An anti-aging composition containing a retinol derivative, and a method of preparing and using the same

Abstract

The application discloses a kind of anti-aging compositions containing retinol derivatives and its preparation method and application in the technical field of pharmaceutical preparation, and anti-aging composition includes the following weight percentage components: oil phase 15-22%;Polyhydric alcohol 10-15%;Composite emulsifier 7.5-12%;Retinol derivative 0.5-2%;Deionized water, remainder;Wherein, composite emulsifier includes inulin stearyl urea 2-4%, behenyl alcohol polyether 5-7% And behenyl trimethyl ammonium methyl sulfate 0.5-1.0%.By optimization of emulsifier system, the problem of low stability, low permeability of retinol derivatives is overcome, in addition, the application adds the following weight percentage of raw materials on the basis of anti-aging composition components: flavonoid compound 0.5-1.5%;EDTA-disodium 0.05-0.1%;Phenoxyethanol 0.15-0.3%;Ethylhexyl glycerol 0.05-0.2%;pH regulator 0.1-0.5% And antioxidant 0.2-0.5%, obtainable external repair preparation for solving the problem of skin oxidative damage induced by ultraviolet rays, formula is mild and stable, preparation process is simple, and application prospect is wide.

Description

Technical Field

[0001] This invention relates to the field of pharmaceutical preparation technology, specifically to an anti-aging composition containing retinol derivatives, its preparation method, and its application. Background Technology

[0002] Retinol derivatives include natural and synthetic retinol compounds, whose parent structure consists of a β-ionone ring and several all-trans isoprenoid side chains. Retinol esters are one type of retinol derivative, commonly including retinyl propionate, retinyl palmitate, and retinyl palmitate. The biological activity of retinol ester compounds depends on the RAR / RXR nuclear receptor system: retinoic acid binds to retinoic acid-binding protein 2 (CRABP-2) and is transported to the nucleus, activating the RARα / β / γ and RXR heterodimers, which bind to the retinoic acid response element (RARE) and regulate downstream gene transcription. Network pharmacology and multi-omics studies have revealed the multi-target synergistic anti-aging mechanism of retinol esters: MAPK and ErbB signaling pathways: By regulating core proteins such as JUN, PRKCA, and RASGRP3, they affect cell proliferation and inflammatory responses; ATM-CHK2-p53 pathway: The combined use of retinol and retinyl palmitate can activate RARβ receptors, trigger the expression of DNA homologous recombination (HR) repair genes, and significantly enhance the ability to repair UVB damage; PPAR-α pathway: Retinyl palmitate, as a PPAR-α agonist, shows a 192% synergistic effect on collagen III synthesis when used in combination with 10-hydroxystearic acid (10-HSA), confirming its synergistic potential.

[0003] Although the anti-aging activity of retinyl esters is well-established, their unique structure makes them susceptible to various chemical changes, including free radical reactions, isomerization, and photodegradation, under conditions of strong ultraviolet radiation, high temperature, and reactive oxygen species. Furthermore, this structure endows retinyl esters with high hydrophobicity; their polar functional groups significantly affect their solubility in organic solvents. Moreover, due to their high hydrophobicity, retinyl esters hardly penetrate the stratum corneum, thus reducing their bioavailability. Therefore, overcoming the low stability of retinyl esters and improving their permeability are urgent problems that need to be addressed.

[0004] Oil-in-water emulsions are multiphase dispersion systems in which one or more oil solutions are uniformly dispersed in water in the form of small droplets and stabilized by an emulsifier. Through the arrangement of the emulsifier at the oil-water interface or a special emulsion structure, the oil phase carrying retinol esters can be isolated from free oxygen in the water, which can reduce the probability of oxidation and improve stability. Based on this, it is hoped that products with high stability and anti-aging activity and high bioavailability can be developed. It is clear that the specific choice of emulsifier in oil-in-water emulsions affects the effect of stabilizing retinol esters. Summary of the Invention

[0005] The purpose of this invention is to solve the above-mentioned technical problems by providing an anti-aging composition containing retinol derivatives, its preparation method, and its application.

