Composition capable of whitening skin and improving micro-ecological health and preparation method thereof
By combining stearyl glycyrrhetinic acid ester, colloidal oat flour, citrus peel extract, and yeast fermentation product extract, the problems of skin irritation and unhealthy microbiome associated with existing whitening products are solved, achieving the effects of skin whitening and microbiome improvement.
Patent Information
- Application Number
- CN202510616520.3
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2025-05-14
- Publication Date
- 2025-10-21
AI Technical Summary
Existing whitening products mainly target melanin production and exfoliation, which can easily cause skin irritation and fail to effectively improve the health of the skin's microbiome, affecting the evenness and health of skin tone.
This product uses a combination of stearyl glycyrrhetinic acid ester, colloidal oat flour, citrus peel extract, and yeast fermentation product extract to inhibit melanin production, promote skin microecological balance, and enhance skin radiance and smoothness.
While achieving skin whitening, it also improves the health of the skin's microbiome, reduces melanin content, enhances skin brightness and smoothness, and strengthens skin safety.
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Figure CN120815022A_ABST
Abstract
Description
Technical Field
[0001] The present application belongs to the field of cosmetic technology, and in particular relates to a composition and a preparation method for both skin whitening and microecological health enhancement. Background Art
[0002] With the rapid development of cosmetic science, the role of cosmetics in improving and promoting skin health and enhancing people's quality of life is gaining increasing attention. Among the many functional benefits, consumer demand for skin whitening continues to grow and develop. Typically, skin whitening is achieved by inhibiting melanin production in melanocytes, inhibiting melanin transfer to keratinocytes, and enhancing keratin exfoliation.
[0003] The skin microbiome is an ecosystem composed of microorganisms such as bacteria, fungi and viruses, skin cells and their secretions, and the immune system. Under normal circumstances, there are a large number of microorganisms on the skin surface, which are divided into resident bacteria (such as Propionibacterium acnes and Staphylococcus epidermidis) and transient bacteria (such as Corynebacterium, etc.) according to their presence. Imbalance in skin flora is associated with a variety of skin diseases, which may cause pigmentation and uneven skin color, affecting the appearance of skin color. Studies have shown that the number of live Propionibacterium acnes in the lesional area of melasma is significantly lower than that in normal skin, while the number of Corynebacterium and aerobic Gram-negative rods is significantly increased compared to normal skin; certain skin commensal bacteria such as Staphylococcus epidermidis can promote the survival of cells that have DNA damage in melanocytes after UVB radiation, while Propionibacterium acnes inhibits the survival and proliferation of melanocytes by increasing cell apoptosis, leading to melanocyte death. More and more studies have shown that different species of bacteria in the skin flora have direct or indirect effects on the survival and function of melanocytes. The impact of the skin flora on melanin is also multifaceted, including direct interaction with melanocytes, affecting the melanin production signaling pathway, association with skin diseases, and protective effects on melanocytes. Summary of the Invention
[0004] Purpose of the Invention: This application provides a composition and preparation method for both skin whitening and microbiome health enhancement. This composition inhibits pigment production in melanocytes, promotes skin pigment metabolism, and enhances skin microbiome diversity. It reduces melanin content, improves skin brightness and smoothness, and enhances skin microbiome health.
[0005] Technical solution: The embodiment of the present application provides a composition that has the effects of both skin whitening and improving microecological health, wherein the composition comprises stearyl glycyrrhetinate, colloidal oatmeal, citrus peel extract, and yeast fermentation product extract.
[0006] In some embodiments, based on the total mass of the composition, the mass percentage of the stearyl glycyrrhetinate is 0.05% to 1%, the mass percentage of the colloidal oatmeal is 0.1% to 2%, the mass percentage of the citrus peel extract is 0.5% to 10%, and the mass percentage of the yeast fermentation product extract is 0.5% to 10%.
[0007] In some embodiments, the composition further comprises β-glucan; based on the total mass of the composition, the mass percentage of the β-glucan is 0.05% to 2%.
[0008] In some embodiments, the composition further comprises oil; based on the total mass of the composition, the mass percentage of the oil is 3% to 5%.
[0009] In some embodiments, the composition further comprises sodium polyacryloyldimethyl taurate; based on the total mass of the composition, the mass percentage of the sodium polyacryloyldimethyl taurate is 0.1% to 0.8%.
[0010] In some embodiments, the oil includes meadowfoam seed oil, squalane and oat kernel oil; the mass ratio of meadowfoam seed oil, squalane and oat kernel is (0.5-1.5): (0.5-1.5): (1.5-2.5).
[0011] In some embodiments, the composition further comprises a polyol; based on the total mass of the composition, the mass percentage of the polyol is 1% to 10%.
[0012] In some embodiments, the mass ratio of the stearyl glycyrrhetinate to the oil is (0.01-0.3):1.
[0013] The present invention also provides a method for preparing a composition having the effects of both skin whitening and improving microecological health, comprising the following steps:
[0014] (1) Preparation of oil phase: Weigh meadowfoam seed oil, squalane, and oat kernel oil, mix with stearyl glycyrrhetinate, and dissolve at 80°C to 85°C;
[0015] (2) Preparation of thickening phase: colloidal oatmeal, sodium polyacryloyldimethyl taurate, and 1,2-pentanediol were weighed, mixed, and then water was added. The mixture was heated and stirred at 80°C to 85°C to obtain a thickening phase;
[0016] (3) Preparation of a first active substance solution: Weigh β-glucan and propylene glycol and mix to obtain a first active substance solution;
[0017] (4) Preparation of a second active substance solution: Weigh the citrus peel extract and the yeast fermentation product extract, stir and mix, and obtain a second active substance solution;
[0018] (5) The dissolved oil phase is added to the thickening phase and mixed, and then high-speed homogenization is performed at 80°C to 85°C. After homogenization, the system is cooled, and the first active substance solution and the second active substance solution are added respectively, and low-speed homogenization is performed to obtain an emulsion.
