Delivery of active DACH-Pt anticancer species by biodegradable amphiphilic polymers using thiol-ene radical addition

Macromol Biosci. 2012 Mar;12(3):367-73. doi: 10.1002/mabi.201100320. Epub 2011 Dec 23.

Abstract

A biodegradable and amphiphilic copolymer, mPEG-b-P(LA-co-MAC/TMA) that contains pendant 1,2-bidentate carboxyl groups is synthesized by thiol-ene radical addition and is further used to chelate with the active anticancer species (DACH-Pt) of oxaliplatin to form an mPEG-b-P(LA-co-MAC/TMA-Pt-DACH) complex. The polymer platinum complex can self-assemble into micelles. In vitro studies show that the DACH-Pt micelles display enhanced or comparable cytotoxicity against SKOV-3 and MCF-7 cancer cells, while they show reduced toxicity to HeLa cells compared with oxaliplatin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antineoplastic Agents / chemistry*
  • Antineoplastic Agents / pharmacology
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Drug Carriers / chemical synthesis*
  • Humans
  • Inhibitory Concentration 50
  • Magnetic Resonance Spectroscopy
  • Micelles
  • Organoplatinum Compounds / chemistry*
  • Organoplatinum Compounds / pharmacology
  • Oxaliplatin
  • Polyesters / chemical synthesis*
  • Polyethylene Glycols / chemical synthesis*
  • Sulfhydryl Reagents / chemistry*
  • Surface-Active Agents / chemical synthesis*

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Micelles
  • Organoplatinum Compounds
  • Polyesters
  • Sulfhydryl Reagents
  • Surface-Active Agents
  • Oxaliplatin
  • Polyethylene Glycols