[0006] The present invention achieves the above objectives through the following technical solutions:

[0007] As a first aspect of the present invention, an anti-aging composition containing a retinol derivative is provided, comprising the following components in weight percentage:

[0008] Oil phase 15-22%;

[0009] Polyols 10-15%;

[0010] Compound emulsifier 7.5-12%;

[0011] Retinol derivatives 0.5-2%;

[0012] Deionized water balance;

[0013] The composite emulsifier includes 2-4% inulin stearyl carbamate, 5-7% behenyl alcohol polyether, and 0.5-1.0% behenyl trimethylammonium methyl sulfate.

[0014] As a further optimization of the present invention, the retinol derivative includes retinol propionate or retinol palmitate.

[0015] As a further optimization of the present invention, the polyol is at least one of glycerol and 1,3-butanediol.

[0016] As a further optimization of the present invention, the oil phase is at least one of caprylic / capric triglyceride, diethylhexyl carbonate, squalane, or polydimethylsiloxane.

[0017] As a second aspect of the present invention, a method for preparing an anti-aging composition containing a retinol derivative as described above is also provided, comprising the following steps:

[0018] (A-1) Add polyol and composite emulsifier to deionized water and homogenize at 80-85℃ and 10000-15000 rpm for 30-60s to obtain an aqueous phase;

[0019] (A-2) Dissolve the retinol derivative in the oil phase to obtain a mixture;

[0020] (A-3) Add the mixture to the aqueous phase and homogenize it at 10,000-15,000 rpm for 60-120 s to obtain a crude emulsion. Homogenize it under high pressure at 600-800 bar and 10,000-15,000 rpm for 60-90 s, and then degas, stir slowly, and let it cool to obtain the final product.

[0021] As a third aspect of the invention, the use of the anti-aging composition as described above in the preparation of a topical repair formulation for anti-photoaging of the skin is also provided.

[0022] As a fourth aspect of the present invention, a topical repair formulation for anti-photoaging of the skin is also provided, which, in addition to the anti-aging composition components as described in any of the above, further comprises the following components in weight percentage:

[0023] Flavonoids 0.5-1.5%;

[0024] Phenoxyethanol 0.15-0.3%;

[0025] Ethylhexylglycerin 0.05-0.2%;

[0026] pH adjuster 0.1-0.5%;

[0027] Antioxidant 0.2-0.5%.

[0028] As a further optimization of the present invention, the flavonoid compound includes one of vitexin or naringenin.

[0029] As a further optimization of the present invention, the pH adjuster is arginine; the antioxidant is tocopheryl acetate and butylated hydroxytoluene.

[0030] As a fifth aspect of the present invention, a method for preparing a topical repair agent for anti-photoaging of the skin as described in any of the above-mentioned methods is also provided, comprising the following steps:

[0031] (B-1) Add polyol, disodium EDTA, phenoxyethanol and ethylhexylglycerol to deionized water and mix to obtain an aqueous phase;

[0032] (B-2) Dissolve the retinol derivative in the oil phase to obtain mixture A;

[0033] (B-3) Mix the remaining components except for the pH adjuster, and homogenize them at 80-85℃ and 10000-15000rpm for 30-60s to obtain mixture B;

[0034] (B-4) Add mixture A to mixture B, heat to 80-85℃ and keep warm for 60-90s, then add to the aqueous phase and homogenize at 10000-15000rpm for 60-120s to obtain crude emulsion;

[0035] (B-5) Cool the crude emulsion to 50-55℃, add pH adjuster, homogenize the resulting emulsion under high pressure at 600-800 bar and 10000-15000 rpm for 60-90s, and then degas, stir slowly, and let it cool to obtain the final product.

