High-permeability multi-channel whitening composition modified by polyquaternium-51 and preparation method of high-permeability multi-channel whitening composition

Abstract

The invention provides a polyquaternium-51 modified high-permeability multi-channel whitening composition, which is prepared from the following raw materials in percentage by mass: 0.001 to 2 percent of tetrahydrocurcumin, 1 to 5 percent of phospholipid, 0.001 to 1 percent of resveratrol, 0.1 to 5 percent of ascorbyl tetraisopalmitate, 0.25 to 5 percent of polysorbate-80, 0.001 to 1 percent of tocopherol, 2 to 10 percent of caprylic / capric triglyceride, 0.001 to 0.1 percent of polyquaternium-51 and the balance of water. The invention relates to an anti-rust agent, which is prepared from the following raw materials in percentage by mass: 30 to 45 percent of polyhydric alcohol, 2 to 10 percent of tranexamic acid, 0.001 to 3 percent of alpha-arbutin and the balance of deionized water, and the sum of the mass percent of all the raw materials is 100 percent. The invention also provides a preparation method of the high-permeability multi-channel whitening composition. The polyquaternium-51 modified high-permeability multi-channel whitening composition provided by the invention has a multi-channel whitening effect and relatively good stability and permeability.

Description

TECHNICAL FIELD

[0001] The present application relates to a whitening composition, in particular to a high penetration multi-channel whitening composition modified by polyquaternium-51 and a preparation method thereof. BACKGROUND

[0002] Skin pigmentation is regulated by more than 120 genes, mainly depending on the interaction of melanocytes in the basal layer of the epidermis and the cells adjacent to them, which jointly regulate the synthesis, transport and metabolism of melanin, involving the regulation of various cytokines and signals. Skin whitening usually involves the following aspects: 1. Protecting against ultraviolet rays; 2. Inhibiting melanin synthesis, including inhibiting the activity of tyrosinase and a-melanocyte stimulating hormone (a-mSh) receptor inhibitors; 3. Reducing the synthesized melanin; 4. Preventing the transport of melanin to keratinocytes; 5. Accelerating the exfoliation of melanin; 6. Promoting melanin metabolism.

[0003] Current whitening cosmetics generally have the following problems: single whitening pathway, gaps in the mechanism of action, resulting in less obvious whitening effect; whitening ingredients are unstable and prone to discoloration and decomposition in light and high temperature environments; at the same time, due to the barrier function of the skin, the transdermal penetration ability of whitening raw materials is weak. In order to improve the stability, transdermal penetration, etc. of the active substances of whitening cosmetics, nanocarrier technology can be used to encapsulate the active substances of cosmetics, such as liposomes, ethosomes, microemulsions and nanoemulsions, etc. However, the liposomes and ethosomes in the prior art are prone to Ostwald ripening at high temperatures (≥45℃), so their high-temperature stability is poor. In addition, the skin surface is usually negatively charged, so positively charged substances are more easily absorbed by the skin. Therefore, cationic polymer modified nanocarriers can effectively inhibit the Ostwald ripening of liposomes at high temperatures (≥45℃), and better interact with the skin surface to improve the transdermal absorption efficiency.

[0004] Chinese invention patent with publication number CN118662393A discloses a high-stability, strong-penetration whitening nanocomposite and its preparation and application. The whitening nanocomposite is formed by cationic polymer encapsulating glutathione and a stabilizer. This patent belongs to a whitening nanocomposite modified by cationic polymer, but still has problems such as single whitening pathway, gaps in the mechanism of action, resulting in less obvious effect, etc. SUMMARY

[0005] The technical problem to be solved by the present application is to provide a high penetration multi-channel whitening composition modified by polyquaternium-51, which has a multi-channel whitening effect and good stability and permeability.

[0006] To solve the above technical problems, the technical scheme of the present application is as follows:

[0007] A polyquaternium-51 modified high permeability multi-channel whitening composition is made of the following raw materials in mass percentage: tetrahydrocurcumin 0.001-2%, phospholipid 1-5%, resveratrol 0.001-1%, ascorbic acid tetraisopalmitate 0.1-5%, polysorbate-80 0.25-5%, tocopherol 0.001-1%, caprylic / capric triglyceride 2-10%, polyquaternium-51 0.001-0.1%, polyhydric alcohol 30-45%, tranexamic acid 2-10%, alpha-arbutin 0.001-3%, and the balance is deionized water, the sum of the mass percentages of the raw materials is 100%.

