Due to poor water solubility of hydrophobic anti-cancer drugs and inefficient tumor targeting delivery, the development of safe and efficient drug delivery systems (DDSs) for clinic application is still a challenge. Herein, we have constructed a facile DDS based on biodegradable polymeric micelles which cross-linked by stimuli-cleavable drug dimers. Firstly, a double hydrophilic copolymer containing cyclodextrin pendant groups was synthesized by ring-opening polymerization and click chemistry and a drug dimer was formed by linking two doxorubicins with disulfide bond. Secondly, they co-assembled into micelles in water via host-guest interaction and the average size was around 100 nm. It is fit for passive targeting delivery by EPR effect. Drug dimers were utilized as cross-linkers to stabilize the micelles. Owing to the disulfide bonds of drug dimers, these supramolecular micelles were dissociated by treating with dithiothreitol (DTT). In the meanwhile, the free drugs were recovered and released from cavities of cyclodextrins because of dynamic equilibrium. Therefore, it can be served as a novel and controlled drug delivery system.

Drug dimer cross-linked supramolecular micelles for cancer therapy

246th National Meeting (2013)

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