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

• Published in: Journal of radioanalytical and nuclear chemistry Vol. 288; no. 1; pp. 59 - 64
• Main Authors: Shah, Syed Qaiser, Khan, Aakif Ullah, Khan, Muhammad Rafiullah
• Format: Journal Article
• Language: English
• Published: Dordrecht Springer Netherlands 01.04.2011
• Subjects: Chemistry; Chemistry and Materials Science; Diagnostic Radiology; Hadrons; Heavy Ions; Inorganic Chemistry; Nuclear Chemistry; Nuclear Physics; Physical Chemistry; Staphylococcus aureus; Garenoxacin dithiocarbamate; [; MDRSA; Tc-N; PRSC
• ISSN: 0236-5731; 1588-2780
• DOI: 10.1007/s10967-010-0871-3

Garenoxacin (GXN) was modified to its dithiocarbamate followed by radiolabeling with technetium-99m ( 99m Tc) through [ 99m Tc-N] 2+ core. The suitability of the 99m TcN–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 99m TcN–GXND showed maximum RCP of 98.00 ± 0.22% and remained more than 90% stable up to 4 h. The 99m TcN–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 99m TcN–GXND complex for in vivo investigation of MDRSA and PRSC infection in human.