Whitening liposome wrapping whitening component as well as preparation method and application of whitening liposome

Abstract

The invention discloses a whitening liposome wrapping whitening components and a preparation method and application thereof, and belongs to the technical field of cosmetics. The whitening component is a whitening composition composed of a achillea millefolium extract, an olive leaf extract and a pyracantha fortuneana fruit extract. According to the whitening composition provided by the invention, all the raw materials are reasonably compounded and have a synergistic effect, so that an excellent whitening effect is obtained, the whitening liposome provided by the invention contains the whitening composition, resveratrol, tetrahydrocurcumin, glabridin, ascorbyl tetraisopalmitate, nicotinamide and the like, and the raw materials have a synergistic effect, so that the whitening effect is good. Under the conditions of specific pressure and homogenization time, the whitening liposome with the particle size of 90-400 nm is formed, and the whitening liposome with the particle size has excellent permeability and whitening effect.

Description

Technical Field

[0001] The present application relates to the technical field of cosmetics, and in particular to a whitening liposome encapsulating whitening ingredients, and a preparation method and application thereof. Background Art

[0002] Although the whitening products currently on the market have significant effects, they often have shortcomings such as chemical ingredient safety issues, stability and transdermal absorption issues, and limited effects of single ingredients. In contrast, plant extracts are increasingly favored by the market and consumers due to their natural origin, wide range of pharmacological activities, safety and mildness. Plant extracts can not only provide more comprehensive and mild beauty and skin care effects, but also meet the needs of modern consumers for natural and organic products. Their multi-effects also make them more attractive in whitening compositions, making them an ideal choice in the field of whitening skin care.

[0003] As a common drug delivery system, liposomes are widely used in the fields of biomedicine and cosmetics. Liposomes can improve the stability and skin permeability of active ingredients, enhance the effect of surfactants, achieve long-term sustained release, and have targeted properties, which can more effectively deliver nutrients to the deep layers of the skin. In addition, liposomes can nourish the skin, keep it moisturized, resist oxidation, and reduce the deposition of excess fat and toxins on the skin, thereby providing a more efficient, safe and comfortable skin care experience. In the process of liposome preparation, different particle sizes often have a great impact on their effects. The smaller the particle size, the stronger the penetration effect, and the particle size of common cosmetic liposomes is above the micron level.

[0004] Therefore, it is necessary to provide a whitening liposome using plant extracts as whitening ingredients, and then using liposome preparation technology to prepare it into nano-scale particle size to meet market demand. Summary of the invention

[0005] The purpose of the present invention is to provide a whitening liposome encapsulating a whitening component and a preparation method and application thereof. The whitening component is prepared using plant extracts as raw materials, has high safety and has excellent whitening effect.

[0006] In order to achieve the above object, the present invention adopts the following technical solutions:

[0007] In a first aspect, the present invention provides a whitening composition comprising the following components: yarrow extract, olive leaf extract, and pyracantha fruit extract.

[0008] Preferably, the whitening composition consists of the following components in parts by weight:

[0009] 5-7 parts of yarrow extract, 8-15 parts of olive leaf extract, and 2-5 parts of pyracantha fruit extract.

[0010] Most preferably, the whitening composition consists of the following components in parts by weight:

[0011] 6 parts of yarrow extract, 12 parts of olive leaf extract, and 4 parts of pyracantha fruit extract.

[0012] In a second aspect, the present invention provides a whitening liposome containing a whitening composition, wherein the whitening composition is the whitening composition described in the first aspect, and a preparation method thereof comprises the following steps:

[0013] (1) mixing the whitening composition with deionized water to obtain an aqueous phase;

[0014] (2) dissolving tocopherol, tocopherol acetate, phosphatidylcholine, and cholesterol in butanediol, dissolving by ultrasonication, and then transferring to a rotary evaporator to evaporate butanediol to obtain an oil phase;

[0015] (3) mixing the water phase and the oil phase and stirring them evenly to obtain a pre-emulsion;

[0016] (4) homogenizing the pre-emulsion using a microfluidizer to obtain whitening liposomes;

[0017] The mass ratio of the whitening composition to deionized water is 1:(20-60); the mass ratio of tocopherol, tocopherol acetate, phosphatidylcholine, cholesterol, and butanediol is 1:(0.5-1.2):(0.7-1):(0.7-1):(40-60); the volume ratio of the water phase to the oil phase is 1:(0.9-1.3);

[0018] The homogenization pressure of the microfluidizer in the homogenization process is 50-150 MPa;

[0019] The homogenization time of the microfluidizer in the homogenization process is 30-90 minutes.

