A novel supramolecular reduction-sensitive biodegradable system was exploited for triggered and sustained intracellular release of doxorubicin (DOX). In this study, polyrotaxane micelles were synthesized based on partially threaded a-cyclodextrin (a-CD) and 8-arm polyethylene glycol (PEG) with disulfide-linkage.   The polyrotaxane (PR) could self-assemble to micelle structure in water and the resulted micelles, though sufficiently stable in water, were prone to fast degradation in the presence of dithiothreitol (DTT), due to the reductive cleavage of the intermediate disulfide bonds.   After encapsulating DOX, the nano-sized particles showed great potential to be used as carrier for the release of doxorubicin (DOX) with high drug loading efficiency and stimuli-responsive in vitro release. Remarkably, the micelles significantly enhanced the cellular uptake of DOX and its cytotoxicity against cancer cells. As a continuation of current study, these biodegradable polyrotaxane micelles highlight a great potential as carriers for triggered, sustained and efficient intracellular drug delivery.

Supramolecular micelles as vectors for stimuli-responsive drug release

243rd National Meeting (2012)

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