RGD-HK Peptide-Functionalized Gold Nanorods Emerge as Targeted Biocompatible Nanocarriers for Biomedical Applications

ABSTRACT: Gold nanorods (GNRs) have been nominated as a promising candidate for a variety of biological applications; however, the cationic surfactant layer that surrounds a nanostructure places limits on its biological applicability. Herein, CTAB-GNRs were functionalized via a ligand exchange method using a (C(HK)4-mini PEG-RGD)-peptide to target the overexpressed αvβ3 integrin in cancerous cells, increase the biocompatibility, and gain the ability of gene/drug delivery, simultaneously. To confirm an acceptable functionalization, UV–Visible, FTIR, and Raman spectroscopy, zeta potential, and transmission electron microscopy of nanostructures were done. MTT assay was applied to study the cytotoxicity of nanostructures on two cell lines, HeLa and MDA-MB-231, as positive and negative αvβ3 integrin receptors, respectively. The cytotoxic effect of peptide-functionalized GNRs (peptide-f-GNRs) was less than that of CTAB-coated GNRs (CTAB-GNRs) for both cell lines. Uptake of peptide-f-GNRs and CTAB-GNRs was evaluated in two cell lines, using dark-field imaging and atomic absorption spectroscopy. Peptide-f-GNRs showed a proper cell uptake on the HeLa rather than MDA-MB-231 cell line according to the RGD (Arg-Gly-Asp) sequence in the peptide. The ability of peptide-f-GNRs to conjugate to antisense oligonucleotides (ASO) was also confirmed using zeta potential, which was due to the repeated HK (His-Lys) sequence inside the peptide. The result of these tests highlights the functionalization method as a convenient and cost-effective strategy for promising applications of targeted GNRs in the biological gene/drug delivery systems, and the repeated histidine-lysine pattern could be a useful carrier for negatively charged drug/gene delivery, too. GRAPHICAL ABSTRACT: [Image: see text]