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

Hardeep S OberoiNatalia V NukolovaYi ZhaoSamuel M CohenAlexander V KabanovTatiana K Bronich
Published in: Chemotherapy research and practice (2012)
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.
Keyphrases
  • drug delivery
  • cancer therapy
  • drug release
  • emergency department
  • type diabetes
  • adverse drug
  • drug induced
  • mass spectrometry
  • tandem mass spectrometry