Method of making controlled release carrier with synergistic keratolytic composition and controlled release carrier containing the composition
By combining adenosine, N-acetylneuraminic acid, and lactobionic acid with nanocarrier technology, the high irritation and safety issues of traditional exfoliating ingredients are solved, achieving gentle exfoliation and prevention of clogged pores on sensitive skin.
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- GUANGZHOU KEYING COSMETICS CO LTD
- Filing Date
- 2026-03-21
- Publication Date
- 2026-06-19
AI Technical Summary
Traditional chemical controlled-release carriers are limited in their application among people with sensitive skin due to their high irritation, and the high concentration of existing exfoliating ingredients can easily cause skin damage, making it difficult to meet consumer safety requirements.
The exfoliating ingredient is a combination of adenosine, N-acetylneuraminic acid, and lactobionic acid, which is encapsulated in a nanocarrier. The release is controlled by a combination of lipid materials and modifiers, and the exfoliating ingredient is released rapidly in oily areas of the skin under the action of lipase.
It achieves a gentle exfoliation effect on sensitive skin, reduces irritation to healthy skin, prevents clogged pores and skin symptoms, and has a high degree of safety and targeted exfoliation effect.
Smart Images
Figure CN122229702A_ABST
Abstract
Description
Technical Field
[0001] This invention relates to the field of cosmetics, and in particular to a method for preparing a synergistic exfoliating composition and a controlled-release carrier containing the composition. Background Technology
[0002] Traditional chemical controlled-release carriers (such as glycolic acid and salicylic acid) often cause erythema, stinging or barrier damage due to their high irritation, which limits their application in people with sensitive skin.
[0003] In addition, existing exfoliating ingredients require relatively high concentrations to ensure good exfoliation ability. These high concentrations of exfoliating ingredients are quite irritating. Even people with normal skin can easily suffer skin damage under the influence of high concentrations of irritating ingredients. Their safety is difficult to meet consumer needs, so there is still room for improvement. Summary of the Invention
[0004] In order to maintain good exfoliation efficacy while reducing skin irritation, this application provides a method for preparing a synergistic exfoliating composition and a controlled-release carrier containing the composition.
[0005] In a first aspect, this application provides a synergistic exfoliating composition, employing the following technical solution: A synergistic exfoliating composition is formulated from adenosine, N-acetylneuraminic acid, and lactobionic acid.
[0006] By adopting the above technical solution and specifically selecting the combination of adenosine, N-acetylneuraminic acid, and lactobionic acid, the synergistic effect of their active ingredients can significantly promote the exfoliation of keratinocytes, resulting in a good exfoliation effect. At the same time, adenosine, N-acetylneuraminic acid, and lactobionic acid are all low-irritant raw materials, ensuring that the composition will not cause strong irritation. This makes the composition milder, more skin-friendly, suitable for sensitive skin, and highly safe, thus well meeting consumer needs.
[0007] Preferably, the mass ratio of adenosine, N-acetylneuraminic acid, and lactobionic acid is 5-10:0.1-1:3-6.
[0008] By adopting the above technical solution and by specifically selecting the mass ratio of adenosine, N-acetylneuraminic acid, and lactobionic acid, the synergistic effect of each active ingredient is better, and the exfoliation effect is more significant.
[0009] Secondly, this application provides a controlled-release carrier with a synergistic exfoliating composition, employing the following technical solution: A controlled-release carrier containing the above-mentioned synergistic exfoliating composition includes the synergistic exfoliating composition and a nanocarrier, wherein the synergistic exfoliating composition is encapsulated in the nanocarrier.
[0010] By adopting the above technical solution, and by encapsulating the synergistic exfoliating composition in a nanocarrier, the release of the composition can be better controlled, thus controlling the release of exfoliating ingredients and resulting in better skincare effects.
[0011] Preferably, the nanocarrier is composed of a lipid material and a modifier.
