Method for carrying out liposome modification on compound with free hydroxyl groups

A technology of liposomes and compounds, applied in the direction of steroids, chemical instruments and methods, organic chemistry, etc., can solve the problems of epothilone clinical application limitations, limited tumor treatment applications, and lack of side effects, so as to improve anticancer effect, improve hydrophobicity, and reduce systemic toxicity
CN109675047AActive Publication Date: 2019-04-26INST OF CHEM CHINESE ACAD OF SCI
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
INST OF CHEM CHINESE ACAD OF SCI
Publication Date
2019-04-26

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Abstract

The invention relates to a method for carrying out liposome modification on compound with free hydroxyl groups, in particular to liposome modified taxol and analogues thereof, as well as nanoparticlescontaining the liposome modified drug. According to the method disclosed by the invention, the taxol modified by liposome N,N'-di-dodecyl-L-glutamate diamide (LG-C12), 10-hydroxycamptothecine, irinotecan and epothilone B are specifically designed and successfully prepared, and the hydrophobicity of drugs is improved; then NH2-mPEG-DSPE bonded by mPEG-DSPE and mitochondrial targeted molecular triphenylphosphonium bromide (TPP) is utilized to coat liposome modified drugs to assemble into nanoparticles which improve the cytotoxic effect of the drugs on cancer cells and also reduce the toxic andside effects of the drugs on humans or animals.
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Description

technical field

[0001] The present invention relates to the field of drug modification, in particular to a method for liposome modification of compounds with free hydroxyl groups, more specifically to a liposome-modified paclitaxel and its analogues, and liposome-modified drugs containing the nanoparticles, etc. Background technique

[0002] There were an estimated 4,292,000 new cancer cases and 2,814,000 cancer deaths in China in 2015. Over the past few decades, great efforts have been made to treat these serious diseases. Among various therapies, chemotherapy is currently one of the most effective ways to treat cancer clinically. Although a variety of anticancer drugs have been developed and used in chemotherapy, they often cause adverse side effects in patients, cause physical and mental pain, and the treatment efficiency is very low. Chemotherapeutic drugs commonly used in clinical practice include doxorubicin, paclitaxel, 10-hydroxycamptothecin, irinotecan and so on....

Claims

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