[0036] The beneficial effects of this invention are as follows:

[0037] (1) A stable oil-in-water structure was constructed using a special composite emulsifier system composed of inulin stearyl carbamate, behenyl alcohol polyether, and behenyl trimethylammonium methyl sulfate, which effectively isolates the oil phase from free oxygen in the water, reducing the risk of oxidation and photodegradation of retinol derivatives. After storage at 50°C in the dark for 30 days, the retention rate reached over 75%, which is far superior to the effect of single or modified emulsifier systems. In addition, the synergistic effect of the composite emulsifier optimized the particle size distribution of the anti-aging composition and improved the penetration ability of hydrophobic retinol derivatives in the stratum corneum and dermis of the skin. Transdermal experiments showed that this invention solved the problem of traditional retinol derivatives being difficult to penetrate the stratum corneum and having low bioavailability. This invention provides an excellent carrier material for the stable exertion of the anti-aging activity of retinol derivatives.

[0038] (2) Based on the anti-aging composition, the present invention adds vitexin or naringenin to develop a topical repair preparation for anti-photoaging of the skin. The preparation forms a synergistic antioxidant system through flavonoid compounds and retinol derivatives, and significantly promotes the proliferation of human fibroblasts, enhances the skin repair ability, and strengthens the anti-photoaging effect.

[0039] (3) The formulation provided by the present invention is mild and stable, and the preparation process is simple. It can specifically solve the problem of skin oxidative damage induced by ultraviolet rays and has broad application prospects in the field of topical repair preparations. Detailed Implementation

[0040] The present application will now be described in further detail. It should be noted that the following specific embodiments are only used to further illustrate the present application and should not be construed as limiting the scope of protection of the present application. Those skilled in the art can make some non-essential improvements and adjustments to the present application based on the above application content.

[0041] Unless otherwise specified, all reagents and materials used below are commercially available products. Unless otherwise specified, all methods used below are conventional methods known to those skilled in the art.

[0042] Example 1: Preparation of an anti-aging composition containing retinol derivatives

[0043] (A-1) Add polyol and composite emulsifier to deionized water and homogenize at 80-85℃ and 10000-15000rpm for 30-60s to obtain an aqueous phase, preferably at 85℃ and 15000rpm for 30s.

[0044] (A-2) Dissolve the retinol derivative in the oil phase to obtain a mixture;

[0045] (A-3) Add the mixture to the aqueous phase and homogenize it at 10,000-15,000 rpm for 60-120 s to obtain a crude emulsion. Preferably, homogenize it at 15,000 rpm for 60 s, then homogenize it at 600-800 bar and 10,000-15,000 rpm for 60-90 s, preferably at 600 bar and 10,000 rpm for 90 s. After degassing, slow stirring, and cooling, the emulsion is obtained.

[0046] The formulations of anti-aging compositions containing retinol derivatives are shown in Table 1.

[0047] Table 1 Formulations of anti-aging compositions containing retinol derivatives (weight percentage, %)

[0048]

[0049] Note: "-" indicates that it has not been added.

[0050] To investigate the effect of the composite emulsifier system on the performance of anti-aging compositions containing retinol derivatives, the composite emulsifier system was adjusted based on the formulation of the anti-aging composition containing retinol derivatives defined by Y-1 in Table 1 (Table 2), and anti-aging compositions containing retinol derivatives were prepared according to the above preparation method, denoted as Y-5~Y-9.

[0051] Table 2 Design of Composite Emulsifier System

[0052]

[0053] Note: "-" indicates no addition; the amount of inulin lauryl carbamate in group Y-8 was the same as in Y-1; the amount of inulin lauryl carbamate in group Y-9 was the same as in Y-7.