[0008] Further, the polyhydric alcohol in the present application is one or more of sorbitol, glycerol, butanediol, 1,3-propanediol or propylene glycol.

[0009] Further, the phospholipid in the present application is soybean lecithin or egg yolk lecithin with phosphatidylcholine content ≥70wt%.

[0010] Further, the average particle size of the high permeability multi-channel whitening composition in the present application is 10-20nm.

[0011] Another technical problem to be solved by the present application is to provide a preparation method of the above-mentioned polyquaternium-51 modified high permeability multi-channel whitening composition.

[0012] To solve the above technical problems, the technical solution is:

[0013] A preparation method of a polyquaternium-51 modified high permeability multi-channel whitening composition, comprising the following steps:

[0014] S1. The raw materials are weighed according to the mass percentage, and tetrahydrocurcumin, phospholipid, resveratrol, ascorbic acid tetraisopalmitate, polysorbate-80, tocopherol and caprylic / capric triglyceride are mixed, stirred at 45-50℃ for 10-30min to obtain mixture A;

[0015] S2. Polyquaternium-51, polyhydric alcohol, tranexamic acid, alpha-arbutin and deionized water are mixed and stirred at 45-50℃ until evenly mixed to obtain mixture B;

[0016] S3. Mixture B obtained in step S2 is added to mixture A obtained in step S1 under heating at 45-50℃, and stirred until evenly mixed to obtain mixture C;

[0017] S4. Mixture C obtained in step S3 is homogenized 2-3 times, and cooled to room temperature to obtain the polyquaternium-51 modified high permeability multi-channel whitening composition.

[0018] Further, in step S1, the stirring speed is 600-800rpm.

[0019] Further, in the step S2, the stirring speed is 600-800 rpm.

[0020] Further, in the step S3, the stirring speed is 1300-1500 rpm.

[0021] Further, in the step S4, the pressure for homogenization is 20-25 MPa.

[0022] The high-permeability multi-path whitening composition prepared by the present application can be applied to creams, lotions, serums, water agents, facial cleansers, and the like.

[0023] Compared with the prior art, the present application has the following beneficial effects:

[0024] (1) The present application prepares a whitening composition with a polyquaternium-51 modified liposome structure by stirring, mixing, and homogenization of each raw material, wherein polyquaternium-51 is a cationic polymer that can be adsorbed on the surface of the liposome through electrostatic interaction and hydrogen bonding, enhancing the electrostatic repulsion between liposomes, preventing liposome aggregation, avoiding the increase in particle size due to the Ostwald ripening effect, and further wrapping the phospholipid molecules of the liposome to reduce the probability of contact with oxygen, thereby reducing the oxidation and decomposition rate of the liposome and improving the stability of the high-permeability multi-path whitening composition prepared by the present application.

[0025] (2) The skin surface is usually negatively charged, and positively charged substances are more easily absorbed by the skin, and the polyquaternium-51 modified high-permeability multi-path whitening composition prepared by the present application is positively charged, so it can better interact with the skin surface and has good transdermal permeability and absorption efficiency.

[0026] (3) The high-permeability multi-path whitening composition prepared by the present application has a multi-path whitening effect: resveratrol and tetrahydrocurcumin can prevent UV rays, inhibit the NF-κB inflammatory pathway, and reduce tanning; resveratrol and arbutin can inhibit the activity of tyrosinase and effectively reduce melanin; ascorbic acid tetraisopalmitate can reduce the synthesized melanin; and tranexamic acid can effectively promote melanin metabolism. BRIEF DESCRIPTION OF DRAWINGS

[0027] The accompanying drawings, which are included to provide a further understanding of the present application and constitute a part of this application, illustrate embodiments of the present application and together with the description serve to explain the principle of the present application, and do not constitute an improper limitation on the present application, and in the drawings:

[0028] Figure 1 Picture after 3-month accelerated stability test of Example 1, Figure 1The stability conditions from left to right are, in turn, light (4000lx), heat resistance 45℃, refrigeration 4℃, cold resistance-18℃, high-low temperature cycle, 18-25℃;

[0029] Figure 2 The picture of Example 1 after 3 months of accelerated stability test, Figure 2 The stability conditions from left to right are, in turn, light (4000lx), heat resistance 45℃, refrigeration 4℃, cold resistance-18℃, high-low temperature cycle, 18-25℃;

[0030] Figure 3 The fluorescence chart of Example 1 and Comparative Example 1 after transdermal 30min, Figure 3 The left is Comparative Example 1, and the right is Example 1. DETAILED DESCRIPTION

[0031] The present application will be described in detail below with specific examples and the accompanying drawings of the specification, which are used to explain the present application, but not as a limitation of the present application.

