Erlotinib-loaded albumin nanoparticles: A novel injectable form of erlotinib and its in vivo efficacy against pancreatic adenocarcinoma ASPC-1 and PANC-1 cell lines

Int J Pharm. 2017 Oct 5;531(1):299-305. doi: 10.1016/j.ijpharm.2017.08.102. Epub 2017 Aug 25.

Abstract

Erlotinib was loaded on albumin nanoparticles for the first time and the cytotoxic effect of the resulting nanoparticles against ASPC-1 and PANC-1 pancreatic adenocarcinoma cell lines was evaluated. The carrier (albumin nanoparticles, ANPs) was synthesized by desolvation method using a mixed solvent followed by thermal crosslinking for stabilization. ANPs and the drug-loaded ANPs were characterized by field emission scanning and transmission electron microscopies, particle size analysis and Fourier transform infrared spectroscopy. The nanoformulation had a size of <14nm with a good monodispersity. Drug loading and encapsulation efficiencies were evaluated as 27 and 44%. Cytotoxicity assays after 72h revealed the potential of ANPs to improve erlotinib toxicity (54% against 34% of free drug toward ASPC-1 cell line, and 52% against 30% toward PANC-1 cell line). Values of IC50 were obtained for both cell lines and indicated significant reduction in the erlotinib dose necessary for killing the cells, while, ANPs were completely safe. The results demonstrated that erlotinib-loaded ANPs had a remarkable potential for pancreatic cancer drug delivery.

Keywords: Bovine serum albumin; Cytotoxicity; Erlotinib; Pancreatic cancer.

MeSH terms

  • Adenocarcinoma / drug therapy*
  • Albumins / chemistry*
  • Cell Line, Tumor
  • Drug Carriers / chemistry*
  • Erlotinib Hydrochloride / administration & dosage*
  • Humans
  • Nanoparticles / chemistry*
  • Pancreatic Neoplasms / drug therapy*

Substances

  • Albumins
  • Drug Carriers
  • Erlotinib Hydrochloride