Preparation, characterization, biodistribution and antitumor efficacy of hydroxycamptothecin nanosuspensions

Hydroxycamptothecin (HCPT) has shown activity against a broad spectrum of cancers, but its therapeutic efficacy is impaired by its poor solubility and delivery challenges. In this study, HCPT nanosuspensions were prepared with precipitation-combined ultrasonication and characterized by dynamic light scattering (DLS), scanning electron microscopy (SEM) and X-ray powder diffraction (XRD). The HCPT nanosuspensions were spherical with a smooth surface and a small size of 150-200 nm. The lyophilized powders for the HCPT nanosuspensions were amorphous and displayed sustained release in vitro. Compared to commercial HCPT injection, in vivo experiments with HCPT nanosuspensions showed significantly increased HCPT concentrations in the blood and all tissues of the tested as well as improved tumor targetability and liver targetability. Meanwhile, nanosuspensions displayed better anticancer efficacy than injection on H22 bearing mice (81.20% vs. 56.39%, in tumor inhibition rate). Therefore, HCPT nanosuspensions seem very promising for the treatment of hepatic cancer. (C) 2013 Elsevier B.V. All rights reserved.