[0032] The raw materials used in the examples and comparative examples are all conventional commercially available raw materials unless otherwise specified, and the process methods used in the examples and comparative examples are all conventional methods in the art unless otherwise specified.

[0033] Example 1

[0034] The high-penetration multi-path whitening composition modified by polyquaternary ammonium salt-51 is made of the following raw materials in mass percentage: tetrahydrocurcumin 0.1%, soybean lecithin with phosphatidylcholine content of 75wt% 3%, resveratrol 1%, ascorbic acid tetraisopalmitate 2%, polysorbate-80 0.25%, tocopherol 0.05%, caprylic / capric triglyceride 8%, polyquaternary ammonium salt-51 0.05%, butanediol 20%, glycerol 10%, tranexamic acid 10%, alpha-arbutin 0.5%, and the balance is deionized water, the sum of the mass percentages of each raw material is 100%.

[0035] The preparation method of Example 1 includes the following steps:

[0036] S1. Weigh each raw material according to mass percentage, mix tetrahydrocurcumin, phospholipid, resveratrol, ascorbic acid tetraisopalmitate, polysorbate-80, tocopherol, caprylic / capric triglyceride, and stir at 48℃ and 700rpm for 20min to obtain mixture A;

[0037] S2. Mix polyquaternary ammonium salt-51, butanediol, glycerol, tranexamic acid, alpha-arbutin, and deionized water, and stir at 48℃ and 700rpm until mixed evenly to obtain mixture B;

[0038] S3. The mixture B obtained in step S2 was added into the mixture A obtained in step S1 under heating at 48℃, and stirred at 1400 rpm until mixed evenly to obtain mixture C;

[0039] S4. The mixture C obtained in step S3 was homogenized 3 times under 22 MPa pressure, and cooled to room temperature to obtain the polyquaternium-51 modified high penetration multi-channel whitening composition.

[0040] Example 2

[0041] The polyquaternium-51 modified high penetration multi-channel whitening composition was prepared from the following raw materials in mass percentage: tetrahydrocurcumin 0.05%, soybean lecithin with phosphatidylcholine content of 80wt% 5%, resveratrol 0.2%, ascorbic acid tetraisopalmitate 1%, polysorbate-80 0.5%, tocopherol 0.1%, caprylic / capric triglyceride 10%, polyquaternium-51 0.1%, butanediol 20%, 1,3-propanediol 20%, tranexamic acid 5%, a-arbutin 0.5%, and the balance was deionized water, the sum of the mass percentages of each raw material was 100%.

[0042] The preparation method of Example 2 includes the following steps:

[0043] S1. Each raw material was weighed according to mass percentage, and tetrahydrocurcumin, phospholipid, resveratrol, ascorbic acid tetraisopalmitate, polysorbate-80, tocopherol, and caprylic / capric triglyceride were mixed, and stirred at 45℃ and 800 rpm for 25 min to obtain mixture A;

[0044] S2. Polyquaternium-51, butanediol, glycerol, tranexamic acid, a-arbutin, and deionized water were mixed, and stirred at 45℃ and 800 rpm until mixed evenly to obtain mixture B;

[0045] S3. The mixture B obtained in step S2 was added into the mixture A obtained in step S1 under heating at 45℃, and stirred at 1500 rpm until mixed evenly to obtain mixture C;

[0046] S4. The mixture C obtained in step S3 was homogenized 2 times under 24 MPa pressure, and cooled to room temperature to obtain the polyquaternium-51 modified high penetration multi-channel whitening composition.

[0047] Example 3

[0048] A polyquaternium-51 modified high permeability multi-channel whitening composition is made from the following raw materials in mass percentage: tetrahydrocurcumin 2%, soybean lecithin with phosphatidylcholine content of 85wt% 3%, resveratrol 0.1%, ascorbic acid tetraisopalmitate 5%, polysorbate-80 4%, tocopherol 0.5%, caprylic / capric triglyceride 8%, polyquaternium-51 0.1%, glycerin 15%, 1,3-propanediol 20%, tranexamic acid 3%, alpha-arbutin 3%, and the balance is deionized water, the sum of the mass percentages of each raw material is 100%.

