A composition containing nicotinamide ethyl retinoate and a preparation method thereof

Abstract

The present invention relates to a composition containing nicotinamide ethyl retinoate and a preparation method thereof, which is characterized in that it is composed of the following components in mass percentages: 0.1% - 15% of nicotinamide ethyl retinoate, 0.025 - 15% of a mercapto-containing glycine derivative, 1 - 30% of an auxiliary agent, 0.25 - 5% of a co-emulsifier, 0.5 - 10% of inulin lauryl carbamate, 10% - 70% of a polyol, and the balance of water. The composition containing nicotinamide ethyl retinoate prepared by the present invention solves the problems of dissolution, easy color change, instability and irritation of nicotinamide ethyl retinoate. The composition not only has the beneficial effects of convenient use, good stability, good mildness, significant whitening and anti-wrinkle effects, but also has a synergistic effect.

Description

Technical Field

[0001] The present invention relates to the field of cosmetics, and particularly to a composition containing niacinamidoethyl retinoate and a preparation method thereof. Background Art

[0002] Niacinamidoethyl retinoate is an innovative vitamin A derivative synthesized from retinoic acid and hydroxyethyl nicotinamide, and its structural formula is as Figure 1 shown.

[0003] Niacinamidoethyl retinoate simultaneously has the functions of two popular functional ingredients in the skin care products industry, namely vitamin A (retinol) and vitamin B3 (niacinamide). It is reported that niacinamidoethyl retinoate has the effects of whitening and brightening the skin color, and can significantly reduce fine lines and wrinkles, providing a fresh, even skin color and a healthy glow.

[0004] However, niacinamidoethyl retinoate also has disadvantages. One is that its stability is not good enough. Because it contains more double bonds in its molecular structure, it is easily attacked by oxygen free radicals and degraded in water. Through experiments, when 0.1% niacinamidoethyl retinoate and 0.1% Tween-20 are mixed and dissolved in water, and stored in a transparent bottle inside the south window for 1 week, the content of niacinamidoethyl retinoate will be reduced to 73% of the original content, and the content of retinoic acid can be detected as 70 ppm; in a light-proof environment, when stored at 45 °C for 1 month, the content will also be reduced to 82% of the original content, and the content of retinoic acid can be detected as 30 ppm. Since retinoic acid is a prohibited ingredient in cosmetics, a method to stabilize niacinamidoethyl retinoate is particularly needed to prevent its decomposition, maintain the stability during the shelf life, and ensure that the cosmetics meet the regulatory requirements. The other is that the irritation of niacinamidoethyl retinoate is still relatively large. According to the evaluation principle of the skin occlusion patch test, among 30 subjects, the number of subjects with grade 1 skin adverse reactions should not exceed 5 cases (excluding 5 cases), or the number of subjects with grade 2 skin adverse reactions should not exceed 2 cases (for the patch test of deodorant products, the number of subjects with grade 1 skin adverse reactions should not exceed 10 cases, and the number of subjects with grade 2 skin adverse reactions should not exceed 5 cases), or no case of grade 3 or above skin adverse reaction should occur. If the above principle requirements are exceeded, it indicates that the test substance may cause adverse reactions to human skin. For the sample of 0.1% niacinamidoethyl retinoate and 0.1% Tween-20 mixed and dissolved in water, the patch test shows that among 30 subjects, the number of subjects with grade 1 skin adverse reactions is 12 cases. Therefore, it is judged that the irritation is strong and it cannot pass the human skin patch test specified in the "Technical Specifications for Cosmetics Safety". Therefore, a method to reduce the irritation of niacinamidoethyl retinoate is also needed.

[0005] N-(2-Mercaptopropionyl) glycine, also known as tiopronin with CAS No: 1953-02-2, is a drug used to improve the liver function of various acute and chronic hepatitis. This molecule can eliminate free radicals by combining with free radicals through its mercapto group. Its structural formula is as shown in Figure 2 shown.

[0006] 2-mercaptonicotinoyl glycine, whose structural formula is as shown in Figure 3 shown, is similar to N-(2-mercaptopropionyl) glycine and also has a mercapto group, which can eliminate free radicals.

