Bakuchiol liposome with whitening and anti-aging effects as well as preparation method and application of bakuchiol liposome
By dissolving components such as psoralophenol, resveratrol and retinol and lipids in an organic solvent, combined with emulsifiers and stabilizers, and undergoing high-pressure homogenization, bone pulmonary pulmonary pulmonary pulmonary pulmonary pulmonary pulmonary pulmonary pulmonary pulmonary pulmonary pulmonary pulmonary pulmonary pulmonary pulmonary pulmonary Lipophenolic liposomes solve the problems of poor stability and poor effect in the prior art, and achieve better skin retention and antioxidant and anti-inflammatory effects.
Patent Information
- Application Number
- CN202411282564.9
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2024-09-13
- Publication Date
- 2024-12-13
- Estimated Expiration
- Not applicable · inactive patent
AI Technical Summary
The existing psoral peroxide liposomes have poor stability, poor whitening and anti-aging effects in aqueous systems, and increasing the amount of psoral peroxide will lead to strong irritation and cytotoxicity problems, limiting its application scope.
1-5 parts of psoralophenol, 0.1-1 parts of resveratrol, 0.1-0.5 parts of retinol and lipid are dissolved in an organic solvent, combined with emulsifier, emulsifier, stabilizer, and through high pressure Homogenized treatment and pH adjustment were made to prepare psoralophenolic liposomes with whitening and anti-aging effects.
It significantly improves the stability of psoralophenol liposomes and whitening and anti-aging effects, enhances the retention amount and transdermal absorption of active ingredients, improves the antioxidant and anti-inflammatory effects, has a uniform particle size, and is suitable for a wide range of applications.
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Figure CN119112706A_ABST
Abstract
Description
Technical Field
[0001] The present application belongs to the technical field of liposomes, and in particular relates to a bakuchiol liposome with whitening and anti-aging effects, and a preparation method and application thereof. Background Art
[0002] Bakuchiol, a natural ingredient extracted from Psoralea corylifolia, has been shown to have significant antioxidant, anti-inflammatory and antibacterial properties and is considered a natural alternative to retinol. However, single bakuchiol has problems such as poor solubility in aqueous systems, harsh storage conditions, easy oxidation and low permeability, which limits its application range.
[0003] In order to better exert the comprehensive performance of bakuchiol, the prior art has disclosed the use of liposomes to encapsulate bakuchiol, thereby improving the stability of bakuchiol liposomes. However, in order to improve the whitening and anti-aging effects, the amount of bakuchiol added is usually greatly increased, which has the problems of strong irritation and cytotoxicity, and increases the cost. Therefore, how to improve the comprehensive performance of bakuchiol is a problem that needs to be solved at present. Summary of the invention
[0004] The present application discloses a bakuchiol liposome with whitening and anti-aging effects, and a preparation method and application thereof, aiming to solve the technical problems of poor stability, poor whitening and anti-aging effects of existing bakuchiol liposomes.
[0005] In order to achieve the above purpose, the technical solution of this application is:
[0006] The first aspect of the present application provides a method for preparing bakuchiol liposomes, the method comprising:
[0007] Dissolve 1-5 parts by weight of bakuchiol, 0.1-1 parts by weight of resveratrol, 0.1-0.5 parts by weight of retinol, and lipid in an organic solvent to obtain phase A;
[0008] Dissolve the emulsifier, co-emulsifier and stabilizer in water to obtain phase B;
[0009] After the phase A and the phase B are subjected to high pressure homogenization treatment, the pH is adjusted to obtain the bakuchiol liposome.
[0010] In combination with the first aspect, preferably, the method includes:
[0011] Dissolve 2-4 parts by weight of bakuchiol, 0.2-0.7 parts by weight of resveratrol, 0.2-0.4 parts by weight of retinol, and lipid in an organic solvent to obtain phase A;
[0012] Dissolve the emulsifier, co-emulsifier and stabilizer in water to obtain phase B;
[0013] After the phase A and the phase B are subjected to high pressure homogenization treatment, the pH is adjusted to obtain the bakuchiol liposome.
[0014] In combination with the first aspect, preferably, the method includes:
[0015] Dissolve 4 parts by mass of bakuchiol, 0.7 parts by mass of resveratrol, 0.4 parts by mass of retinol, and lipid in an organic solvent to obtain phase A;
[0016] Dissolve the emulsifier, co-emulsifier and stabilizer in water to obtain phase B;
[0017] After the phase A and the phase B are subjected to high pressure homogenization treatment, the pH is adjusted to obtain the bakuchiol liposome.