[0049] The preparation method of Example 3 includes the following steps:

[0050] S1. Weigh each raw material according to mass percentage, mix tetrahydrocurcumin, phospholipid, resveratrol, ascorbic acid tetraisopalmitate, polysorbate-80, tocopherol, caprylic / capric triglyceride, stir at 50℃ and 600rpm for 10min to obtain mixture A;

[0051] S2. Mix polyquaternium-51, butanediol, glycerin, tranexamic acid, alpha-arbutin, and deionized water, stir at 50℃ and 600rpm until mixed evenly to obtain mixture B;

[0052] S3. Add mixture B obtained in step S2 to mixture A obtained in step S1 under heating at 50℃, stir at 1300rpm until mixed evenly to obtain mixture C;

[0053] S4. Homogenize mixture C obtained in step S3 under 25MPa pressure for 2 times, cool to room temperature to obtain a polyquaternium-51 modified high permeability multi-channel whitening composition.

[0054] Example 4

[0055] A polyquaternium-51 modified high permeability multi-channel whitening composition is made from the following raw materials in mass percentage: tetrahydrocurcumin 0.001%, soybean lecithin with phosphatidylcholine content of 90wt% 4%, resveratrol 0.001%, ascorbic acid tetraisopalmitate 2%, polysorbate-80 0.25%, tocopherol 0.01%, caprylic / capric triglyceride 10%, polyquaternium-51 0.1%, sorbitol 25%, propylene glycol 20%, tranexamic acid 2%, alpha-arbutin 0.005%, and the balance is deionized water, the sum of the mass percentages of each raw material is 100%.

[0056] The preparation method of Example 4 includes the following steps:

[0057] S1. Weigh each raw material according to the mass percentage, mix tetrahydrocurcumin, phospholipid, resveratrol, ascorbic acid tetraisopalmitate, polysorbate-80, tocopherol, caprylic / capric acid triglyceride, stir at 46℃ and 700rpm for 30min to obtain mixture A;

[0058] S2. Mix polyquaternium-51, butanediol, glycerol, tranexamic acid, alpha-arbutin, deionized water, stir at 46℃ and 700rpm until mixed evenly to obtain mixture B;

[0059] S3. Add mixture B obtained in step S2 to mixture A obtained in step S1 under heating at 46℃, stir at 1400rpm until mixed evenly to obtain mixture C;

[0060] S4. Homogenize mixture C obtained in step S3 under 20MPa pressure for 3 times, cool to room temperature to obtain polyquaternium-51 modified high permeability multi-channel whitening composition.

[0061] Example 5

[0062] The polyquaternium-51 modified high permeability multi-channel whitening composition is made of the following mass percentage of raw materials: tetrahydrocurcumin 0.1%, egg lecithin with phosphatidylcholine content of 70wt% 4%, resveratrol 0.1%, ascorbic acid tetraisopalmitate 2%, polysorbate-80 5%, tocopherol 0.05%, caprylic / capric acid triglyceride 6%, polyquaternium-51 0.1%, 1,3-propanediol 25%, propylene glycol 20%, tranexamic acid 2%, alpha-arbutin 0.001%, and the balance is deionized water, the sum of the mass percentages of each raw material is 100%.

[0063] The preparation method of example 5 includes the following steps:

[0064] S1. Weigh each raw material according to the mass percentage, mix tetrahydrocurcumin, phospholipid, resveratrol, ascorbic acid tetraisopalmitate, polysorbate-80, tocopherol, caprylic / capric acid triglyceride, stir at 45℃ and 700rpm for 15min to obtain mixture A;

[0065] S2. Mix polyquaternium-51, butanediol, glycerol, tranexamic acid, alpha-arbutin, deionized water, stir at 45℃ and 700rpm until mixed evenly to obtain mixture B;

[0066] S3. Add mixture B obtained in step S2 to mixture A obtained in step S1 under heating at 45℃, stir at 1500rpm until mixed evenly to obtain mixture C;

[0067] S4. Homogenize the mixture C obtained in step S3 for 3 times under 21 MPa pressure, and obtain the polyquaternium-51 modified high-permeability multi-channel whitening composition after cooling to room temperature.