[0012] By adopting the above technical solution, through the combination of lipid materials and modifiers, the rapid disintegration of nanocarriers under the action of lipase can be controlled, thereby achieving targeted exfoliation in areas of the skin with excessive oil production. This reduces the accumulation of keratin in oily areas that leads to clogged pores, effectively preventing skin symptoms such as acne and inflammation, and providing better skin care results.
[0013] Preferably, the lipid material is one or more of the following: hydrogenated lecithin, lecithin, caprylic / capric triglyceride, beeswax, glyceryl stearate, PEG-20 glyceryl triisostearate, glyceryl distearate, PEG-50 shea butter, polyglycerol-2 laurate, PEG-6 caprylic / capric triglyceride, hydrogenated coconut oil triglyceride, PEG-7 glyceryl coconut oil ester, polyglycerol-3 diisostearate, and polyglycerol-2 triisostearate.
[0014] By adopting the above technical solution and specifically selecting lipid materials, the nanocarriers can be more easily and rapidly broken down under the action of lipase, resulting in a better targeted release of exfoliating ingredients.
[0015] Preferably, the modifier is one or more of ceramide NP, ceramide NH, ceramide AS, ceramide NS, ceramide EOS, and ceramide EOP.
[0016] By adopting the above technical solution and specifically selecting modifiers, it is possible to accelerate the rapid breakdown of nanocarriers under the action of lipase, and improve the stability of nanocarriers in the absence of lipase. This makes it less likely for exfoliating ingredients to be released on healthy skin, reducing the negative effects of excessive exfoliation on healthy skin, and enabling more targeted exfoliation of oily areas to prevent clogged pores.
[0017] Preferably, the lipid material is a compound of hydrogenated lecithin, lecithin, caprylic / capric triglyceride, beeswax, and glyceryl stearate, and the modifier is ceramide NP. The mass ratio of hydrogenated lecithin, lecithin, caprylic / capric triglyceride, beeswax, glyceryl stearate, and ceramide NP is 2.8-3.2: 1.8-2.2: 4.8-5.2: 0.09-0.11: 0.13-0.17: 0.18-0.22.
[0018] By adopting the above technical solution, and by using hydrogenated lecithin, lecithin, caprylic / capric triglyceride, beeswax, glyceryl stearate, and ceramide NP in a specific ratio, the nanocarrier can break down more quickly under the action of lipase, thereby rapidly releasing exfoliating ingredients. Furthermore, without the action of lipase, the nanocarrier is more stable and less likely to release large amounts of exfoliating ingredients in healthy skin areas, resulting in better intelligent identification of oily skin areas.
[0019] Thirdly, this application provides an application of a controlled-release carrier with a synergistic exfoliating composition, employing the following technical solution: An application of the above-mentioned controlled-release carrier having a synergistic exfoliating composition, wherein the controlled-release carrier having a synergistic exfoliating composition is added to a cosmetic formulation to prepare a cosmetic with exfoliating effects.
[0020] By adopting the above technical solution, the cosmetics produced can effectively prevent clogged pores, thereby achieving the effect of preventing acne and inflammation.
[0021] Fourthly, this application provides a method for preparing a controlled-release carrier of a synergistic exfoliating composition, employing the following technical solution: A method for preparing a controlled-release carrier of the above-mentioned synergistic exfoliating composition includes the following steps: Step 1), N-acetylneuraminic acid, lactobionic acid, and adenosine are dissolved in an aqueous solvent to form the aqueous phase; Step 2), the lipid material and modifier are dissolved in an alcohol solvent to form a composite lipid phase; Step 3), mix the aqueous phase with the composite lipid phase to obtain a mixed phase; Step 4) The mixed phase is homogenized to obtain a controlled-release carrier with a synergistic exfoliating composition.
[0022] By adopting the above technical solution, the controlled-release carrier with synergistic exfoliating composition can be rapidly released in areas with high lipase content in the skin, achieving the effect of intelligently identifying oily areas of the skin, thereby effectively preventing pore blockage and reducing the negative effects of excessive exfoliation on healthy skin areas. Moreover, the controlled-release carrier with synergistic exfoliating composition has low irritation and high safety.
