] In this application, no restrictions are placed on the content of excipients and active ingredients in the composition, which can be conventionally selected as needed.

[0042] In this application, no restrictions are placed on the preparation method of the composition. It can be prepared by conventional methods in the art, such as dissolving baicalin and hyaluronic acid in water to obtain the composition.

[0043] The composition described in this application exhibits synergistic effects of baicalin and hyaluronic acid, resulting in excellent antioxidant efficacy. Compared to the combined ORAC values ​​of baicalin and hyaluronic acid alone, the ORAC value of the composition is significantly greater than the combined ORAC values ​​of baicalin and hyaluronic acid alone.

[0044] The composition described in this application has a stronger protective effect against the destructive effects of free radicals and reactive oxygen species, and the baicalin and hyaluronic acid-like substances in the composition exhibit synergistic antioxidant activity.

[0045] In this application, no restrictions are placed on the method for determining antioxidant activity. Conventional methods in the field can be used, such as chemical reaction spectrophotometry, fluorescence method, and chemical titration. Currently, oxygen free radical absorption capacity (ORAC) is an internationally recognized and commonly used fluorescence decay method for determining the oxygen free radical absorption capacity of a sample.

[0046] ORAC stands for Oxygen Radical Absorbance Capacity. The ORAC method is one of the most commonly used methods for detecting the ROS-resistant capabilities of antioxidants. Its principle involves mixing a free radical initiator, such as the azo initiator compound 2,2-azobis(2,-methylpropylimidazolium) hydrochloride, with a fluorescent probe (fluorescein sodium), which destroys the fluorescent probe, causing a change in fluorescence intensity. The decay of fluorescence is then quantified using fluorometry. The free radical initiator generates peroxide radicals, which, in the absence of inhibitors, rapidly destroy the fluorescence of the fluorescein dye. By tracking the fluorescence decay over time and comparing the results with and without the test substance, the free radical scavenging ability of the test substance can be estimated. Using the vitamin E water-soluble analog Trolox as a quantitative standard, analysis was performed using a fluorescence analyzer to determine the protective effect of the compound compared to the standard antioxidant Trolox. The results are expressed as the μMol equivalent of Trolox. Devices that can automatically measure and calculate capabilities are commercially available, such as the Fluoroskan FL microplate fluorescence and chemiluminescence analyzer from Thermo Scientific.

[0047] Publicly available references for ORAC assays include: Cao G, Alessio H, Cutler R (1993). "Oxygen-radical absorbance capacity assay for antioxidants". Free Radic Biol Med 14(3):303-11; Ou B, Hampsch-Woodill M, Prior R (2001). "Comparing antioxidant values ​​with the ORAC method". Alternat. Complement. Ther. 2004, 10, 167-160; Cronin, JR

[0048] This experiment used the ORAC Assay kit (ab233473) purchased from Abcam. Different concentrations of baicalin, acetylated sodium hyaluronate, and sodium hyaluronate sample solutions were prepared. 25 μL of the sample or 25 μL of diluted standard (Trolox) control solution was added to each well of a 96-well plate. Then, 150 μL of fluorescein solution was added to each well, mixed thoroughly, and incubated at 37°C for 30 minutes. 25 μL of free radical initiator solution was added, mixed thoroughly, and immediately placed in a microplate fluorescence and chemiluminescence analyzer. Data were read at an excitation wavelength of 485 nm and an emission wavelength of 538 nm, with a measurement temperature of 37°C and a measurement time of 60 minutes, with data read every 1 minute.

[0049] Antioxidant activity calculation method:

[0050] Synergistic effects are determined by comparing the actual ORAC measured for the composition with the expected or cumulative values ​​for the individual compounds. The predicted ORAC is the combined (cumulative) antioxidant capacity of the various antioxidant compounds in the composition, where the expected ORAC value for a given combination can be calculated using the following equation if each antioxidant compound is measured individually and assumed to act independently: ORAC(total) = ORAC1 + ORAC2 + ... + ORACn (where n is the number of active ingredients).