[0068] Example 6

[0069] The polyquaternium-51 modified high-permeability multi-channel whitening composition is prepared from the following raw materials in mass percentage: tetrahydrocurcumin 0.5%, soybean lecithin with phosphatidylcholine content of 70 wt% 4%, resveratrol 0.1%, ascorbic acid tetraisopalmitate 0.1%, polysorbate-80 0.5%, tocopherol 1%, caprylic / capric triglyceride 2%, polyquaternium-51 0.001%, glycerol 15%, propylene glycol 15%, tranexamic acid 6%, a-arbutin 0.005%, and the balance is deionized water, the sum of the mass percentages of each raw material is 100%.

[0070] The preparation method of Example 6 comprises the following steps:

[0071] S1. Weigh each raw material according to mass percentage, mix tetrahydrocurcumin, phospholipid, resveratrol, ascorbic acid tetraisopalmitate, polysorbate-80, tocopherol, and caprylic / capric triglyceride, and stir at 48°C and 600 rpm for 25 min to obtain mixture A;

[0072] S2. Mix polyquaternium-51, butanediol, glycerol, tranexamic acid, a-arbutin, and deionized water, and stir at 48°C and 600 rpm until well mixed to obtain mixture B;

[0073] S3. Add mixture B obtained in step S2 to mixture A obtained in step S1 under heating at 48°C, and stir at 1500 rpm until well mixed to obtain mixture C;

[0074] S4. Homogenize mixture C obtained in step S3 for 3 times under 20 MPa pressure, and obtain the polyquaternium-51 modified high-permeability multi-channel whitening composition after cooling to room temperature.

[0075] Example 7

[0076] The polyquaternium-51 modified high-permeability multi-channel whitening composition is prepared from the following raw materials in mass percentage: tetrahydrocurcumin 0.6%, soybean lecithin with phosphatidylcholine content of 75 wt% 1%, resveratrol 0.4%, ascorbic acid tetraisopalmitate 1.5%, polysorbate-80 1.5%, tocopherol 0.06%, caprylic / capric triglyceride 7%, polyquaternium-51 0.1%, butanediol 15%, propylene glycol 20%, tranexamic acid 3%, a-arbutin 0.1%, and the balance is deionized water, the sum of the mass percentages of each raw material is 100%.

[0077] The preparation method of Example 7 comprises the following steps:

[0078] S1. According to the mass percentage, each raw material was weighed, tetrahydrocurcumin, phospholipid, resveratrol, ascorbic acid tetraisopalmitate, polysorbate-80, tocopherol, caprylic / capric acid triglyceride were mixed, stirred at 50℃ and 700rpm for 15min to obtain mixture A;

[0079] S2. Polyquaternium-51, butanediol, glycerol, tranexamic acid, alpha-arbutin, deionized water were mixed, stirred at 50℃ and 700rpm until mixed uniformly to obtain mixture B;

[0080] S3. The mixture B obtained in step S2 was added to the mixture A obtained in step S1 under heating at 50℃, and stirred at 1300rpm until mixed uniformly to obtain mixture C;

[0081] S4. The mixture C obtained in step S3 was homogenized twice under a pressure of 25MPa, and cooled to room temperature to obtain a polyquaternium-51 modified high-osmotic multi-path whitening composition.

[0082] Comparative Example 1

[0083] The difference from Example 1 is that the polyquaternium-51 in the raw materials is replaced by deionized water, i.e. the raw materials do not include polyquaternium-51.

[0084] Comparative Example 2

[0085] The difference from Example 1 is that the polyquaternium-51 in the raw materials is replaced by chitosan.

[0086] Comparative Example 3:

[0087] The difference from Example 1 is that the polysorbate-80 in the raw materials is replaced by polysorbate-20.

[0088] Comparative Example 4:

[0089] The difference from Example 1 is that the soybean lecithin in the raw materials is replaced by hydrogenated soybean lecithin.

[0090] Test Example 1: Physicochemical property test

[0091] The test results of the physicochemical indexes of the samples prepared in Examples 1-7 and Comparative Examples 1-4 are shown in Table 1:

[0092]

[0093] Table 1

[0094] As can be seen from Table 1, the particle size and dispersion index of Examples 1-7 are better than those of Comparative Example 3, indicating that polysorbate-80 with unsaturated fatty chains has better co-emulsifying ability than polysorbate-20, and can form liposomes with smaller particle size and more uniform distribution. In addition, the appearance, particle size and dispersion index of Examples 1-7 are better than those of Comparative Example 4, indicating that liposomes prepared from non-hydrogenated soy lecithin have smaller particle size and more uniform particle size distribution than liposomes prepared from hydrogenated lecithin.

