To address the outstanding challenge in micelle-based drug delivery of achieving highly stable micelles capable of on-demand drug release, we developed camptothecin (CPT)-conjugated, core-crosslinking micelles (CCMs) that both CPT release and the micellar structure disruption were subject to redox-responsive cleavage of disulfide bonds. CCMs were prepared via coprecipitation of disulfide-containing CPT-poly(a-hydroxy acid) conjugate and mono-methoxy poly(ethylene glycol)-b-poly(a-hydroxy acid), followed by crosslinking of the core of the micelles via azide-alkyne click chemistry. CCMs exhibited excellent stability under physiological conditions but were rapidly disassembled upon treatment of dithiothreitol (DTT). CPT, stably conjugated to micelle without noticeable release in the absence of DTT, was also burst released once DTT was applied to disassemble micellar structure. Furthermore, in vitro cytotoxicity study showed excellent anti-cancer efficacy of redox-responsive CCMs?

Redox-responsive core-crosslinking micelles capable of on-demand, concurrent drug release and structure disassembly

246th National Meeting (2013)

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