[0007] N-(2-Mercaptopropionyl) glycine and 2-mercaptonicotinoyl glycine have a mercapto group in their molecular structures, possess reducibility, and can protect components that are easily oxidized. N-(2-Mercaptopropionyl) glycine and 2-mercaptonicotinoyl glycine also have whitening effects. It is reported that in the same cosmetic formulation, 0.5% of 2-mercaptonicotinoyl glycine has a better anti-pigmentation effect than 7% of vitamin C. In theory, they can also be used as useful whitening components in cosmetics.

[0008] Inulin lauryl carbamate is a high-molecular emulsifier. Due to its high molecular weight, it brings a steric effect and has a slow penetration rate through the skin cutin layer. The emulsion formed by emulsifying with it as the main emulsifier has the effects of long-term slow release and reducing irritation. However, the emulsifying power of inulin lauryl carbamate is not strong, and usually a co-emulsifier needs to be compounded to obtain better emulsification stability. Therefore, for some cosmetic efficacy active substances with irritation, by using inulin lauryl carbamate as the main emulsifier and compounding a small amount of other co-emulsifiers, a stable emulsion with less skin irritation can be obtained. Summary of the Invention

[0009] The technical problem to be solved by the present invention is to provide a composition containing nicotinamide ethyl retinoate and its preparation method.

[0010] To solve the above technical problem, the present invention adopts the following technical scheme. A composition containing nicotinamide ethyl retinoate is characterized by comprising the following raw material components in mass percentages: 0.1% - 15% nicotinamide ethyl retinoate, 0.025 - 15% glycine derivative containing a mercapto group, 1 - 30% auxiliary agent, 0.25 - 5% co-emulsifier, 0.5 - 10% inulin lauryl carbamate, 10% - 70% polyol, and the balance being water; the mass ratio of nicotinamide ethyl retinoate to glycine mercapto derivative is 1:0.25 - 1.

[0011] The mercapto-containing glycine derivative is preferably one of N-(2-mercaptopropionyl)-glycine and 2-mercaptonicotinoyl glycine, or any mixture thereof in any mass ratio.

[0012] The nicotinamide ethyl retinoate, of analytical grade, is from Aladdin Reagent (Shanghai) Co., Ltd.

[0013] The N-(2-mercaptopropionyl)-glycine, with CAS number 1953-02-2 and of analytical grade, is from Sigma-Aldrich (Shanghai) Trading Co., Ltd.

[0014] The 2-mercaptonicotinoyl glycine, of analytical grade, is from Tokyo Chemical Industry Co., Ltd.

[0015] The inulin lauryl carbamate, of analytical grade, is from Shanghai Macklin Biochemical Co., Ltd.

[0016] The auxiliary agent is selected from a synthetic oil or a vegetable oil, and examples include isononyl isononanoate, caprylic / capric triglyceride, hexyl decanol, octyldodecanol, propylene carbonate, C12-15 alkyl benzoate, squalane, hydrogenated polyisobutene, macadamia nut oil, and Limnanthes alba seed oil, or any mixture thereof in any ratio.

[0017] The co-emulsifier is selected from lecithin, hydrogenated lecithin, lysolecithin, hydrogenated lysolecithin, polysorbate-20, polysorbate-40, polysorbate-60, polysorbate-80, sucrose laurate, sucrose palmitate, sucrose stearate, polyglyceryl-10 laurate, polyglyceryl-10 myristate, polyglyceryl-10 stearate, polyglyceryl-10 oleate, and polyglyceryl-10 dioleate, or any mixture thereof in any ratio.

[0018] The polyol is one of glycerol, 1,2-propanediol, 1,3-propanediol, 1,3-butanediol, dipropylene glycol, 1,2-pentanediol, and 1,2-hexanediol, or any mixture thereof in any proportion.