[0018] In combination with the first aspect, preferably, the lipid is one or more of lecithin, caprylic / capric triglyceride, monostearate glyceryl, butyloctanol salicylate, and acetylated monoglyceride;
[0019] And / or, the lipid is added in an amount of 4-8 parts by mass.
[0020] In combination with the first aspect, preferably, the emulsifier is one or more of polyglyceryl 10 stearate, PEG-8 caprylic / capric glyceride, sucrose stearate, cetearyl olive oil ester, sorbitan olive oil ester, laureth-23, PEG-4 olive oil ester, steareth-21, palmityl alcohol, PEG-75 stearate, glyceryl stearate, steareth-20, cetyl alcohol, cetyl alcohol ether-20, and steareth-20;
[0021] And / or, the emulsifier is added in an amount of 2-16 parts by weight.
[0022] In combination with the first aspect, preferably, the stabilizer is one or more of 1,3-butylene glycol, hydrogenated olive oil, olive oil, unsaponifiable matter of olive oil, cetyl palmitate, sorbitan palmitate, and sorbitan olivate;
[0023] And / or, the stabilizer is added in an amount of 1-5 parts by weight.
[0024] In combination with the first aspect, preferably, when 1-5 parts by mass of bakuchiol, 0.1-1 parts by mass of resveratrol, 0.1-0.5 parts by mass of retinol, and lipid are dissolved in an organic solvent, the reaction temperature is 40-50° C., and the reaction time is 0.5-2 h.
[0025] In combination with the first aspect, preferably, the conditions for the high-pressure homogenization treatment are: a pressure of 90-120 MPa, and a number of cycles of 2-3 times;
[0026] And / or, the pH is adjusted to 6.5-7.0.
[0027] The second aspect of the present application provides bakuchiol liposomes with whitening and anti-aging effects prepared by the preparation method described in the first aspect.
[0028] The third aspect of the present application provides the use of the bakuchiol liposomes with whitening and anti-aging effects described in the second aspect in the preparation of skin care products.
[0029] Compared with the prior art, the advantages or beneficial effects of the embodiments of the present application include at least:
[0030] The preparation method of bakuchiol liposomes with whitening and anti-aging effects provided in the present application can not only exert the mutual synergistic enhancement between bakuchiol, resveratrol and retinol, inhibit the production of melanin from multiple dimensions, thereby greatly improving the skin structure and skin color, and significantly improving its whitening and anti-aging effects, but also increase the retention of active ingredients in the skin and enhance the transdermal absorption effect by controlling the composition ratio of the three, thereby improving the durability after application. At the same time, it can greatly enhance its antioxidant and anti-inflammatory effects, and the obtained particle size is more uniform and the stability is better. The preparation process is simple and easy, and has broad market application prospects. BRIEF DESCRIPTION OF THE DRAWINGS
[0031] In order to more clearly illustrate the technical solutions of 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 recorded in the present application, and for ordinary technicians in this field, other drawings can be obtained based on these drawings without creative work.
