Amphiphilic oligomer-based micelles as cisplatin nanocarriers for cancer therapy

Nanoscale. 2013 Oct 7;5(19):8925-9. doi: 10.1039/c3nr03262k. Epub 2013 Aug 9.

Abstract

Polymeric micelles (∼10 nm) have been prepared from the amphiphilic oligomer comprising oligomeric polystyrene as the hydrophobic inner core and half of EDTA (-N(CH₂COOH)₂) as the hydrophilic outermost shell. After chelating cisplatin with -N(CH₂COOH)₂ in water, polymeric micelles containing Pt on the spherical surface have been easily obtained. Since the chelate group is introduced into the amphiphilic oligomer as the terminal group by a RAFT agent, the chelation of cisplatin with PS(COOH)₂ is almost stoichiometric. The drug carrier based on PS(COOH)₂ showed a high loading efficiency (>70%) towards cisplatin. The release of the therapeutic Pt from the cisplatin-loaded composites (PS(COOH)₂-Pt) triggered under weak acidic conditions resulted in good Pt-release and accumulation in tumor cells. Both in vitro and in vivo, the chelated cisplatin inhibited Sk-Br3 cancer more effectively than the intact cisplatin does. Furthermore, neither PS(COOH)₂ nor PS(COOH)₂-Pt showed obvious systematic toxicity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Cisplatin / administration & dosage*
  • Cisplatin / chemistry
  • Cisplatin / toxicity
  • Coordination Complexes / chemistry
  • Coordination Complexes / toxicity
  • Drug Carriers / chemistry*
  • Edetic Acid / chemistry
  • Female
  • Humans
  • Hydrogen-Ion Concentration
  • Hydrophobic and Hydrophilic Interactions
  • Mice
  • Mice, Nude
  • Micelles*
  • Nanoparticles / chemistry*
  • Neoplasms / drug therapy*
  • Neoplasms / pathology
  • Polystyrenes / chemistry
  • Transplantation, Heterologous

Substances

  • Coordination Complexes
  • Drug Carriers
  • Micelles
  • Polystyrenes
  • Edetic Acid
  • Cisplatin