A polyrotaxane-based pH-labile drug delivery system

Abstract

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 β-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.