[0032] Figure 1 This is a statistical graph of the cell viability results of the A1-liposome provided in the examples of the present application;
[0033] Figure 2 This is a statistical chart of the cell anti-inflammatory experiment results of A1-liposome provided in the examples of the present application;
[0034] Among them, compared with the LPS group, *P<0.05, **P<0.01, ***P<0.005, ****P<0.0001;
[0035] Figure 3 A schematic diagram of the results of the melanoma cell inhibition experiment of A1-liposomes provided in the examples of the present application;
[0036] Figure 4 A schematic diagram of the cell viability results in the anti-aging experiment of A1-liposomes provided in the examples of the present application;
[0037] Figure 5 This is a statistical graph of the cell viability results of the A2-liposomes provided in the examples of the present application;
[0038] Figure 6 This is a statistical chart of the cell anti-inflammatory experiment results of A2-liposome provided in the examples of the present application;
[0039] Among them, compared with the LPS group, *P<0.05, **P<0.01, ***P<0.005, ****P<0.0001;
[0040] Figure 7 A schematic diagram of the results of the melanoma cell inhibition experiment of A2-liposomes provided in the examples of the present application;
[0041] Figure 8 A schematic diagram of the cell viability results in the anti-aging experiment of A2-liposomes provided in the examples of the present application;
[0042] Fig. 9 This is a statistical graph of the cell viability results of A3-liposomes provided in the examples of this application;
[0043] Fig.10 This is a statistical chart of the cell anti-inflammatory experiment results of A3-liposome provided in the examples of the present application;
[0044] Among them, compared with the LPS group, *P<0.05, **P<0.01, ***P<0.005, ****P<0.0001;
[0045] Fig.11 A schematic diagram of the results of the melanoma cell inhibition experiment of A3-liposomes provided in the examples of the present application;
[0046] Fig.12 A schematic diagram of the cell viability results in the anti-aging experiment of A3-liposomes provided in the examples of the present application;
[0047] Fig.13 This is a statistical graph of the cell viability results of A4-liposomes provided in the examples of this application;
[0048] Fig.14 This is a statistical chart of the cell anti-inflammatory experiment results of A4-liposome provided in the examples of the present application;
[0049] Among them, compared with the LPS group, *P<0.05, **P<0.01, ***P<0.005, ****P<0.0001;
[0050] Fig.15 A schematic diagram of the results of the melanoma cell inhibition experiment of A4-liposomes provided in the examples of the present application;
[0051] Fig.16 This is a schematic diagram of the cell viability results in the anti-aging experiment of A4-liposomes provided in the examples of the present application. DETAILED DESCRIPTION
[0052] The technical solutions in the embodiments of the present application will be described clearly and completely below in conjunction with the drawings in the embodiments of the present application. Obviously, the described embodiments are part of the embodiments of the present application, rather than all of the embodiments. Based on the embodiments in the present application, all other embodiments obtained by ordinary technicians in this field without creative work are within the scope of protection of this application.
[0053] In the following description of this embodiment, the term "and / or" is used to describe the association relationship of associated objects, indicating that there may be three relationships. For example, A and / or B can represent: A exists alone, B exists alone, and A and B exist at the same time. A and B can be singular or plural. The character " / " generally indicates that the associated objects before and after are in an "or" relationship.
[0054] In the following description of this embodiment, the term "at least one" refers to one or more, and "plurality" refers to two or more. "At least one of the following" or similar expressions refers to any combination of these items, including any combination of single items or plural items. For example, "at least one of a, b or c", or "at least one of a, b and c", can all represent: a, b, c, ab (i.e., a and b), ac, bc, or abc, where a, b, c can be single or multiple, respectively.
[0055] Those skilled in the art should understand that in the following description of the embodiments of the present application, the order of serial numbers does not mean the order of execution, some or all of the steps can be executed in parallel or sequentially, and the execution order of each process should be determined by its function and internal logic, and should not constitute any limitation on the implementation process of the embodiments of the present application.
[0056] The terms used in the embodiments of the present application are only for the purpose of describing specific embodiments, and are not intended to limit the present application. The singular forms "a", "an" and "the" used in the embodiments of the present application and the appended claims are also intended to include plural forms, unless the context clearly indicates other meanings.
[0057] Unless otherwise specified, all raw materials and reagents used in the examples of the present application are purchased on the market or prepared according to conventional methods well known to those skilled in the art.
[0058] In a first aspect, the present invention provides a method for preparing bakuchiol liposomes having whitening and anti-aging effects, the method comprising:
[0059] Dissolve 1-5 parts by weight of bakuchiol, 0.1-1 parts by weight of resveratrol, 0.1-0.5 parts by weight of retinol, and lipid in an organic solvent to obtain phase A;
[0060] Dissolve the emulsifier, co-emulsifier and stabilizer in water to obtain phase B;
[0061] After the phase A and the phase B are subjected to high pressure homogenization treatment, the pH is adjusted to obtain the bakuchiol liposome.
[0062] Among them, not only can the mutual synergistic enhancement between bakuchiol, resveratrol and retinol be brought into play, the production of melanin can be inhibited from multiple dimensions, thereby greatly improving the skin structure and skin color, but also by controlling the composition ratio of the three, the retention amount of active ingredients in the skin is increased and the transdermal absorption effect is enhanced, thereby improving the durability after application. At the same time, its antioxidant and anti-inflammatory effects can be greatly improved, and the obtained particle size is more uniform and the stability is better. The preparation process is simple and easy, and has broad market application prospects.