[0020] Preferably, a method for preparing whitening liposomes containing a whitening composition comprises the following steps:

[0021] (1) mixing the whitening composition with deionized water to obtain an aqueous phase;

[0022] (2) dissolving tocopherol, tocopherol acetate, phosphatidylcholine, cholesterol, resveratrol, tetrahydrocurcumin, glabridin, ascorbyl tetraisopalmitate, and ascorbyl palmitate in butanediol, dissolving by ultrasonication, and then transferring to a rotary evaporator to evaporate butanediol to obtain an oil phase;

[0023] (3) mixing the water phase and the oil phase and stirring them evenly to obtain a pre-emulsion;

[0024] (4) homogenizing the pre-emulsion using a microfluidizer to obtain whitening liposomes;

[0025] The mass ratio of the whitening composition to deionized water is 1:(20-60); the mass ratio of tocopherol, tocopherol acetate, phosphatidylcholine, cholesterol, resveratrol, tetrahydrocurcumin, glabridin, ascorbyl tetraisopalmitate, ascorbyl palmitate, and butanediol is 1:(0.5-1.2):(0.7-1):(0.7-1):(0.1-0.3):(0.1-0.3):(0.2-0.4):(0.5-0.7):(0.3-0.6):(40-60); the volume ratio of the water phase to the oil phase is 1:0.9-1.3.

[0026] In a third aspect, the present invention provides an application of a whitening liposome in preparing cosmetics with whitening effect, wherein the whitening liposome is the whitening liposome described in the second aspect.

[0027] Compared with the prior art, the present invention has the following beneficial effects: the present invention provides a whitening liposome encapsulating a whitening component, wherein the whitening component is a whitening composition compounded from yarrow extract, olive leaf extract, and Pyracantha fortuneana fruit extract, wherein the biphenyl glycoside compounds and dibenzofuran compounds contained in the Pyracantha fortuneana fruit have a significant effect of inhibiting tyrosinase; the olive leaf extract contains oleuropein and hydroxytyrosol which can reduce inflammation and indirectly affect the activity of tyrosinase; the yarrow extract can inhibit the formation of melanin by reducing the activation of tyrosine by free radicals, and studies have found that when the yarrow extract, olive leaf extract, and Pyracantha fortuneana fruit extract are used together, there is a synergistic effect, so that the whitening composition can significantly inhibit the activity of tyrosinase, thereby obtaining an excellent whitening effect. DETAILED DESCRIPTION

[0028] In order to better understand the present invention, the present invention is further described below in conjunction with a specific composition, wherein the terms used in the composition are for describing specific embodiments and do not constitute limitations on the scope of protection of the present invention.

[0029] The experimental methods in the following examples without specifying specific conditions are usually carried out under conventional conditions or conditions recommended by the manufacturer. Unless otherwise specified, the calculation is based on mass percentage and mass fraction.

[0030] Some raw materials and their sources are as follows:

[0031] The yarrow extract was purchased from BASF AG, item number: A00112;

[0032] The olive leaf extract was purchased from Shanghai Jiakai Biological Co., Ltd.

[0033] The Pyracantha fortuneana fruit extract was purchased from BASF SE, product number BC10170;

[0034] The microfluidizer is a Microfluidizer.

[0035] The components and weight proportions of the whitening composition are shown in Table 1 below.

[0036] Table 1 Components and mass ratios of whitening composition

[0037]

[0038]

[0039] The preparation methods of the above compositions 1-3 and compositions ①-⑨ are as follows:

[0040] The components of the whitening composition are placed in an emulsifying pot and homogenized for 0.5 h to obtain the whitening composition.

[0041] Test 1: Tyrosinase inhibition test

[0042] The tyrosinase inhibition test was used to verify the inhibitory ability of compositions 1-3 and compositions ①-⑨ on tyrosinase.

[0043] Tyrosinase is a key enzyme in the synthesis of melanin. Inhibiting its activity can effectively reduce the synthesis of melanin and play a whitening role.

[0044] The test method refers to T / GDCA 006-2021 "Guangdong Cosmetics Association Group Standard-Test Method for Tyrosinase Activity Inhibition of Cosmetic Raw Materials (In Vitro Method)".

[0045] Test samples: Compositions 1-3, compositions ①-⑨, each composition was diluted with PBS buffer to a sample solution with a concentration of 4 wt%.

[0046] Positive samples: Dilute kojic acid with PBS buffer to a kojic acid solution with a mass concentration of 0.005 g / L.

[0047] The tyrosinase inhibition rate was calculated with the inhibition rate of positive samples as 100%.

