Abstract

A prodrug-participating catanionic system was developed for effective delivery of the chemotherapeutic agent chlorambucil (CLB). The catanionic aggregates were easily formed by mixing as-synthesized cationic CLB prodrug, N-(2-amino-ethyl)-4-{4-[bis-(2-chloro-ethyl)-amino]-phenyl}-butyramide (CLBM) and conventional anionic surfactant sodium bis (2-ethylhexyl) sulfosuccinate (AOT). The aggregation properties, morphology and release behaviour of the CLBM-AOT aggregates were investigated. In vitro results proved CLBM-AOT aggregates owned the significantly higher cytotoxicity and intracellular accumulation compared with the respective CLB and CLBM. The desirable sustained drug release and improved anticancer activity make CLBM-AOT aggregates a promising strategy for chemotherapy.

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