[0063] The present application unexpectedly discovered that when the active components are preferably 1-5 parts by mass of bakuchiol, 0.1-1 parts by mass of resveratrol, and 0.1-0.5 parts by mass of retinol, the particle size uniformity, stability, durability, antioxidant and anti-inflammatory effects, and whitening effects of bakuchiol liposomes can be significantly improved, and compared with a single active component or a simple superposition combination of several other active components, it has a certain synergistic effect.
[0064] It should be noted that bakuchiol is preferably 2-4 parts by mass, more preferably 4 parts by mass, resveratrol is preferably 0.2-0.7 parts by mass, more preferably 0.7 parts by mass, and retinol is preferably 0.2-0.4 parts by mass, more preferably 0.4 parts by mass. By controlling the material selection and addition amount of bakuchiol, resveratrol and retinol, bakuchiol can inhibit the activity of tyrosinase and reduce the synthesis of melanin. Tyrosinase is the key enzyme for melanin production, and inhibiting its activity can directly reduce the production of melanin; resveratrol has antioxidant and anti-inflammatory properties, and can inhibit melanocyte activation by reducing ultraviolet-induced oxidative stress. Retinol (vitamin A) can promote skin cell renewal and help remove keratinocytes containing melanin. In addition, it can also inhibit the generation of melanin by regulating skin cell metabolism. Bakuchiol, resveratrol and retinol inhibit the generation of melanin from multiple dimensions, thereby greatly improving skin structure and skin color, and greatly improving its whitening and anti-aging effects.
[0065] Resveratrol: is a powerful antioxidant widely used in cosmetics to improve skin health. Its main benefits include anti-aging, anti-inflammatory and whitening. Resveratrol can neutralize free radicals and reduce oxidative damage to the skin, thereby slowing down the aging process and reducing the appearance of fine lines and wrinkles. At the same time, it has significant anti-inflammatory effects, helping to relieve redness and irritation and improve skin texture. In addition, resveratrol can inhibit the production of melanin and has a whitening effect. Its mechanism is mainly through activating the antioxidant enzyme system in the skin, reducing oxidative stress, and improving the overall health and radiance of the skin by regulating the inflammatory response and pigmentation of skin cells. Retinol: is a vitamin A derivative widely used in cosmetics, mainly known for its anti-aging and repair effects. Its main benefits include promoting skin cell renewal, reducing fine lines and wrinkles, and improving skin texture and color. Retinol slows down the signs of aging by promoting cell proliferation and differentiation in the epidermis and dermis of the skin, enhancing the thickness and elasticity of the skin. In addition, it can accelerate the renewal of the stratum corneum on the surface of the skin, reduce pore blockage, and help improve acne and uneven skin tone. Its mechanism is mainly through conversion into retinoic acid, binding to retinoic acid receptors in the cell nucleus, regulating gene expression, promoting the synthesis of collagen and elastin, and inhibiting melanin production, thereby improving skin structure and skin color.
[0066] In the embodiment of the present application, the lipid is preferably one or more of lecithin, caprylic / capric triglyceride, monostearate glyceryl, butyloctanol salicylate, and acetylated monoglyceride; the added amount is preferably 4-8 parts by weight. Among them, by selecting these lipids, the oil-soluble active ingredients can be better dissolved and stabilized, greatly improving the stability of the active in the system.
[0067] In the embodiment of the present application, the emulsifier is preferably one or more of polyglycerol 10 stearate, PEG-8 caprylic / capric glyceride, sucrose stearate, cetearyl olive oil ester, sorbitan olive oil ester, laureth-23, PEG-4 olive oil ester, steareth-21, palmityl alcohol, PEG-75 stearate, glyceryl stearate, steareth-20, hexadecanol, hexadecanol ether-20, and steareth-20, and the added portion is preferably 2-16 parts by weight. Among them, through the selection of these emulsifiers, the oil phase and the water phase can be effectively mixed together, so that each component forms a stable and uniform emulsion, maintaining the stability of the product, and at the same time, these emulsifiers are mild and non-irritating, environmentally friendly, and suitable for large-scale application.
[0068] In the embodiment of the present application, the stabilizer is preferably one or more of 1,3-butylene glycol, hydrogenated olive oil, olive oil, unsaponifiable olive oil, cetyl palmitate, sorbitan palmitate, and sorbitan olivate, and the amount of the stabilizer added is preferably 1-5 parts by weight. Among them, by adding these stabilizers, the structural stability of the liposomes can be increased by interacting with the phospholipid molecules on the membrane surface, reducing the aggregation and fusion of the liposomes, and further enhancing the stability of the liposomes.