[0023] Preferably, the aqueous solvent is PBS buffer, the pH of the PBS buffer is 6.5-7, and the alcohol solvent is ethanol.
[0024] By adopting the above technical solutions, the production process becomes less difficult, a microemulsion state can be formed more effectively, and the product quality is better.
[0025] In summary, this application has the following beneficial effects: 1. Because this application specifically selects adenosine, N-acetylneuraminic acid, and lactobionic acid to form a compound, the synergistic effect of their active ingredients can significantly promote the exfoliation of keratinocytes, resulting in a good exfoliation effect. At the same time, adenosine, N-acetylneuraminic acid, and lactobionic acid are all low-irritant raw materials, so the composition will not cause strong irritation, making the composition milder and more skin-friendly, suitable for sensitive skin, and with high safety, thus well meeting consumer needs.
[0026] 2. In this application, the combination of lipid materials and modifiers can control the rapid disintegration of nanocarriers under the action of lipase, thereby achieving targeted exfoliation in areas of the skin with high oil production. This reduces the accumulation of keratin in oily areas that leads to clogged pores, effectively preventing skin symptoms such as acne and inflammation, and providing better skin care.
[0027] 3. In this application, hydrogenated lecithin, lecithin, caprylic / capric triglyceride, beeswax, glyceryl stearate, and ceramide NP are preferably compounded in a specific ratio, so that the nanocarrier can break down more quickly under the action of lipase, thereby rapidly releasing the exfoliating ingredients. Moreover, without the action of lipase, the nanocarrier is more stable and less likely to release large amounts of exfoliating ingredients in healthy skin areas, and the effect of intelligently identifying oily skin areas is better. Attached Figure Description
[0028] Figure 1 This is a release rate-time trend graph for Example 1 used in Experiment 3; Figure 2 This is a release rate-time trend graph for example 2 used in Experiment 3; Figure 3 This is a release rate-time trend graph for example 3 used in experiment 3; Figure 4 This is a release rate-time trend graph for comparison application example 1 in Experiment 3. Detailed Implementation
[0029] The present application will be further described in detail below with reference to the embodiments.
[0030] Example 1
[0031] A synergistic exfoliating composition is formulated from adenosine, N-acetylneuraminic acid, and lactobionic acid.
[0032] The mass ratio of adenosine, N-acetylneuraminic acid, and lactobionic acid is 0.09:0.25:0.45.
[0033] Example 2
[0034] A synergistic exfoliating composition is formulated from adenosine, N-acetylneuraminic acid, and lactobionic acid.
[0035] The mass ratio of adenosine, N-acetylneuraminic acid, and lactobionic acid is 0.1:0.3:0.5.
[0036] Example 3
[0037] A synergistic exfoliating composition is formulated from adenosine, N-acetylneuraminic acid, and lactobionic acid.
[0038] The mass ratio of adenosine, N-acetylneuraminic acid, and lactobionic acid is 0.11:0.35:0.55.
[0039] Comparative Example 1 A synergistic exfoliating composition, differing from Example 2 only in that: Papain was used to replace N-acetylneuraminic acid in an equal amount.
[0040] Papain was purchased from Guangzhou Longde Biotechnology Co., Ltd., with an enzyme activity of 100,000 u / g.
[0041] Comparative Example 2 A synergistic exfoliating composition, differing from Example 2 only in that: Salicylic acid was used to replace lactobionic acid in equal amounts.
[0042] Salicylic acid was purchased from Shandong Binzhou Zhiyuan Biotechnology Co., Ltd., with a content of 40%.
[0043] Comparative Example 3 A synergistic exfoliating composition, differing from Example 2 only in that: Bromelain was used to replace adenosine in an equal amount.
[0044] Bromelain was purchased from Guangdong Mingtong Biotechnology Co., Ltd., with an enzyme activity of 100,000 u / g.
