Synthesis of 99mTc ‐roxithromycin: A novel diagnostic agent to discriminate between septic and aseptic inflammation

Roxithromycin (second ‐generation macrolide antibiotic) was labeled with gamma‐emitting radionuclide (i.e.,99mTc) to diagnose the early stage bacterial action by accumulation of the radiopharmaceutical at targeted site (infected byStaphylococcus aureus). In vivo studies of newly synthesized radiopharmaceutical illustrated that99mTc ‐roxithromycin can be used as potential infection imaging agent. AbstractRoxithromycin is a second ‐generation macrolide antibiotic derived from erythromycin. In the current study, roxithromycin (ROX) was successfully labeled with technetium‐99m for early diagnosis of bacterial infection and discrimination between septic and aseptic inflammation. The highest radiochemical purity of ≥95% was achieved by investigating different labeling parameters such as pH, ligand/reducing agent concentration, temperature, and amount of stabilizing agent. For this purpose, 0.3–0.5 mg ligand, 2–6 μg SnCl2·2H2O as a reducing agent at basic pH (8 –10 pH) and 2 mg mannitol used as a stabilizing agent, in the end, 370 MBq99mTc added into the reaction vials and incubated for a wide range of temperature ( −4 to 65°C). The percent radiochemical purity of99mTc ‐roxithromycin was assessed with the help of the radio‐thin‐layer chromatography technique. The characterization studies were carried out using electrophoresis and Radio‐HPLC techniques as well as saline stability and serum stability studies were also performed. Furthermore, biodistr...
Source: Chemical Biology and Drug Design - Category: Biology Authors: Tags: SPECIAL ISSUE Source Type: research