Radiosynthesis and biodistribution of 99mTcN-Garenoxacin dithiocarbamate complex a potential infection imaging agent

摘要

Garenoxacin (GXN) was modified to its dithiocarbamate followed by radiolabeling with technetium-99m (99mTc) through [ 99mTc-N]2+ core. The suitability of the 99mTcN-Garenoxacin dithiocarbamate (GXND) complex as a potential multiresistant Staphylococcus aureus (MDRSA) and penicillin-resistant Streptococci (PRSC) infection radiotracer was assessed in artificially infected rats (AFRT). The radiolabeled complex was investigated for its radiochemical purity (RCP), permanence in serum using HPLC and TLC methods. In vitro binding with MDRSA and PRSC was performed at 37 °C. The 99mTcN-GXND showed maximum RCP of 98.00 ± 0.22% and remained more than 90% stable up to 4 h. The 99mTcN-GXND showed saturated in vitro binding with living MDRSA and PRSC, respectively. The complex showed normal biodistribution in healthy rats (HRT), however in AFRT, seven fold uptakes was observed in infected muscle as compared to inflamed and normal muscles. Based on the high RCP, stability in serum, better in vitro binding with bacteria, biodistribution behavior and the target to non-target (infected to inflamed muscle) ratio, we recommend the 99mTcN-GXND complex for in vivo investigation of MDRSA and PRSC infection in human.