[0045] Comparative Example 4 A synergistic exfoliating composition, differing from Example 2 only in that: Papain was used to replace N-acetylneuraminic acid in equal amounts, salicylic acid was used to replace lactobionic acid in equal amounts, and bromelain was used to replace adenosine in equal amounts.
[0046] Papain was purchased from Guangzhou Longde Biotechnology Co., Ltd., with an enzyme activity of 100,000 u / g.
[0047] Salicylic acid was purchased from Shandong Binzhou Zhiyuan Biotechnology Co., Ltd., with a content of 40%.
[0048] Bromelain was purchased from Guangdong Mingtong Biotechnology Co., Ltd., with an enzyme activity of 100,000 u / g.
[0049] Application Example 1 A controlled-release carrier for a synergistic exfoliating composition is prepared as follows: Step 1): Add 0.09 kg N-acetylneuraminic acid, 0.25 kg lactobionic acid, 0.45 kg adenosine, and 58.41 kg PBS buffer with pH 6.5-7 into a stirred tank and stir at 60 r / min for 5-8 min to obtain the aqueous phase.
[0050] Step 2): 2.8 kg hydrogenated lecithin, 1.8 kg lecithin, 4.8 kg caprylic / capric triglyceride, 0.09 kg beeswax, 0.13 kg glyceryl stearate, 0.18 kg ceramide NP, and 31 kg ethanol are added to a stirring vessel and stirred at 60 r / min for 5-8 min to obtain a composite lipid phase.
[0051] Step 3) Inject the composite lipid into the aqueous phase and stir at 10-20 r / min for 60-70 min to obtain the mixed phase.
[0052] Step 4) The mixed phase is fed into a high-pressure microjet device and homogenized and circulated 3 times at a pressure of 15000psi. The product is then discharged to obtain a controlled-release carrier with a synergistic exfoliating composition.
[0053] N-acetylneuraminic acid was purchased from Guangzhou Yuexing Cosmetics Co., Ltd.
[0054] Lactobionic acid was purchased from Zhejiang Ruiyan New Materials Technology Co., Ltd.
[0055] Adenosine was purchased from Guilin Huazhang Chuangmei Biotechnology Co., Ltd.
[0056] PBS buffer was purchased from Shanghai Shangbao Biotechnology Co., Ltd., specification: 0.01M, pH 6.8.
[0057] Hydrogenated lecithin was purchased from Guangzhou Chengzhi Trading Co., Ltd.
[0058] Lecithin was purchased from Guangzhou Chengzhi Trading Co., Ltd.
[0059] Caprylic / capric triglyceride was purchased from Gosei Chemical Industry Co., Ltd.
[0060] The beeswax was purchased from Henan Fumei Biotechnology Co., Ltd.
[0061] Glyceryl stearate was purchased from Zhejiang Wumart Biotechnology Co., Ltd.
[0062] Ceramide NP was purchased from Hangzhou Weibaolai Biotechnology Co., Ltd.
[0063] The ethanol was commercially available and had a concentration of 95%.
[0064] Application Example 2 A controlled-release carrier for a synergistic exfoliating composition is prepared as follows: Step 1): Add 0.1 kg N-acetylneuraminic acid, 0.3 kg lactobionic acid, 0.5 kg adenosine, and 56.65 kg PBS buffer with pH 6.5-7 into a stirred tank and stir at 60 r / min for 5-8 min to obtain the aqueous phase.
[0065] Step 2): Add 3 kg of hydrogenated lecithin, 2 kg of lecithin, 5 kg of caprylic / capric triglyceride, 0.1 kg of beeswax, 0.15 kg of glyceryl stearate, 0.2 kg of ceramide NP, and 32 kg of ethanol into a stirring vessel and stir at 60 r / min for 5-8 min to obtain a composite lipid phase.
