Development of Radiolabeling Methods for 5 Fluorouracil (5FU) with Technetium-99mfor Preclinical Nuclear Imaging (PNI)

Background: 5-Fluorouracil (5-FU) is a well known anti metabolites and extensively used inchemotherapy. The search of target specific radiopharmaceutical is always on in field of radiopharmaceutical anddiagnostic nuclear imaging. In this study we have developed the radiolabling methodology for the 5-FU with Technetium-99m for preclinical nuclear imaging evaluation of 99mTc- labeled 5-FU.

Methods: We have used radio pharmacy lab and its equipments of Bhagwan Mahaveer Cancer Hospital &Research Centre (BMCHRC), Jaipur, Rajasthan, India. We have used simple basic radiochemical reactions for theradiolabeling of the 5-FU. 99mTc pertechnetate, an elute from 99Mo-99mTc generator used for tagging. A series of highgrade and analytical chemical were used and a few from outside without further purification e.g. L-Cysteine Monohydraeacid, SnCl2.2.H2O, Normal Saline, Distilled water, pH meter. SnCl2.2H2O was used for the reduction reaction. Postradiolableing paper and ITL chromatography techniques used for the standardization and characterization of the labeledradiopharmaceutical.

Results: We have observed >95.66% radiolabeling efficiency of 5-Fluorouracil (5-FU) with Technetium-99m by the paperchromatography (PC) and instant thin layer chromatography (ITLC) radiochemical efficiency labelling techniques.

Conclusions: As per our observation and study 99mTc-5-FU has a potential to be of becoming a useful tool for the NuclearImaging of solid tumor. The labeled drug can be used for the gamma imaging after conducting further clinical trials onanimal and human. Key-words: Radiolabeling, Preclinical Nuclear Imaging (PNI), 5-Fluorouracil (5-FU), Paper Chromatography (PC) andInstant Thin Layer Chromatography (ITLC)