Radiocomplexation and biological characterization of the 99mTcN-trovafloxacin dithiocarbamate. A novel methicillin-resistant Staphylococcus aureus infection imaging agent

The radiolabeling of trovafloxacin dithiocarbamate (TVND) with technetium-99m using [99mTc-N]2+ core was investigated and biologically assessed as prospective infection imaging agent. The achievability of the 99mTcN-TVND complex as a future MRSA infection radiotracer was investigated in artificially methicillin-resistant Staphylococcus aureus (MRSA) infected male Sprague-Dawley rats (MSDR). Radiochemically the 99mTcN-TVND complex was characterized in terms of radiochemical purity (RCP) in saline, in vitro permanence in serum, in vitro binding with MRSA and biodistribution in living and heat killed MRSA infected MSDR. Radiochemically the complex showed stability in saline with a 97.90 ± 0.22% yield and serum at 37 deg C up to 4 h. The 99mTcN-TVND complex showed saturated in vitro binding with MRSA. Normal in vivo uptake in the MRSA infected MDRS was observed with a five fold uptake in the infected muscle as compared to inflamed and normal muscles. The high RCP values, in vitro permanence in serum, better in vitro binding with MRSA, biodistribution behavior and the target to non-target (infected to inflamed muscle) ratios posed the 99mTcN-TVND complex as a promising MRSA infection radiotracer. (author)