[0019] In some embodiments, the rotation speed of the high-speed homogenizer is 2900 rpm to 3000 rpm.
[0020] In some embodiments, the low-speed homogenization condition is 1500 rpm to 2000 rpm.
[0021] The embodiments of the present application also provide the use of the above-mentioned composition having both skin whitening and microecological health enhancement or the composition prepared by the preparation method of the above-mentioned composition having both skin whitening and microecological health enhancement in the preparation of cosmetics.
[0022] Beneficial Effects: This application provides a composition and preparation method that combines skin whitening and microecological health enhancement. The composition comprises stearyl glycyrrhetinate, colloidal oatmeal, citrus peel extract, and yeast fermentation product extract. The composition can inhibit pigment production in melanocytes, promote skin pigment metabolism, and enhance skin microbial diversity. It reduces skin melanin content, improves skin brightness and smoothness, and enhances skin microecological health. BRIEF DESCRIPTION OF THE DRAWINGS
[0023] In order to more clearly illustrate the technical solutions in the embodiments of the present application, the following briefly introduces the drawings required for use in the description of the embodiments. Obviously, the drawings described below are only some embodiments of the present application. For those skilled in the art, other drawings can be obtained based on these drawings without creative work.
[0024] Figure 1 These are the test results of the tyrosinase inhibition rate in B16-F10 cells in some examples of this application;
[0025] Figure 2 This is a comparison chart of the effects of comparative example 6 and example 4 on promoting skin pigment metabolism in the examples of this application;
[0026] Figure 3 This is a photo of the effect of the emulsion prepared in Example 4 of the present application on improving skin oil and porphyrin;
[0027] Figure 4 Changes in skin melanin content after 4 weeks of use of the emulsion prepared in Example 4 of the present application;
[0028] Figure 5 Changes in skin gloss after 4 weeks of use of the emulsion prepared in Example 4 of the present application;
[0029] Figure 6 Changes in skin roughness after 4 weeks of use of the emulsion prepared in Example 4 of the present application;
[0030] Figure 7 The change in skin smoothness after using the lotion prepared in Example 4 of the present application for 4 weeks;
[0031] Figure 8 This is a photo showing improvement in skin roughness and pigmentation after using the emulsion prepared in Example 4 of the present application for 4 weeks;
[0032] Figure 9 The results of the test on the changes in the Beta diversity of the skin flora after using the lotion prepared in Example 4 of the present application for 4 weeks;
[0033] Figure 10 The test results of the changes in the abundance of facial skin flora (Bacteroidetes) after using the lotion prepared in Example 4 of the present application for 4 weeks;
[0034] Figure 11 These are the test results of the changes in the abundance of facial skin flora (Chryseobacterium indologenes) after using the emulsion prepared in Example 4 of the present application for 4 weeks. DETAILED DESCRIPTION
[0035] The following, in conjunction with the accompanying drawings, provides a clear and complete description of the technical solutions in the embodiments of the present application. It should be noted that the described embodiments are only a portion of the embodiments of the present application, and are not intended to be exhaustive. All other embodiments derived by persons skilled in the art based on the embodiments of the present application without inventive effort are intended to fall within the scope of protection of the present application. Furthermore, in the description of the present application, the term "including" means "including but not limited to." The terms "first," "second," and "third," etc., are used merely as designations and do not impose numerical requirements or establish a sequence. The various embodiments of the present application may be presented in the form of a range. It should be understood that describing in a range format is merely for convenience and brevity and should not be construed as a rigid limitation on the scope of the present application. Therefore, the range description should be considered to specifically disclose all possible subranges and individual numerical values within the range. For example, a range description of 1 to 6 should be considered to specifically disclose subranges, such as 1 to 3, 1 to 4, 1 to 5, 2 to 4, 2 to 6, 3 to 6, etc., as well as individual numerical values within the range, such as 1, 2, 3, 4, 5, and 6, regardless of the range. Additionally, whenever a numerical range is indicated herein, it is meant to include any cited numeral (fractional or integral) within the indicated range.
[0036] Unless otherwise indicated, all technical and scientific terms used herein have the same meaning as commonly understood by those skilled in the art to which this application relates. Although this application describes only preferred methods and materials, any methods and materials similar or equivalent to those described herein may also be used in the practice or testing of this application. All documents mentioned in this specification are incorporated by reference to disclose and describe the methods and / or materials related to the documents. In the event of conflict with any incorporated document, the content of this specification shall prevail. Unless otherwise indicated, "%" is a percentage based on mass.