[0095] Test Example 2: Stability test

[0096] The samples prepared in Examples 1-4 and Comparative Examples 1-2 were subjected to particle size test and accelerated stability test.

[0097] The test method was as follows:

[0098] A Malvern Nano ZS90 particle size potential detector was used for testing, the test sample was diluted 500 times with ultrapure water, the test angle was 90°, the test temperature was 25°C, and the test was repeated 3 times.

[0099] After the samples of Examples 1-4 and Comparative Examples 1-2 were prepared, they were placed in heat-resistant 45°C, refrigerated 4°C, cold-resistant-18°C, light (4000lx), high and low temperature cycle, 18-25°C conditions, and their particle size, PDI, appearance state and odor were measured on the day of preparation (0 represents), one month later, two months later and three months later.

[0100] The test pictures of the samples of Example 1 and Comparative Example 1 are shown in Figure 1 and Figure 2 The test results of the samples of Examples 1-4 and Comparative Examples 1-2 are shown in Tables 2-7, respectively.

[0101]

[0102] Table 2: Stability test results of the sample of Example 1

[0103]

[0104] Table 3: Stability test results of the sample of Example 2

[0105]

[0106]

[0107] Table 4: Stability test results of the sample of Example 3

[0108]

[0109] Table 5: Stability test results of the sample of Example 4

[0110]

[0111]

[0112] Table 6 - Stability test results of Comparative Example 1 sample

[0113]

[0114] Table 7 - Stability test results of Comparative Example 2 samples

[0115] Depend on Figures 1-2 Table 2-7 shows that the heat and cold resistance (particle size, dispersion index, appearance, and odor) of samples from Examples 1-4 were better than those of Comparative Example 1 over three months. This indicates that the high-penetration multi-pathway whitening composition system modified with polyquaternium-51 can achieve a better protective barrier effect after high-speed shearing under high-pressure microjets, and can play a good stabilizing role in indicators such as liposome particle size, dispersion index, appearance, and odor. In addition, the heat and cold resistance of samples from Examples 1-4 were better than those of Comparative Example 2 over three months. Polyquaternium-51 can be adsorbed on the surface of liposomes through electrostatic interaction and hydrogen bonding, enhancing the electrostatic repulsion between liposomes and preventing liposome aggregation; at the same time, it encapsulates the phospholipid molecules of liposomes, reducing their probability of contact with oxygen, thereby reducing the oxidative decomposition rate of liposomes and improving the stability of liposomes and the whitening composition. Compared with other types of cationic polymers, polyquaternium-51 can play a better protective barrier role for the whitening composition.

[0116] Test Example 3: Biosafety Test

[0117] Test sample: The whitening composition (prepared in Examples 1-7) was mixed with deionized water to prepare a deionized aqueous solution of the whitening composition, wherein the final concentration of the whitening composition was 5 wt%.

[0118] The irritation of cosmetics was evaluated using the 2015 Cosmetic Safety Technical Specifications as a reference standard. The test method was a skin patch test, and 30 people aged 16-65 years were randomly distributed to participate in the test.

[0119] Test method: Place the test sample into a patch applicator (0.025g). Cover the patch applicator with non-irritating adhesive tape onto the back or flexor side of the forearm of the subject. Gently press with the palm of your hand to ensure even adhesion to the skin surface. Leave on for 24 hours. Remove the patch applicator 30 minutes after the pressure mark has disappeared and observe the skin reaction. If the result is negative, observe again at 24 and 48 hours after the patch test.

[0120] Evaluation criteria:

[0121] Grade 0: Negative reaction;

[0122] Grade 1: Suspected reaction, only weak erythema;

[0123] Grade 2: Weak positive reaction, erythema, infiltration, edema, and possibly papules;

[0124] Grade 3: Strong positive reaction, erythema, infiltration, edema, and possibly papules, and the reaction may extend beyond the test area;

[0125] Grade 4: Very strong positive reaction, obvious erythema, severe infiltration, edema, and confluent blisters, and the reaction extends beyond the test area.

[0126] Test results: The human skin closed patch test showed that no positive reactions occurred in 30 people in each group, according to the provisions of the “Cosmetic Safety Technical Specifications” (2015 edition), Examples 1-7 will not cause skin adverse reactions to the batch of subjects.

