NDLI: Study on the preparation and biological evaluation of $^{99m}$Tc–gatifloxacin and $^{99m}$Tc

Content Provider	Springer Nature Link
Author	Motaleb, M. A. El Kolaly, M. T. Ibrahim, A. B. Abd El Bary, A.
Copyright Year	2011
Abstract	The aim of this work is the development of new radiopharmaceuticals for imaging infection and inflammation in human. Gatifloxacin (fluoroquinolone derivative) and cefepime (cephalosporine derivative) are antibiotics used to treat bacterial infections were investigated to label with one of the most important radioactive isotopes (technetium-99m). The reaction parameters that affect the labeling yield such as substrate concentration, stannous chloride dihydrate concentration, pH of the reaction mixture, and reaction time were studied to optimize the labeling conditions. Maximum radiochemical yield of $^{99m}$Tc–gatifloxacin (90 ± 1.8%) complex was obtained by using 50 μg SnCl$_{2}$·2H$_{2}$O and 2.5 mg gatifloxacin at pH 10 while $^{99m}$Tc–cefepime was prepared at pH 8 with a maximum radiochemical yield of 98 ± 1.4% by adding $^{99m}$Tc to 5 mg cefepime in the presence of 50 μg SnCl$_{2}$·2H$_{2}$O. Biological distribution of $^{99m}$Tc–gatifloxacin and $^{99m}$Tc–cefepime was carried out in experimentally induced infection rats, in the left thigh, using Escherichia coli. Both thighs of the rats were dissected and counted and the ratio of bacterial infected thigh/contralateral thigh was then evaluated. T/NT for both $^{99m}$Tc–gatifloxacin and $^{99m}$Tc–cefepime was found to be 4.5 ± 0.3 and 8.4 ± 0.1, respectively, which was higher than that of the commercially available $^{99m}$Tc–ciprofloxacin. The abscess to normal muscle ratio indicated that $^{99m}$Tc–cefepime could be used for infection imaging. Besides, in vitro studies showed that $^{99m}$Tc–cefepime can differentiate between bacterial infection and sterile inflammation.
Starting Page	57
Ending Page	65
Page Count	9
File Format	PDF
ISSN	02365731
Journal	Journal of Radioanalytical and Nuclear Chemistry
Volume Number	289
Issue Number	1
e-ISSN	15882780
Language	English
Publisher	Springer Netherlands
Publisher Date	2011-04-05
Publisher Place	Dordrecht
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Cefepime Gatifloxacin Technetium-99m Infection Inflammation Diagnosis Nuclear Chemistry Physical Chemistry Inorganic Chemistry Diagnostic Radiology Nuclear Physics, Heavy Ions, Hadrons
Content Type	Text
Resource Type	Article
Subject	Spectroscopy Pollution Health, Toxicology and Mutagenesis Radiology, Nuclear Medicine and Imaging Analytical Chemistry Public Health, Environmental and Occupational Health Nuclear Energy and Engineering

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4	Project PI / Joint PI	Principal Investigator and Joint Principal Investigators of the project	Dr. B. Sutradhar bsutra@ndl.gov.in Prof. Saswat Chakrabarti will be added soon
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