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CN-121971389-A - Ginsenoside liposome and preparation method thereof

CN121971389ACN 121971389 ACN121971389 ACN 121971389ACN-121971389-A

Abstract

The invention belongs to the technical field of biological medicines and health-care products, and in particular relates to a ginsenoside liposome and a preparation method thereof. The ginsenoside liposome comprises ginsenoside, soybean lecithin, cholesterol, soybean oil, sucrose erucic acid ester and sucrose fatty acid ester with HLB value of 15-18. According to the invention, soybean oil, sucrose erucic acid ester and sucrose fatty acid ester with HLB value of 15-18 are introduced into the existing liposome constructing system of lecithin and cholesterol, so that the film forming property can be improved, and the stability and dissolution property of the liposome can be improved.

Inventors

  • Wu Shuaiting
  • CHENG KAIMING
  • YANG RUOMENG
  • JI PENGFEI

Assignees

  • 无锡百万遍科技有限公司

Dates

Publication Date
20260505
Application Date
20250909

Claims (9)

  1. 1. A ginsenoside liposome is characterized by comprising the following raw materials of ginsenoside, soybean lecithin, cholesterol, soybean oil, sucrose erucic acid ester and sucrose fatty acid ester with HLB value between 15 and 18.
  2. 2. The ginsenoside liposome of claim 1, wherein the mass ratio of ginsenoside (soybean lecithin + cholesterol + soybean oil) to sucrose erucate to sucrose fatty acid ester is 1 (10-30) to 1-5.
  3. 3. A method for preparing ginsenoside liposome according to claim 1 or 2, comprising the steps of: (1) Mixing soybean lecithin, cholesterol, soybean oil and sucrose erucic acid ester, homogenizing in a high-pressure homogenizer under the condition of introducing protective gas to obtain a homogenized solution; (2) Mixing ginsenoside and sucrose fatty acid ester in water, heating and stirring to dissolve to obtain ginsenoside solution; (3) Adding the homogeneous liquid drop into ginsenoside solution under stirring, and performing ultrasonic treatment to obtain liposome dispersion liquid containing ginsenoside; (4) And (3) treating the liposome dispersion liquid in high-pressure micro-jet equipment under the condition of introducing protective gas, and freeze-drying to obtain the ginsenoside liposome.
  4. 4. A method according to claim 3, wherein the homogenisation is carried out at a temperature of 25-50 ℃ and a pressure of 15-30MPa for a period of 10-30 minutes.
  5. 5. A method of preparation according to claim 3, wherein the heating and stirring is carried out at 40-80 ℃.
  6. 6. A method of manufacture according to claim 3 wherein the ultrasonic power of the ultrasonic treatment is 20% -40% and the single ultrasonic time is 2-5s, spaced 1-3s apart.
  7. 7. A method according to claim 3, characterized in that the treatment in the high-pressure microfluidic device is carried out 3-6 times at 100-150 Mpa.
  8. 8. A method of producing according to claim 3, wherein the shielding gas is nitrogen or argon.
  9. 9. A method of preparation according to claim 3, wherein the stirring speed is 100-600rpm.

Description

Ginsenoside liposome and preparation method thereof Technical Field The invention belongs to the technical field of biological medicines and health-care products, and in particular relates to a ginsenoside liposome and a preparation method thereof. Background Ginsenoside is the main active ingredient in Ginseng radix, and has various pharmacological effects such as anti-tumor, immunity regulating, antioxidant and antifatigue effects. However, due to the specificity of the molecular structure of ginsenoside, the solubility of ginsenoside in water is low, the oral absorption rate is limited, and the bioavailability is low, so that the clinical application of ginsenoside is limited. The liposome is a nano vesicle carrier formed by phospholipid bilayer, has good biocompatibility and targeting property, and can improve the solubility of insoluble drugs, prolong the in vivo circulation time and improve the stability and bioavailability of the drugs. Most of the existing ginsenoside liposome only adopts lecithin and cholesterol to construct a membrane structure, and the problems of limited encapsulation efficiency, insufficient stability and the like still exist. Therefore, there is a need to develop a novel ginsenoside liposome and a preparation method thereof, so as to improve the solubility and stability of ginsenoside and improve the curative effect of the medicament. Disclosure of Invention In order to solve the above problems, in a first aspect, the present invention provides a ginsenoside liposome comprising the following raw materials of ginsenoside, soybean lecithin, cholesterol, soybean oil, sucrose erucate and sucrose fatty acid ester with HLB value between 15-18. Further, the mass ratio of ginsenoside (soybean lecithin + cholesterol + soybean oil) to sucrose erucic acid ester to sucrose fatty acid ester is 1 (10-30), 1-5 and 1-5. The mass ratio of soybean lecithin, cholesterol and soybean oil may be routinely determined by those skilled in the art, and by way of example, the mass ratio of soybean lecithin, cholesterol and soybean oil may be 5-8:1:0.5-1. Further, the ginsenoside may be prepared by methods well known in the art, or may be directly commercially available. Further, the ginsenoside may be any one of various ginsenoside compounds, for example, the ginsenoside may be one or more of ginsenoside Rg1, rg2, rg3, re, rb1, rb2, rb3, rc, rd, rh2, CK. In a second aspect, the present invention provides a method of preparing a ginsenoside liposome as described herein, comprising the steps of: (1) Mixing soybean lecithin, cholesterol, soybean oil and sucrose erucic acid ester, homogenizing in a high-pressure homogenizer under the condition of introducing protective gas to obtain a homogenized solution; (2) Mixing ginsenoside and sucrose fatty acid ester in water, heating and stirring to dissolve to obtain ginsenoside solution; (3) Adding the homogeneous liquid drop into ginsenoside solution under stirring, and performing ultrasonic treatment to obtain liposome dispersion liquid containing ginsenoside; (4) And (3) treating the liposome dispersion liquid in high-pressure micro-jet equipment under the condition of introducing protective gas, and freeze-drying to obtain the ginsenoside liposome. Further, the homogenizing treatment is carried out at 25-50 ℃ and 15-30MPa for 10-30 minutes. Further, the heating and stirring are performed at 40-80 ℃. Further, the ultrasonic power of the ultrasonic treatment is 20% -40% (relative to the maximum power of the equipment), and the single ultrasonic time is 2-5s, and the interval is 1-3s. Further, the treatment in the high pressure micro-jet device is performed 3 to 6 times at 100 to 150 Mpa. As used herein, the shielding gas is nitrogen or argon. As used herein, the speed of agitation is 100-600rpm. The beneficial effects of the invention are that The soybean oil introduced into the existing liposome constructing system of lecithin and cholesterol is used as a natural oil phase to improve the fluidity of the membrane, the sucrose erucic acid ester is used as a stabilizer to reduce particle aggregation, and the sucrose fatty acid ester with the HLB value of 15-18 is selected to obviously improve the stability and dissolution performance of the liposome in the hydrophilic-lipophilic balance. Drawings FIG. 1 shows a transmission electron microscope image of a ginsenoside liposome prepared in example 1. FIG. 2 shows a particle size distribution diagram of ginsenoside liposome prepared in example 1. FIG. 3 shows comparison of the oral administration and the blood absorption effects of the gastric lavage drugs of the ginsenoside liposome prepared in example 1. Detailed Description The present invention is further illustrated below with reference to specific examples, which are not intended to limit the invention in any way. Unless specifically stated otherwise, the reagents, methods and apparatus employed in the present invention are those conventional in the art. Example