[0037] For whitening products, simply acting on melanin and enhancing keratin exfoliation has limited effects and is prone to skin irritation. The external appearance of skin color is not only related to melanin, but also to the texture and barrier of the skin and the health of the microbiome. For a healthy and bright complexion, in addition to regulating melanin, improving the health of the skin's microecology can not only enhance the effect of skin whitening, but also improve the safety of the skin. The composition provided by this application that has both whitening and improving the health of the skin's microecology includes at least stearyl glycyrrhetinate, colloidal oatmeal, citrus peel extract, and yeast fermentation product extract. The stearyl glycyrrhetinate of this application can act on melanocytes, inhibiting the production of tyrosinase during melanin production and thus controlling the production of melanin in the skin. Colloidal oatmeal can provide prebiotics for the health of the skin's microecology, promote the growth and balance of beneficial bacteria in the skin, and relieve skin irritation. Citrus peel extract can promote the expression of keratin in the stratum corneum of the skin, enhance the structure of the stratum corneum of the skin, and accelerate epidermal metabolism to enhance the skin whitening effect. Yeast fermentation product extract is a postbiotic that improves the skin microecology. The cell wall fragment components, exopolysaccharides, small molecule peptides, organic acids and vitamins therein can synergistically enhance the diversity of skin flora, increase the abundance of beneficial bacteria, and have a synergistic skin whitening effect. The composition of the present application can regulate the skin's microecological flora while whitening the skin, maintain the health of the skin's microecological flora, and thus enhance the health and whitening of the skin color. In addition, the composition of the present application can also increase the solubility of stearyl glycyrrhetinate and improve its transdermal absorption effect.
[0038] In some embodiments, based on the total mass of the composition, the mass percentage of stearyl glycyrrhetinate is 0.05% to 1%; in some embodiments, the mass percentage of colloidal oatmeal is 0.1% to 2%; in some embodiments, the mass percentage of citrus peel extract is 0.5% to 10%; in some embodiments, the mass percentage of yeast fermentation product extract is 0.5% to 10%.
[0039] In some embodiments, the mass percentage of stearyl glycyrrhetinate is any value of 0.05%, 0.1%, 0.15%, 0.2%, 0.3%, 0.4%, 0.5%, 0.6%, 0.7%, 0.8%, 0.9%, 1.0%, or a range consisting of any two values. For example, in some embodiments, the mass percentage of stearyl glycyrrhetinate is 0.05% to 0.15%.
[0040] In some embodiments, the mass percentage of colloidal oatmeal is any value of 0.1%, 0.2%, 0.3%, 0.4%, 0.5%, 1.0%, 1.5%, 2.0%, or a range consisting of any two values, such as the mass percentage of colloidal oatmeal is 0.1% to 0.5%.
[0041] In some embodiments, the mass percentage of citrus peel extract is any value of 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, or a range consisting of any two values, such as the mass percentage of citrus peel extract is 0.5% to 5%.
[0042] In some embodiments, the mass percentage of the yeast fermentation product extract is any value of 0.5%, 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, or a range consisting of any two values, such as the mass percentage of the yeast fermentation product extract is 0.5% to 5%.
[0043] In some embodiments, the composition further comprises β-glucan; based on the total weight of the composition, the weight percentage of β-glucan is 0.05% to 2%. For example, the weight percentage of β-glucan is any value of 0.05%, 0.1%, 0.2%, 0.3%, 0.4%, 0.5%, 1.0%, 1.5%, 2.0%, or a range consisting of any two values. For example, in some embodiments, the weight percentage of β-glucan is 0.05% to 0.5%.
[0044] In some embodiments, the composition further comprises sodium polyacryloyldimethyl taurate; based on the total mass of the composition, the mass percentage of sodium polyacryloyldimethyl taurate is 0.1% to 0.8%, such as the mass percentage of sodium polyacryloyldimethyl taurate is any value selected from 0.1%, 0.2%, 0.3%, 0.4%, 0.5%, 0.6%, 0.7%, 0.8%, or a range consisting of any two values. In this application, sodium polyacryloyldimethyl taurate is compounded with natural oils to replace traditional emulsifiers, forming a refreshing emulsion with good fluidity and low viscosity. The composition of this application is safe, mild, and easy to use.
[0045] In some embodiments, the composition further comprises oil; based on the total mass of the composition, the mass percentage of the oil is 3% to 5%, such as the mass percentage of the oil is any value of 3%, 3.5%, 4.0%, 4.5%, 5.0%, or a range consisting of any two values.
[0046] In some embodiments, the oil comprises meadowfoam seed oil, squalane and oat kernel oil, and the mass ratio of meadowfoam seed oil, squalane and oat kernel oil is (0.5-1.5): (0.5-1.5): (1.5-2.5).
[0047] In some embodiments, the mass ratio of meadowfoam seed oil, squalane, and oat kernel oil is (0.8-1): (0.8-1): (1.8-2.2).
[0048] In some embodiments, the mass ratio of meadowfoam seed oil, squalane, and oat kernel oil is 1:1:2.
[0049] In some embodiments, the composition further comprises a polyol, and the weight percentage of the polyol is 1% to 10% based on the total weight of the composition, such as 1%, 2%, 3%, 4%, 5%, 6%, 7%, 8%, 9%, 10%, or any range consisting of any two values.
[0050] In some embodiments, the polyol includes 1,2-pentanediol and propylene glycol.
[0051] In some embodiments, based on the total mass of the composition, the mass percentage of 1,2-pentanediol is 0.5% to 5%, such as the mass percentage of 1,2-pentanediol is any value of 0.5%, 1%, 2%, 3%, 4%, 5%, or a range consisting of any two values.
[0052] In some embodiments, based on the total mass of the composition, the mass percentage of propylene glycol is 0.5% to 5%, such as the mass percentage of propylene glycol is any value among 0.5%, 1%, 2%, 3%, 4%, 5%, or a range consisting of any two values.
[0053] In some embodiments, the mass ratio of stearyl glycyrrhetinate to oil is (0.01-0.3):1, such as the mass ratio of stearyl glycyrrhetinate to oil is any value among 0.01:1, 0.02:1, 0.03:1, 0.05:1, 0.1:1:0.15:1, 0.2:1, 0.25:1:0.3:1, or a range consisting of any two values.
