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Preparation of novel double-targeted pectin-dobby polyethylene glycol-combined anticancer drug

A technology of multi-arm polyethylene glycol and anticancer drugs, which is applied in the fields of advanced nanotechnology, biopharmaceuticals, and polymer materials. It can solve the problems of sudden release, short blood circulation time, and poor water solubility of embedding. Achieve the effect of improving drug loading rate, strong selective cure and high yield

Inactive Publication Date: 2018-02-27
BEIJING FORESTRY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can kill cancer cells through a variety of inhibitory pathways, but its poor water solubility, short half-life, and short blood circulation time limit the clinical application of dihydroartemisinin. The existing solution is to deliver the drug by embedding However, simple embedding is prone to burst release, which brings burden to patients

Method used

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  • Preparation of novel double-targeted pectin-dobby polyethylene glycol-combined anticancer drug
  • Preparation of novel double-targeted pectin-dobby polyethylene glycol-combined anticancer drug
  • Preparation of novel double-targeted pectin-dobby polyethylene glycol-combined anticancer drug

Examples

Experimental program
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Effect test

Embodiment 1

[0035] (1) Dissolve 2.0 g of folic acid in dimethyl sulfoxide, add the activator 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC), and react for 30 minutes, Then add ethylenediamine and pyridine, react at room temperature and avoid light for 24 hours to obtain aminated folic acid, transfer it to the dialysis membrane, dialyze overnight, collect the coupling substance solution in the dialysis membrane, and freeze-dry to obtain a yellow powder;

[0036] (2) Dissolve 1.0 g of aminated folic acid and 0.5 g of pectin in deionized water, add activator EDC to react for 30 minutes, then add catalyst 4-dimethylaminopyridine (DMAP) to react for 24 hours, dialyze the solution after reaction Overnight, collect the coupling substance solution in the dialysis membrane, and freeze-dry to obtain folic acid-pectin yellow powder;

[0037] (3) Dissolve 5.0 g of multi-armed polyethylene glycol in pyridine, add activator EDC to react for 30 minutes, then add 1.0 g of anticancer dr...

Embodiment 2

[0042] (1) Dissolve 2.0 g of folic acid in dimethyl sulfoxide, add the activator 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC), and react for 30 minutes, Then add ethylenediamine and pyridine, react at room temperature and avoid light for 24 hours to obtain aminated folic acid, transfer it to the dialysis membrane, dialyze overnight, collect the coupling substance solution in the dialysis membrane, and freeze-dry to obtain a yellow powder;

[0043] (2) Dissolve 0.5 g of aminated folic acid and 0.2 g of pectin in deionized water, add activator EDC to react for 30 minutes, then add catalyst 4-dimethylaminopyridine (DMAP) to react for 24 hours, dialyze the solution after reaction Overnight, collect the coupling substance solution in the dialysis membrane, and freeze-dry to obtain folic acid-pectin yellow powder;

[0044] (3) Dissolve 3.0 g of multi-armed polyethylene glycol in pyridine, add activator EDC and react for 30 minutes, then add 1.0 g of anticancer d...

Embodiment 3

[0049] (1) Dissolve 2 g of folic acid in dimethyl sulfoxide, add activator 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC), react for 30 minutes, and then Add ethylenediamine and pyridine, react at room temperature and avoid light for 24 hours to obtain aminated folic acid, transfer it to the dialysis membrane, dialyze overnight, collect the coupling substance solution in the dialysis membrane, and freeze-dry to obtain a yellow powder;

[0050] (2) Dissolve 2 g of aminated folic acid and 1.0 g of pectin in deionized water, add the activator EDC to react for 30 minutes, then add the catalyst 4-dimethylaminopyridine (DMAP) to react for 24 hours, and dialyze the reacted solution overnight , collecting the coupling substance solution in the dialysis membrane, and freeze-drying to obtain folic acid-pectin yellow powder;

[0051] (3) Dissolve 1.0 g of multi-armed polyethylene glycol in pyridine, add activator EDC to react for 30 minutes, then add 0.1 g of anticance...

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Abstract

The invention discloses a preparation method of a novel double-targeted pectin-dobby polyethylene glycol-combined anticancer drug. The double-targeted nanometer drug is prepared by comprising the following steps: coupling a folic acid-modified pectin with a drug-carrying dobby polyethylene glycol to form a precursor drug, then mixing the precursor drug with another hydrophobic anticancer drug according to a certain ratio, and self-assembling to obtain a nanometer drug with double-targeted function on colon cancer. The double-targeted nanometer drug prepared by adopting the method solves the problems that the most of anticancer drugs are poor in water solubility, low in bioavailability and the like by utilizing the good biocompatibility, bioactivity, biodegradability and tissue adhesion action of natural pectin, double-targeted function endows the nanometer drug with stronger selective healing function on the colon cancer. The nanometer drug prepared has stable drug carrying rate, encapsulation efficiency and good particle size distribution, thus having good clinical application prospects.

Description

technical field [0001] The invention relates to a preparation method of a new type of anticancer drug using natural plant polysaccharide gum as a drug carrier, specifically a preparation method of a new type of double-targeting pectin-multi-armed polyethylene glycol combined anticancer drug, which belongs to the application of polymer materials, fields of advanced nanotechnology and biopharmaceuticals. Background technique [0002] Since Tu Youyou discovered artemisinin, derivatives of artemisinin have also been discovered. Among them, dihydroartemisinin has dozens of times the anti-malarial effect of artemisinin, and has anti-inflammatory and immune-regulating effects. In recent years, It has been found that it has anti-tumor, anti-initiative mutation, and induction of apoptosis in cancer cells, such as melanoma, colon cancer, breast cancer, and lung cancer. It can kill cancer cells through a variety of inhibitory pathways, but its poor water solubility, short half-life, a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/60A61K47/61A61K47/54A61K31/4745A61K31/357A61P35/00
CPCA61K31/357A61K31/4745A61K2300/00
Inventor 雷建都刘彦雪曹永丽郑督罗敏肖萌
Owner BEIJING FORESTRY UNIVERSITY
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