Synthesis and biological evaluation of ¹³¹I‐labelled pyronaridine

Abstract

Abstract:131 I-Labelled pyronaridine, an antimalarial drug was synthesized and evaluated for its stability and biodistribution in rabbits. We observed that there was >99% yield of the labelled compound as determined by HPLC and radio-TLC in our study. Dynamic imaging studies in rabbits showed that 131 I-labelled pyronaridine was not concentrated in the thyroid for up to 30 min as that of Na 131 I. Biodistribution studies in the blood, liver, heart, spleen, kidney and lung of rats revealed that the maximum percentage of the injected dose (% ID) and the percentage of the injected dose per gram organ weight (% ID/g) of 131 I-labelled pyronaridine was found in the blood and liver when compared to the other organs even after 6 days of the drug administration. Results suggest that 131 I-labelled pyronaridine can be effectively used as an imaging agent to study the metabolism and mode of a response of pyronaridine.