[0054] (1) Determination of the retention rate of retinyl propionate in the anti-aging composition

[0055] Y-1 and Y-5~Y-9 were dispensed into 50mL transparent plastic bottles and stored in a dark oven at 50℃. The residual retinol derivative content in the anti-aging composition was determined on day 30 of storage in the oven. 20-50mg of the anti-aging composition sample was placed in a sample bottle, dissolved by sonication in 4mL of anhydrous ethanol, and appropriately diluted. The absorbance of the retinyl propionate-anhydrous ethanol solution was measured at 325nm using a UV spectrophotometer, and the retinyl propionate content in the anti-aging composition was calculated based on the standard working curve. The retention rate of retinyl propionate in the anti-aging composition was calculated using the following formula.

[0056]

[0057] In the formula: A1 represents the retinyl propionate content in the anti-aging composition obtained by measuring absorbance value; A0 represents the retinyl propionate content in the initial anti-aging composition.

[0058] (2) Particle size and zeta potential determination

[0059] Take the freshly prepared anti-aging composition and the anti-aging composition stored at 50°C in a dark oven for 30 days, and dilute them with deionized water by 10%. 3 The solution to be tested was obtained by multiplying the sample size. The particle size (average value) and zeta potential were measured five times at 25℃ and 90° scattering angle using a ZetaPALS nanoparticle size analyzer based on dynamic light scattering technology.

[0060] The results are shown in Table 3.

[0061] Table 3 Characterization results of the anti-aging composition

[0062]

[0063] As shown in Table 3, the anti-aging composition prepared using the composite emulsifier system can effectively stabilize retinyl propionate, with a retention rate of over 75% after 30 days of storage at 50°C. Results from group Y-5 indicate that increasing the amount of behenyltrimethylammonium methyl sulfate in the composite emulsifier system triggers the degradation of retinyl propionate. Results from groups Y-5 to Y-9 show that the three components—inulin stearyl carbamate ISC, behenyltrimethylammonium methyl sulfate, and behenyl alcohol polyether—collectively affect the stability of retinyl propionate in the anti-aging composition. In the interfacial layer formed by the mixed emulsifiers, hydrogen bonding, electrostatic interaction, and hydrophobic interaction occur simultaneously, inhibiting the diffusion and migration of retinyl propionate at the interface and ensuring its stability. Further surface tension measurements of the composite emulsifier systems (Table 2) show that the composite emulsifier system used in group Y-1 has the lowest interfacial tension, which is beneficial for forming a highly stable anti-aging composition.

[0064] The particle size of each anti-aging composition ranged from 75.42 to 88.76 nm. After storage at 50°C for 30 days, the particle size of all compositions decreased significantly. Different composite emulsifier systems had varying effects on the particle size of the anti-aging compositions. The composite emulsifier system used in group Y-1 resulted in a smaller increase in the particle size of the anti-aging composition. In addition, after storage at 50°C for 30 days, the absolute value of the zeta potential of each anti-aging composition approached 0 mV.

[0065] (2) Transdermal performance test

[0066] In vitro transdermal experiments were conducted using the Franz diffusion method. Fresh, intact pig skin was collected, subcutaneous fat was removed, and the pig skin was cut into pieces approximately 4 cm in length. 2 The circular object, after being washed, is installed in the diffusion chamber with the epidermal side facing towards the drug delivery chamber. The surface area of ​​the diffusion chamber is 2.2 cm². 2 Simultaneously, 6.5 mL of physiological saline was added to the receiving chamber as the receiving solution. The temperature of the diffusion cell inside the transdermal diffusion apparatus was maintained at (32±0.1)℃, and the stirring speed was 300 rpm.

