The use of polymeric platinum(IV) prodrugs to deliver multinuclear platinum(II) drugs with reduced systemic toxicity and enhanced antitumor efficacy

Biomaterials. 2012 Nov;33(33):8657-69. doi: 10.1016/j.biomaterials.2012.08.015. Epub 2012 Aug 28.

Abstract

Two dinuclear platinum(IV) prodrugs were prepared from cisplatin and oxaliplatin, and tethered to amphiphilic biodegradable block copolymers. The polymeric dinuclear platinum(IV) prodrugs were allowed to self-assemble into nanomicelles, which showed reduced systemic toxicity, relatively long blood circulation, and enhanced antitumor efficacy. In this way, the bottleneck of present multinuclear platinum drugs, especially their severe systemic toxicity, might be overcome.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Cisplatin / chemistry
  • Cisplatin / therapeutic use
  • Humans
  • Mice
  • Microscopy, Confocal
  • Nanostructures / chemistry*
  • Organoplatinum Compounds / chemistry
  • Organoplatinum Compounds / therapeutic use
  • Oxaliplatin
  • Platinum / chemistry*
  • Polymers / chemistry*
  • Prodrugs / chemistry
  • Prodrugs / therapeutic use*
  • Xenograft Model Antitumor Assays

Substances

  • Organoplatinum Compounds
  • Polymers
  • Prodrugs
  • Oxaliplatin
  • Platinum
  • Cisplatin