Colloidal gold nanoparticle conjugates of gefitinib

Abstract

Gefitinib (GF) is a US Food and Drug Administration-approved epidermal growth factor receptor (EGFR)tyrosine kinase inhibitor for treating the lung cancers. We fabricated colloidal gold nanoparticle (AuNP) conjugates of the GF anticancer drug by self-assembly to test their potency against A549, NCI-H460, and NCI-H1975 lung cancer cells. GF adsorption on AuNP surfaces was examined by UV vis absorption spectra and surface-enhanced Raman scattering. Density functional theory calculations were performed to estimate the energetic stabilities of the drug-AuNP composites. The N1 nitrogen atom of the quinazoline ring of GF was calculated to be more stable than the N3 in binding Au cluster atoms. The internalizations of GF-coated AuNPs were examined by transmission electron and dark-field microscopy. A cell viability test of AuNP GF conjugates with the EGFR antibody exhibited much higher reductions than free GF for A549, NCI-H460, and NCI-H1975 lung cancer cells after treatment for 48 h. (C) 2014 Elsevier B.V. All rights reserved.