[0066] Step 3) Inject the composite lipid into the aqueous phase and stir at 10-20 r / min for 60-70 min to obtain the mixed phase.
[0067] Step 4) The mixed phase is fed into a high-pressure microjet device and homogenized and circulated 3 times at a pressure of 15000psi. The product is then discharged to obtain a controlled-release carrier with a synergistic exfoliating composition.
[0068] N-acetylneuraminic acid was purchased from Guangzhou Yuexing Cosmetics Co., Ltd.
[0069] Lactobionic acid was purchased from Zhejiang Ruiyan New Materials Technology Co., Ltd.
[0070] Adenosine was purchased from Guilin Huazhang Chuangmei Biotechnology Co., Ltd.
[0071] PBS buffer was purchased from Shanghai Shangbao Biotechnology Co., Ltd., specification: 0.01M, pH 6.8.
[0072] Hydrogenated lecithin was purchased from Guangzhou Chengzhi Trading Co., Ltd.
[0073] Lecithin was purchased from Guangzhou Chengzhi Trading Co., Ltd.
[0074] Caprylic / capric triglyceride was purchased from Gosei Chemical Industry Co., Ltd.
[0075] The beeswax was purchased from Henan Fumei Biotechnology Co., Ltd.
[0076] Glyceryl stearate was purchased from Zhejiang Wumart Biotechnology Co., Ltd.
[0077] Ceramide NP was purchased from Hangzhou Weibaolai Biotechnology Co., Ltd.
[0078] The ethanol was commercially available and had a concentration of 95%.
[0079] Application Example 3 A controlled-release carrier for a synergistic exfoliating composition is prepared as follows: Step 1): Add 0.11 kg N-acetylneuraminic acid, 0.35 kg lactobionic acid, 0.55 kg adenosine, and 54.89 kg PBS buffer with pH 6.5-7 into a stirred tank and stir at 60 r / min for 5-8 min to obtain the aqueous phase.
[0080] Step 2): Add 3.2 kg hydrogenated lecithin, 2.2 kg lecithin, 5.2 kg caprylic / capric triglyceride, 0.11 kg beeswax, 0.17 kg glyceryl stearate, 0.22 kg ceramide NP, and 33 kg ethanol into a stirred tank and stir for 5-8 minutes at 60 r / min to obtain a composite lipid phase.
[0081] Step 3) Inject the composite lipid into the aqueous phase and stir at 10-20 r / min for 60-70 min to obtain the mixed phase.
[0082] Step 4) The mixed phase is fed into a high-pressure microjet device and homogenized and circulated 3 times at a pressure of 15000psi. The product is then discharged to obtain a controlled-release carrier with a synergistic exfoliating composition.
[0083] N-acetylneuraminic acid was purchased from Guangzhou Yuexing Cosmetics Co., Ltd.
[0084] Lactobionic acid was purchased from Zhejiang Ruiyan New Materials Technology Co., Ltd.
[0085] Adenosine was purchased from Guilin Huazhang Chuangmei Biotechnology Co., Ltd.
[0086] PBS buffer was purchased from Shanghai Shangbao Biotechnology Co., Ltd., specification: 0.01M, pH 6.8.
[0087] Hydrogenated lecithin was purchased from Guangzhou Chengzhi Trading Co., Ltd.
[0088] Lecithin was purchased from Guangzhou Chengzhi Trading Co., Ltd.
[0089] Caprylic / capric triglyceride was purchased from Gosei Chemical Industry Co., Ltd.
[0090] The beeswax was purchased from Henan Fumei Biotechnology Co., Ltd.
[0091] Glyceryl stearate was purchased from Zhejiang Wumart Biotechnology Co., Ltd.
[0092] Ceramide NP was purchased from Hangzhou Weibaolai Biotechnology Co., Ltd.
[0093] The ethanol was commercially available and had a concentration of 95%.
[0094] Comparative Application Example 1 A controlled-release carrier for a synergistic exfoliating composition, differing from Application Example 2 only in that: The ceramide NP was replaced with an equal amount of Tween-80.