[0069] In the embodiment of the present application, the conditions of the high-pressure homogenization treatment are preferably: the pressure is preferably 90-120 MPa, the number of cycles is preferably 2-3 times, and the pH is preferably adjusted to 6.5-7.0. Among them, the high-pressure homogenization treatment can reduce the particle size of the dispersed phase in the material, obtain fine and uniform particles, provide better stability, improve storage quality, improve homogeneity, improve absorption quality, save expensive additives, change viscosity and reduce reaction time, and then adjust the pH to neutral, which is convenient for the subsequent storage of liposomes and gives them excellent stability.
[0070] The second aspect of the present application provides bakuchiol liposomes with whitening and anti-aging effects prepared by the preparation method described in the first aspect. The bakuchiol liposomes have uniform particle size, stability, durability, significantly improved whitening effect, and antioxidant and anti-inflammatory properties.
[0071] The third aspect of the present application provides the use of the bakuchiol liposomes with whitening and anti-aging effects described in the second aspect in the preparation of skin care products. Among them, based on the above-mentioned bakuchiol liposomes having uniform particle size, stability, durability, and significantly improved whitening and anti-aging effects, and having antioxidant and anti-inflammatory properties, thus giving excellent product competitiveness.
[0072] The technical solution of the present application will be further described below in conjunction with specific embodiments.
[0073] Example 1
[0074] This example provides a method for preparing A1-liposomes, which specifically includes:
[0075] S101: dissolving 4-8 parts of lipid in an organic solvent, adding bakuchiol, ultrasonicating to obtain an emulsion, and evaporating under reduced pressure to remove the organic solvent to obtain phase A;
[0076] S102: Heat 2-16 parts of emulsifier, 1-10 parts of co-emulsifier, and 1-5 parts of stabilizer to 80° C., add into 100 parts of deionized water, stir and mix evenly, to obtain phase B;
[0077] S103: Add phase A to phase B, homogenize at a speed of 10000 rpm for 10 min, homogenize 3 times at 80°C and a pressure of 100 MPa, stir for 0.5-1 h, add a pH adjuster to adjust the pH value to 6.5-7, and obtain A1-liposomes.
[0078] In this example, different amounts of bakuchiol were added to obtain bakuchiol liposomes with different contents for corresponding performance tests.
[0079] Test 1: Particle size test
[0080] The hydrodynamic particle size of the sample was determined using dynamic light scattering technology. The prepared liposomes were used as samples, diluted with deionized water to a certain concentration, and then measured three times in parallel at 25°C to record the average particle size of the sample.
[0081] Test 2: Storage stability
[0082] Place the test object in a sealed container and leave it at room temperature for the same day, 10 days, 30 days, 60 days and 90 days. Check the sample properties for agglomeration or stratification at the initial state and after 10 days, 30 days, 60 days and 90 days. The inspection results can be expressed as uniformity and the presence of crystal precipitation.
[0083] Test 3: Antioxidant test
[0084] The present application provides a test experiment for the cellular antioxidant capacity of each product: HaCaT cells in logarithmic growth phase were cultured at 8×10 3 / well was inoculated in a 96-well plate, with a system of 100 μL per well. The outermost circle of the 96-well plate was sealed with 100 μL of PBS. After the cells were completely attached to the wall, they were replaced with the matrix to be tested. After the cells were cultured for 24 hours, the CCK-8 method was used to detect cell activity. After that, a hydrogen peroxide dilution (diluted to 800 μM with DMEM medium) was given, and the model was cultured in an incubator for 4 hours. After 4 hours, the cell activity was immediately detected by CCK8 method. The prepared products were diluted with DMEM medium to a final concentration of 20 μg / mL of the active substance as the matrix to be tested; at the same time, a blank group without hydrogen peroxide damage and a H2O2 group without drug administration were set up to detect the cellular antioxidant capacity of each sample.