[0127] Test Example 4: Transdermal absorption capacity test

[0128] The vertical Franz diffusion cell method was used to evaluate the in vitro transdermal performance of the samples prepared in Comparative Example 1 and Comparative Example 1, and the effective diffusion area of the diffusion cell was 1.77 cm 2 , and the receiving pool volume was 22.5 mL.

[0129] Assembly and fixation of the test model: The pigskin was fixed between the diffusion chamber and the receiving chamber of the Franz cell diffusion cell, with the stratum corneum facing the diffusion chamber and the dermis facing the receiving chamber, so that the dermis of the pigskin was in close contact with the receiving liquid.

[0130] The Franz cell diffusion cell was fixed in the transdermal absorption diffusion instrument, the electromagnetic stirrer was started at a speed of 300 rpm, a constant temperature water bath at (37±1) °C was maintained, and it was ensured that there were no air bubbles in the water bath interlayer.

[0131] Loading: After the water bath temperature of the diffusion instrument was constant, 400 μL of sample was added to the surface of the pigskin using a pipette.

[0132] (1) Skin retention amount (μg / cm -2 )

[0133] At the end of transdermal absorption (transdermal time 12 h), the pigskin was removed, the surface residual drug was wiped with a cotton swab, and the pigskin was repeatedly washed with 0.9% normal saline, the water was absorbed with filter paper, the effective skin was collected, and the physiological saline was added, then it was homogenized at high speed, 5 mL of methanol was added for ultrasonic extraction for 30 min, 1 mL of the extract was taken, centrifuged at 8000 r / min for 10 min, the supernatant was taken, the concentration of resveratrol was determined by HPLC, and the retention amount of resveratrol in the pigskin was calculated.

[0134] The test results are shown in Table 8:

[0135]

[0136] Table 8

[0137] (2) Fluorescence coloration test

[0138] At the end of the transdermal test (30 min of transdermal time), the pig skin was removed, the surface was wiped with a cotton swab to remove residual drug, and then repeatedly washed with 0.9% saline, and the water was absorbed with filter paper. The pig skin was quickly frozen at -80°C after being embedded with OTC. The skin was sliced in the vertical direction from the epidermis to the dermis at a thickness of 20 μm at -20°C. The slices were fixed with acetone for 5 min and stored at -20°C. The frozen sections were warmed for 30 min. The water-soluble embedding agent was removed by soaking in PBS for 10 min, and then washed twice and the water was absorbed with filter paper. DAPI-containing anti-fluorescence quencher was added for mounting, and the fluorescence in the tissue was observed under a fluorescence microscope. The test results are shown in Table 8. Figure 3

[0139] As can be seen from Table 8 and Figure 3 , the resveratrol retention amount of Example 1 is 1.88 times that of Comparative Example 1 in the same time; the fluorescence coloration test shows that Comparative Example 1 can only enter the surface layer of the skin in the same time, while Example 1 can enter the deep layer of the skin. In summary, the high-penetration multi-path whitening composition modified by polyquaternary ammonium salt-51 (Example 1) has stronger transdermal penetration and absorption capacity than the whitening composition not modified by cationic polymer (Comparative Example 1).

[0140] Test Example 5: Human whitening efficacy test

[0141] Human evaluation method: The human test was carried out in accordance with the “Cosmetic Safety Technical Specifications” (2015 edition). Female volunteers were selected as test subjects, the melanin content in human skin was measured, and the whitening efficacy of the test sample was evaluated. The test sample was a whitening anti-aging skincare serum to which Example 1 (5 wt% addition amount) and Comparative Example 1 (5 wt% addition amount) were added. The melanin content, ITA° value, and visual skin color grade of the facial skin were measured using a skin pigment meter 1 day before use and after 28 days of continuous use. The test environment: temperature 20°C, humidity 50%. The test subjects used the test sample once a day, and the use method was as follows: after cleaning the facial skin, the test subjects applied the test sample to the facial skin with their hands. The test subjects did not use other whitening products during the test period.

[0142] ​ITA° growth rate = (individual type angle ITA° value of the day before using the test sample - individual type angle ITA° value after 28 days of continuous use of the test sample) / individual type angle ITA° value of the day before using the test sample x 100%. The higher the individual type angle ITA° growth rate, the more obvious the whitening effect.

[0143] Melanin reduction rate = (melanin content of the day before using the test sample - melanin content after 28 days of continuous use of the test sample) / melanin content of the day before using the test sample x 100%. The higher the melanin reduction rate, the more obvious the whitening effect.