[0051] The composition provides stronger protection against the damaging effects of free radicals and reactive oxygen species. The combination of components in this embodiment exhibits synergistic antioxidant activity, wherein the activity of the composition of this application is greater than the sum of the individual antioxidant activities of each component (cumulative value).

[0052] This application provides the use of the above composition in cosmetics.

[0053] In some embodiments, the cosmetic product may be used in forms including but not limited to serums, gels, lotions, foundations, or creams.

[0054] This application provides the use of the above composition in antioxidation.

[0055] This application provides the use of hyaluronic acid-like substances in enhancing the antioxidant activity of baicalin. The hyaluronic acid-like substances are selected from one or more of acetylated hyaluronic acid or its salts, hyaluronic acid or its salts, preferably, the hyaluronic acid or its salts include hydrolyzed hyaluronic acid or its salts. The mass ratio of baicalin to the hyaluronic acid-like substances is 1:(0.001-100). Preferably, the mass ratio of baicalin to the hyaluronic acid-like substances is 1:(0.01-70).

[0056] Baicalin has a strong antioxidant effect. This application combines hyaluronic acid with baicalin to enhance the antioxidant effect of baicalin. In other words, hyaluronic acid and baicalin work synergistically to achieve excellent antioxidant effects.

[0057] Example

[0058] The ORAC Assay kit (ab233473) purchased from Abcam was used for testing. Different concentrations of baicalin, acetylated sodium hyaluronate, and sodium hyaluronate sample solutions were prepared. 25 μL of the sample or 25 μL of diluted standard (Trolox) control solution was added to each well of a 96-well plate. Then, 150 μL of fluorescein solution was added to each well, mixed thoroughly, and incubated at 37°C for 30 minutes. 25 μL of free radical initiator solution was added, mixed thoroughly, and immediately incubated in a microplate. A fluorescence and chemiluminescence analyzer was used to read the data at an excitation wavelength of 485 nm and an emission wavelength of 538 nm. The measurement temperature was 37°C, the measurement time was 60 min, and data were read every 1 min.

[0059] The antioxidant activity of each component, both individually and in combination, was evaluated, and the results are shown in the examples below. Assuming that the antioxidant effects are additive, predictions were made for each composition, and these were compared with the actual activity measurements of the combinations in this application, as presented in the table.

[0060] When baicalin is combined with hyaluronic acid-like substances, as shown by oxygen radical uptake capacity (ORAC) assays, the combination produces a significant synergistic effect, thereby enhancing the resistance to reactive substances, especially superoxide radicals. These synergistic antioxidant effects, combined with other known benefits of the compounds individually, make them advantageous for use in skincare compositions.

[0061] Concentration unit: mass%; ORAC unit: (μmol Trolox / g)

[0062] Examples 1 to 26, Comparative Example 39

[0063] Baicalin (purchased from Shanghai Tongtian Biotechnology Co., Ltd., content > 98%) and acetylated sodium hyaluronate (purchased from Bloomage Biotechnology Co., Ltd., content 100%, batch number: 22062321) were dissolved in water to obtain the compositions of Examples 1-12. Baicalin and sodium hyaluronate (3-5 wDa, purchased from Bloomage Biotechnology Co., Ltd., content 100%) were dissolved in water to obtain the compositions of Examples 13-26. Baicalin and sodium hyaluronate (110-130 wDa, purchased from Bloomage Biotechnology Co., Ltd., content 100%) were dissolved in water to obtain the composition of Comparative Example 39. The content of baicalin, acetylated sodium hyaluronate and sodium hyaluronate in the composition, as well as the mass and antioxidant determination values ​​of baicalin and acetylated sodium hyaluronate, or baicalin and sodium hyaluronate, are shown in Table 2.