[0095] Tween-80 was purchased from Jinan Aoxing Chemical Co., Ltd., with a purity of 99%.
[0096] Comparison of application examples A controlled-release carrier for a synergistic exfoliating composition is prepared as follows: Step 1): Add 0.09 kg N-acetylneuraminic acid, 0.25 kg lactobionic acid, 0.45 kg adenosine, and 58.41 kg PBS buffer with pH 6.5-7 into a stirred tank and stir at 60 r / min for 5-8 min to obtain the aqueous phase.
[0097] Step 2): 2.8 kg hydrogenated lecithin, 1.8 kg lecithin, 4.8 kg caprylic / capric triglyceride, 0.09 kg beeswax, 0.13 kg glyceryl stearate, 0.18 kg ceramide NP, and 31 kg ethanol are added to a stirring vessel and stirred at 60 r / min for 5-8 min to obtain a composite lipid phase.
[0098] Step 3) Inject the composite lipid into the aqueous phase and stir at 10-20 r / min for 60-70 min to obtain a controlled-release carrier with a synergistic exfoliating composition.
[0099] N-acetylneuraminic acid was purchased from Guangzhou Yuexing Cosmetics Co., Ltd.
[0100] Lactobionic acid was purchased from Zhejiang Ruiyan New Materials Technology Co., Ltd.
[0101] Adenosine was purchased from Guilin Huazhang Chuangmei Biotechnology Co., Ltd.
[0102] PBS buffer was purchased from Shanghai Shangbao Biotechnology Co., Ltd., specification: 0.01M, pH 6.8.
[0103] Hydrogenated lecithin was purchased from Guangzhou Chengzhi Trading Co., Ltd.
[0104] Lecithin was purchased from Guangzhou Chengzhi Trading Co., Ltd.
[0105] Caprylic / capric triglyceride was purchased from Gosei Chemical Industry Co., Ltd.
[0106] The beeswax was purchased from Henan Fumei Biotechnology Co., Ltd.
[0107] Glyceryl stearate was purchased from Zhejiang Wumart Biotechnology Co., Ltd.
[0108] Ceramide NP was purchased from Hangzhou Weibaolai Biotechnology Co., Ltd.
[0109] The ethanol was commercially available and had a concentration of 95%.
[0110] Experiment 1 The effect of the analyte on the cytotoxicity of HaCaT and RAW 264.7 cells was determined by MTT assay: HaCaT or RAW264.7 cells were used at a cell density of 8000 cells / cm³. 2 The cells were seeded into 96-well plates. After co-culturing the test samples prepared in each example or comparative example with HaCaT cells for 48 hours, MTT reagent was added, and the cells were incubated for 4 hours. DMSO was then added, and the absorbance of each group of cells was measured at 490 nm. Cell viability (%) was calculated. The formula for calculating cell viability is as follows: Cell viability = (A 样品组 -A 空白对照组 ) / (A 阴性对照组 -A 空白对照组 ) Where A represents the absorbance value, the negative control group is the absorbance of cells that have not been treated with the drug, the blank control group is the absorbance of the 96-well plate itself, and the sample group is the absorbance of cells treated with the drug in each example or comparative example.
[0111] Test sample: Take 0.9g of the synergistic exfoliating composition and 99.1g of deionized water, mix them evenly to obtain the test sample.
[0112] Experiment 2 HaCaT cells in the logarithmic growth phase with good morphology were seeded into 6-well plates at a density of 10⁶ cells / well. A blank control group and test samples prepared according to various examples or comparative examples were set up and incubated at 37°C in a 5% CO₂ incubator for 12 hours. Except for the blank control group, each well contained samples from various examples or comparative examples and was incubated for 12 hours. The cell supernatant was collected, and the number of exfoliated keratinocytes was determined using a cell counter.
