(99m) Tc-Doxycycline hyclate: a new radiolabeled antibiotic for bacterial infection imaging

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. Huma...

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Veröffentlicht in:Journal of labelled compounds & radiopharmaceuticals 2014-01, Vol.57 (1), p.36-41
Hauptverfasser: Ïlem-Özdemir, Derya, Asikoglu, Makbule, Ozkilic, Hayal, Yilmaz, Ferda, Hosgor-Limoncu, Mine, Ayhan, Semin
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container_issue 1
container_start_page 36
container_title Journal of labelled compounds & radiopharmaceuticals
container_volume 57
creator Ïlem-Özdemir, Derya
Asikoglu, Makbule
Ozkilic, Hayal
Yilmaz, Ferda
Hosgor-Limoncu, Mine
Ayhan, Semin
description 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.
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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. 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subjects Animals
Anti-Bacterial Agents - adverse effects
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacokinetics
Doxycycline - administration & dosage
Doxycycline - chemistry
Doxycycline - pharmacokinetics
Drug Stability
Escherichia coli Infections - diagnostic imaging
Humans
Isotope Labeling
Radiochemistry
Radionuclide Imaging
Rats
Rats, Wistar
Technetium
title (99m) Tc-Doxycycline hyclate: a new radiolabeled antibiotic for bacterial infection imaging
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