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Folacin-carboxymethyl chitosan modified pH sensitive taxol nanoliposome

A carboxymethyl chitosan and nanoliposome technology is applied in the field of folic acid-carboxymethyl chitosan modified pH-sensitive paclitaxel nanoliposome and its preparation, which can solve problems such as cardiotoxicity and side effects, and achieve stable performance , prolong the long cycle performance, reduce the effect of environmental pollution

Inactive Publication Date: 2012-06-13
EAST CHINA UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Paclitaxel, commonly known as taxol, porphyrin, and special element, is an antibiotic antineoplastic drug commonly used in clinic. It has a broad anticancer spectrum and wide curative effect, and can treat various tumors. Side effects, especially severe heart damage, bone marrow suppression and other side effects limit its clinical application

Method used

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  • Folacin-carboxymethyl chitosan modified pH sensitive taxol nanoliposome
  • Folacin-carboxymethyl chitosan modified pH sensitive taxol nanoliposome
  • Folacin-carboxymethyl chitosan modified pH sensitive taxol nanoliposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Under sterile conditions, 2 g of soybean lecithin for injection, 0.5 g of cholesterol, 0.01 g of paclitaxel and 0.025 g of vitamin E were taken. Put the above materials in a suitable container, add 100ml of absolute ethanol and ultrasonically shake until completely dissolved into a solution, transfer the above solution to a pear-shaped bottle, and rotate under reduced pressure in a constant temperature water bath to form a transparent light yellow film. Take 100ml of PBS (pH=7.4) buffer solution to elute, and wash the membrane slowly. After washing the membrane, use an ultrasonic cell pulverizer with a power of 200-300w, an interval time of 5s, an ultrasonic time of 3s, and a working time of 30min to ultrasonically pulverize the particle size between 50nm and 200nm, filter and sterilize with a 0.22 micron filter membrane, and add A certain amount of folic acid-carboxymethyl chitosan solution was hydrated for 0.5 h to obtain a pH-sensitive paclitaxel nanoliposome solutio...

Embodiment 2

[0025] Under aseptic conditions, 1.6 g of egg yolk lecithin for injection, 0.4 g of cholesterol, 0.008 g of paclitaxel and 0.020 g of vitamin E were taken. Put the above materials in a suitable container, add 80ml of absolute ethanol and ultrasonically shake until completely dissolved into a solution, transfer the above solution to a pear-shaped bottle, and rotate under reduced pressure in a constant temperature water bath until a transparent light yellow film is formed. Take 80ml of PBS (pH=7.4) buffer solution to elute, and wash the membrane slowly. After washing the membrane, use high-pressure homogenization to circulate 10 times at a pressure parameter of 80 MPa, add a certain amount of folic acid-carboxymethyl chitosan solution, and hydrate for 0.5 h to obtain folic acid-carboxymethyl chitosan modified pH-sensitive paclitaxel nanolipids body solution.

Embodiment 3

[0027] Take egg yolk lecithin 0.4g, cholesterol 0.1g, paclitaxel 0.002g and vitamin E 0.005g under aseptic condition. Put the above materials in a suitable container, add 20ml of absolute ethanol and ultrasonically shake until completely dissolved into a solution, transfer the above solution to a pear-shaped bottle, and rotary evaporate under reduced pressure in a constant temperature water bath until a transparent light yellow film is formed. Take 20ml of PBS (pH=7.4) buffer solution to elute, and wash the membrane slowly. After washing the membrane, use an ultrasonic cell pulverizer with a power of 200-300w, an interval time of 5s, an ultrasonic time of 3s, and a working time of 30min to ultrasonically pulverize the particle size between 50nm and 200nm, filter and sterilize with a 0.22 micron filter membrane, and add A certain amount of folic acid-carboxymethyl chitosan solution was hydrated for 0.5 h to obtain a folic acid-carboxymethyl chitosan modified pH-sensitive doxoru...

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Abstract

The invention relates to a folacin-carboxymethyl chitosan modified pH sensitive taxol nanoliposome and its preparation method. The liposome is composed of taxol, phosphatide, cholesterol, vitamin E, folacin-carboxymethyl chitosan and the like. The prepared liposome possesses pH sensitivity, tumor targeting and long-circulating active targetable drug delivery function.

Description

technical field [0001] The invention relates to a folic acid-carboxymethyl chitosan modified pH-sensitive paclitaxel nanoliposome and a preparation method thereof. Background technique [0002] Paclitaxel, commonly known as taxol, porphyrin, and special element, is an antibiotic antineoplastic drug commonly used in clinic. It has a broad anticancer spectrum and wide curative effect, and can treat various tumors. Side effects, especially severe heart damage, bone marrow suppression and other side effects limit its clinical application. Over the years, scientists from various countries have been looking for effective ways to reduce its toxic and side effects, such as adjusting the dosage regimen, developing paclitaxel analogues with low cardiotoxicity, combining drugs and changing drug dosage forms to reduce its severe cardiotoxicity. The toxicity of liposome-encapsulated paclitaxel is 50-70% lower than that of free drug (Budai M, et al. Liposomes as drug carrier systems: pre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/337A61K47/36A61P35/00
Inventor 钱秀珍徐云龙田文寅王丽丹杨盛兵邢万里侯娟梁婧杨勇强
Owner EAST CHINA UNIV OF SCI & TECH
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