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99m Tc‐Doxycycline hyclate: a new radiolabeled antibiotic for bacterial infection imaging
Author(s) -
İlemÖzdemir Derya,
Asikoglu Makbule,
Ozkilic Hayal,
Yilmaz Ferda,
HosgorLimoncu Mine,
Ayhan Semin
Publication year - 2014
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3135
Subject(s) - biodistribution , chemistry , doxycycline , spleen , in vivo , antibiotics , scintigraphy , technetium , kidney , pharmacology , nuclear medicine , medicine , biochemistry , biology , in vitro , microbiology and biotechnology , nuclear chemistry
Radiolabeled antibiotics are promising radiopharmaceuticals for the precise diagnosis and detection of infectious lesions. Doxycycline Hyclate (DOX) was chosen to investigate new 99m Tc‐labeled antibacterial agent. Ready to use freeze dry kits were formulated with optimum labeling conditions. Human serum stability, sterility, and pyrogenicity of kits were estimated, and gamma scintigraphy, in vivo biodistribution, and histopathological studies with bacterial infected rats were performed. DOX were successfully labeled by 99m Tc with high radiochemical purity, and the labeled compound was stable in human serum. Kits were sterile, pyrogen‐free, and stable up to 6 months. Static images depicted rapid distribution throughout the body and high uptake in bacterial infected thigh muscle. The uptake ratios of radiopharmaceuticals in infected thigh muscle were found above 2 up to 5 h. Five hours after injection, the rats were sacrificed, and biodistribution was determined. Samples of bacterial infected muscle, healthy muscle, blood, liver, spleen, lung, kidney, stomach, intestine, urine and heart were weighed, and the radioactivity was measured by using a gamma counter. The %ID/g of 99m Tc‐DOX was found 0.23 ± 0.06 for infected thigh muscle. According to the imaging, biodistribution, and histopathological studies, the promising characteristics of 99m Tc‐DOX make the new radiopharmaceutical valuable to examine for future studies. Copyright © 2013 John Wiley & Sons, Ltd.