[0067] Approximately 0.5g of the anti-aging composition was applied to the surface of pigskin, with a transdermal time of 12 hours. After the test, the pigskin was removed and the surface moisture was dried. The pigskin surface was repeatedly peeled back using an adhesive tape method 21 times: the first layer of tape was discarded, and the remaining 20 layers were collected in a 10mL brown sample bottle. 3mL of methanol was added to the sample bottle, and the mixture was ultrasonically extracted for 30 minutes to collect retinyl propionate from the stratum corneum of the pigskin. The remaining pigskin was cut into small pieces, collected in a brown sample bottle, and 3mL of methanol was added and ultrasonically extracted for 30 minutes to obtain retinyl propionate from the dermis of the pigskin. The extract was filtered through a 0.22μm organic filter membrane, and the retinyl propionate content in the extract was determined by HPLC, thus obtaining the retinyl propionate content in the stratum corneum and dermis of the pigskin. Measurement conditions: Benetnach C18 column (250*4.6mm); mobile phase V. 甲醇 V 水 = 98:2; flow rate 1 mL / min; UV detector wavelength 325 nm; injection volume 20 μL. The content of retinyl propionate in the dermis was calculated using the following formula:

[0068] (Unit: μg / cm) 2 )

[0069] In the formula, N is the content of retinyl propionate calculated by HPLC peak area; S is the diffusion cell area (2.2 cm²). 2 ).

[0070] The results are shown in Table 4.

[0071] Table 4 Results of transdermal performance testing

[0072]

[0073] As shown in Table 4, the anti-aging compositions prepared using the composite emulsifier system exhibit good skin permeability. Different composite emulsifier systems result in varying degrees of transdermal permeability of the anti-aging compositions. Increasing the amount of behenyltrimethylammonium methyl sulfate in the composite emulsifier system relatively improves the transdermal permeability of the anti-aging compositions, while decreasing the amount of behenyl alcohol polyether has a relatively small impact on the transdermal permeability of the anti-aging compositions.

[0074] Example 2: Preparation of topical repair agents

[0075] Based on the results of the investigation of the composite emulsifier system in Example 1, this example describes the preparation of a topical repair formulation based on the anti-aging composition components and formulation shown in group Y-1. The formulation of the topical repair formulation is shown in Table 5.

[0076] Table 5. Formulations of topical skin repair agents containing retinol derivatives for anti-photoaging (weight percentage, %)

[0077]

[0078] Note: "-" indicates no addition; arginine was prepared as a 10% solution.

[0079] The preparation method of the topical repair agent includes the following steps:

[0080] (B-1) Add polyol, disodium EDTA, phenoxyethanol and ethylhexylglycerol to deionized water and mix to obtain an aqueous phase;

[0081] (B-2) Dissolve the retinol derivative in the oil phase to obtain mixture A;

[0082] (B-3) Mix the remaining components except for the pH adjuster, and homogenize them at 80-85°C and 10000-15000 rpm for 30-60 s to obtain mixture B, preferably at 85°C and 15000 rpm for 30 s.

[0083] (B-4) Add mixture A to mixture B, heat to 80-85℃ and keep warm for 60-90s, then add to the aqueous phase. Preferably, heat to 80℃ and keep warm for 90s, then homogenize at 10000-15000rpm for 60-120s, preferably at 15000rpm for 60s, to obtain a crude emulsion.

[0084] (B-5) Cool the crude emulsion to 50-55℃, preferably 50℃, add a pH adjuster, and homogenize the resulting emulsion under high pressure at 600-800 bar and 10000-15000 rpm for 60-90s, preferably 600 bar and 10000 rpm for 90s. Then, after degassing, slow stirring, and cooling, the emulsion is obtained.

[0085] To investigate the efficacy of topical repair preparations, two control groups (denoted as DZ-1 group and DZ-2 group) were set up based on the formulation of the components shown in the ZJ-1 group topical repair preparation: DZ-1 group: quercetin was used instead of vitexin; DZ-2 group: vitexin was not added; DZ-3 group: the addition of retinyl propionate in the ZJ-1 group topical repair preparation was omitted.