[0054] In some embodiments, the preparation method of the composition of the present application for both skin whitening and improving microecological health comprises the following steps:
[0055] (1) Preparation of oil phase: Weigh meadowfoam seed oil, squalane, and oat kernel oil, mix with stearyl glycyrrhetinate, and dissolve at 80°C to 85°C;
[0056] (2) Preparation of thickening phase: colloidal oatmeal, sodium polyacryloyldimethyl taurate, and 1,2-pentanediol were weighed, mixed, and then water was added. The mixture was heated and stirred at 80°C to 85°C to obtain a thickening phase;
[0057] (3) Preparation of a first active substance solution: Weigh β-glucan and propylene glycol and mix to obtain a first active substance solution;
[0058] (4) Preparation of a second active substance solution: Weigh the citrus peel extract and the yeast fermentation product extract, stir and mix, and obtain a second active substance solution;
[0059] (5) The dissolved oil phase is added to the thickening phase and mixed, and then high-speed homogenization is performed at 80°C to 85°C. After homogenization, the system is cooled, and the first active substance solution and the second active substance solution are added respectively, and low-speed homogenization is performed to obtain an emulsion.
[0060] In some embodiments, the rotation speed of the high-speed homogenization is 2900 rpm to 3000 rpm; and the rotation speed of the low-speed homogenization is 1500 rpm to 2000 rpm.
[0061] The composition having both skin whitening and microecological health enhancement prepared in the examples of the present application, or the composition prepared by the preparation method of the composition having both skin whitening and microecological health enhancement in the examples of the present application, is used to prepare cosmetics.
[0062] Unless otherwise specified, the experimental methods used in the following examples are all conventional methods; the reagents, materials, instruments, etc. used in the following examples, unless otherwise specified, can all be obtained from commercial channels. Stearyl glycyrrhetinate in this application is from Gansu Panzhi Pharmaceutical. Colloidal oatmeal is from Oat Services, and citrus peel extract is from Japan Ichimaru Natural Beauty Co., Ltd. Yeast fermentation product extract is from Shanghai Huiwen Biotechnology Co., Ltd. β-glucan is from Sichuan Celicon Co., Ltd. Sodium polyacryloyldimethyl taurate is from Clariant Chemical Technology (Shanghai) Co., Ltd. Meadowfoam seed oil, squalane and oat kernel oil are from Elementis (Shanghai) New Material Co., Ltd., Aprinnova LLC and Oat Services, respectively. 1,2-Pentanediol is from Dezhixin Flavors and Fragrances (Nantong) Co., Ltd. Propylene glycol is from Dow Chemical (Shanghai) Co., Ltd.
[0063] 1. Sample preparation
[0064] Example 1: Preparation of a composition having both skin whitening and microecological health-enhancing effects
[0065] (1) Preparation of oil phase: Weigh the natural oils of meadowfoam seed oil, squalane and oat kernel oil, mix the three natural oils and stearyl glycyrrhetinate, heat in a water bath to 80°C to 85°C, stir, and keep warm for 30 minutes, observe the solubility of stearyl glycyrrhetinate in the oil, and confirm the oil phase state if the oil phase is clear and transparent without particles, which indicates complete dissolution.
[0066] (2) Preparation of thickening phase: Weigh colloidal oatmeal, sodium polyacryloyldimethyl taurate and 1,2-pentanediol, mix well, add water, heat and stir at 80°C to 85°C to swell, and form a thickening phase; the thickening phase is a translucent, uniform, non-flowable gel.
[0067] (3) Preparation of the first active substance solution: Weigh β-glucan and propylene glycol, mix them, add water and stir until they become clear, uniform and transparent to obtain the first active substance solution.
[0068] (4) Preparation of the second active substance solution: Weigh the citrus peel extract and the yeast fermentation product extract, stir and mix until they become clear, and obtain the second active substance solution.
[0069] (5) Preparation of emulsion
[0070] The preparation process is as follows:
[0071] The dissolved oil phase was added to the thickening phase and mixed, and then high-speed homogenization was performed at 80°C to 85°C, with a rotation speed of 2900rpm to 3000rpm and a homogenization time of 6 minutes.
[0072] After homogenization, the system was cooled to below 50° C., and the first active substance solution and the second active substance solution were added respectively. The mixture was homogenized at a low speed of 1500 rpm to 2000 rpm for 3 minutes, followed by low-speed stirring for 10 minutes to obtain a white, translucent, flowable emulsion. The contents of the components in the emulsion are detailed in Table 1. The water balance in Table 1 refers to water added to 100 parts by mass, the same below.
[0073] Example 2 to Example 3: The preparation method is the same as that of Example 1, except that the weight ratio of stearyl glycyrrhetinate to natural oil is adjusted. See Table 1 for details. The mass ratios of stearyl glycyrrhetinate to natural oil are adjusted to 0.15:4 and 1:4, respectively.
[0074] Examples 4 to 5: The preparation method is the same as that of Example 1, except that the weight ratio of colloidal oatmeal, sodium polyacryloyldimethyl taurate and 1,2-pentanediol is adjusted. See Table 1 for details. The weight ratios of colloidal oatmeal, sodium polyacryloyldimethyl taurate and 1,2-pentanediol are adjusted to 0.5:0.8:3 and 2:0.8:3, respectively.
[0075] Example 6-Example 7: The preparation method is the same as that of Example 4, except that the amount of β-glucan is adjusted, see Table 1 for details.
[0076] Example 8 to Example 9: The preparation method is the same as that of Example 4, except that the amount of sodium polyacryloyldimethyltaurate is adjusted, as shown in Table 1.
