Catanionic drug-derivative nano-objects constructed by chlorambucil and its derivative for efficient leukaemia...

A new carrier-free catanionic drug-derivative nano-object strategy is developed for leukaemia therapy. The as-prepared drug-derivative nano-objects are formed by ionic pairs of hydrophobic anticancer drug chlorambucil (CLB) and its derivative N-(2-Amino-ethyl)-4-{4-[bis-(2-chloro-ethyl)-amino]-phenyl}-butyramide (CLBM). The designed drug delivery system has the advantage of 100% drug content without additional carrier materials. The ionic pairs are formed by proton exchange between CLB and CLBM. Due to the amphiphilicity of the ionic pairs, they can assemble into well-defined drug-derivative (CLB-CLBM) nano-objects. Series of techniques such as transmission electron microscopy (TEM), dynamic light scattering (DLS) and electrical conductivity are used to investigate the property of the solution and aggregation behaviour of as-prepared drug-derivative ionic pairs. In vitro drug release study of the as-prepared nano-objects shows their prolonged drug release behavior. Specifically, in vitro cytotoxicity results of these nano-objects show obviously higher cytotoxicity, which is promising for clinical efficacy. This study may pave the way for the fabrication of carrier-free drug delivery system with efficient cancer therapy.