In vitro and in vivo evaluation of camptothecin nanosuspension: a novel formulation with high antitumor efficacy and low toxicity

Abstract

The purpose of this study was to evaluate the in vitro and in vivo antitumor efficacy and the dose dependent toxicity of camptothecin nanosuspension (Nano-CPT) comparing with that of topotecan (TPT). A novel supercritical antisolvent (SAS) process-high pressure homogenization technique has been developed to prepare Nano-CPT. The cytotoxicity of Nano-CPT and TPT was investigated against MCF-7, HCT-8, and PC-3 cell lines using MTT assay, antitumor activity in vivo were evaluated against HCT-8 xenograft model, and the dose dependent toxicity in vivo during the treatment were investigated by body weight changes and relative organ weight variations. The Nano-CPT presents about 6 times in vitro cytotoxicity active than TPT against cell lines MCF-7, nearly the same in vivo antitumor activity with TPT and lower toxicity. The results confirm that Nano-CPT is a novel potential formulation with high antitumor efficacy and low toxicity.