[0144] Visual skin color grade reduction rate = (visual skin color grade of the day before using the test sample - visual skin color grade after 28 days of continuous use of the test sample) / visual skin color grade of the day before using the test sample x 100%. The higher the visual skin color grade reduction rate, the more obvious the whitening effect.

[0145] The individual type angle ITA° test results are shown in Table 9, the melanin index test results are shown in Table 10, and the visual skin color grade test results are shown in Table 11.

[0146]

[0147] Table 9

[0148]

[0149] Table 10

[0150]

[0151]

[0152] Table 11

[0153] As can be seen from Tables 9-11, after 28 days of continuous use of the sample of Example 1, the melanin is reduced by 20.01%, the ITA° value is increased by 61.97%, and the visual skin color grade is reduced by 20.22%; after 28 days of continuous use of the sample of Comparative Example 1, the melanin is reduced by 15.99%, the ITA° value is increased by 43.41%, and the visual skin color grade is reduced by 15.30%, indicating that both Example 1 and Comparative Example 1 have a whitening effect, and the whitening effect of Example 1 is obviously better than that of Comparative Example 1, indicating that the polyquaternium-51 modified high-penetration multi-path whitening composition prepared in the application has a better whitening effect.

[0154] The above embodiments are only illustrative of the principles of the present application and its efficacy, and are not intended to limit the present application. Any modification or change made by any person skilled in the art without departing from the spirit and scope of the present application shall be covered by the claims of the present application.

Claims

1. A high-penetration, multi-pathway whitening composition modified with polyquaternium-51, characterized in that: It is made from the following raw materials in the following weight percentages: tetrahydrocurcumin 0.001-2%, phospholipids 1-5%, resveratrol 0.001-1%, ascorbic acid tetraisopalmitate 0.1-5%, polysorbate-80 0.25-5%, tocopherol 0.001-1%, caprylic / capric triglyceride 2-10%, polyquaternium-51 0.001-0.1%, polyol 30-45%, tranexamic acid 2-10%, α-arbutin 0.001-3%, with the balance being deionized water. The sum of the weight percentages of all raw materials is 100%.

2. The high-penetration multi-pathway whitening composition modified with polyquaternium-51 according to claim 1, characterized in that: The polyol is one or more of sorbitol, glycerol, butylene glycol, 1,3-propanediol, or propylene glycol.

3. The high-penetration multi-pathway whitening composition modified with polyquaternium-51 according to claim 1, characterized in that: The phospholipid is soybean lecithin or egg yolk lecithin with a phosphatidylcholine content ≥70wt%.

4. The high-penetration multi-pathway whitening composition modified with polyquaternium-51 according to claim 1, characterized in that: The average particle size of the high-penetration multi-pathway whitening composition is 10-20 nm.

5. The method for preparing the polyquaternium-51 modified high-penetration multi-pathway whitening composition according to any one of claims 1 to 4, characterized in that: Includes the following steps: S1. Weigh each raw material according to the mass percentage, and mix tetrahydrocurcumin, phospholipids, resveratrol, ascorbate tetraisopalmitate, polysorbate-80, tocopherol, and caprylic / capric triglyceride. Stir at 45-50℃ for 10-30 min to obtain mixture A. S2. Mix polyquaternium-51, polyol, tranexamic acid, α-arbutin and deionized water, and stir at 45-50℃ until the mixture is homogeneous to obtain mixture B; S3. Add the mixture B obtained in step S2 to the mixture A obtained in step S1 under heating conditions of 45-50℃, and stir until the mixture is uniform to obtain mixture C; S4. Homogenize the mixture C obtained in step S3 2-3 times, and cool it to room temperature to obtain a high-penetration multi-channel whitening composition modified with polyquaternium-51.

6. The method for preparing the polyquaternium-51 modified high-penetration multi-pathway whitening composition according to claim 5, characterized in that: In step S1, the stirring speed is 600-800 rpm.

7. The method for preparing the polyquaternium-51 modified high-penetration multi-pathway whitening composition according to claim 5, characterized in that: In step S2, the stirring speed is 600-800 rpm.

8. The method for preparing the polyquaternium-51 modified high-penetration multi-pathway whitening composition according to claim 5, characterized in that: In step S3, the stirring speed is 1300-1500 rpm.

9. The method for preparing the polyquaternium-51 modified high-penetration multi-pathway whitening composition according to claim 5, characterized in that: In step S4, the homogenization pressure is 20-25 MPa.

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