[0077] Example 10-Example 11: The preparation method is the same as that of Example 4, except that the amount of yeast fermentation product extract is adjusted, see Table 2 for details.
[0078] Example 12-Example 13: The preparation method is the same as that of Example 4, except that the amount of citrus peel extract is adjusted, see Table 2 for details.
[0079] Comparative Example 1: The preparation method is the same as that of Example 4, except that stearyl glycyrrhetinate is not added to the emulsion, see Table 2 for details.
[0080] Comparative Example 2: The preparation method is the same as that of Example 4, except that colloidal oatmeal is not added to the emulsion, see Table 2 for details.
[0081] Comparative Example 3: The preparation method is the same as that of Example 4, except that β-glucan is not added to the emulsion, see Table 2 for details.
[0082] Comparative Example 4: The preparation method is the same as that of Example 4, except that sodium polyacryloyldimethyltaurate is not added to the emulsion, see Table 2 for details.
[0083] Comparative Example 5: The preparation method is the same as that of Example 4, except that no citrus peel extract is added to the emulsion, see Table 2 for details.
[0084] Comparative Example 6: The preparation method is the same as that of Example 4, except that no yeast fermentation product extract is added to the emulsion, see Table 2 for details.
[0085] Table 1 Component dosage of Examples 1 to 9 (unit, parts by mass)
[0086]
[0087] Table 2 Component dosages of Examples 10 to 13 and Comparative Examples 1 to 6 (unit, parts by mass)
[0088]
[0089] “-” in Table 2 means that the component was not added to the composition; the remainder refers to the addition of water to 100 parts by mass.
[0090] 2. Performance Testing
[0091] 1. Investigation of the physical and chemical properties and stability of the emulsion
[0092] 24 hours after the emulsion was prepared, the product appearance was observed, the viscosity index was measured, and the centrifugal stability test was performed. After the emulsion was allowed to stand for 24 hours, the stability of the formula system was determined by high temperature accelerated test.
[0093] Viscosity test conditions: DV2T viscometer (BROOKFIELD), conditions: 3.0 rpm, 25° C., 1 min.
[0094] Centrifugal stability test conditions: 2000 rpm / min, 30 min.
[0095] High temperature accelerated test conditions: 50±2℃, relative humidity 75±5%, 30 days.
[0096] Table 3 Emulsion physicochemical properties and stability test results
[0097]
[0098] In Table 3, “-” means that the emulsion is unstable, forming an inhomogeneous liquid, and there is no centrifugal stability and high temperature accelerated stability data.
[0099] From the results of Examples 1, 2, and 3, it can be seen that stearyl glycyrrhetinate can be dissolved in oils and fats by heating, but different contents of stearyl glycyrrhetinate have different solubility in fixed-ratio natural oils and fats, thereby affecting the final state of the oil phase. Therefore, the content of stearyl glycyrrhetinate has a certain influence on the state of the oil phase of the system. In Example 3, when the weight ratio of stearyl glycyrrhetinate to natural oils and fats is adjusted to 1:4, the solubility of the substance is limited during the preparation process, resulting in poor stability of the emulsion, thus affecting the final uniform state of the emulsion. Therefore, in this application, the mass ratio of stearyl glycyrrhetinate to natural oils and fats is controlled within the range of (0.01 to 0.04):1, especially the mass ratio of stearyl glycyrrhetinate to natural oils and fats is controlled within the range of (0.0125 to 0.0375):1, which can improve the stability of the emulsion.
[0100] In the thickening phase, colloidal oatmeal is a powder. To address the problem of colloidal oatmeal dispersion in the emulsion, the inventors selected a dispersion system consisting of a polyol and sodium polyacryloyldimethyl taurate for use in dispersing the colloidal oatmeal. The colloidal oatmeal content also affects the state of the thickening phase. Data from Examples 2, 4, and 5 show that the colloidal oatmeal, sodium polyacryloyldimethyl taurate, and 1,2-pentanediol weight ratio of 2:0.8:3 prevents the colloidal oatmeal from being evenly dispersed in the thickening phase, thus affecting the subsequent homogeneity of the emulsion. Controlling the mass ratio of the dispersion system consisting of colloidal oatmeal, 1,2-pentanediol, and sodium polyacryloyldimethyl taurate within the range of (0.026-0.13):1 improves the stability of the emulsion.
[0101] Comparison of the results of Examples 6 and 7 with those of Example 4 shows that when the mass percentage of β-glucan in the first active substance solution in the emulsion is higher than 1%, the viscosity thereof is too high, affecting the uniformity and fluidity of the overall emulsion. Therefore, the mass percentage of β-glucan in the emulsion of the present application is controlled to be below 0.5%. Furthermore, in the examples of the present application, the mass percentage of β-glucan is controlled to be 0.05%.
[0102] The results of Examples 8, 9, and Comparative Example 4 show that the content of the emulsifying thickener sodium polyacryloyldimethyl taurate not only affects the dispersion of the colloidal oatmeal but also significantly influences the overall formation of the emulsion and the emulsification of the oil phase. When the addition amount of sodium polyacryloyldimethyl taurate is too low or the sodium polyacryloyldimethyl taurate is absent, a stable emulsion appearance cannot be achieved. In the present application, controlling the mass percentage of sodium polyacryloyldimethyl taurate in the emulsion within the range of 0.8% to 1% can improve the stability of the emulsion.
