Abstract
Technetium-99m-sarafloxacin was synthesized and formulated for the development of a potential diagnostic imaging agent for the bacterial infection and inflammation with higher efficiency than the commercially available Tc-99m-ciprofloxacin. Factors influencing the labeling yield such as sarafloxacin amount, pH of the labeling reaction, SnCl2 amount and reaction time were optimized. The labeled drug was subjected to preclinical evaluations in mice. The biodistribution studies indicated that Tc-99m-sarafloxacin displayed relatively high uptake in the infectious lesion (T/NT = 4.2 +/- 0.1) at 2 h post-injection. The results revealed that Tc-99m-sarafloxacin cannot discriminate infection from sterile inflammation.