[0048] Table 2 Tyrosinase inhibition rate

[0049] sample Inhibition rate % ± SD% Composition 1 93.57±0.42 Composition 2 91.42±0.71 Composition 3 90.33±0.33 Composition ① 27.55±0.57 Composition ② 31.64±0.41 Composition ③ 25.41±0.36 Composition ④ 60.55±0.74 Composition ⑤ 54.36±0.93 Composition ⑥ 60.57±0.88 Composition ⑦ 83.24±0.37 Composition⑧ 79.36±0.26 Composition ⑨ 81.51±0.51 Positive samples 100

[0050] According to the results of compositions 1-3 in Table 2, the whitening composition provided by the present invention can effectively inhibit the activity of tyrosinase, thereby inhibiting the formation of melanin, and thus has the effect of whitening the skin. In particular, composition 1 has a good tyrosinase inhibitory effect.

[0051] Comparing the results of composition 1 with compositions ①-⑨, it can be seen that the components in the whitening composition provided by the present invention have a synergistic effect when used in combination according to a certain dosage ratio.

[0052] The preparation method of whitening liposome is as follows:

[0053] Whitening liposome 1:

[0054] (1) mixing a whitening composition (composition 1) with deionized water to obtain an aqueous phase;

[0055] (2) dissolving tocopherol, tocopherol acetate, phosphatidylcholine, and cholesterol in butanediol, dissolving by ultrasonication, and then transferring to a rotary evaporator to evaporate butanediol to obtain an oil phase;

[0056] (3) mixing the water phase and the oil phase and stirring them evenly to obtain a pre-emulsion;

[0057] (4) homogenizing the pre-emulsion using a microfluidizer to obtain whitening liposomes;

[0058] The mass ratio of the whitening composition to deionized water is 1:40; the mass ratio of tocopherol, tocopherol acetate, phosphatidylcholine, cholesterol, and butanediol is 1:0.8:0.9:0.8:50; the volume ratio of the water phase to the oil phase is 1:1.1;

[0059] The homogenizing pressure of the microfluidizer during the homogenization process is 100 MPa;

[0060] The homogenization time of the microfluidizer in the homogenization process is 60 minutes.

[0061] Whitening Liposome 2:

[0062] (1) mixing a whitening composition (composition 1) with deionized water to obtain an aqueous phase;

[0063] (2) dissolving tocopherol, tocopherol acetate, phosphatidylcholine, and cholesterol in butanediol, dissolving by ultrasonication, and then transferring to a rotary evaporator to evaporate butanediol to obtain an oil phase;

[0064] (3) mixing the water phase and the oil phase and stirring them evenly to obtain a pre-emulsion;

[0065] (4) homogenizing the pre-emulsion using a microfluidizer to obtain whitening liposomes;

[0066] The mass ratio of the whitening composition to deionized water is 1:20; the mass ratio of tocopherol, tocopherol acetate, phosphatidylcholine, cholesterol, and butanediol is 1:0.5:0.7:1:40; the volume ratio of the water phase to the oil phase is 1:0.9;

[0067] The homogenization pressure of the microfluidizer in the homogenization process is 50 MPa;

[0068] The homogenization time of the microfluidizer in the homogenization process is 90 minutes.

[0069] Whitening Liposome 3:

[0070] (1) mixing a whitening composition (composition 1) with deionized water to obtain an aqueous phase;

[0071] (2) dissolving tocopherol, tocopherol acetate, phosphatidylcholine, and cholesterol in butanediol, dissolving by ultrasonication, and then transferring to a rotary evaporator to evaporate butanediol to obtain an oil phase;

[0072] (3) mixing the water phase and the oil phase and stirring them evenly to obtain a pre-emulsion;

[0073] (4) homogenizing the pre-emulsion using a microfluidizer to obtain whitening liposomes;

[0074] The mass ratio of the whitening composition to deionized water is 1:60; the mass ratio of tocopherol, tocopherol acetate, phosphatidylcholine, cholesterol, and butanediol is 1:1.2:1:0.7:60; the volume ratio of the water phase to the oil phase is 1:1.3;

[0075] The homogenization pressure of the microfluidizer in the homogenization process is 150 MPa;

[0076] The homogenization time of the microfluidizer in the homogenization process is 30 minutes.