[0103] In the emulsion composition of the present application, the citrus peel extract and the yeast fermentation product extract are water-soluble. At the same time, the two active substances have certain ionicity and a low pH. The amount of citrus peel extract and yeast fermentation product extract added will affect the viscosity and stability of the emulsion. After adding to the system, it is necessary to examine their effects on the viscosity, appearance, fluidity and uniformity of the overall emulsion system to determine the final addition ratio. It can be seen from the results of Examples 10 and 11 that when the mass percentage of the yeast fermentation product extract in the emulsion is controlled within the range of 0.5% to 5%, especially when the yeast fermentation product extract is controlled within the range of 1% to 2%, the stability of the emulsion can be improved; from Examples 12 and 13, it can be seen that when the mass percentage of the citrus peel extract exceeds 5%, the system discolors and reduces viscosity. It can be seen that excessive content of the above two substances will reduce the viscosity of the emulsion and the high-temperature stability of the emulsion.
[0104] 3. In vitro efficacy experiments
[0105] According to the physicochemical properties and stability test results of the emulsion, the tyrosinase inhibition rate of B16-F10 mouse skin melanoma cells was determined for Examples 1, 2, 4 and 10, and Comparative Examples 1, 2, 3, 5 and 6.
[0106] B16-F10 cells in logarithmic growth were seeded into 6-well cell culture plates and cultured at 37°C in a 5% CO2 incubator for 24 hours. The culture medium was then aspirated. Samples diluted in DMEM were added at concentrations of 1%, 0.5%, 0.1%, and 0.05%. A control group received the same volume of DMEM. After 24 hours of culture, the supernatant was discarded and the cells were washed once with PBS. 250 μL of trypsin was added to each well. Once all cells were detached, 250 μL of complete DMEM was added to terminate the digestion. The cells were centrifuged at 1000 rpm for 5 minutes. The supernatant was discarded, and 100 μL of 0.1% cell lysis buffer was added to each well. Lysis was continued for 1-2 minutes, and the supernatant was collected by centrifugation. 50 μL of the supernatant was transferred to a 96-well plate, and 50 μL of 0.1% levodopa was added. Three replicates of each concentration were set up and the cells were incubated in a CO2 incubator for 1 hour. The absorbance at 475 nm was measured. The inhibition rate of tyrosinase in the cell reaction system was calculated according to the following formula.
[0107] A 细胞 =100-(OD 样品 -OD 空白对照 ) / (OD 细胞对照 -OD 空白对照 )×100%
[0108] Where: A 细胞 ——Tyrosinase inhibition rate in cell reaction system, %; OD 样品 ——Absorbance of the reaction system containing the sample to be tested; OD 空白对照 ——Absorbance of an empty plate without any substance; OD 细胞对照 ——Absorbance of the reaction system without the sample to be tested. The tyrosinase inhibition rate of each example at different concentrations is as follows Figure 1 shown.
[0109] The inhibitory effect on tyrosinase in melanocytes is an important pathway in skin whitening. Figure 1It can be seen that the tyrosinase inhibition rates of Comparative Examples 1 and 5 are both low, and at the experimental concentration, the tyrosinase inhibition rate of Example 1 is low, while the tyrosinase inhibition rates of Examples 2, 4 and 10, Comparative Examples 2, 3 and 6 are better. From the above results, it can be seen that stearyl glycyrrhetinate is the main active ingredient in inhibiting tyrosinase activity, and the citrus peel extract contains polyphenols and flavonoids, which can synergistically enhance the effect of inhibiting melanin.
[0110] 4. Skin Pigment Metabolism Experiment
[0111] According to the experimental results of tyrosinase inhibition rate, Example 2, Example 4, Example 10, Comparative Example 2, Comparative Example 3 and Comparative Example 6 were subjected to human skin pigment metabolism experiment. Healthy adults aged 18 to 45 years (both male and female) were screened, those without serious systemic diseases, immunodeficiency or autoimmune diseases, those without active allergic diseases, those with no history of severe allergies to cosmetics, those who were not pregnant, breastfeeding, or preparing for pregnancy, those who had not used hormone drugs and immunosuppressants in the past month, and those who had no scars, pigments, atrophy, port-wine stains or other blemishes on the skin test site that affected the test results. Each group had 6 people, and the inner side of the subject's arm was selected, and two 1×1 cm marks were marked on the corresponding positions of the subject's forearm flexion side. 2 Each test area was spaced at least 1 cm to 1.5 cm apart, with corresponding locations randomly assigned as blank and sample areas. 5% dihydroxyacetone was applied to the corresponding locations on the left arm and then evenly applied again 2 hours later. After 24 hours, a successful model was established. After testing the initial skin color values of the melanin model, the sample was applied to the sample area twice daily. The melanin index, erythema index, and internationally recognized CIELAB (L*, a*, b*) values of the skin were tested before the first use and on the seventh day. Changes in skin pigmentation in the melanin model after seven days of use were calculated. The testing instrument used was a Dermalab skin colorimetry probe. The test results are shown in Table 4.
[0112] Table 4 Changes in skin chromaticity values of each group after 7 days of use
[0113] Group M value change rate (%) E value change rate (%) L value change rate (%) Example 2 4.93% 10.51% 2.23% Example 4 8.32% 19.26% 4.34% Example 10 7.22% 16.36% 4.26% Comparative Example 2 7.15% 17.26% 4.12% Comparative Example 3 7.56% 18.25% 3.90% Comparative Example 6 4.58% 9.65% 2.57%
[0114] The M value is an indicator of skin melanin pigmentation and can be used to assess the level of pigment in the skin. The higher the M value, the more pigment the skin has. The E value is the erythema index of the skin and can be used to estimate the hemoglobin level in the skin. The higher the E value, the redder the skin. CIEL*a*b* is the skin color encoded in the CIELab color space. This measurement method is used to measure the color of the skin. Among them, L* is the brightness of the skin. The higher the L* value, the brighter the skin. Figure 2As shown in the test results, Example 4 is more effective in promoting skin metabolism, while Comparative Example 6 is less effective in promoting keratin pigment metabolism. The citrus peel extract and yeast fermentation product extract contained in Example 4 have a synergistic effect in promoting skin keratin renewal and pigment metabolism. The citrus peel extract can promote the expression of keratin in the skin's stratum corneum, accelerate epidermal metabolism, and strengthen the skin's stratum corneum structure. The yeast fermentation product extract is rich in vitamins and organic acids, which can synergistically enhance pigment metabolism.
