Water-soluble VE (Vitamin E) prepared from artificial cell membrane and preparation method of water-soluble VE

By using artificial cell membrane materials to modify vitamin E liposomes, combined with surfactant and temperature regulation control, the difficulty of using vitamin E in aqueous formulas in the prior art has been solved, and the long-term stable and transparent aqueous solution of vitamin E liposomes is achieved, which is suitable for skin care products and health products.

CN119548427APending Publication Date: 2025-03-04WANLAN PHARM (SUZHOU) CO LTD
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Patent Information

Application Number
CN202411709571.2
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-11-27
Publication Date
2025-03-04

AI Technical Summary

Technical Problem

The prior art is difficult to effectively use vitamin E in aqueous formulations, and cannot obtain a transparent aqueous solution system. The complex process affects biological activity, complex operation, low production efficiency, poor stability, and easy precipitation problems.

Method used

The artificial cell membrane material polyquaternary ammonium salt-51 is used to modify vitamin E liposomes. A transparent aqueous solution system is prepared by combining surfactant and water-soluble and oil-soluble ingredients and combined with temperature regulation control.

Benefits of technology

It achieves long-term stability of vitamin E liposomes in the range of 4-60°C, and is suitable for skin care products or health products that need to be presented in the form of transparent aqueous solutions.

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Abstract

The invention discloses water-soluble VE (vitamin E) prepared from an artificial cell membrane. The water-soluble VE is prepared from the following components in parts by weight: 1 to 2 parts of vitamin E, 1 to 2 parts of tween-80, 5 to 10 parts of cholesterol, 5 to 10 parts of lecithin, 1 to 2 parts of polyquaternium-51, 10 to 20 parts of polyethylene glycol, 10 to 20 parts of polyhydric alcohol and 40 to 60 parts of deionized water. The preparation method comprises the following steps: 1, dissolving vitamin E, Tween-80, lecithin and cholesterol in anhydrous ether, and evaporating the solvent ether by using a rotary evaporator to form a layer of transparent liposome film on the inner wall of a round-bottom flask; 2, dissolving polyquaternium-51 in deionized water at room temperature, and adding polyol; and 3, mixing the aqueous solution obtained in the step 2 with polyethylene glycol, adding the obtained mixed solution into the solution obtained in the step 1, hydrating for 1 hour to obtain an emulsion, performing ultrasonic treatment until the liquid is transparent, filling nitrogen for protection, and preserving in a dark place at the temperature of more than or equal to 4 DEG C. By applying the method, a transparent aqueous solution system which is stable for a long time within the range of 4-60 DEG C can be obtained.
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Description

Technical Field

[0001] The invention relates to the preparation of water-soluble VE, in particular to a water-soluble VE prepared by using an artificial cell membrane and a preparation method thereof. Background Art

[0002] Vitamin E is the general name for tocopherols, a fat-soluble vitamin found in nature. It can be divided into two categories: tocopherols and tocotrienols according to its molecular structure. It has the functions of regulating metabolism, anti-oxidation and anti-aging in human body cells, and has important applications in skin care products and health care products.

[0003] Since vitamin E is a fat-soluble molecule, its poor solubility in water limits its use in aqueous formulations. In order to make vitamin E suitable for aqueous formulations, the following methods are commonly used: (1) including vitamin E solid in water-soluble starch or microcrystalline fiber materials such as γ-cyclodextrin. This method cannot obtain a transparent aqueous solution system; (2) chemically modifying vitamin E to increase hydrophilic groups. This method is relatively complex and may affect the biological activity of vitamin E; (3) preparing vitamin E into water-soluble nano-microbeams by nanoprecipitation or thin film hydration. This method can obtain a stable and transparent aqueous solution system, but there are problems such as complex operation and low production efficiency; (4) using a combination of surfactants to achieve solubilization of vitamin E in an aqueous system. This method is simple to operate and low in cost, but the thermal stability of the system is poor, and the product may precipitate when heated or cooled. Summary of the invention

[0004] The purpose of the present invention is to overcome the shortcomings of the prior art and provide a water-soluble VE prepared by artificial cell membrane and a preparation method thereof, so as to solve the problems that a transparent aqueous solution system cannot be obtained, the process is complicated and affects the biological activity, the operation is complicated, the production efficiency is low, the stability is poor, and precipitation is easy to occur.