[0064] Comparative Examples 1 to 38

[0065] Comparative Examples 1-10 were obtained by dissolving baicalin in water, Comparative Examples 11-25 were obtained by dissolving acetylated sodium hyaluronate in water, Comparative Examples 26-37 were obtained by dissolving sodium hyaluronate (3-5 wDa, purchased from Bloomage Biotechnology Co., Ltd., 100% content) in water, and Comparative Example 38 was obtained by dissolving sodium hyaluronate (110-130 wDa, purchased from Bloomage Biotechnology Co., Ltd., 100% content) in water. The content of baicalin, acetylated sodium hyaluronate, or sodium hyaluronate in the composition and the antioxidant assay values ​​are shown in Table 1.

[0066] Table 1. Individual antioxidant activity of each component

[0067]

[0068]

[0069] Table 2

[0070]

[0071]

[0072] Determination of antioxidant properties in experimental cases

[0073] The compositions obtained in the examples and comparative examples were subjected to antioxidant assays, and the results are shown in Tables 1 and 2. The antioxidant assays were performed using the ORAC (Oxygen Radical Absorbance Capacity) method. Using the vitamin E water-soluble analog Trolox as a quantitative standard, analysis was performed using a fluorescence analyzer to determine the protective effect of the compounds compared to the standard antioxidant Trolox. Results are expressed as μmol equivalents of Trolox, and the tests were conducted using the ORAC Assay kit purchased from Abcam. The specific procedure is as follows:

[0074] The compositions of the examples and comparative examples were added to phosphate buffer, and then 25 μL of the compositions of the examples and comparative examples or 25 μL of diluted standard (Trolox) control group were added to a 96-well plate. Subsequently, 150 μL of fluorescein solution was added to each well, mixed thoroughly, and incubated at 37°C for 30 minutes. 25 μL of free radical initiator solution was added, mixed thoroughly, and immediately placed in a microplate fluorescence and chemiluminescence analyzer. Data were read at an excitation wavelength of 485 nm and an emission wavelength of 538 nm, at a temperature of 37°C, for 60 minutes, with data read every 1 minute. The synergistic effect was determined by comparing the actual ORAC measured for the composition with the expected or cumulative value of the individual compounds. The predicted ORAC is the combined (cumulative) antioxidant capacity of the various antioxidant compounds in the combination. If each antioxidant compound is measured individually and assumed to act independently, the expected ORAC value of a combination can be calculated using the following equation: ORAC(total) = ORAC1 + ORAC2 + ... + ORACn (where n is the number of active ingredients). Hyaluronic acid compounds themselves have no antioxidant activity. When the actual ORAC measurement value is greater than the expected value, it suggests that the combination of the two substances enhances antioxidant activity. When the actual ORAC measurement value is at least 25% greater than the expected value, it suggests that the combination of the two substances significantly enhances antioxidant activity.

[0075] 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 skincare composition comprising: (a) Baicalin, and (b) Selected from one or more of acetylated hyaluronic acid or its salts or hydrolyzed hyaluronic acid or its salts; The mass ratio of (a) to (b) is 1:(0.01-70). The molecular weight of the hydrolyzed hyaluronic acid or its salt is 5000 Da-10 wDa.

2. The composition according to claim 1, wherein, The percentage of (a) by mass percentage of the total mass of the composition is 0.03wt%-2wt%.

3. The composition according to claim 2, wherein, The percentage of (a) by mass percentage of the total mass of the composition is 0.03wt%-1wt%.

4. The composition according to claim 1, wherein, The percentage of (b) by mass percentage of the total mass of the composition is 0.001 wt% to 10 wt%.

5. The composition according to claim 4, wherein, The percentage of (b) by mass percentage of the total mass of the composition is 0.001 wt% to 5 wt%.

6. Use of the composition according to any one of claims 1 to 5 in the preparation of cosmetics.

7. Use of the composition according to any one of claims 1 to 5 in the preparation of antioxidant products.

8. The use of hyaluronic acid derivatives in enhancing the antioxidant activity of baicalin; The hyaluronic acid substance is selected from one or more of acetylated hyaluronic acid or its salt, hydrolyzed hyaluronic acid or its salt; The mass ratio of baicalin to hyaluronic acid is 1:(0.01-70). The molecular weight of the hydrolyzed hyaluronic acid or its salt is 5000 Da-10 wDa.

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