Synthesis and in vitro evaluation of an antiangiogenic cancerspecific dual-targeting 177Lu-Au-nanoradiopharmaceutical

Abstract

The aim of this research was to synthesize and chemically characterize a cancer-specific 177Lu-Aunanoradiopharmaceutical based on gold nanoparticles (NPs), the nuclear localization sequence (NLS)-Arg-Gly- Asp peptide and an aptamer (HS-pentyl-pegaptanib) to target both the a(v)b(3) integrin and the vascular endothelial growth factor (VEGF) overexpressed in the tumor neovasculature, as well as to evaluate by the tube formation assay, the nanosystem capability to inhibit angiogenesis. 177Lu-NP-RGD-NLS-Aptamer was obtained with a radiochemical purity of 99 ± 1%. Complete inhibition of tube formation (angiogenesis) was demonstrated when endothelial cells (EA.hy926), cultured in a 3D-extracellular matrix support, were treated with the developed nanosystem.