Preparation method and application of 20 (R)-ginsenoside Rg3/soya bean lecithin/cholesterol/folic acid lipidosome medicine

A technology of soybean lecithin and ginsenoside, applied in the directions of liposome delivery, drug combination, pharmaceutical formulation, etc., can solve the problems of low water solubility and fat solubility, low bioavailability, etc., and achieve strong targeting and cytotoxicity. Low, the effect of enhancing immunity

Inactive Publication Date: 2016-06-29
DALIAN NATIONALITIES UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The disadvantage of using Rg3 alone is its low water solubility and fat solubility, therefore, low bioavailability

Method used

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  • Preparation method and application of 20 (R)-ginsenoside Rg3/soya bean lecithin/cholesterol/folic acid lipidosome medicine
  • Preparation method and application of 20 (R)-ginsenoside Rg3/soya bean lecithin/cholesterol/folic acid lipidosome medicine
  • Preparation method and application of 20 (R)-ginsenoside Rg3/soya bean lecithin/cholesterol/folic acid lipidosome medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Weigh soybean lecithin and dissolve it in chloroform (1mg / 1mL), add cholesterol (the molar ratio of soybean lecithin to cholesterol is 1:1), oscillate to mix well. Blow dry with nitrogen flow to form a uniform film, place in a vacuum oven overnight to prepare liposomes.

[0030] Dissolve 20(R)-ginsenoside Rg3 in absolute ethanol in advance to prepare a 2 mg / mL solution, and then add the corresponding volume in proportion. Add ginsenoside Rg3 absolute ethanol and double distilled water (ratio 2:8) according to the ratio of lipid to drug 5:1, soak for about 2 hours, repeat ultrasonic oscillation at 55°C to dissolve the film until clear, and obtain drug lipids Body 20(R)-Ginsenoside Rg3 Liposome.

[0031] Add folic acid solution with a final concentration of 10 μg / mL, 20 μg / mL, 30 μg / mL, and 40 μg / mL to compound 20(R)-ginsenoside Rg3 liposome drug respectively, and ultrasonically oscillate at room temperature until clarified to obtain folic acid-targeted Modified drug li...

Embodiment 2

[0033] Weigh soybean lecithin and dissolve it in chloroform (1mg / 1mL), add cholesterol (the molar ratio of soybean lecithin to cholesterol is 3:1), oscillate to mix well. Blow dry with nitrogen flow to form a uniform film, place in a vacuum oven overnight to prepare liposomes.

[0034] Dissolve 20(R)-ginsenoside Rg3 in absolute ethanol in advance to prepare a 2 mg / mL solution, and then add the corresponding volume in proportion. Add 20(R)-ginsenoside Rg3 absolute ethanol and double distilled water (ratio 2:8) according to the ratio of lipid to drug 10:1, soak for about 2 hours, repeat ultrasonic oscillation at 55°C to dissolve the film until clear, Preparation of drug liposomes.

[0035] Add folic acid solution with a final concentration of 10 μg / mL, 20 μg / mL, 30 μg / mL, and 40 μg / mL to compound 20(R)-ginsenoside Rg3 liposome drug respectively, and ultrasonically oscillate at room temperature until clarified to obtain folic acid targeting Modified drug liposomes FA10-PC-Chol-...

Embodiment 3

[0037] Weigh soybean lecithin and dissolve it in chloroform (1mg / 1mL), add cholesterol (the molar ratio of soybean lecithin to cholesterol is 6:1), oscillate to mix well. Blow dry with nitrogen flow to form a uniform film, place in a vacuum oven overnight to prepare liposomes.

[0038] Dissolve 20(R)-ginsenoside Rg3 in absolute ethanol in advance to prepare a 2 mg / mL solution, and then add the corresponding volume in proportion. Add 20(R)-ginsenoside Rg3 absolute ethanol and double distilled water (ratio: 2:8) according to the ratio of lipid to drug ratio of 15:1, soak for about 2 hours, repeat ultrasonic oscillation at 55°C to dissolve the film until clear, Preparation of drug liposomes.

[0039] Add folic acid solution with a final concentration of 10 μg / mL, 20 μg / mL, 30 μg / mL, and 40 μg / mL to compound 20(R)-ginsenoside Rg3 liposome drug respectively, and ultrasonically oscillate at room temperature until clarified to obtain folic acid targeting Modified drug liposomes.

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Abstract

The invention relates to a preparation method and application of a 20 (R)-ginsenoside Rg3/soya bean lecithin/cholesterol/folic acid lipidosome medicine and belongs to the field of medicine health care products.By optimizing the ratio of soya bean lecithin, cholesterol and an encapsulation medicine to obtain 20 (R)-ginsenoside Rg3 lipidosome, the grain diameters of the 20 (R)-ginsenoside Rg3 lipidosome are reduced, and meanwhile the stability of the lipidosome medicine is enhanced; folic acid is used for conducting target modification on the encapsulated 20 (R)-ginsenoside Rg3 medicine lipidosome, and then target medicine delivery of cancer cells is achieved.Experimental results show that the encapsulation rate of the 20 (R)-ginsenoside Rg3 lipidosome can be up to 90% or above.The preparation method of the composite lipidosome medicine is simple and efficient.The prepared composite lipidosome is low in cytotoxicity, has the slow release feature and is capable of prolonging the curative effect, safe, efficient and high in targeting, good evaluating effects are obtained in physical representation and extracorporeal biological study, and a new approach is provided for research and development of anti-cancer medicines.

Description

technical field [0001] The invention relates to a preparation method and application of 20(R)-ginsenoside Rg3 / soybean lecithin / cholesterol / folate liposome medicine, belonging to the field of medicine and health products. Background technique [0002] Ginsenoside Rg3 (ginsenosides Rg3) is a protopanaxadiol-type tetracyclic triterpene saponin with a molecular formula of C 42 h 72 o 13 , the relative molecular mass is 784.30, and the chemical name is 20(R)-dammarane diol-3-O-β-D-glucopyranosyl (l-2)-β-D-glucopyranose. Ginsenoside Rg3 mainly has two common configurations, 20(R)-Propanaxadiol and 20(S)-Propanaxadiol, and 20(R)-Propanaxadiol is the dominant configuration. 20(R)-ginsenoside Rg3 (20(R)-ginsenosidesRg3) is the first new anti-cancer drug of traditional Chinese medicine monomer in China. Furthermore, it inhibits the growth and metastasis of tumors, and has a good therapeutic effect on cancers such as prostate cancer, lung cancer, gastric cancer, and liver cancer. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/704A61K47/48A61P35/00
CPCA61K31/704
Inventor 崔韶晖张树彪陈会英海华周泉
Owner DALIAN NATIONALITIES UNIVERSITY
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