Enhancing the efficiency of bortezomib conjugated to pegylated gold nanoparticles: an in vitro study on human pancreatic cancer cells and adenocarcinoma human lung alveolar basal epithelial cells

Expert Opin Drug Deliv. 2016 Aug;13(8):1075-81. doi: 10.1080/17425247.2016.1178234. Epub 2016 May 2.

Abstract

Objectives: Gold nanoparticles have become promising vectors for cancer diagnosis and treatment. The present study investigates the effect of bortezomib (BTZ), a proteasome inhibitor, conjugated with pegylated gold nanoparticles (PEGAuNPs) in pancreatic and lung cancer cells.

Methods: Synthesized gold nanoparticles (PEGAuNPs) were conjugated with bortezomib antitumor drug. We investigated the cytotoxicity induced by BTZ conjugated with functionalized gold nanoparticles in vitro, in the human pancreatic (S2-013) and lung (A549) cancer cell lines.

Results: We found an efficient of conjugation of BTZ with PEGAuNPs. In vitro assays showed that after 72 h' incubation with PEGAuNPs-BTZ cancer cells revealed alterations in morphology; also for S2-013 and A549 cancer cells, the IC50 value of free BTZ is respectively 1.5 and 4.3 times higher than the IC50 value of PEGAuNPs-BTZ. Furthermore, for TERT-HPNE, the IC50 value is around 63 times lower for free BTZ than the conjugated nanovehicle. Cell growth inhibition results showed a remarkable enhancement in the effect of BTZ when conjugated with AuNPs.

Conclusions: Our findings showed that conjugation with PEGAuNPs enhance the BTZ growth-inhibition effect on human cancer cells (S2-013 and A549) and decreases its toxicity against normal cells (TERT-HPNE).

Keywords: Bortezomib; gold nanoparticles; lung cancer; pancreatic cancer.

MeSH terms

  • Adenocarcinoma / drug therapy*
  • Adenocarcinoma of Lung
  • Antineoplastic Agents / administration & dosage*
  • Antineoplastic Agents / therapeutic use
  • Bortezomib / administration & dosage*
  • Cell Line, Tumor
  • Epithelial Cells / drug effects
  • Gold / chemistry
  • Humans
  • Lung Neoplasms / drug therapy*
  • Nanoparticles
  • Pancreatic Neoplasms / drug therapy*
  • Proteasome Inhibitors / administration & dosage

Substances

  • Antineoplastic Agents
  • Proteasome Inhibitors
  • Bortezomib
  • Gold