[0113] Cell counting method: The cell counting chamber method was used. 10 μL of cell suspension was taken and 10 μL of PBS was added and mixed by pipetting. 10 μL of the above liquid was then dropped onto the grid area of the counting chamber and the cells were counted under a microscope.
[0114] The calculation formula is as follows: Cell count (cells / mL) = (N / 4) × 2 × 10000; N is the total number of cells on the counting plate; 4 represents the four areas used for counting on the counting board; 2 represents the dilution factor.
[0115] Test sample: Take 0.9g of the synergistic exfoliating composition and 99.1g of deionized water, mix them evenly to obtain the test sample.
[0116] The detailed experimental data for Experiments 1-2 are shown in Table 1.
[0117]
[0118] According to the data in Table 1, the combination of adenosine, N-acetylneuraminic acid, and lactobionic acid in the embodiment not only has a more significant effect on exfoliating keratinocytes, but also has lower irritation, achieving better removal of keratin while being gentle and low-irritant.
[0119] Experiment 3 Preparation of dialysis bag samples: Experimental group: Dialysis bags with a permeability of 1000 Da were used and completely immersed in water. 8 mL of PBS, 1 mL of each application example or control application example, and 1 mL of lipase solution with an enzyme activity of 20 U / g were added to the dialysis bag.
[0120] Control group 1: A dialysis bag with a permeability of 1000 Da was selected, and it was completely soaked in water. 8 mL of PBS, 1 mL of each application case or control application case, and 1 mL of water were added to the dialysis bag.
[0121] Control group 2: A dialysis bag with a permeability of 1000 Da was selected, and it was completely soaked in water. 8 mL of PBS, 1 mL of control application example, and 1 mL of water were added to the dialysis bag.
[0122] Experimental steps: After completely sealing the dialysis bag, place it in a beaker and add 30% ethanol solution as the receiving solution. Set the water bath temperature to 37±1℃ and continuously stir the receiving solution at 600rpm. Take samples of the receiving solution at 0h, 2h, 4h, 8h, 12h, 24h, and 48h, centrifuge at 12000rpm for 10min, collect the supernatant, filter it through a 0.22μm filter membrane, and perform ultraviolet spectrophotometric detection to calculate the cumulative release.
[0123] Dialysis bags can effectively separate the encapsulated object from the encapsulated material, allowing the encapsulated object to pass through the dialysis membrane into the receiving solution, thereby reducing errors in subsequent testing.
[0124] Ultraviolet spectrophotometric testing method (using adenosine release rate as the test standard): 1. Preparation of standard curve: Take an appropriate amount of adenosine, dissolve it in PBS, and prepare samples with concentrations of (1 mg / mL, 3 mg / mL, 5 mg / mL, 7 mg / mL, 9 mg / mL, 11 mg / mL). Measure the absorbance at 256 nm and plot the standard curve. R² ≥ 0.99 is required.
[0125] 2. Perform dialysis as described above, collect the receiving solution at the set time points, and replenish the receiving solution in the receiving pool.
[0126] 3. Take the above receiving solution and perform ultraviolet spectrophotometry at 256 nm. The absorbance shown is recorded as A. Substitute A into the above standard curve to calculate the adenosine concentration at the sampling time point, and record it as c.
[0127] 4. Calculate the cumulative release rate using the following formula: Cumulative release rate (%) = V × cn (c1 + c2 + c3) Vq / M.
[0128] In the formula: V is the total volume of the receiving liquid; cn represents the adenosine concentration at the nth sampling point; c1 / c2 / c3 represent the concentrations of adenosine during the 1st, 2nd, and 3rd samplings; Vq is the sampling volume; M represents the total mass of adenosine.
[0129] For detailed experimental data of Experiment 3, please refer to [link / reference]. Figure 1-4 .
[0130] according to Figure 1-4 It can be seen that in each application example, under the action of lipase, the nanocarrier can break down more quickly, thereby rapidly releasing the synergistic exfoliating composition. However, without the action of lipase, the nanocarrier has higher stability and will not rapidly release the synergistic exfoliating composition, thus achieving the effect of intelligently identifying oily areas of the skin and achieving targeted exfoliation in the oily areas of the skin.
