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Hydroxyl camptothecin flexible liposome and preparation method thereof

A technology of hydroxycamptothecin and flexible liposomes, which can be used in liposome delivery, pharmaceutical formulations, organic active ingredients, etc. It can solve the problems of poor stability and inability to be used in clinical practice, so as to increase stability and improve disposal methods , increase the effect of curative effect

Inactive Publication Date: 2012-04-04
GUANGXI ZHUANGDU BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Chinese patent document CN100356919C discloses a kind of preparation method of hydroxycamptothecin liposome and long-circulation liposome, and its long-circulation liposome uses Poloxamer F68 as surfactant, and this liposome particle diameter is big to 500nm, and stability is poor , basically cannot be used in clinical

Method used

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  • Hydroxyl camptothecin flexible liposome and preparation method thereof
  • Hydroxyl camptothecin flexible liposome and preparation method thereof
  • Hydroxyl camptothecin flexible liposome and preparation method thereof

Examples

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Embodiment 1

[0022] 1) Dissolve 1.0 mg of hydroxycamptothecin, 100.0 mg of soybean lecithin, and 1.0 mg of cholesterol in 10 ml of ethanol to obtain solution A. The solution A was formed into a film by rotary evaporation in a water bath at 50° C. to obtain film B.

[0023] 2) 10 mg of chitosan was dissolved in 5 ml of phosphate buffer with pH=6.8 to obtain solution C.

[0024] 3) Add solution C to membrane B, refrigerate at below 5°C for 30 minutes to fully hydrate the membrane, and then vortex and mix for 15 minutes to obtain the product of the present invention.

[0025] Get the hydroxycamptothecin flexible liposome (HCPT-lipo) solution that embodiment 1 prepares appropriate, measure wherein the content of HCPT (W T ); directly filter with 0.22 μm microporous membrane, measure the content of HCPT in membrane solution (W F ), using ER(%)=(W T -W F ) / W Z ×100% to calculate the encapsulation rate. As a result, the encapsulation rate of HCPT in HCPT-lipo was 71%.

[0026] Take an appro...

Embodiment 2

[0029] 1) Dissolve 10.0 mg of hydroxycamptothecin, 60.0 mg of soybean lecithin, and 5.0 mg of cholesterol in 10 ml of ethanol to obtain solution A, and form a film of solution A by rotary evaporation in a water bath at 55° C. to obtain film B.

[0030] 2) 5 mg of carboxymethyl chitosan was dissolved in 0.5 ml of phosphate buffer solution with pH=3.0 to obtain solution C.

[0031] 3) Add solution C to membrane B, refrigerate at below 1°C for 20 minutes to fully hydrate the membrane, and then vortex and mix for 60 minutes to obtain the product of the present invention.

Embodiment 3

[0033] 1) Dissolve 5 mg of hydroxycamptothecin, 80 mg of phosphatidylcholine, and 10 mg of cholesterol in a mixture of 10 ml of ethanol and chloroform (the volume ratio of ethanol and chloroform is 1:1) to obtain solution A, and place solution A in a water bath at 60°C Film was formed by rotary evaporation to obtain film B.

[0034] 2) 8 mg of chitosan was dissolved in 0.2 ml of phosphate buffer with pH=9.0 to obtain solution C.

[0035] 3) Add solution C to membrane B, refrigerate at -4°C for 50 minutes to fully hydrate the membrane, and then vortex and mix for 30 minutes to prepare the product.

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Abstract

The invention discloses a hydroxyl camptothecin flexible liposome and a preparation method thereof. The method comprises the following steps of: dissolving hydroxyl camptothecin and carrier materials, such as phospholipid, cholesterol and the like, in an organic solvent; forming the mixture into a membrane in water bath through rotary evaporation; and adding buffer solution which contains chitosan into the membrane to form the hydroxyl camptothecin flexible liposome. The hydroxyl camptothecin flexible liposome is relatively lower in toxicity, relatively longer in residence time in a body, high in stability in a solution phase and smalllow in particle size, and the particle size of the liposome is not obviously changed after the liposome is lyophilized.

Description

technical field [0001] The invention relates to a hydroxycamptothecin liposome preparation and a preparation method thereof. Background technique [0002] Hydroxycamptothecin is the 10-hydroxyl derivative of camptothecin, which belongs to the same class of cellular anticancer drugs as camptothecin. In recent years, studies have also found that the target of hydroxycamptothecin is topoisomerase, which kills At the same time as cancer cells, it also affects normal cell metabolism. There are literatures reporting the preparation method of hydroxycamptothecin and its physical and chemical performance parameters (Lei Yingjie, Wang Zuoquan, Liu Hong, et al. Preparation and mechanism of 10-hydroxycamptothecin, Shaanxi Chemical Industry, 1999, 28(4): 10) , the substance is a water-insoluble and fat-insoluble drug, and has certain toxicity, and because of its large particle size and poor stability, it is easily swallowed by the endothelial reticular system in the body, and its clini...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/4745A61K47/36A61P35/00
Inventor 蒋桂秀奉建芳蒋满州
Owner GUANGXI ZHUANGDU BIO TECH
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