[0077] Whitening Liposome 4:

[0078] (1) mixing a whitening composition (composition 1) with deionized water to obtain an aqueous phase;

[0079] (2) dissolving tocopherol, tocopherol acetate, phosphatidylcholine, cholesterol, resveratrol, tetrahydrocurcumin, glabridin, ascorbyl tetraisopalmitate, and ascorbyl palmitate in butanediol, dissolving by ultrasonication, and then transferring to a rotary evaporator to evaporate butanediol to obtain an oil phase;

[0080] (3) mixing the water phase and the oil phase and stirring them evenly to obtain a pre-emulsion;

[0081] (4) homogenizing the pre-emulsion using a microfluidizer to obtain whitening liposomes;

[0082] The mass ratio of the whitening composition to deionized water is 1:40; the mass ratio of tocopherol, tocopherol acetate, phosphatidylcholine, cholesterol, resveratrol, tetrahydrocurcumin, glabridin, ascorbyl tetraisopalmitate, ascorbyl palmitate, and butanediol is 1:0.8:0.9:0.8:0.2:0.2:0.3:0.6:0.5:50; the volume ratio of the water phase to the oil phase is 1:1.1;

[0083] The homogenizing pressure of the microfluidizer during the homogenization process is 100 MPa;

[0084] The homogenization time of the microfluidizer in the homogenization process is 60 minutes.

[0085] Whitening Liposome 5

[0086] (1) mixing a whitening composition (composition 1) with deionized water to obtain an aqueous phase;

[0087] (2) dissolving tocopherol, tocopherol acetate, phosphatidylcholine, cholesterol, resveratrol, tetrahydrocurcumin, glabridin, ascorbyl tetraisopalmitate, and ascorbyl palmitate in butanediol, dissolving by ultrasonication, and then transferring to a rotary evaporator to evaporate butanediol to obtain an oil phase;

[0088] (3) mixing the water phase and the oil phase and stirring them evenly to obtain a pre-emulsion;

[0089] (4) homogenizing the pre-emulsion using a microfluidizer to obtain whitening liposomes;

[0090] The mass ratio of the whitening composition to deionized water is 1:40; the mass ratio of tocopherol, tocopherol acetate, phosphatidylcholine, cholesterol, resveratrol, tetrahydrocurcumin, glabridin, ascorbyl tetraisopalmitate, ascorbyl palmitate, and butanediol is 1:0.8:0.9:0.8:0.1:0.3:0.2:0.5:0.6:50; the volume ratio of the water phase to the oil phase is 1:1.1;

[0091] The homogenizing pressure of the microfluidizer during the homogenization process is 100 MPa;

[0092] The homogenization time of the microfluidizer in the homogenization process is 60 minutes.

[0093] Whitening Liposome 6

[0094] (1) mixing a whitening composition (composition 1) with deionized water to obtain an aqueous phase;

[0095] (2) dissolving tocopherol, tocopherol acetate, phosphatidylcholine, cholesterol, resveratrol, tetrahydrocurcumin, glabridin, ascorbyl tetraisopalmitate, and ascorbyl palmitate in butanediol, dissolving by ultrasonication, and then transferring to a rotary evaporator to evaporate butanediol to obtain an oil phase;

[0096] (3) mixing the water phase and the oil phase and stirring them evenly to obtain a pre-emulsion;

[0097] (4) homogenizing the pre-emulsion using a microfluidizer to obtain whitening liposomes;

[0098] The mass ratio of the whitening composition to deionized water is 1:40; the mass ratio of tocopherol, tocopherol acetate, phosphatidylcholine, cholesterol, resveratrol, tetrahydrocurcumin, glabridin, ascorbyl tetraisopalmitate, ascorbyl palmitate, and butanediol is 1:0.8:0.9:0.8:0.3:0.1:0.4:0.7:0.3:50; the volume ratio of the water phase to the oil phase is 1:1.1;

[0099] The homogenizing pressure of the microfluidizer during the homogenization process is 100 MPa;

[0100] The homogenization time of the microfluidizer in the homogenization process is 60 minutes.

[0101] Test 2: Patch test

[0102] The present invention experiments verify the biological safety of whitening liposomes 1-6.

[0103] Sample: Whitening liposomes and deionized water are prepared into a whitening liposome deionized water solution, wherein the final concentration of the whitening liposomes is 3wt%.

[0104] The 2015 "Technical Specifications for Safety of Cosmetics" was used as a reference standard for the irritation evaluation of cosmetics. The test method was a skin patch test, and 60 people aged 16-65 years were randomly distributed and tested.

[0105] Test method: Put the test substance into the patch tester, the dosage is 0.020-0.025g, cover the patch tester with the test substance on the back or forearm of the subject with non-irritating cloth-based tape, and gently press it with the palm to make it evenly adhere to the skin surface for 24 hours. After removing the test patch tester, observe the skin reaction after the indentation disappears 30 minutes later. If the result is negative, observe again 24 hours and 48 hours after the patch test.