[0115] 5. Skin microecological regulation test
[0116] According to the results of the skin pigment metabolism experiment, Example 4, Example 10, Comparative Example 2, and Comparative Example 3 were selected to perform skin oil metabolism and TEWL value tests.
[0117] The subjects were selected between the ages of 18 and 35, who self-assessed themselves as having oily skin with large pores. During the test phase, the skin was not allergic and no medications that could affect the experiment were taken; no oil-control products (except sunscreen and makeup) were used within 1 month before the test, and no similar tests were participated in. The subjects were able to strictly abide by the requirements of the test methods and sign the informed consent. Exclusion criteria: those who had adverse reactions during the test or did not comply with the test requirements. Under the management of the testers, the volunteers used an alkaline soap-based cleansing product to clean their faces, rinsed with clean water, and dried with a dandruff-free absorbent paper towel. They sat quietly in a standard test environment with their foreheads exposed, relaxed, and avoided touching their foreheads. A skin surface sebum tester was used to measure the amount of sebum on the skin surface of the forehead. The amount of sebum on the volunteers' foreheads exceeded 20μg / cm within 8 hours. 2 were included as subjects.
[0118] Six subjects were selected for each group. Facial data was collected and photographed using the VISIA before testing. The product was used continuously for seven days, with a focus on the T-zone. Data measurements and photographs were taken after seven days. The test environment temperature was 20-22°C, and the relative humidity was 40%-60%. Testing occurred on days 0 and 7. Testing instruments included the VISIA and Dermalab skin colorimeter probes. Test indicators included TEWL and changes in facial porphyrin counts using the VISIA. The changes in facial data for different components are shown in Table 5.
[0119] Table 5 Changes in skin oil and TEWL values in each group after 7 days of trial
[0120]
[0121] The skin microecology and the physiological functions of the skin are mutually regulated and related. Changes in the beneficial bacteria and pathogens on the skin will affect physiological indicators such as the skin barrier and oil secretion. The imbalance of the skin microecological health will aggravate abnormal sebum secretion and sensitivity. After being irradiated with VISIA ultraviolet light, it will show fluorescence. Therefore, the VISIA skin detector can observe the oil content on the skin surface under ultraviolet light. The yellow fluorescence color represents the skin oil metabolites. The orange fluorescence represents the porphyrin metabolite of Propionibacterium acnes in the skin. The overall statistics of the number of skin porphyrins in the VISIA skin detector represent the total amount of these two substances. The TEWL value represents the skin barrier function. A lower TEWL value means less transepidermal water loss per unit time, which means that the barrier function is improved.
[0122] From the experimental results, it can be seen that Example 4 can effectively reduce the content of rhodopsin in the skin, reduce the oil content of oily skin, and reduce the production of metabolites of Propionibacterium acnes in the skin. Figure 3 The following are the test results of a typical case using the emulsion of Example 4 of this application before and after four weeks. Figure 3 It can be seen from the test results that the emulsion prepared in the embodiment of the present application can reduce the TEWL value and improve the skin barrier function. Among them, yeast fermentation product extract, β-glucan and colloidal oatmeal powder have a synergistic effect of improving the skin microecology. Yeast fermentation product extract contains amino acids, small molecule peptides and organic acids, etc., which can promote the growth balance of beneficial bacteria in the skin as postbiotics, thereby improving the skin's oil metabolism and health; β-glucan can activate skin immune cells, resist the invasion of microorganisms such as bacteria, fungi and viruses, and at the same time enhance the vitality of keratinocytes and fibroblasts, regulate the health of skin microecology while enhancing barrier health. Colloidal oatmeal contains the polyphenol avenanthramide, which can provide prebiotics for the health of skin microecology while soothing skin irritation and improving moisturizing.
[0123] 6. Human Clinical Efficacy Testing
[0124] Based on the results of the microecological regulation test, the sample from Example 4 was subjected to human clinical efficacy testing. Thirty-two healthy Chinese subjects aged 18 to 60 years with facial pigmentation, enlarged pores, dull, and rough skin were selected. Exclusion criteria included pregnant or lactating women, or those planning to conceive in the near future; those with a highly sensitive constitution, allergic diseases, or a history of cosmetic allergies; those with skin diseases such as psoriasis, eczema, atopic dermatitis, severe acne, or other chronic systemic diseases; and those who had participated in a cosmetic clinical trial in the past month. The sample from Example 4 was used continuously for four weeks, and changes in skin melanin content, brightness, roughness, and smoothness were measured before and after sample use. Testing instruments included: Glossymeter GL200 skin brightness probe (Courage & Khazaka, Germany); VisioScan VC20 plus (Courage & Khazaka, Germany); Dermalab skin colorimetry probe; and skin VISIA detector. The grading of adverse skin reactions during the test period shall be determined according to the grading standards for adverse skin reactions in human trials specified in the 2015 edition of the "Technical Specifications for Safety of Cosmetics". See Tables 6 and 7 for details.
