Technetium-99m Tricarbonyl Labeled a Broad-spectrum Quinolone as a Specific Imaging Agent in Infection Diseases

Iran J Pharm Res. Spring 2017;16(2):611-618.


Nuclear medicine imaging has been used to localize infection sites, and efforts have been continued to develop modified infection specific radiopharmaceuticals. In this study gemifloxacin as a broad-spectrum quinolone has been labeled with [99mTc (CO)3 (H2O)3]+ core in order to evaluate its feasibility as an infection imaging agent for in-vivo use. The stability of radioconjugate was checked in human serum at 37 °C and biodistribution was studied in mice. Labeling yield of > 95% was obtained corresponding to a specific activity of 0.14 GBq/μmol. The radioconjugate showed good stability in human serum. Our main achievement was the high accumulation in the infected muscle in mice (T/NT = 2.93 ± 0.3 at 1 h post injection), which may diagnostically be beneficial for differentiate sites of infection from sites of inflammation.

Keywords: 99mTc-carbonyl; Gemifloxacin; Imaging; Infection; Quinolone.