Labeling Sultamicillin with Tc-99m and Evaluation of its Infection Detection Potential
Project no. 214 · Status: Kapanmış · 2017
Summary
Bacterial infections continue to be one of the major causes of morbidity and mortality especially in developing countries. Early detection of the site of infection non-invasively with radiolabeled compounds is important for the success of treatment. Several radiolabeled compounds reported in the literature for the diagnosis of infection, such as radiolabeled antimicrobial peptides, cytokines and antibiotics. Technetium-99m labeled antibiotics have potential to discriminate between bacterial infection and sterile inflammation. The use of radiolabeled antibiotics provides a promising approach to the precise diagnosis and detection of infectious lesions because they bind specifically to the bacterial component. Antibiotic Sultamicillin which is used in this study is the tosylate salt of the double ester of sulbactam plus ampicillin. Sultamicillin was labeled with 99mTc according to stannous chloride method with a yield 97.8±3 %. Quality control studies of radiolabeled antibiotic were performed using RTLC and RHPLC methods. Antimicrobial efficiency of 99mTc-sultamicillin was determined by in vitro binding assays in gram positive Staphylococcus aureus and gram negative Escherichia coli strains.. Maximum bacterial uptake of 99mTc-sultamicillin was determined 80.7±11 % at four hours for Staphylococcus aureus and 93.2±4 % at two hours for Escherichia coli.