Local delivery of imatinib mesylate (STI571)-incorporated nanoparticle ex vivo suppresses vein graft neointima formation

Circulation. 2008 Sep 30;118(14 Suppl):S65-70. doi: 10.1161/CIRCULATIONAHA.107.740613.

Abstract

Background: Clinical outcome of surgical revascularization using autologous vein graft is limited by vein graft failure attributable to neointima formation. Platelet-derived growth factor (PDGF) plays a central role in the pathogenesis of vein graft failure. Therefore, we hypothesized that nanoparticle (NP)-mediated drug delivery system of PDGF-receptor (PDGF-R) tyrosine kinase inhibitor (imatinib mesylate: STI571) could be an innovative therapeutic strategy.

Methods and results: Uptake of STI571-NP normalized PDGF-induced cell proliferation and migration. Excised rabbit jugular vein was treated ex vivo with PBS, STI571 only, FITC-NP, or STI571-NP, then interposed back into the carotid artery position. NP was detected in many cells in the neointima and media at 7 and 28 days after grafting. Significant neointima was formed 28 days after grafting in the PBS group; this neointima formation was suppressed in the STI571-NP group. STI571-NP treatment inhibited cell proliferation and phosphorylation of the PDGF-R-beta but did not affect inflammation and endothelial regeneration.

Conclusions: STI571-NP-induced suppression of vein graft neointima formation holds promise as a strategy for preventing vein graft failure.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Aorta / cytology
  • Aorta / metabolism
  • Benzamides
  • Cell Movement / drug effects
  • Cell Proliferation / drug effects
  • Cells, Cultured
  • Coronary Vessels / cytology
  • Coronary Vessels / metabolism
  • Drug Delivery Systems*
  • Humans
  • Imatinib Mesylate
  • In Vitro Techniques
  • Intracellular Membranes / metabolism
  • Jugular Veins / drug effects
  • Jugular Veins / transplantation*
  • Male
  • Muscle, Smooth, Vascular / cytology
  • Myocytes, Smooth Muscle / cytology
  • Myocytes, Smooth Muscle / metabolism
  • Myocytes, Smooth Muscle / physiology
  • Nanoparticles*
  • Phosphorylation / drug effects
  • Piperazines / administration & dosage*
  • Piperazines / pharmacokinetics
  • Piperazines / pharmacology
  • Protein Kinase Inhibitors / administration & dosage*
  • Protein Kinase Inhibitors / pharmacokinetics
  • Protein Kinase Inhibitors / pharmacology
  • Pyrimidines / administration & dosage*
  • Pyrimidines / pharmacokinetics
  • Pyrimidines / pharmacology
  • Rabbits
  • Rats
  • Receptor, Platelet-Derived Growth Factor beta / metabolism
  • Tissue Distribution
  • Tunica Intima / drug effects*
  • Tunica Intima / pathology

Substances

  • Benzamides
  • Piperazines
  • Protein Kinase Inhibitors
  • Pyrimidines
  • Imatinib Mesylate
  • Receptor, Platelet-Derived Growth Factor beta