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Nuclear Medicine and Biology
Clinical scale synthesis of intrinsically radiolabeled and cyclic RGD peptide functionalized 198Au nanoparticles for targeted cancer therapy
Rubel Chakravarty a,d, , Sudipta Chakraborty a,d, Apurav Guleria b, Chandan Kumar a, Amit Kunwar b, K.V. Vimalnath Nair a, Haladhar Dev Sarma c, Ashutosh Dash a,d
a Radiopharmaceuticals Division, Bhabha Atomic Research Centre, Trombay, Mumbai 400 085, India
b Radiation and Photochemistry Division, Bhabha Atomic Research Centre, Trombay, Mumbai 400 085, India
c Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Trombay, Mumbai 400 085, India
d Homi Bhabha National Institute, Anushaktinagar, Mumbai 400 094, India
Article history:
Keywords: 198Au
Cancer therapy
Intrinsically radiolabeled nanoparticles
Radiolabeling
Radionanomedicine
RGD 
Introduction: The emerging concept of intrinsically radiolabeled nanoparticles has the potential to transform the preclinical and clinical studies by improving the in vivo stability and demonstrating minimal alteration in the in-herent pharmacokinetics of the nanoparticles. In this paper, a simple and efficient single-step method for clinical scale synthesis of intrinsically radiolabeled 198Au nanoparticles conjugated with cyclic arginine−glycine−aspar-rtate peptide (198AuNP-RGD) is reported for potential use in targeted cancer therapy.
Methods: Large radioactive doses (N37 GBq) of 198AuNP-RGD were synthesized by reaction of 198Au-HAuCl4 with cyclic RGD peptide. The synthesized nanoparticles were characterized by various analytical techniques. In vitro cell binding studies were carried out in B16F10 (murine melanoma) cell line. Biodistribution studies were carried out in melanoma tumor bearing C57BL/6 mice to demonstrate the tumor targeting ability of 198AuNP-RGD. The therapeutic efficacy of 198AuNP-RGD was evaluated by carrying out systematic tumor regression studies in mel-anoma tumor bearing mice after intravenous administration of the radioactive doses.