[0086] (1) Antioxidant capacity test

[0087] (1.1) DPPH radical scavenging ability

[0088] Experimental Principle: The DPPH method is used to determine the free radical scavenging ability of topical repair agents. DPPH is a stable nitrogen-centered free radical; its ethanol solution is purple, with maximum absorbance at 515 nm. When an antioxidant is added to the DPPH solution, its lone pairs of electrons are paired, causing the absorption to disappear or weaken, resulting in a lighter solution color, appearing yellow or pale yellow, and a decrease in absorbance at 515 nm. The degree of change is linearly related to the degree of free radical scavenging. The concentration of antioxidant required to remove half of the DPPH free radicals (EC50) is determined by measuring this concentration. 50 ) and time (TEC) 50 This is used to react with the activity of antioxidants.

[0089] Experimental method: Preparation of DPPH solution: Weigh DPPH and dilute to 250 mL in a brown volumetric flask with anhydrous ethanol to obtain 2 × 10⁻⁶ DPPH solution. -4 Store the mol / L DPPH solution in a refrigerator protected from light.

[0090] The test procedure is as follows: Take 4.0 mL of 2×10 -4 After mixing and stabilizing a 1.0 mL solution of DPPH (mol / L) and 1.0 mL of 95% ethanol, the absorbance was measured at 515 nm using 95% ethanol as a reference, and recorded as A0. Then, 4.0 mL of 95% ethanol and 1.0 mL of the test sample solution (topical repair preparations prepared from groups ZJ-1~ZJ-4 and DZ-1~DZ-3) were mixed and stabilized. The absorbance was measured at 515 nm using 95% ethanol as a reference, and recorded as A1. Finally, 4.0 mL of 2×10⁻⁶ mol / L DPPH solution was mixed and stabilized, and recorded as A1. -4After mixing 1.0 mL of mol / L DPPH solution and the test sample and allowing the reaction to stabilize, the absorbance was measured at 515 nm using 95% ethanol as a reference, and recorded as A2. The DPPH scavenging rate was calculated according to the following formula: DPPH scavenging rate (100%) = [1 - (A2 - A1) / A0] × 100%.

[0091] (1.2) ABTS free radical scavenging ability

[0092] Experimental Principle: ABTS is a water-soluble free radical initiator and colorimetric agent. After oxidation by reactive oxygen species, ABTS generates stable blue-green cationic free radicals ABTS· + The test substance is added to it. If the substance contains antioxidants, it will react with ABTS. + The reaction causes the reaction system to decolorize, and then ABTS· + The change in absorbance was detected at the maximum absorption wavelength (734 nm), and compared with a control standard system containing water-soluble vitamin E (trolox) to calculate the total antioxidant capacity of the tested substance.

[0093] ABTS· + Solution preparation: Prepare a 2 mmol / L ABTS solution with distilled water. Take 50 mL of the 2 mmol / L ABTS solution. + The solution was mixed thoroughly with 200 mL of K₂S₂O₈ aqueous solution (70 mmol / L) and left to stand in the dark for 8 hours to obtain ABTS· + Solution.

[0094] The test procedure is as follows: ABTS· is prepared by mixing 0.2 mol / L NaH2PO4 and 0.2 mol / L Na2HPO4 in a volume ratio of 30:9, pH=6.3 with phosphate buffer. + Dilute the solution to an absorbance of 1.0; take 1 mL of the topical repair preparation to be tested and add 1.9 mL of diluted ABTS· + Mix the solution thoroughly; let it stand for 10 minutes, and then measure the absorbance at 734 nm using a spectrophotometer. Calculate the ABTS radical scavenging rate using the following formula: S = (A0 - A1) / A0 × 100%, where A0 is the ABTS radical scavenging rate. + The absorbance of the solution, A1 is ABTS· + The absorbance of the solution after mixing the solution and the sample to be tested.

[0095] The results of the antioxidant capacity test are shown in Table 6.