[0019] A preparation method of a composition containing nicotinamide ethyl retinoate, characterized by the following steps:

[0020] A. Weigh 0.1% - 15% of nicotinamide ethyl retinoate, 0.025% - 15% of the mercapto-containing glycine derivative, 1% - 30% of the auxiliary agent, 0.25% - 5% of the co-emulsifier, 0.5% - 10% of inulin lauryl carbamate, 10% - 60% of the polyol, and the balance of water by mass percentage;

[0021] B. Weigh the nicotinamide ethyl retinoate, mercapto-containing glycine derivative, and auxiliary agent obtained in step A, and stir them at a speed of 400 - 1000 rpm with a stirrer at 60 - 70 °C until they are evenly mixed to obtain the internal phase;

[0022] C. Weigh the inulin lauryl carbamate, co-emulsifier, water, and polyol obtained in step A, and stir them at a speed of 400 - 1000 rpm with a stirrer at 60 - 70 °C until they are evenly mixed to obtain the external phase;

[0023] D. Load the internal phase obtained in step B and the external phase obtained in step C into a lipid nanoparticle synthesizer, set the mass ratio of the internal phase to the external phase to 1:0.5 - 90, and the total flow rate of the internal and external phases to 10 - 20 mL / min. Collect the effluent liquid at the outlet to obtain a composition containing nicotinamide ethyl retinoate with a particle size of 50 - 300 nm.

[0024] The lipid nanoparticle synthesizer is the lipid nanoparticle synthesizer model LNP - S1 produced by Shanghai Pengzan Biotechnology Co., Ltd.

[0025] The beneficial effects of the present invention are as follows: (1) The composition containing nicotinamide ethyl retinoate obtained in the present invention has good stability, without stratification, color change, or precipitation, and the retinoic acid content is not detected under various stability test conditions; (2) The composition containing nicotinamide ethyl retinoate obtained in the present invention is mild in nature and has no irritation through patch testing; (3) The composition containing nicotinamide ethyl retinoate obtained in the present invention has the effects of whitening and anti-wrinkle enhancement, and has a better effect compared with the same content of nicotinamide ethyl retinoate used alone.

[0026] To prove the beneficial effects of the present invention, the following experiments were conducted.

[0027] Prepare the composition containing nicotinamide ethyl retinoate according to the mass percentages of each substance shown in Table 1 and the preparation method described in each embodiment. The specific composition and process operations of Examples 1 - 5 can be seen in the detailed description of the example part later.

[0028] Comparative Example 1 uses the same components as Example 3, but does not use the preparation method described in Example 3 of the present invention, and only simply stirs and mixes them.

[0029] Comparative Example 2 uses the preparation method described in Example 3 of the present invention, but does not add the mercapto-containing glycine derivative, and the other components are the same as those in Example 3.

[0030] Comparative Example 3 uses the preparation method described in Example 3 of the present invention, but does not add the auxiliary agent, and the other components are the same as those in Example 3.

[0031] Comparative Example 4 uses the preparation method described in Example 3 of the present invention, but does not add the co-emulsifier, and the other components are the same as those in Example 3.

[0032] Comparative Example 5 adopted the preparation method described in Example 3 of the present invention, but did not add inulin lauryl carbamate, and other components were the same as those in Example 3.

[0033] Comparative Example 6 adopted the preparation method described in Example 3 of the present invention, but did not add water, and other components were the same as those in Example 3.

[0034] Comparative Example 7 adopted the preparation method described in Example 3 of the present invention, but did not add polyol, and other components were the same as those in Example 3.

[0035] Table 1 Mass percentages of each component and preparation method in examples and comparative examples

[0036]

[0037] Stability test

[0038] The above samples were respectively placed under the conditions of 5 °C, 25 °C, 45 °C and room temperature light for stability experiments, and whether there were precipitation, stratification and discoloration phenomena in the samples was observed at 2 weeks, 4 weeks, 8 weeks and 12 weeks. The stability test results are shown in Table 2.

[0039] Table 2 Stability test results

[0040]

[0041] ○ indicates no stratification and no precipitation; / indicates insoluble.

[0042] As can be seen from the stability test results in Table 2, for the samples of Comparative Examples 1-7 subjected to stability experiments under the conditions of 5 °C, 25 °C, 45 °C and light, there were precipitation, stratification, discoloration and other conditions to varying degrees after 2 weeks, 4 weeks, 8 weeks and 12 weeks. However, there were no precipitation, stratification and discoloration in Examples 1-5 of the present invention under the same test conditions. It shows that the composition of nicotinamide ethyl retinoate prepared by the present invention has better light stability and thermal stability.