[0085] Test 4: Anti-inflammatory test
[0086] RAW264.7 cells (mouse mononuclear macrophage leukemia cells) in the logarithmic growth phase were inoculated in a 24-well plate at a cell density of (2-5)×10 5 / mL, 0.5mL per well, incubate for 24h. After 24h, remove the supernatant and add 0.5mL of the following samples respectively:
[0087] ①Solvent control group: DMEM medium (2% FBS; 1% double antibody) was used to act on cells for 24 hours;
[0088] ②LPS (lipopolysaccharide) inflammation model group: 1 μg / mL LPS continuously stimulated RAW 264.7 cells for 24 h;
[0089] ③ Experimental group: The diluted sample + LPS (1μg / ml) was used to act on the cells for 24 hours. After the sample was treated with cells for 24 hours, the supernatant was aspirated into a centrifuge tube with a pipette, centrifuged at 1000r / min for 5 minutes, the precipitate was discarded and the supernatant was aspirated, and the TNF-α and IL-6 inflammatory factor detection kits were used to detect the changes in the inflammatory factors in the supernatant. The detection method was strictly in accordance with the instructions on the detection kit.
[0090] Test 5: Whitening effect test
[0091] Determination of tyrosinase inhibition rate: Add 80μL PBS buffer, 40μL sample diluent of different concentrations, 40μL tyrosinase solution and 80μL substrate L-tyrosine solution to a 96-well plate, mix well and incubate at 25°C in the dark for 20 minutes. Then detect the absorbance at 475nm on a microplate reader, calculate the effect of the sample on the activity of elastase and calculate the statistical difference P value. The absorbance of the negative and reaction groups is recorded as A0, the absorbance of the negative blank group is recorded as A1, the absorbance of the sample and reaction group is recorded as B0, and the absorbance of the sample and blank group is recorded as B1.
[0092] Tyrosinase inhibition rate = [1-(B0-B1) / (A0-A1)] × 100%.
[0093] The positive control sample substrate is used as the sample solution for reaction control, and the negative control group, i.e., the sample diluent, is used as the sample solution for reaction control.
[0094] Test 6: Anti-aging effect test
[0095] The prepared liposomes were subjected to an anti-UV oxidation efficacy test: the prepared liposomes were diluted with DMEM medium at a final concentration of 10 μg / ml of active substance. HDF cells in logarithmic growth phase were cultured at 8×10 3 Each well was inoculated in a 96-well plate, with a system of 100 μL in each well. The outermost circle of the 96-well plate was sealed with 100 μL of PBS. After the cells were completely attached to the wall, they were replaced with complete culture medium containing the sample to be tested. After continuing to culture the cells for 24 hours, the cell activity was detected by CCK-8 method. The cells cultured with the sample dilution for 24 hours were irradiated with UV for 5 minutes, and the cell activity was detected by CCK8 method after being cultured in the incubator for 24 hours.
[0096] The test results are shown in Table 1:
[0097] Table 1 Comprehensive properties of different amounts of bakuchiol
[0098]
[0099]
[0100] According to Table 1, Figure 1 , Figure 2 , Figure 3 and Figure 4 The test results show that when the amount of bakuchiol added is 4 parts, the obtained liposome particle size is the smallest; the stability is good; the level of cell inflammatory factors is the lowest, the anti-inflammatory effect is the best; the tyrosinase inhibition rate is the highest, the whitening effect is the best; the cell viability in the anti-UV experiment is the highest, and the anti-aging effect is the best. This shows that when the amount of bakuchiol added is 1-5 parts by mass, it has excellent comprehensive performance, and the comprehensive performance is optimal when 4 parts by mass are added.
[0101] Example 2
[0102] In the present application, a method for preparing A2-liposomes is provided by measuring the addition of different amounts of resveratrol, which specifically includes:
[0103] S201: dissolving 4-8 parts of lipid in an organic solvent, adding resveratrol, ultrasonicating to obtain an emulsion, and evaporating under reduced pressure to remove the organic solvent to obtain phase A;
[0104] S202: Heat 2-16 parts of emulsifier, 1-10 parts of co-emulsifier, and 1-5 parts of stabilizer to 80° C., add into 100 parts of deionized water, stir and mix evenly, to obtain phase B;
[0105] S203: Add phase A to phase B, homogenize at a rotation speed of 10000 rpm for 10 min, homogenize 3 times at 80°C and a pressure of 100 MPa, stir for 0.5-1 h, add a pH adjuster to adjust the pH value to 6.5-7, and obtain A2-liposomes.