[0096] Table 6. Results of Antioxidant Capacity Test

[0097]

[0098] As shown in Table 6, compared with the DZ-2 group without added flavonoids, the topical repair preparation with added flavonoids such as vitexin and naringenin has better antioxidant capacity. The antioxidant capacity of the group with added vitexin is slightly better than that of the currently known quercetin. Moreover, the antioxidant capacity increases with the increase of the amount added. After the amount added increases from 1% to 1.5%, the antioxidant capacity does not increase significantly. From an economic point of view, 1.0% is the optimal amount added.

[0099] (2) Test for ability to promote fibroblast proliferation

[0100] Sample solution preparation: The topical repair preparations prepared from ZJ-1~ZJ-4 and DZ-1~DZ-3 were directly diluted with culture medium to a final concentration of 50 μg / mL.

[0101] MTT assay for cell viability: Human fibroblasts in logarithmic growth phase were digested, counted, and seeded in 96-well plates at a density of 1 × 10⁶ cells / well. 5 Cells / mL, cell volume 100μL. After culturing at 37℃ in a 5% CO2 incubator for 24h, sample solutions of different concentrations dissolved in DMEM medium were added. After incubation for 24h, the supernatant was discarded. 100μL of 0.5mg / mL LMTT solution was added to each well, and the cells were incubated for 4h, after which the supernatant was discarded. 100μL of LDMSO was added to each well, and the cells were shaken in a microplate reader for 5-10 min. The absorbance was read at 490nm. Cell proliferation rate was calculated using the following formula:

[0102] ;

[0103] In the formula: A0 is the absorbance of DMSO at 490nm; A1 is the absorbance of the sample group at 490nm; A2 is the absorbance of the blank control group at 490nm.

[0104] The results are shown in Table 7.

[0105] Table 7 Results of tests on the ability to promote fibroblast proliferation

[0106]

[0107] As can be seen from the results in Table 7, the topical repair preparation provided by this invention can promote fibroblast vitality. Its cell proliferation rate is 2-3 times higher than that of the control group DZ-2 without vitexin and naringenin. As can be seen from the table, at the same amount, vitexin is better than naringenin in promoting fibroblast vitality, and the cell proliferation rate first increases and then decreases with the increase of the amount added, reaching a maximum of 26.5%, which makes the topical repair preparation achieve better repair efficacy.

[0108] (3) Determine the inhibitory effect of topical repair agents on ROS production in UV-damaged HaCaT cells.

[0109] Reactive oxygen species (ROS) are byproducts of normal oxygen metabolism, but under strong ultraviolet (UV) radiation, ROS levels can rise sharply, causing cell damage. This study aimed to evaluate the ability of topical repair agents to scavenge ROS at the cellular level by assessing their effect on UV-irradiated keratinocytes' ROS production.

[0110] Test method: 2 × 10⁻⁶ per well 4 HaCaT cells were seeded at a density of [number] cells / mL and incubated for 24 hours. Then, the topical repair agents (ZJ-1~ZJ-4, DZ-1~DZ-3) were added to a final concentration of 200 μg / mL. [Further details about the inoculation process are needed for accurate translation.] 2 Cells were irradiated with UVB for 24 hours. The control group was not irradiated with ultraviolet light and no test substance was added. The model group was irradiated with UVB only and no test substance was added.

[0111] After irradiation, remove the culture medium, wash the cells with HBSS, and then irradiate with 2,7 Dichlorofluorescein diethyl ester (DCFH) DA was diluted with DMSO and added to each well of cells. The cells were incubated in the dark at room temperature for 30 minutes to allow the dye to diffuse into the cells. After incubation, the dye was removed, and serum-free DMEM medium was added. Absorbance was immediately measured at 485 nm and 535 nm. Optical density (OD) values ​​represent the incremental change in intracellular reactive oxygen species (ROS). The formula for calculating ROS scavenging rate is shown below:

[0112]

[0113] The results are shown in Table 8.

[0114] Table 8. Results of changes in the increase of intracellular reactive oxygen species.

