99mTc-amoxicillin: A novel radiopharmaceutical for infection imaging

Amoxicillin, a penicillin derivative was synthesized as ready-to-used single vial kit and radiolabeled with technetium-99m. Various trials have been carried out to optimize the concentration of stannous chloride, amoxicillin, pH and reaction time. Radiochemical purity, in vitro and in vivo stability, partition co-efficient, protein binding and biodistribution in rabbit infected with Streptococcus pneumoniae were studied. The biodistribution studies in rabbit showed that ^99mTc-amoxicillin started to accumulate in the infected area at 1-h postadministration. ^99mTc-amoxicillin may prove itself as potential novel radiopharmaceutical for imaging infections caused by many bacteria.     

Synthesis of 99mTc-gemifloxacin freeze dried kits and their biodistribution in Salmonella typhi,Pseudomonas aeruginosa and Klebsiella pneumoniae

Gemifloxacin, a novel, 4th generation fluoroquinolone derivative, was labeled with^99mTc; its freeze dried kits were prepared and used for infection imaging. Kits showed great stability with higher labeling efficiency. Kits were synthesized through a simple method; developed at room temperature without HCl and heating with low colloidal content. Reaction conditions were optimized in order to get maximum radiochemical purity. Highest labeling efficiency (99 ± 0.05)% was achieved when 1.0 mg gemifloxacin was labeled with 10 mCi sodium pertechnetate in the presence of 50 μg SnCl₂ and 300 μg D-penicillamine at room temperature. Radiolabeled antibiotic kits were preclinically assessed such as in-vitro stability, lipophilicity, protein binding, in-vitro binding with bacterial strains and pharmacokinetic investigations in animals. Kits were found highly stable for 6 h both at room temperature and at 37 °C in serum. Biodistribution showed excellent uptake of activity at infection site (in Pseudomonas aeruginosa, Salmonella typhi and Klebsiella pneumoniae). Biodistribution data showed that ^99mTc-gemifloxacin has the potential and may be used for infection imaging.