Facile One-Pot Strategy for Radiosynthesis of 99m Tc-Doxycycline to Diagnose Staphylococcus aureus in Infectious Animal Models.

The accurate and early diagnosis of infection is an important feature in the biomedical sciences for better treatment and to decrease the rate of morbidity associated with diseases. Doxycycline (DC) is a semisynthetic antibiotic that belongs to tetracycline family and usually prescribed to treat a variety of infections. The objective of the present research work was to develop a new radiopharmaceutical 99m Tc-Doxycycline ( 99m Tc-DC), by using SnCl 2 ·2H 2 O as a reducing agent for diagnostic applications. It was confirmed through this study that 99m Tc-DC possessed high radiolabeling yield (95%). In vitro studies were performed by incubating 99m Tc-DC in human serum at 37 °C. The in vitro binding interaction of the labeled antibiotic was analyzed with bacterial strain (live Staphylococcus aureus cells), and its stability was further determined. Moreover, for in vivo infection imaging study, the infection was induced with S. aureus (gram positive) cells intramuscularly injected in mice models followed by biodistribution studies for 99m Tc-DC that were performed. Biodistribution studies of 99m Tc-DC showed that the radiotracer was significantly accumulated at the site of infection and indicated the renal route of excretion. Scintigraphic images obtained as a result of in vivo study showed good uptake of prepared radiotracer ( 99m Tc-DC) in the infectious lesions at 1-, 4-, and 24-h post-injection. Target-to-non-target ratios for 99m Tc-DC were significantly different for the infectious lesions and non-infected tissues and remained 2.13 ± 0.3 up to 24-h post-injection of 99m Tc-DC. 99m Tc-DC showed preferential binding to living bacterial infected sites as compared to other parts of the body, and thus it can be inferred that 99m Tc-DC might be a potential candidate to diagnose the infection.