Facile One-Pot Synthesis of Intrinsically Radiolabeled and Cyclic RGD Conjugated 199Au Nanoparticles for Potential Use in Nanoscale Brachytherapy

Abstract

The synthesis of intrinsically radiolabeled nanoparticles has shown tremendous prospective in offering an easier, faster, stable, and more specific radiolabeling technique for the development of advanced radionanomedicine agents for cancer treatment. In this study, a facile one-pot synthesis protocol for the preparation of cyclic arginine–glycine–aspartate (RGD) conjugated and intrinsically radiolabeled 199Au (t1/2 = 3.14 d; β1 = 462 keV, 6.0%; β2 = 296 keV, 71.6%; β3 = 250 keV, 22.4%; γ = 159 keV, 37%) nanoparticles has been developed for targeting integrin αvβ3 receptors for potential use in neoadjuvant brachytherapy. The nanoparticles synthesized by this method were characterized by numerous analytical methods to determine the identity, particle size, in vitro stability, biocompatibility, and amenability for clinical use. Large-scale synthesis of intrinsically radiolabeled 199Au nanoparticles could be achieved with excellent yield, and they met all the requirements for clinical use. The biological effi...