Table of Contents
Chemotherapy Research and Practice
Volume 2012 (2012), Article ID 905796, 10 pages
http://dx.doi.org/10.1155/2012/905796
Research Article

Preparation and In Vivo Evaluation of Dichloro(1,2-Diaminocyclohexane)platinum(II)-Loaded Core Cross-Linked Polymer Micelles

1Department of Pharmaceutical Sciences and Center for Drug Delivery and Nanomedicine, College of Pharmacy, University of Nebraska Medical Center, Omaha, NE 68198-5830, USA
2Department of Chemistry, M.V. Lomonosov Moscow State University, Leninskie Gory, V-234, Moscow 119992, Russia
3Department of Pathology and Microbiology and Havlik-Wall Professor of Oncology, University of Nebraska Medical Center, Omaha, NE 68198-3135, USA

Received 24 February 2012; Revised 10 April 2012; Accepted 26 April 2012

Academic Editor: Vassilios A. Georgoulias

Copyright © 2012 Hardeep S. Oberoi et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

The therapeutic performance of oxaliplatin can be improved by incorporating the central cis-dichloro(1,2-diaminocyclohexane)platinum(II) (DACHPt) motif into the core cross-linked block copolymer micelles. We describe here the preparation, cellular uptake, and in vivo evaluation of core cross-linked micelles loaded with DACHPt. Stable drug-loaded micelles were prepared at high drug loading (~25 w/w%) and displayed a considerably increased in vitro cytotoxicity compared to free oxaliplatin against A2780 ovarian cancer cells. The DACHPt-loaded micelle formulation was well tolerated in mice and exhibited improved antitumor activity than oxaliplatin alone in an ovarian tumor xenograft model.