A Polyrotaxane-based pH-labile Drug Delivery System

作者:Jiang Lan*; Gao Ze ming; Ye Lin; Zhang Ai ying; Feng Zeng guo
来源:Periodica Polytechnica - Chemical Engineering, 2014, 58(1): 55-60.
DOI:10.3311/PPch.7202

摘要

A novel polyrotaxane (PR)-based triblock copolymer was exploited as polymeric carrier for doxorubicin (DOX). A sample holding a feed molar ratio of Pluronic F127 to beta-CD to poly(ethylene glycol) methyl ether methacrylate (PEGMA) equal to 1:30:20 was synthesized Via the in situ atom-transfer radical polymerization (ATRP) and then conjugated with DOX using pH sensitive hydrazone linker. The resulting PR-DOX conjugates enabled to self-assemble into nano-particles of about 70 nm in diameter in aqueous solution as evidenced by TEM The release of DOX was varied from 10 % to 37% over 72 h at physiological and acidic pH, respectively The PR-based triblock copolymer without DOX conjugation showed almost non toxicity, while these nano-particles with DOX conjugation presented increased toxicity.