[0131] In contrast, the application example showed a significant decrease in sensitivity to lipase. Even when the nanocarrier disintegrated faster under the action of lipase, the disintegration rate was much lower than that of the application example. Although it could improve the release rate of the synergistic exfoliating composition to some extent, it could not achieve a rapid release effect and could not achieve the effect of intelligently identifying oily areas of the skin.
[0132] This specific embodiment is merely an explanation of this application and is not intended to limit it. After reading this specification, those skilled in the art can make modifications to this embodiment without contributing any inventive step, but such modifications are protected by patent law as long as they fall within the scope of the claims of this application.
Claims
1. A synergistic exfoliating composition, characterized in that: It is composed of adenosine, N-acetylneuraminic acid and lactobionic acid.
2. The synergistic exfoliating composition according to claim 1, characterized in that: The mass ratio of adenosine, N-acetylneuraminic acid, and lactobionic acid is 0.09-0.11:0.25-0.35:0.45-0.
55.
3. A controlled-release carrier comprising the synergistic exfoliating composition as described in claim 1 or 2, characterized in that: It includes a synergistic exfoliating composition and a nanocarrier, wherein the synergistic exfoliating composition is encapsulated in the nanocarrier.
4. The controlled-release carrier of the synergistic exfoliating composition according to claim 3, characterized in that: The nanocarrier is composed of lipid materials and modifiers.
5. A controlled-release carrier for a synergistic exfoliating composition according to claim 4, characterized in that: The lipid material is one or more of the following: hydrogenated lecithin, lecithin, caprylic / capric triglyceride, beeswax, glyceryl stearate, PEG-20 glyceryl triisostearate, glyceryl distearate, PEG-50 shea butter, polyglycerol-2 laurate, PEG-6 caprylic / capric triglyceride, hydrogenated coconut oil triglyceride, PEG-7 glyceryl coconut oil ester, polyglycerol-3 diisostearate, and polyglycerol-2 triisostearate.
6. A controlled-release carrier for a synergistic exfoliating composition according to claim 5, characterized in that: The modifier is one or more of the following: ceramide NP, ceramide NH, ceramide AS, ceramide NS, ceramide EOS, and ceramide EOP.
7. A controlled-release carrier with a synergistic exfoliating composition according to claim 6, characterized in that: The lipid material is a compound of hydrogenated lecithin, lecithin, caprylic / capric triglyceride, beeswax, and glyceryl stearate. The modifier is ceramide NP. The mass ratio of hydrogenated lecithin, lecithin, caprylic / capric triglyceride, beeswax, glyceryl stearate, and ceramide NP is 2.8-3.2: 1.8-2.2: 4.8-5.2: 0.09-0.11: 0.13-0.17: 0.18-0.
22.
8. The application of a controlled-release carrier having a synergistic exfoliating composition according to any one of claims 3-7, characterized in that: The controlled-release carrier of the synergistic exfoliating composition is added to a cosmetic formulation to prepare a cosmetic with exfoliating effects.
9. A method for preparing a controlled-release carrier having a synergistic exfoliating composition according to any one of claims 3-7, characterized in that: Includes the following steps: Step 1), N-acetylneuraminic acid, lactobionic acid, and adenosine are dissolved in an aqueous solvent to form the aqueous phase; Step 2), the lipid material and modifier are dissolved in an alcohol solvent to form a composite lipid phase; Step 3), mix the aqueous phase with the composite lipid phase to obtain a mixed phase; Step 4) The mixed phase is homogenized to obtain a controlled-release carrier with a synergistic exfoliating composition.
10. A method for preparing a controlled-release carrier of a synergistic exfoliating composition according to claim 9, characterized in that: The aqueous solvent is PBS buffer, the pH of the PBS buffer is 6.5-7, and the alcohol solvent is ethanol.