[0005] To achieve the above purpose, the technical solution adopted by the present invention is: a water-soluble VE prepared by artificial cell membrane, wherein the water-soluble VE is composed of the following components in weight ratio: vitamin E: 1-2 parts, Tween-80: 1-2 parts, cholesterol: 5-10 parts, lecithin: 5-10 parts, polyquaternium-51: 1-2 parts, polyethylene glycol: 10-20 parts, polyol: 10-20 parts, and deionized water: 40-60 parts.

[0006] Furthermore, the polyol is one or a combination of butanediol, propylene glycol, glycerol and isomers thereof.

[0007] A method for preparing water-soluble VE prepared by using artificial cell membrane, the preparation steps are as follows:

[0008] (1) Dissolve vitamin E, Tween-80, lecithin, and cholesterol in anhydrous ether, and evaporate the solvent ether using a rotary evaporator to form a transparent liposome film on the inner wall of a round-bottom flask;

[0009] (2) dissolving polyquaternium-51 in deionized water at room temperature, and adding a polyol to obtain an aqueous solution;

[0010] (3) mixing the aqueous solution obtained in (2) with polyethylene glycol, adding the obtained mixed solution into the round-bottom flask in (1), and hydrating the liposome film on the inner wall of the flask at 40±5°C for 1 h to obtain a milky liposome solution;

[0011] (4) ultrasonically treating the emulsion liposome solution obtained in (3) until the liquid becomes transparent, thereby obtaining a transparent oily liposome solution;

[0012] (5) The transparent oily liposome solution obtained in (4) is filled with nitrogen gas for protection and stored at ≥4°C away from light.

[0013] Furthermore, the transparent oily liposome solution can be added into an aqueous system at a ratio of 1:10-1:100 to obtain a transparent aqueous solution containing VE.

[0014] The present invention adopts the above structure to achieve the following beneficial effects: the present invention provides a water-soluble VE prepared with an artificial cell membrane and a preparation method thereof, which has good hydrophilicity and biocompatibility characteristics by imitating the bionic material 2-methacryloyloxyethyl phosphorylcholine polymer of the phospholipid layer structure of the cell membrane, namely polyquaternium-51, also known as artificial cell membrane material. The VE liposome is modified by the 2-methacryloyloxyethyl phosphorylcholine polymer to improve its hydrophilicity and stability in aqueous solution, and a transparent aqueous solution system can be obtained by combining surfactants, water-soluble and oil-soluble components and controlling temperature regulation, thereby achieving long-term stability of the aqueous solution of the vitamin E liposome in the range of 4-60°C, and is suitable for skin care products or health care products that need to be presented in the form of a transparent aqueous solution. DETAILED DESCRIPTION

[0015] In order to enable those skilled in the art to better understand the solution of the present application, the technical solution in the embodiments of the present application will be clearly and completely described below in conjunction with the drawings in the embodiments of the present application. Obviously, the described embodiments are only part of the embodiments of the present application, not all of the embodiments. Based on the embodiments in the present application, all other embodiments obtained by ordinary technicians in this field without creative work should fall within the scope of protection of the present application.

[0016] In response to the demand for VE aqueous solution, the designers of the present invention innovatively proposed a water-soluble VE prepared by artificial cell membrane and a preparation method thereof, which can obtain a transparent aqueous solution system and is long-term stable in the range of 4-60°C.

[0017] The invention discloses a water-soluble vitamin E prepared by using an artificial cell membrane. The water-soluble vitamin E is composed of the following components according to weight ratio: vitamin E: 1-2 parts, Tween-80: 1-2 parts, cholesterol: 5-10 parts, lecithin: 5-10 parts, polyquaternium-51: 1-2 parts, polyethylene glycol: 10-20 parts, polyol: 10-20 parts, and deionized water: 40-60 parts.

[0018] The polyol is one or a combination of butanediol, propylene glycol, glycerol and isomers thereof.

[0019] A method for preparing water-soluble VE prepared by using artificial cell membrane, the preparation steps are as follows:

[0020] (1) Dissolve vitamin E, Tween-80, lecithin, and cholesterol in anhydrous ether, and evaporate the solvent ether using a rotary evaporator to form a transparent liposome film on the inner wall of a round-bottom flask;

[0021] (2) dissolving polyquaternium-51 in deionized water at room temperature, and adding a polyol to obtain an aqueous solution;

[0022] (3) mixing the aqueous solution obtained in (2) with polyethylene glycol, adding the obtained mixed solution into the round-bottom flask in (1), and hydrating the liposome film on the inner wall of the flask at 40±5°C for 1 h to obtain a milky liposome solution;

[0023] (4) ultrasonically treating the emulsion liposome solution obtained in (3) until the liquid becomes transparent, thereby obtaining a transparent oily liposome solution;

[0024] (5) The transparent oily liposome solution obtained in (4) is filled with nitrogen gas for protection and stored at ≥4°C away from light.