[0106] According to the above test process, the A2-liposome was subjected to corresponding performance tests, and the test results are shown in Table 2:
[0107] Table 2 Comprehensive performance of different amounts of resveratrol
[0108]
[0109] According to Table 2, Figure 5 , Figure 6 , Figure 7 and Figure 8The test results show that when the amount of resveratrol added is 0.7 parts, the prepared liposomes have the smallest particle size, good stability, the lowest level of cell inflammatory factors, and the best anti-inflammatory effect; the highest tyrosinase inhibition rate and the best whitening effect; the highest cell viability in the anti-UV experiment and the best anti-aging effect. This shows that when the amount of resveratrol added is 0.1-1 parts by mass, it has excellent comprehensive performance, and the comprehensive performance is optimal when it is added at 0.7 parts by mass.
[0110] Example 3
[0111] In the present application, a method for preparing A3-liposomes is provided by measuring the addition of different amounts of retinol, which specifically includes:
[0112] S301: dissolving 4-8 parts of lipid in an organic solvent, adding retinol, performing ultrasound to obtain an emulsion, and removing the organic solvent by evaporation under reduced pressure to obtain phase A;
[0113] S302: Heat 2-16 parts of emulsifier, 1-10 parts of co-emulsifier, and 1-5 parts of stabilizer to 80° C., add into 100 parts of deionized water, stir and mix evenly, to obtain phase B;
[0114] S303: Add phase A to phase B, homogenize at a speed of 10000 rpm for 10 min, homogenize 3 times at 80°C and a pressure of 100 MPa, stir for 0.5-1 h, add a pH adjuster to adjust the pH value to 6.5-7, and obtain A3-liposomes.
[0115] According to the above test process, the A3-liposome was subjected to corresponding performance tests, and the test results are shown in Table 3:
[0116] Table 3 Comprehensive performance of different amounts of retinol
[0117]
[0118]
[0119] According to Table 3, Fig. 9 , Fig.10 , Fig.11 and Fig.12 The test results show that when the amount of retinol added is 0.4, the A3-liposome prepared has the smallest particle size; good stability; the lowest level of cell inflammatory factors, the best anti-inflammatory effect; the highest tyrosinase inhibition rate, the best whitening effect; the highest cell viability in the anti-UV experiment, and the best anti-aging effect. When the amount of retinol added is 0.1-0.5 parts by mass, it has excellent comprehensive performance, and the comprehensive performance of the prepared liposome is the best when 0.4 parts by mass is added.
[0120] Example 4
[0121] The present application provides a method for preparing A4-liposomes by using different amounts of bakuchiol (A), resveratrol (B) and retinol (C), which specifically includes:
[0122] S301: dissolving 4-8 parts of lipid in an organic solvent, adding bakuchiol (A), resveratrol (B) and retinol (C), ultrasonicating to obtain an emulsion, and removing the organic solvent by evaporation under reduced pressure to obtain phase A;
[0123] S302: Heat 2-16 parts of emulsifier, 1-10 parts of co-emulsifier, and 1-5 parts of stabilizer to 80° C., add into 100 parts of deionized water, stir and mix evenly, to obtain phase B;
[0124] S303: Add phase A to phase B, homogenize at a speed of 10000 rpm for 10 min, homogenize 3 times at 80°C and a pressure of 100 MPa, stir for 0.5-1 h, add a pH adjuster to adjust the pH value to 6.5-7, and obtain A4-liposomes.
[0125] According to the above test process, the A4-liposome was subjected to corresponding performance tests, and the test results are shown in Table 4:
[0126] Table 4 Test results of different amounts of bakuchiol (A), resveratrol (B) and retinol (C)
[0127]
[0128] According to Table 4, Fig.13 , Fig.14 , Fig.15 and Fig.16 The test results show that when the amount of bakuchiol added is 4 parts by mass, the amount of resveratrol added is 0.7 parts by mass, and the amount of retinol added is 0.4 parts by mass, the prepared liposomes have the smallest particle size and good stability; the level of cell inflammatory factors is the lowest, and the anti-inflammatory effect is the best; the tyrosinase inhibition rate is the highest, and the whitening effect is the best; the cell viability in the anti-UV experiment is the highest, and the anti-aging effect is the best. When the amount of bakuchiol added is 4 parts by mass, the amount of resveratrol added is 0.7 parts by mass, and the amount of retinol added is 0.4 parts by mass, the comprehensive performance of the prepared liposomes is the best.
