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- Title
Preparation, purification and primary bioevaluation of radioiodinated ofloxacin: an imaging agent.
- Authors
Kandil, Shaban; Seddik, Usama; El-Tabl, Abdou; Hussien, Hiba; Shaltot, Mohamed
- Abstract
The broad-spectrum antibiotic agents have been demonstrated as promising diagnostic tools for early detection of infectious lesions. We set out ofloxacin (Oflo), a second-generation fluoroquinolone, for the radioiodination process. In particular, this was carried out with 125I via an electrophilic substitution reaction. The radiochemical yield was influenced by different factors; drug concentration, different oxidizing agents, e.g. chloramine-T, iodogen and n-bromosuccinimide, pH of medium, reaction time, temperature and different organic media. These parameters were studied to optimize the best conditions for labeling with ofloxacin. We found that radiolabeling in ethanol medium showed a 70% radiochemical yield of 125I-ofloxacin. The radioiodination was determined by means of TLC and HPLC. The cold labeled Oflo (127I-Oflo) was prepared and controlled by HPLC. The cold labeled Oflo was also confirmed by NMR and MS techniques. Furthermore, biodistribution studies for labeled 125I-Oflo were examined in two independent groups (3 mice in each one); control and E. Coli-injected (inflamed). The radiotracer showed a good localization in muscle of thigh for inflamed group as compared to control. In conclusion, ofloxacine might be a promising target as an anti-inflammatory imaging agent.
- Subjects
ANTIBIOTICS; FLUOROQUINOLONES; BROMOSUCCINIMIDE; NOVOBIOCIN; ESCHERICHIA coli
- Publication
Radiochimica Acta, 2015, Vol 103, Issue 7, p523
- ISSN
0033-8230
- Publication type
Article
- DOI
10.1515/ract-2014-2340