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- Title
Technetium‐99m radiolabeling and biological study of epirubicin for in vivo imaging of multi‐drug‐resistant Staphylococcus aureus infections via single photon emission computed tomography.
- Authors
Khan, Naeem‐Ul‐Haq; Naqvi, Syed Ali Raza; Khan, Zulfiqar Ali; Zahoor, Ameer Fawad; Roohi, Samina; Sherazi, Tauqir A.
- Abstract
The development of functional imaging is a promising strategy for diagnosis and treatment of infectious and cancerous diseases. In this study, epirubicin was developed as a [99mTc]‐labeled radiopharmaceutical for the imaging of multi‐drug‐resistant Staphylococcus aureus infections. The labeling was carried out using sodium pertechnetate (Na99mTcO4; ~370 MBq). The other parameters such as amount of ligand, reducing agent (SnCl2.2H2O), and pH were optimized. The highest labeling yield ≥96.98% was achieved when 0.3 mg epirubicin, 13 μg SnCl2.2H2O, and ~370 MBq Na99mTcO4 were incubated at pH 7 for 15 min in the presence of ascorbic acid at room temperature. Radiochemical purity, stability, charge, and glomerular filtration rate were studied to evaluate the biological compatibility for in vivo administration. Biodistribution investigations showed radiotracer uptake (13.89 ± 1.56% ID/gm organ) by liver and 7.79 ± 0.38% ID/gm organ by kidneys at 30 min post‐injection which promisingly wash out at 24 hr post‐injection. Scintigraphy study showed selective uptake in S. aureus‐infected tissues in contrast to turpentine oil‐induced inflamed tissues. Target‐to‐non‐target ratio (6.7 ± 0.05) was calculated at 1 hr post‐injection using SPECT gamma camera. The results of this study reveal that the [99mTc]‐epirubicin can be a choice of imaging and monitoring the treatment process of multi‐drug resistant S. aureus bacterial infections. Epirubicin is a cell‐permeable antineoplastic antitumor drug of the anthracycline family, and it is considered a target‐specific anticancer drug and also target infection causing bacteria. The protocol of radiolabeling of epirubicin with 99mTc was developed to target the multi‐drug resistant Staphylococcus aureus (MDRSA) infection, induced in rat model. The results showed promising uptake in S. aureus infection, and it can be investigated clinically for MDRSA bacterial infection imaging.
- Subjects
EPIRUBICIN; DIAGNOSTIC imaging; STAPHYLOCOCCUS aureus infections; TECHNETIUM; RADIOLABELING; DRUG resistance in bacteria; SINGLE-photon emission computed tomography
- Publication
Chemical Biology & Drug Design, 2019, Vol 93, Issue 2, p154
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.13393