[0125] Table 6 Skin reaction grading standards for human trial tests
[0126] Skin reactions Grading No response 0 Faint erythema 1 Erythema, infiltration, papules 2 Erythema, edema, papules, blisters 3 Erythema, edema, bullae 4
[0127] Table 7 Adverse reaction severity grading standards
[0128]
[0129]
[0130] At the same time, skin samples were collected from the subjects before use (BL) and 4 weeks after use (W4), and 16s analysis and sequencing of skin flora microorganisms were performed to detect changes in the composition of skin microbial communities.
[0131] After using it for 4 weeks, the subjects' facial melanin content decreased by 12.19%, the cheek skin glossiness increased by 9.38%, the cheek roughness improved by 24.26%, and the skin smoothness increased by 8.29%. Figures 4 to 7 After 4 weeks of use, the subjects' skin spots were reduced, and the skin smoothness and fineness were improved. Figure 8 No adverse reactions occurred during the test. The adverse reaction monitoring results are shown in Table 8. According to the 16s sequencing results, after 4 weeks of using the sample, the Beta diversity of the skin flora increased and the abundance of the Bacteroidetes phylum decreased significantly. The abundance of the pathogenic bacterium Chryseobacterium indole-producing was significantly reduced. Figures 9 to 11 shown.
[0132] Table 8 Adverse reaction evaluation results
[0133]
[0134] Test results show that the emulsion prepared in this application can significantly reduce skin melanin production, lighten skin spots, significantly improve skin brightness and smoothness, and reduce skin roughness. It also significantly increases the diversity of skin flora and reduces skin pathogens. It has the effect of both whitening skin and improving the health of the skin microbiome.
[0135] The above is a detailed introduction to a composition and preparation method for skin whitening and microecological health enhancement provided in the examples of the present application. Specific examples are used herein to illustrate the principles and implementation methods of the present application. The description of the above embodiments is only used to help understand the method of the present application and its core idea. At the same time, for those skilled in the art, according to the ideas of the present application, there will be changes in the specific implementation methods and application scopes. In summary, the content of this specification should not be understood as limiting the present application.
Claims
1. A composition that whitens skin and improves microecological health, characterized in that: The composition includes stearyl glycyrrhetinate, colloidal oatmeal, citrus peel extract and yeast fermentation product extract.
2. The composition for both skin whitening and microecological health enhancement according to claim 1, characterized in that: Based on the total mass of the composition, the mass percentage of the stearyl glycyrrhetinate is 0.05% to 1%, the mass percentage of the colloidal oatmeal is 0.1% to 2%, the mass percentage of the citrus peel extract is 0.5% to 10%, and the mass percentage of the yeast fermentation product extract is 0.5% to 10%.
3. The composition for both skin whitening and microecological health enhancement according to claim 1, characterized in that: The composition also includes beta-glucan; based on the total mass of the composition, the mass percentage of the beta-glucan is 0.05% to 2%.
4. The composition for both skin whitening and microecological health enhancement according to claim 1, characterized in that: The composition further comprises oil; the mass percentage of the oil is 3% to 5% based on the total mass of the composition; and / or, The composition further comprises sodium polyacryloyldimethyl taurate; based on the total mass of the composition, the mass percentage of the sodium polyacryloyldimethyl taurate is 0.1% to 0.8%.
5. The composition for whitening skin and improving microecological health according to claim 4, characterized in that: The oil comprises meadowfoam seed oil, squalane and oat kernel oil; the mass ratio of the meadowfoam seed oil, squalane and oat kernel is (0.5-1.5): (0.5-1.5): (1.5-2.5).
6. The composition for both skin whitening and microecological health enhancement according to claim 3, characterized in that: The composition further comprises a polyol; based on the total mass of the composition, the mass percentage of the polyol is 1% to 10%.
7. The composition for both skin whitening and microecological health enhancement according to claim 4, characterized in that: The mass ratio of the stearyl glycyrrhetinate to the oil is (0.01-0.3):
1.
8. A method for preparing a composition having both skin whitening and microecological health enhancement properties, characterized in that: The following steps are involved: (1) Preparation of oil phase: Weigh meadowfoam seed oil, squalane, and oat kernel oil, mix with stearyl glycyrrhetinate, and dissolve at 80°C to 85°C; (2) Preparation of thickening phase: colloidal oatmeal, sodium polyacryloyldimethyl taurate, and 1,2-pentanediol were weighed, mixed, and then water was added. The mixture was heated and stirred at 80°C to 85°C to obtain a thickening phase; (3) Preparation of a first active substance solution: Weigh β-glucan and propylene glycol and mix to obtain a first active substance solution; (4) Preparation of a second active substance solution: Weigh the citrus peel extract and the yeast fermentation product extract, stir and mix, and obtain a second active substance solution; (5) The dissolved oil phase is added to the thickening phase and mixed, and then high-speed homogenization is performed at 80°C to 85°C. After homogenization, the system is cooled, and the first active substance solution and the second active substance solution are added respectively, and low-speed homogenization is performed to obtain an emulsion.
9. The method for preparing the composition for both skin whitening and microecological health enhancement according to claim 8, characterized in that: The rotation speed of the high-speed homogenization is 2900 rpm to 3000 rpm; the condition of the low-speed homogenization is 1500 rpm to 2000 rpm.
10. Use of a composition having both skin whitening and microecological health enhancement as claimed in any one of claims 1 to 7 or a composition prepared by the method for preparing a composition having both skin whitening and microecological health enhancement as claimed in any one of claims 8 to 9 in the preparation of cosmetics.