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

Hardeep S. Oberoi | Zendy; N. V. Nukolova | Zendy; Yi Zhao | Zendy; Samuel M. Cohen | Zendy; Alexander V. Kabanov | Zendy; Tatiana K. Bronich | Zendy

Open Access

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

Author(s) -

Hardeep S. Oberoi,

N. V. Nukolova,

Yi Zhao,

Samuel M. Cohen,

Alexander V. Kabanov,

Tatiana K. Bronich

Publication year - 2012

Publication title -

chemotherapy research and practice

Language(s) - English

Resource type - Journals

eISSN - 2090-2115

pISSN - 2090-2107

DOI - 10.1155/2012/905796

Subject(s) - oxaliplatin , micelle , in vivo , ovarian cancer , cytotoxicity , in vitro , chemistry , platinum , pharmacology , medicine , combinatorial chemistry , biophysics , nuclear chemistry , cancer research , biochemistry , cancer , organic chemistry , aqueous solution , colorectal cancer , biology , microbiology and biotechnology , catalysis

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.

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