[0106] Evaluation criteria:

[0107] Grade 0: negative reaction;

[0108] Grade 1: Suspicious reaction, only slight erythema;

[0109] Grade 2: weak positive reaction, erythema, infiltration, edema, and papules may be present;

[0110] Grade 3: Strong positive reaction, erythema, infiltration, edema, papules, and the reaction may extend beyond the test area;

[0111] Grade 4: Very strong positive reaction, obvious erythema, severe infiltration, edema, confluent herpes, and the reaction exceeds the test area.

[0112] Test results: Skin reactions were negative in all subjects.

[0113] Test 3: Particle size analysis

[0114] The particle size of the whitening liposomes was analyzed using a nanoparticle size analyzer (Zeta potential and particle size analyzer, OFAMEGA);

[0115] Analytical samples Whitening Liposomes 1-6;

[0116] For detailed analysis of the data, see Table 3.

[0117] Table 3 Particle size analysis

[0118] Experimental Group 95% particle size range Whitening Liposome 1 100-150nm Whitening Liposome 2 200-400nm Whitening Liposome 3 90-300mn Whitening Liposome 4 100-150nm Whitening Liposome 5 110-160nm Whitening Liposome 6 90-150nm

[0119] It can be seen from the data in Table 3 that the liposomes prepared by the whitening liposomes 1-6 of the present invention are all in the range of 90-400nm. Comparing the particle size ranges of whitening liposomes 1 and 4-6, it can be seen that the particle size ranges of the whitening liposomes obtained under the same homogenization time and homogenization pressure conditions are not much different; comparing the results of whitening liposomes 1-3, it can be seen that the particle size range distribution of whitening liposome 1 is more concentrated and the stability is higher.

[0120] The embodiments described above are part of the embodiments of the present application, rather than all of the embodiments. The detailed description of the embodiments of the present application is not intended to limit the scope of the present application for protection, but merely represents the selected embodiments of the present application. Based on the embodiments in the present application, all other embodiments obtained by those skilled in the art without making creative work are within the scope of protection of the present application.

Claims

1. A whitening composition, characterized in that: It is composed of the following components by mass: 5-7 parts of Yarrow extract; 8-15 parts of olive leaf extract; 2-5 parts of Pyracantha fortuneana fruit extract.

2. The whitening composition according to claim 1, characterized in that It is composed of the following components by mass: Yarrow extract 6 parts; Olive leaf extract 12 parts; 4 parts of Pyracantha fortuneana fruit extract.

3. Use of the whitening composition as claimed in claim 1 or 2 in the preparation of whitening liposomes.

4. The method for preparing whitening liposomes according to claim 3, characterized in that: The following steps are involved: (1) mixing the whitening composition with deionized water to obtain an aqueous phase; (2) dissolving tocopherol, tocopherol acetate, phosphatidylcholine, and cholesterol in butanediol, dissolving by ultrasonication, and then transferring to a rotary evaporator to evaporate butanediol to obtain an oil phase; (3) mixing the water phase and the oil phase and stirring them evenly to obtain a pre-emulsion; (4) homogenizing the pre-emulsion using a microfluidizer to obtain whitening liposomes; The mass ratio of the whitening composition to deionized water is 1:(20-60); the mass ratio of tocopherol, tocopherol acetate, phosphatidylcholine, cholesterol, and butanediol is 1:(0.5-1.2):(0.7-1):(0.7-1):(40-60); the volume ratio of the water phase to the oil phase is 1:(0.9-1.3); The homogenization pressure of the microfluidizer in the homogenization process is 50-150 MPa; The homogenization time of the microfluidizer in the homogenization process is 30-90 minutes.

5. The preparation method according to claim 4, characterized in that: The microfluidizer is a Microfluidizer.

6. The preparation method according to claim 4, characterized in that: The oil phase also includes resveratrol, tetrahydrocurcumin, glabridin, ascorbyl tetraisopalmitate, and ascorbyl palmitate. The mass ratio of resveratrol, tetrahydrocurcumin, glabridin, ascorbyl tetraisopalmitate, and ascorbyl palmitate to tocopherol is (0.1-0.3): (0.1-0.3): (0.2-0.4): (0.5-0.7): (0.3-0.6):

1.

7. Use of the whitening liposome according to any one of claims 4 to 6 in preparing cosmetics with whitening effect, characterized in that: The cosmetic is an aqueous solution, an emulsion, a cream, an ointment or a facial mask.

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