Theranostic Radiopharmaceuticals Based on Gold Nanoparticles Labeled with 177Lu and Conjugated to Peptides

Gold nanoparticles (AuNPs) have been proposed for a variety of medical applications such as localized heat sources for cancer treatment and drug delivery systems. The conjugation of peptides to AuNPs produces stable multimeric systems with target-specific molecular recognition. Lutetium- 177 (177Lu) has been successfully used in peptide radionuclide therapy. Recently, 177Lu-AuNPs conjugated to different peptides have been proposed as a new class of theranostic radiopharmaceuticals. These radioconjugates may function simultaneously as molecular imaging agents, radiotherapy systems and thermal-ablation systems. This article covers advancements in the design, synthesis, physicochemical characterization, molecular recognition assessment and preclinical therapeutic efficacy of gold nanoparticles radiolabeled with 177Lu and conjugated to RGD (-Arg-Gly-Asp-), Lys3-Bombesin and Tat(49-57) peptides.