Bevacizumab loaded solid lipid nanoparticles prepared by the coacervation technique: preliminary in vitro studies

Nanotechnology. 2015 Jan 26;26(25):255102. doi: 10.1088/0957-4484/26/25/255102. Epub 2015 Jun 5.

Abstract

Glioblastoma, the most common primary brain tumor in adults, has an inauspicious prognosis, given that overcoming the blood-brain barrier is the major obstacle to the pharmacological treatment of brain tumors. As neoangiogenesis plays a key role in glioblastoma growth, the US Food and Drug Administration approved bevacizumab (BVZ), an antivascular endothelial growth factor antibody for the treatment of recurrent glioblastoma in patients whose the initial therapy has failed. In this experimental work, BVZ was entrapped in solid lipid nanoparticles (SLNs) prepared by the fatty-acid coacervation technique, thanks to the formation of a hydrophobic ion pair. BVZ activity, which was evaluated by means of four different in vitro tests on HUVEC cells, increased by 100- to 200-fold when delivered in SLNs. Moreover, SLNs can enhance the permeation of fluorescently labelled BVZ through an hCMEC/D3 cell monolayer-an in vitro model of the blood brain barrier. These results are promising, even if further in vivo studies are required to evaluate the effective potential of BVZ-loaded SLNs in glioblastoma treatment.

MeSH terms

  • Angiogenesis Inhibitors / administration & dosage*
  • Angiogenesis Inhibitors / chemistry
  • Angiogenesis Inhibitors / therapeutic use
  • Bevacizumab / administration & dosage*
  • Bevacizumab / chemistry
  • Bevacizumab / therapeutic use
  • Cells, Cultured
  • Drug Carriers / chemistry*
  • Fatty Acids / chemistry*
  • Glioblastoma / drug therapy
  • Human Umbilical Vein Endothelial Cells
  • Humans
  • Hydrophobic and Hydrophilic Interactions
  • In Vitro Techniques
  • Nanoparticles / administration & dosage*
  • Nanoparticles / chemistry
  • Particle Size
  • Permeability

Substances

  • Angiogenesis Inhibitors
  • Drug Carriers
  • Fatty Acids
  • Bevacizumab