[0043] For the samples of the above stability experiments respectively placed under the conditions of 25 °C, 45 °C and light, the retinoic acid content was measured by HPLC at 2 weeks, 4 weeks, 8 weeks and 12 weeks. The specific method was to use methanol as the mobile phase, and the chromatographic column was selected as Eclipse XDB-C18, 5 μm, 250 mm * 4.6 mm or an equivalent chromatographic column, the column temperature was 35 °C, the flow rate was 1.0 mL / min, the detection wavelength was 355 nm, and the injection volume was 10 μL. The detection results of retinoic acid are shown in Table 3.

[0044] Table 3 Test Results of Retinoic Acid Content

[0045]

[0046] As can be seen from the test results of retinoic acid in Table 3, for the samples of Comparative Examples 1-7 subjected to stability experiments at 25 °C, 45 °C and under light conditions, retinoic acid was detected in varying degrees after 2 weeks, 4 weeks, 8 weeks and 12 weeks. Among them, the detected value of retinoic acid in Comparative Example 2 was as high as 300 ppm after 12 weeks at 45 °C. However, for the samples of Examples 1-5 of the present invention subjected to stability experiments at 25 °C, 45 °C and under light conditions, no retinoic acid was detected after 2 weeks, 4 weeks, 8 weeks and 12 weeks. This further demonstrates that the composition of nicotinamide ethyl retinoate prepared by the present invention has better light stability and thermal stability.

[0047] Gentleness Experiment<s

[0048] Sixty volunteers aged 18-60 years were selected for gentleness testing according to the "Cosmetics Safety and Technology Standards 2015 Edition" - Human Skin Patch Test. The exclusion criteria for the subjects met the "Diagnostic Criteria and Treatment Principles for Cosmetic Contact Dermatitis" of GB17\(1492 - 1997\), with no serious systemic diseases, no immunodeficiency or autoimmune diseases, no active allergic diseases, no history of allergies to skin care cosmetics, no systemic use of hormonal drugs and immunosuppressants within 1 month, not pregnant or lactating, and no ethical taboos.

[0049] Table 4 Composition of the Cream Samples for Gentleness Test

[0050]

[0051] Examples 1-5 were added to the cream at a dosage of 2% respectively, and the cream formula composition is shown in Table 4. Since the pure nicotinamide ethyl retinoate has strong irritation, out of humanitarian spirit, no human patch test was conducted. The above samples were placed in a patch tester and applied to the back of the subjects with non-irritating tape for 24 h. At the same time, a blank patch tester was applied as a blank control. After removing the test patch tester, the skin reactions were observed at \(0.5\) h, 24 h and 48 h respectively. The reaction results were recorded according to the grading standard. Grade 0 indicates no stinging sensation, Grade 1 indicates almost no stinging sensation, Grade 2 indicates mild stinging sensation, Grade 3 indicates moderate stinging sensation, and Grade 4 indicates severe stinging sensation, which was used as the standard for evaluating gentleness. The experimental results are shown in Table 5.

[0052] Table 5 Test Results of Gentleness Experiment

[0053]

[0054] As can be seen from Table 5, in the patch tests conducted on Examples 1-5, the subjects had no adverse reactions, indicating that the composition containing nicotinamide ethyl retinoate prepared by the present invention has good mildness.

[0055] Human efficacy test

[0056] According to the principle of voluntariness, 90 non-pregnant, non-lactating and non-puerperal female volunteers aged 18-55 with dull skin color and wrinkles at the corners of the eyes were selected and randomly divided into three groups: an experimental group and control groups A and B. In the experimental group, the cream described in Table 4 above containing Example 4 was used after morning and evening face cleansing for 28 consecutive days. Control group A used a blank control cream without the composition containing nicotinamide ethyl retinoate (the usage amount was kept consistent, about 0.5 g / time), and control group B used a cream containing the pure product of nicotinamide ethyl retinoate with the same content of nicotinamide ethyl retinoate as in Example 4 (the usage amount was kept consistent, about 0.5 g / time). During the period, no other skin care products were used. The experiment required the volunteers to mainly engage in indoor activities during the test period and avoid long-term unprotected exposure to sunlight. The faces and corners of the eyes of the volunteers were selected as the test sites, and the tests were conducted after the volunteers' face cleansing before use and 28 days after use. The skin melanin content of the subjects was tested using the MX18 melanin meter of CK Company, Germany. The lower the measured value, the less the skin melanin content; the skin glossiness value was detected using the Glossymeter GL 200 skin moisture tester. The higher the measured value, the higher the skin glossiness; the number of wrinkles and the average depth of total wrinkles were measured using the PROMIS LITE wrinkle meter of LMI Technologies Company, Germany. The human efficacy test results are shown in Table 6.

