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Blank liposome taking ginsenoside Rg3 or analogue thereof as membrane material, and preparation method and application thereof

A technology of blank liposomes and ginsenosides, applied in the direction of liposome delivery, glycoside steroids, organic chemical methods, etc., can solve the problems of poor water solubility, etc.

Active Publication Date: 2020-06-05
XIAMEN GINPOSOME PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But all do not have patent or document openly to report about the long circulation liposome that takes ginsenoside as membrane material
[0007] and the lipophilic section of ginsenoside Rg3 and Rh2 only contains a double bond, poor water solubility, soluble in methanol, ethanol, insoluble in ether, chloroform (see International Pharmacy Journal of Research, June 2017, Volume 44, Issue 6 "Research Progress of Ginsenoside Rg3 Formulations")

Method used

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  • Blank liposome taking ginsenoside Rg3 or analogue thereof as membrane material, and preparation method and application thereof
  • Blank liposome taking ginsenoside Rg3 or analogue thereof as membrane material, and preparation method and application thereof
  • Blank liposome taking ginsenoside Rg3 or analogue thereof as membrane material, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0135] The preparation of embodiment 1 common Rg3 liposome

[0136] Add 1g of egg yolk lecithin, 0.1g of cholesterol, and 0.1g of ginsenoside 20(S)-Rg3 (without micronization treatment) into 20mL of absolute ethanol, and stir at room temperature to form a clear solution. In a constant temperature water bath at ℃, remove the organic solvent by rotary evaporation, and form a film, add 20mL of 5% trehalose aqueous solution (the stated percentage refers to the percentage of the quality of trehalose in the total mass of trehalose aqueous solution), and sonicate until the liposome particles 0.1-0.3 micron, pass through a microporous membrane of 0.22 micron to obtain an aqueous solution containing ginsenoside Rg3 liposome, and then put the solution in a vial. Put the above aqueous solution into a freeze dryer to freeze dry for 72 hours, pass through a protective gas (argon or nitrogen), seal it, and obtain the common ginsenoside Rg3 liposome. After testing, the D10 of the liposome w...

Embodiment 2

[0137] The preparation of embodiment 2 Rg3 blank liposomes

[0138] Add 1g of egg yolk lecithin and 0.1g of superfine powdered ginsenoside 20(S)-Rg3 into 200mL of chloroform, stir at room temperature to form a clear solution, and remove the organic solvent by rotary evaporation in a constant temperature water bath at 40-50°C. To form a film, add 20mL of 5% trehalose aqueous solution (the percentage refers to the percentage of the quality of trehalose in the total mass of trehalose aqueous solution), sonicate until the liposome particles are at 0.1-0.3 microns, and pass through a 0.22 micron microporous membrane , to obtain an aqueous solution of blank liposomes containing ginsenoside Rg3, and then the solution is divided into vials. Put the above aqueous solution into a freeze dryer to freeze dry for 72 hours, pass through a protective gas (argon or nitrogen), seal it, and obtain the ginsenoside Rg3 blank liposome. After testing, the D10 of the liposome was 66nm, the D50 was ...

Embodiment 3

[0139] The preparation of embodiment 3 Rg5 blank liposomes

[0140] By the same method as in Example 2, Rg3 was replaced by Rg5 to prepare Rg5 blank liposomes. After testing, the D10 of the liposome was 70nm, the D50 was 96nm, and the D90 was 111nm.

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Abstract

The invention discloses a blank liposome taking ginsenoside Rg3 or an analogue thereof as a membrane material, and a preparation method and application thereof. The ginsenoside as shown in the formulaI is blank liposome of a membrane material, wherein the blank liposome is provided with a membrane, and the membrane comprises lipid substances and the ginsenoside as shown in the formula I. The blank liposome disclosed by the invention has the characteristics of good film-forming property, encapsulation efficiency, targeting property, long circulation, stability, safety and uniformity, is used for encapsulating active substances, biological agents, polynucleotides or oligonucleotides in medicines and cosmetics to form the liposome loaded with the active substances, and is simple and convenient in preparation process.

Description

technical field [0001] The invention relates to a blank liposome using ginsenoside Rg3 or its analogs as a membrane material, its preparation method and application. Background technique [0002] Liposome is a targeted drug carrier, which belongs to a new dosage form of targeted drug delivery system. It can embed drug powder or solution in microparticles with a diameter of nanometers. This kind of microparticles is similar to the bilayer microvesicles of the biological membrane structure. The distribution of the drug in the body makes the drug mainly accumulate in the target tissue, thereby improving the therapeutic index of the drug, reducing the therapeutic dose of the drug and reducing the toxicity of the drug. [0003] CN201210151597.0 discloses a ginsenoside Rg3 liposome and its preparation method. The patent discloses that ginsenoside Rg3, phospholipids, cholesterol, etc. are dissolved in solvents such as n-butanol, ethanol or sorbitol to prepare Rg3 liposome . CN20...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/28
CPCA61K47/28A61K31/337A61P35/00A61K9/1271A61K9/1277A61K9/127A61K31/4745A61K33/243A61K31/704A61K45/06C07B63/04C07J17/005
Inventor 王建新洪超朱颖夏加璇王丹陈颖江詹华杏
Owner XIAMEN GINPOSOME PHARM CO LTD
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