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1. (WO2018120544) METHOD FOR PREPARING CHARGE-CONVERTIBLE, REDUCTION-SENSITIVE REVERSIBLE CROSS-LINKED NANO-MICELLE

Pub. No.:    WO/2018/120544    International Application No.:    PCT/CN2017/082114
Publication Date: Fri Jul 06 01:59:59 CEST 2018 International Filing Date: Fri Apr 28 01:59:59 CEST 2017
IPC: C08J 3/07
A61K 47/34
Applicants: JIANGNAN UNIVERSITY
江南大学
Inventors: ZHANG, Liping
张丽萍
NI, Caihua
倪才华
DING, Yuanyuan
丁媛媛
SHI, Gang
石刚
SANG, Xinxin
桑欣欣
Title: METHOD FOR PREPARING CHARGE-CONVERTIBLE, REDUCTION-SENSITIVE REVERSIBLE CROSS-LINKED NANO-MICELLE
Abstract:
Disclosed is a method for preparing a charge-convertible, reduction-sensitive reversible cross-linked nano-micelle, which belongs to the technical field of biomedical materials. The present invention comprises: using lipoic acid and ethylenediamine to synthesize lipoyl ethylenediamine in the presence of N,N'-carbonyldiimidazole catalyst; polymerizing the lipoyl ethylenediamine, polyethylene glycol diglycidyl ether and lysine by means of nucleophilic addition mechanism to prepare a poly(lysine-co-polyethylene glycol diglycidyl ether-co-lipoyl ethylenediamine) terpolymer, and then providing micelles with excellent anti-protein, non-specific adsorption and enhanced cell uptake properties by means of self-assembly, and protonation/deprotonation. A disulfide bond in the lipoyl can form a linear polydisulfide structure under the action of 1,4-dithiothreitol, so that the micelle core is crosslinked and a cross-linked structure is destroyed under reduction conditions in cells, and thus the controlled release of a drug can be achieved. The nano-micelle of the present invention is expected to be a drug carrier in cancer therapy.