[0057] Table 6 Human efficacy test results

[0058]

[0059] As can be seen from Table 6, after 28 days of continuous use, the melanin content in the skin of the experimental group decreased significantly by 23.40%, the skin gloss increased by 36.34%; the number of wrinkles decreased by 24.47%, and the average depth of total wrinkles also decreased by 21.71%. However, the cream of control group A that did not use the nicotinamide ethyl retinoate composition prepared by the present invention had no obvious improvement effect on melanin content, skin gloss, number of wrinkles, and average depth of total wrinkles. In control group B, a pure cream with the same content of nicotinamide ethyl retinoate as in the experimental group was used. After 28 days of continuous use, the melanin content in the skin only decreased by 11.57%, the skin gloss increased by 21.85%; the number of wrinkles decreased by 12.29%, and the average depth of total wrinkles also decreased by 11.67%. The relevant test data were significantly lower than those of the experimental group. This shows that a nicotinamide ethyl retinoate composition prepared by the present invention has better whitening and anti-wrinkle effects. In addition, in control group B with the same content of nicotinamide ethyl retinoate as in the experimental group, during the test, 8 testers reported allergies and stopped using, while no allergic reactions occurred in the subjects of the experimental group. This also shows that the sample of the embodiment of the present invention has good mildness.

[0060] In summary, a nicotinamide ethyl retinoate composition prepared by the present invention has the beneficial effects of good stability, good mildness, and remarkable whitening and anti-wrinkle effects. Brief Description of the Drawings

[0061] Figure 1 is the structural formula of nicotinamide ethyl retinoate;

[0062] Figure 2 is the structural formula of N-(2-mercaptopropionyl)-glycine;

[0063] Figure 3 is the structural formula of 2-mercaptonicotinoyl glycine. Detailed Embodiments

[0064] Example 1: A nicotinamide ethyl retinoate composition and its preparation method, which are characterized by adopting the following steps:

[0065] A. Weigh 0.1% of nicotinamide ethyl retinoate, 0.025% of 2-mercaptonicotinoyl glycine, 1% of caprylic / capric triglyceride, 0.25% of sucrose laurate, 0.5% of inulin lauryl carbamate, 50% of glycerol, 10% of 1,3-butanediol and the balance of water by mass percentage; the ratio of nicotinamide ethyl retinoate to glycine mercapto derivative is 1:0.25;

[0066] B. Stir the nicotinamide ethyl retinoate, glycine derivative containing mercapto, and auxiliary agent weighed in step A at 60 °C with a stirrer at a speed of 400 rpm until evenly mixed as the internal phase;

[0067] C. Weigh the inulin lauryl carbamate, co-emulsifier, water, and polyol weighed in step A, and stir them at 60 °C with a stirrer at a speed of 400 rpm until they are evenly mixed to obtain the external phase.

[0068] D. Load the internal phase obtained in step B and the external phase obtained in step C into a lipid nanoparticle synthesizer model LNP-S1 produced by Shanghai Pengzan Biotechnology Co., Ltd., set the mass ratio of the internal phase to the external phase to 1:87.8, and the total flow rate of the internal and external phases to 10 mL / min. Collect the effluent liquid at the outlet to obtain a composition containing nicotinamide ethyl retinoate, and the measured particle size is 102 nm.

[0069] Example 2: A composition containing nicotinamide ethyl retinoate and its preparation method, characterized by the following steps:

[0070] A. Weigh 1% of nicotinamide ethyl retinoate, 0.5% of N-(2-mercaptopropionyl)-glycine, 5% of propylene carbonate, 0.5% of polysorbate-20, 1% of inulin lauryl carbamate, 30% of glycerol, 20% of dipropylene glycol, and the balance of water by mass percentage; the ratio of nicotinamide ethyl retinoate to glycine mercapto derivative is 1:0.5.