[0025] The transparent oily liposome solution can be added into an aqueous system at a ratio of 1:10-1:100 to obtain a transparent aqueous solution containing VE, and is stable for a long time within the range of 0-50°C.

[0026] The specific preparation method of this embodiment is as follows:

[0027] (1) Weigh 1 g of vitamin E, 1 g of Tween-80, 5 g of lecithin and 5 g of cholesterol, add 50 mL of anhydrous ether to dissolve, and evaporate the solvent ether using a rotary evaporator to form a transparent liposome film on the inner wall of a round-bottom flask;

[0028] (2) Take 50 g of deionized water, add 10 g of butylene glycol, stir evenly, then add 1 g of polyquaternium-51 and stir to dissolve;

[0029] (3) Add 10 g of polyethylene glycol-200 to the solution in (2), stir evenly, and then add to the round-bottom flask in (1), and hydrate with the liposome film on the inner wall of the flask at 40±5°C for 1 h to obtain a milky liposome solution;

[0030] (4) ultrasonically treating the emulsion liposome solution obtained in (3) until the liquid becomes transparent, thereby obtaining a transparent oily liposome solution;

[0031] (5) The obtained transparent oily liposome solution was protected by nitrogen gas and stored at ≥4°C away from light.

[0032] The present invention adopts the above structure to achieve the following beneficial effects: the present invention provides a water-soluble VE prepared with an artificial cell membrane and a preparation method thereof, which has good hydrophilicity and biocompatibility characteristics by imitating the bionic material 2-methacryloyloxyethyl phosphorylcholine polymer of the phospholipid layer structure of the cell membrane, namely polyquaternium-51, also known as artificial cell membrane material. The VE liposome is modified by the 2-methacryloyloxyethyl phosphorylcholine polymer to improve its hydrophilicity and stability in aqueous solution, and a transparent aqueous solution system can be obtained by combining surfactants, water-soluble and oil-soluble components and controlling temperature regulation, thereby achieving long-term stability of the aqueous solution of the vitamin E liposome in the range of 4-60°C, and is suitable for skin care products or health care products that need to be presented in the form of a transparent aqueous solution.

[0033] As described above, the above embodiments are only used to illustrate the technical solutions of the present application, rather than to limit them. Although the present application has been described in detail with reference to the aforementioned embodiments, those skilled in the art should understand that they can still modify the technical solutions described in the aforementioned embodiments, or make equivalent replacements for some of the technical features therein. However, these modifications or replacements do not deviate the essence of the corresponding technical solutions from the spirit and scope of the technical solutions of the embodiments of the present application.

Claims

1. A water-soluble VE prepared by artificial cell membrane, characterized in that: The water-soluble VE is composed of the following components in a weight ratio Composition: Vitamin E: 1-2 parts, Tween-80: 1-2 parts, cholesterol: 5-10 parts, lecithin: 5-10 parts, polyquaternium-51: 1-2 parts, polyethylene glycol: 10-20 parts, polyol: 10-20 parts, deionized water: 40-60 parts.

2. The water-soluble VE prepared by using an artificial cell membrane as claimed in claim 1, characterized in that: The polyol is one or a combination of butanediol, propylene glycol, glycerol and isomers thereof.

3. A method for preparing water-soluble VE prepared by using artificial cell membrane according to claim 1, characterized in that: The preparation steps are as follows: (1) Dissolve vitamin E, Tween-80, lecithin, and cholesterol in anhydrous ether, and evaporate the solvent ether using a rotary evaporator to form a transparent liposome film on the inner wall of a round-bottom flask; (2) dissolving polyquaternium-51 in deionized water at room temperature, and adding a polyol to obtain an aqueous solution; (3) mixing the aqueous solution obtained in (2) with polyethylene glycol, adding the obtained mixed solution into the round-bottom flask in (1), and hydrating the liposome film on the inner wall of the flask at 40±5°C for 1 h to obtain a milky liposome solution; (4) ultrasonically treating the emulsion liposome solution obtained in (3) until the liquid becomes transparent, thereby obtaining a transparent oily liposome solution; (5) The transparent oily liposome solution obtained in (4) is filled with nitrogen gas for protection and stored at ≥4°C away from light.

4. The method for preparing water-soluble VE prepared by using artificial cell membrane as claimed in claim 3, characterized in that: The transparent oily liposome solution can be added into an aqueous system at a ratio of 1:10-1:100 to obtain a transparent aqueous solution containing VE.