Pharmacokinetics and Tissue Distribution of Folate-Decorated Human Serum Albumin Loaded With Nano-Hydroxycamptothecin for Tumor Targeting

Abstract

The goal of this work is to develop the method of preparing folate (FA)-decorated human serum albumin (HSA) loaded with nano-hydroxycamptothecin (nHCPT) nanoparticles (NPs) (FA-HSA-nHCPT-NPs) and to explore its antitumor activity in vivo and in vitro. FA-HSA-nHCPT-NPs were obtained by preparing nHCPT by a high-pressure homogenization technique followed with an anti-solvent method. The drug-loading efficiency of the FA-HSA-nHCPT-NPs was 7.8%. We adopted the human breast cancer cells (FA receptor-expressing MCF-7 cells) and BALB/c mice inoculated with human MCF-7 cells to determine the antitumor activity of FA-HSA-nHCPT-NPs in vitro and in vivo, respectively. The antitumor activity of FA-HSA-nHCPT-NPs was stronger than that of the raw HCPT in both conditions. Tissue distribution analysis showed that the FA-HSA-nHCPT-NPs carried more HCPT to tumors than the raw HCPT. The tumor inhibitory rate of FA-HSA-nHCPT-NPs was much higher compared with the raw HCPT. Th7us, the FA-HSA-nHCPT-NPs could serve as a viable delivery system with an obvious target effect on tumor.

Keywords: folate-decorated human serum albumin; hydroxycamptothecin; targeted delivery system; tissue distribution.