[0071] B. Stir the nicotinamide ethyl retinoate, mercapto-containing glycine derivative, and auxiliary agent weighed in step A at 62 °C with a stirrer at a speed of 550 rpm until they are evenly mixed to obtain the internal phase.

[0072] C. Weigh the inulin lauryl carbamate, co-emulsifier, water, and polyol weighed in step A, and stir them at 62 °C with a stirrer at a speed of 550 rpm until they are evenly mixed to obtain the external phase.

[0073] D. Load the internal phase obtained in step B and the external phase obtained in step C into a lipid nanoparticle synthesizer model LNP-S1 produced by Shanghai Pengzan Biotechnology Co., Ltd., set the mass ratio of the internal phase to the external phase to 1:14.4, and the total flow rate of the internal and external phases to 12 mL / min. Collect the effluent liquid at the outlet to obtain a composition containing nicotinamide ethyl retinoate, and the measured particle size is 125 nm.

[0074] Example 3: A composition containing nicotinamide ethyl retinoate and its preparation method, characterized by the following steps:

[0075] A. Weigh 5% of nicotinamide ethyl retinoate, 1% of N-(2-mercaptopropionyl)-glycine, and 2% of 2-mercaptonicotinoyl glycine by mass percentage, 10% of isononyl isononanoate, 1% of lecithin, 3% of inulin lauryl carbamate, 40% of glycerol, and the balance of water; the ratio of nicotinamide ethyl retinoate to glycine mercapto derivatives is 1:0.6;

[0076] B. Stir the nicotinamide ethyl retinoate, mercapto-containing glycine derivatives, and additives weighed in step A at 65 °C with a stirrer at a speed of 700 rpm until evenly mixed as the inner phase;

[0077] C. Stir the inulin lauryl carbamate, co-emulsifier, water, and polyol weighed in step A at 65 °C with a stirrer at a speed of 700 rpm until evenly mixed as the outer phase;

[0078] D. Load the inner phase obtained in step B and the outer phase obtained in step C into a lipid nanoparticle synthesizer of model LNP-S1 produced by Shanghai Pengzan Biotechnology Co., Ltd., set the mass ratio of the inner phase to the outer phase to 1:4.6, and the total flow rate of the inner and outer phases to 15 mL / min. Collect the effluent liquid at the outlet to obtain a composition containing nicotinamide ethyl retinoate, and the measured particle size is 119 nm.

[0079] Example 4: A composition containing nicotinamide ethyl retinoate and its preparation method, characterized by the following steps:

[0080] A. Weigh 10% of nicotinamide ethyl retinoate, 2% of N-(2-mercaptopropionyl)-glycine, and 3% of 2-mercaptonicotinoyl glycine by mass percentage, 8% of triglyceride caprylic / capric acid, 12% of octyldodecanol, 3% of polyglyceryl-10 stearate, 6% of inulin lauryl carbamate, 20% of polyol, and the balance of water; the ratio of nicotinamide ethyl retinoate to glycine mercapto derivatives is 1:0.5;

[0081] B. Stir the nicotinamide ethyl retinoate, mercapto-containing glycine derivatives, and additives weighed in step A at 67 °C with a stirrer at a speed of 850 rpm until evenly mixed as the inner phase;

[0082] C. Stir the inulin lauryl carbamate, co-emulsifier, water, and polyol weighed in step A at 67 °C with a stirrer at a speed of 850 rpm until evenly mixed as the outer phase;

[0083] D. Load the internal phase obtained in step B and the external phase obtained in step C into a lipid nanoparticle synthesizer of model LNP-S1 produced by Shanghai Pengzan Biotechnology Co., Ltd., set the mass ratio of the internal phase to the external phase to 1:1.9, and the total flow rate of the internal and external phases to 18 mL / min. Collect the outlet liquid to obtain a composition containing nicotinamide ethyl retinoate, and the measured particle size is 137 nm.

