ACID-LABILE CORE CROSS-LINKED MICELLES FOR pH-TRIGGERED RELEASE OF DOXORUBICIN

Abstract

A acid-labile core cross-linked micelle system of amphiphilic triblock copolymer of poly(oligo(ethylene glycol) methyl ether methacrylate)-block-poly(styrene-alt-maleic anhydride)-block-poly(styrene) (POEGMA-b-PSMA-b-PS) was prepared. The POEGMA-b-PSMA-b-PS triblock copolymers were synthesized by the reversible addition-fragmentation chain transfer (RAFT) polymerization. Doxorubincin (DOX) was entrapped into micellar structure with POEGMA block as a shell and PSMA-b-PS block as a core. Then, core cross-linking was carried out by amidation reaction between 2,2-bis(aminoethoxy)propane and maleic anhydride group inner core. DOX loading content and efficiency were calculated to be 18 and 90 (wt. %), respectively. Core cross-linked micelles illustrated good stability under physiological condition but disassociated rapidly under acidic pH. The DOX release experiments indicated a rapid DOX release at pH 5.0 compared to pH 7.4.