Hydroxyl camptothecin flexible liposome and preparation method thereof

A technology of hydroxycamptothecin and flexible liposomes, which is applied in the direction of liposome delivery, drug combination, anti-tumor drugs, 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 , to avoid the effect of swallowing

Inactive Publication Date: 2013-06-19
GUANGXI ZHUANGDU BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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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Effect test

Embodiment 1

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

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

[0024] 3) Add solution C to membrane B, refrigerate the membrane at a temperature 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] Take an appropriate amount of the hydroxycamptothecin flexible liposome (HCPT-lipo) solution prepared in Example 1, and determine the content of HCPT (W T ); Directly filter with 0.22μm microporous membrane to determine the content of HCPT in the membrane solution (W F ), using ER(%)=(W T -W F ) / W Z ×100% calculate the encapsulation rate. As a result, the HCPT encapsulation rate in HCPT-lipo was 71%.

[0026]...

Embodiment 2

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

[0030] 2) Dissolve 5 mg of carboxymethyl chitosan in 0.5 ml of phosphate buffer 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 ratio of ethanol to chloroform is 1:1 by volume) to obtain solution A. Place solution A in a 60℃ water bath In the film by rotary evaporation, film B is obtained.

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

[0035] 3) Add solution C to membrane B, refrigerate at below -4°C for 50 minutes to fully hydrate the membrane, and then vortex and mix for 30 minutes to obtain a 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 a 10-position hydroxyl derivative of camptothecin. It is the same cellular anticancer drug as camptothecin. In recent years, studies have also found that the target of hydroxycamptothecin is topoisomerase, which kills Cancer cells also have an impact on normal cell metabolism. There are literature reports on 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) This substance is a water-insoluble, insoluble fat-soluble drug, and has certain toxicity. Moreover, due to its large particle size and poor stability, it is easily swallowed by the endothelial reticulum system in the body, and its clinical application has been li...

Claims

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Application Information

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Patent Type & Authority Patents(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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