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

Abstract EN

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.