Synthesis and evaluation of a (68)Ga labeled folic acid derivative for targeting folate receptors.

Akanksha Jain, Anupam Mathur, Usha Pandey, Jyotsna Bhatt, Archana Mukherjee, Ramu Ram, Haladhar Dev Sarma, Ashutosh Dash

Journal: Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine 2018;116():77-84

PMID: 27501138

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Abstract

Present work evaluates the potential of a newly synthesized (68)Ga-NOTA-folic acid conjugate for PET imaging of tumors over-expressing folate receptors (FRs). NOTA-folic acid conjugate was synthesized and characterized. It was radiolabeled with (68)Ga in ≥ 95% radiolabeling yields. In vitro cell binding studies showed a maximum cell uptake of 1.7±0.4% per million KB cells which was completely blocked on addition of cold folic acid showing specificity towards the FRs. However, further studies in tumor xenografts are warranted in order to assess the potential of (68)Ga-folic acid complex for imaging tumors over-expressing FRs.

Address: Isotope Production and Applications Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400085 India.; Radiopharmaceuticals Program, Board of Radiation and Isotope Technology, Navi Mumbai, 400703 India.; Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400085 India.; Isotope Production and Applications Division, Bhabha Atomic Research Centre, Trombay, Mumbai, 400085 India. Electronic address: [email protected].

DOI: 10.1016/j.apradiso.2016.07.024

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MeSH Terms: Cell Line, Tumor, Cell Survival, Folate Receptors, GPI-Anchored, Folic Acid, Gallium Radioisotopes, Humans, Isotope Labeling, KB Cells, Molecular Targeted Therapy, Neoplasms, Experimental, Radiopharmaceuticals, Radiotherapy, Treatment Outcome