[0084] Example 5: A composition containing nicotinamide ethyl retinoate and its preparation method, characterized by the following steps:

[0085] A. Weigh 15% nicotinamide ethyl retinoate, 10% N-(2-mercaptopropionyl)-glycine, 5% 2-mercaptonicotinoyl glycine, 20% squalane, 10% Limnanthes alba seed oil, 2% hydrogenated lecithin, 3% polysorbate-60, 10% inulin lauryl carbamate, 10% 1,2-pentanediol, and the balance water by mass percentage; the ratio of nicotinamide ethyl retinoate to glycine mercapto derivatives is 1:1.

[0086] B. Stir the nicotinamide ethyl retinoate, mercapto-containing glycine derivatives, and additives weighed in step A at 70 °C with a stirrer at a speed of 1000 rpm until evenly mixed as the internal phase.

[0087] C. Stir the inulin lauryl carbamate, co-emulsifier, water, and polyol weighed in step A at 70 °C with a stirrer at a speed of 1000 rpm until evenly mixed as the external phase.

[0088] D. Load the internal phase obtained in step B and the external phase obtained in step C into a lipid nanoparticle synthesizer of model LNP-S1 produced by Shanghai Pengzan Biotechnology Co., Ltd., set the mass ratio of the internal phase to the external phase to 1:0.67, and the total flow rate of the internal and external phases to 20 mL / min. Collect the outlet liquid to obtain a composition containing nicotinamide ethyl retinoate, and the measured particle size is 152 nm.

Claims

1. A composition containing nicotinamide ethyl retinoate, characterized in that: The composition comprises the following raw material components in percentage by weight: 0.1% to 15% of nicotinamide ethyl retinoate, 0.025% to 15% of a thiol-containing glycine derivative, 1% to 30% of an auxiliary agent, 0.25% to 5% of an emulsifier, 0.5% to 10% of inulin lauryl carbamate, 10% to 70% of a polyol, and the balance water; the thiol-containing glycine derivative is selected from one of N-(2-mercaptopropionyl)-glycine and 2-mercaptonicotinoylglycine, or a mixture thereof in any mass ratio, and the mass ratio of nicotinamide ethyl retinoate to the thiol-containing glycine derivative is 1:0.25 to 1; the composition containing nicotinamide ethyl retinoate is prepared by the following method: A. Weigh, by mass percentage, 0.1%-15% of nicotinamide ethyl retinoate, 0.025-15% of a thiol-containing glycine derivative, 1-30% of an auxiliary agent, 0.25-5% of an emulsifier, 0.5-10% of inulin lauryl carbamate, 10%-60% of a polyol, and the balance water; B. Stir the nicotinamide ethyl retinoate, thiol-containing glycine derivative, and auxiliary agent weighed in step A at 60-70° C. and 400-1000 rpm using a stirrer until uniformly mixed to form the inner phase; C. Stir the inulin lauryl carbamate, co-emulsifier, water and polyol weighed in step A at 60-70° C. with a stirrer at 400-1000 rpm until uniformly mixed to form the outer phase; D. Load the inner phase obtained in step B and the outer phase obtained in step C into a lipid nanoparticle synthesizer, set the mass ratio of the inner phase to the outer phase to 1:0.5-90, and the total flow rate of the inner and outer phases to 10-20 mL / min, collect the outlet liquid, and obtain a composition containing nicotinamide ethyl retinoate with a particle size of 50-300 nm; The structural formula of the nicotinamide ethyl retinoate is: ； The auxiliary agent is selected from one of caprylic / capric triglyceride, propylene glycol carbonate, isononyl isononanoate, octyldodecanol, squalane and meadowfoam seed oil or any mixture thereof; The auxiliary emulsifier is selected from one of lecithin, hydrogenated lecithin, polysorbate-20, polysorbate-60, sucrose laurate and polyglyceryl-10 stearate, or any mixture thereof.

2. The composition containing nicotinamide ethyl retinoate according to claim 1, characterized in that: The polyol is one of glycerol, 1,2-propylene glycol, 1,3-propylene glycol, 1,3-butylene glycol, dipropylene glycol, 1,2-pentanediol and 1,2-hexanediol, or a mixture thereof in any proportion.

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