Morphology control of self-deliverable nanodrug with enhanced anticancer efficiency.

ABSTRACT

The morphology of nanomedicines has a large influence on the anticancer efficiency of therapeutic agents in biological systems. In this study, camptothecin (CPT)-based nanodrugs with helical and spherical shapes were simply built without the need of any additional carriers. Self-deliverable spherical nanodrug represented a therapeutic advantage over the helical one, which was uncovered from the in vitro toxicity assay. Confocal imaging study indicated that the better outcome of spherical nanodrug was ascribed to the faster cellular uptake. With the aid of sonication treatment, helical nanodrugs with different lengths (HD-1, HD-2, HD-3, HD-4) were created. In comparing with the longest HD-1, the drug release kinetics indicated that the shortest HD-4 exhibited a 20% elevation in cumulative drug release at the first 10 h. The internalized drug amount of HD-4 was three-fold higher than that of HD-1 after the cultivation with 4T1 cells for 2 h. These results demonstrated that the anticancer efficacy of helical nanodrugs was inversely proportional to their lengths. The strategy demonstrated here presents great promise for the preparation of nanodrugs with suitable morphology for cancer therapy.