[0115]

[0116] As can be seen from the results in Table 8, the topical repair preparation provided by this invention has a certain inhibitory effect on reactive oxygen species generated in cells after ultraviolet irradiation. This is mainly due to the addition of flavonoid compounds in the topical repair preparation. The comparison in the table shows that vitexin has a better repair effect on oxidative damage to the skin caused by ultraviolet damage than quercetin and naringenin with the same amount of added ingredients, and it has a synergistic effect with retinyl propionate in improving the photoaging repair effect.

[0117] The embodiments described above are merely examples of several implementations of the present invention, and while the descriptions are relatively specific and detailed, they should not be construed as limiting the scope of the present invention. It should be noted that those skilled in the art can make various modifications and improvements without departing from the concept of the present invention, and these modifications and improvements all fall within the scope of protection of the present invention.

Claims

1. An anti-aging composition containing a retinol derivative, characterized in that: Includes the following components by weight percentage: Oil phase 15-22%; Polyols 10-15%; Compound emulsifier 7.5-12%; Retinol derivatives 0.5-2%; Deionized water balance; The composite emulsifier includes 2-4% inulin stearyl carbamate, 5-7% behenyl alcohol polyether, and 0.5-1.0% behenyl trimethylammonium methyl sulfate. The retinol derivative is retinol propionate or retinol palmitate; The polyol is at least one of glycerol and 1,3-butanediol; The oil phase is at least one of caprylic / capric triglyceride, diethylhexyl carbonate, squalane, or polydimethylsiloxane.

2. A method for preparing an anti-aging composition containing a retinol derivative as described in claim 1, characterized in that, Includes the following steps: (A-1) Add polyol and composite emulsifier to deionized water and homogenize at 80-85℃ and 10000-15000 rpm for 30-60s to obtain an aqueous phase; (A-2) Dissolve the retinol derivative in the oil phase to obtain a mixture; (A-3) Add the mixture to the aqueous phase and homogenize it at 10,000-15,000 rpm for 60-120 s to obtain a crude emulsion. Homogenize it under high pressure at 600-800 bar and 10,000-15,000 rpm for 60-90 s, and then degas, stir slowly, and let it cool to obtain the final product.

3. The use of the anti-aging composition containing a retinol derivative as described in claim 1 in the preparation of pharmaceutical formulations.

4. A topical repair preparation for anti-photoaging of the skin, characterized in that, In addition to the anti-aging composition components as described in claim 1, the composition further comprises the following components by weight percentage: Flavonoids 0.5-1.5%; EDTA-disodium 0.05-0.1%; Phenoxyethanol 0.15-0.3%; Ethylhexylglycerin 0.05-0.2%; pH adjuster 0.1-0.5%; Antioxidant 0.2-0.5%; The flavonoid compound is vitexin or naringin.

5. The topical repair preparation for anti-photoaging of skin according to claim 4, characterized in that, The pH adjuster is arginine; the antioxidants are tocopheryl acetate and butylated hydroxytoluene.

6. A method for preparing a topical repair agent for anti-photoaging of the skin as described in any one of claims 4-5, characterized in that, Includes the following steps: (B-1) Add polyol, disodium EDTA, phenoxyethanol and ethylhexylglycerol to deionized water and mix to obtain an aqueous phase; (B-2) Dissolve the retinol derivative in the oil phase to obtain mixture A; (B-3) Mix the remaining components except for the pH adjuster, and homogenize them at 80-85℃ and 10000-15000rpm for 30-60s to obtain mixture B; (B-4) Add mixture A to mixture B, heat to 80-85℃ and keep warm for 60-90s, then add to the aqueous phase and homogenize at 10000-15000rpm for 60-120s to obtain crude emulsion; (B-5) Cool the crude emulsion to 50-55℃, add pH adjuster, homogenize the resulting emulsion under high pressure at 600-800 bar and 10000-15000 rpm for 60-90s, and then degas, stir slowly, and let it cool to obtain the final product.

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