Radioiodination of Atorvastatin as a Model Radiopharmaceutical for Targeting Liver

Atorvastatin was radioiodinated and formulated using chloramine-T via an electrophilic substitution reaction for the development of a potential radiopharmaceutical for targeting liver. The impact of different reaction parameters and conditions that affected the labeling yield such as pH of the reaction, concentration of atorvastatin and reaction time were optimized in order to increase the radioiodination efficiency. The labeling yield was 94.3 ± 1.41 %. In vitro analysis demonstrated that the compound was steady for up to 24 h. The liver uptake was 40.35% and the clearance pathways proceed via the hepatobiliary and renal clearance.