99mTc‐tazobactam, a novel infection imaging agent: Radiosynthesis, quality control, biodistribution, and infection imaging studies. (26th March 2017)

• Record Type: Journal Article
• Authors: Rasheed, Rashid; Naqvi, Syed Ali Raza; Gillani, Syed Jawad Hussain; Zahoor, Ameer Fawad; Jielani, Asif; Saeed, Nidda
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 60:Number 5(2017)
• Page Start: 242
• Page End: 249
• Publication Date: 2017-03-26
• Subjects: 99mTc‐tazobactam -- Beta‐lactamases -- infection diagnosis -- P. aeruginosa -- Radipharmaceuticals -- S. enterica; Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3494
• Languages: English
• ISSNs: 0362-4803

Abstract

Abstract : The radiolabeled drug 99m Tc‐tazobactam ( 99m Tc‐TZB) was developed and assessed as an infection imaging agent in Pseudomonas aeruginosa and Salmonella enterica infection–induced animal models by comparing with inflammation induced animal models. Radiosynthesis of 99m Tc‐TZB was assessed while changing ligand concentration, reducing agent concentration, pH, and reaction time while keeping radioactivity constant (~370 MBq). Percent labeling of the resulting complex was measured using paper chromatography and instant thin layer chromatography. The analysis of the 99m Tc‐TZB complex indicated >95% labeling yield and electrophoresis revealed complex is neutral in nature. The biodistribution study also showed predominantly renal excretion; however liver, stomach, and intestine also showed slight tracer agent uptake. The agent significantly accumulated in Pseudomonas aeruginosa and Salmonella enterica infection induced tissues 3.58 ± 0.26% and 2.43 ± 0.42% respectively at 1 hour postinjection. The inflamed tissue failed to uptake noticeable activity at 1 hour time point. The scintigraphic study results were found in accordance with biodistribution pattern. On the basis of our preliminary results, the newly developed 99m Tc‐TZB can be used to diagnose bacterial infection and to discriminate between infected and inflamed tissues. Abstract : The radiolabeled drug 99m Tc‐tazobactam was developed as a deep‐seated bacterial infection imaging agent. Pseudomonas aeruginosa and Salmonella enterica infection‐induced animal models were used to assess the infection imaging potential. The quality control analysis showed >95% radiochemical yield and significant accumulation in Pseudomonas aeruginosa and Salmonella enterica infection‐induced tissues 3.58 ± 0.26% and 2.43 ± 0.42% ID/gm organ, respectively at 1 hour post injection. The results indicated 99mTc‐tazobactam can be considered for deep‐seated infection imaging and discriminating from inflammation.