[0129] The various embodiments in this specification are described in a progressive manner, and the same or similar parts between the various embodiments can be referenced to each other, and each embodiment focuses on the differences from other embodiments.
[0130] The above embodiments are only used to illustrate the technical solutions of the present application, rather than to limit the present application. Although the present application has been described in detail with reference to the aforementioned embodiments, a person of ordinary skill in the art should understand that the technical solutions recorded in the aforementioned embodiments may still be modified, or some or all of the technical features therein may be replaced by equivalents. However, these modifications or replacements do not cause the essence of the corresponding technical solutions to deviate from the scope of the technical solutions of the present application.
Claims
1. A method for preparing bakuchiol liposomes with whitening and anti-aging effects, It is characterized in that The method comprises: Dissolve 1-5 parts by weight of bakuchiol, 0.1-1 parts by weight of resveratrol, 0.1-0.5 parts by weight of retinol, and lipid in an organic solvent to obtain phase A; Dissolve the emulsifier, co-emulsifier and stabilizer in water to obtain phase B; After the phase A and the phase B are subjected to high pressure homogenization treatment, the pH is adjusted to obtain the bakuchiol liposome.
2. The method for preparing bakuchiol liposomes with whitening and anti-aging effects according to claim 1, It is characterized in that The method comprises: Dissolve 2-4 parts by weight of bakuchiol, 0.2-0.7 parts by weight of resveratrol, 0.2-0.4 parts by weight of retinol, and lipid in an organic solvent to obtain phase A; Dissolve the emulsifier, co-emulsifier and stabilizer in water to obtain phase B; After the phase A and the phase B are subjected to high pressure homogenization treatment, the pH is adjusted to obtain the bakuchiol liposome.
3. The method for preparing bakuchiol liposomes with whitening and anti-aging effects according to claim 1, It is characterized in that The method comprises: Dissolve 4 parts by mass of bakuchiol, 0.7 parts by mass of resveratrol, 0.4 parts by mass of retinol, and lipid in an organic solvent to obtain phase A; Dissolve the emulsifier, co-emulsifier and stabilizer in water to obtain phase B; After the phase A and the phase B are subjected to high pressure homogenization treatment, the pH is adjusted to obtain the bakuchiol liposome.
4. The method for preparing bakuchiol liposomes with whitening and anti-aging effects according to claim 1, It is characterized in that The lipid is one or more of lecithin, caprylic / capric triglyceride, monostearate glyceryl, butyloctanol salicylate, and acetylated monoglyceride; And / or, the lipid is added in an amount of 4-8 parts by mass.
5. The method for preparing bakuchiol liposomes with whitening and anti-aging effects according to claim 1, It is characterized in that The emulsifier is one or more of polyglyceryl 10 stearate, PEG-8 caprylic / capric glyceride, sucrose stearate, cetearyl olivate, sorbitan olivate, laureth-23, PEG-4 olivate, steareth-21, palmityl alcohol, PEG-75 stearate, glyceryl stearate, steareth-20, cetyl alcohol, cetyl alcohol ether-20, and steareth-20; And / or, the emulsifier is added in an amount of 2-16 parts by weight.
6. The method for preparing bakuchiol liposomes with whitening and anti-aging effects according to claim 1, It is characterized in that The stabilizer is one or more of 1,3-butylene glycol, hydrogenated olive oil, olive oil, unsaponifiable matter of olive oil, cetyl palmitate, sorbitan palmitate, and sorbitan olivate; And / or, the stabilizer is added in an amount of 1-5 parts by weight.
7. The method for preparing bakuchiol liposomes with whitening and anti-aging effects according to claim 1, It is characterized in that When 1-5 parts by weight of bakuchiol, 0.1-1 parts by weight of resveratrol, 0.1-0.5 parts by weight of retinol, and lipid are dissolved in an organic solvent, the reaction temperature is 40-50° C., and the reaction time is 0.5-2 hours.
8. The method for preparing bakuchiol liposomes with whitening and anti-aging effects according to claim 1, It is characterized in that The conditions of the high-pressure homogenization treatment are: pressure of 90-120 MPa, and the number of cycles is 2-3 times; And / or, the pH is adjusted to 6.5-7.
0.
9. A bakuchiol liposome with whitening and anti-aging effects prepared according to the preparation method according to any one of claims 1 to 8.
10. Use of the bakuchiol liposome with whitening and anti-aging effects according to claim 9 in the preparation of skin care products.
Citation Information
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