The self-assembly of anticancer compounds has potential to enhance the water solubility, prolong the circulation time and to accumulate selectively chemotherapy drugs in tumors via the enhanced permeability and retention (EPR) effect. Camptothecin (CPT), originally isolated from the Chinese tree Camptotheca acuminate, possesses potent antitumor properties that derive from its inhibition of topoisomerase I. However, the clinical use of CPT has been severely hindered by dose-limiting toxicity, the instability of its E-ring lactone, and due to poor solubility. We report that nanotubes, derived from the aqueous self-assembly of CPT conjugates exhibit significantly improved solubility and hydrolytic stability under physiological conditions.

Self-assembled camptothecin-peptide conjugate prodrugs

245th National Meeting (2013)

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