title: (99m) Tc-Doxycycline hyclate: a new radiolabeled antibiotic for bacterial infection imaging.
abstract: 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.
authors.affiliation: Faculty of Pharmacy, Department of Radiopharmacy, Ege University, Bornova, Izmir, Turkey.
authors.forename: Derya
authors.initials: D
authors.lastname: Ïlem-Özdemir
authors.forename: Makbule
authors.initials: M
authors.lastname: Asikoglu
authors.forename: Hayal
authors.initials: H
authors.lastname: Ozkilic
authors.forename: Ferda
authors.initials: F
authors.lastname: Yilmaz
authors.forename: Mine
authors.initials: M
authors.lastname: Hosgor-Limoncu
authors.forename: Semin
authors.initials: S
authors.lastname: Ayhan
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000009:adverse effects / Q000737:chemistry / Q000493:pharmacokinetics; D004318:Doxycycline / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D004355:Drug Stability; D004927:Escherichia coli Infections / Q000000981:diagnostic imaging*; D006801:Humans; D007553:Isotope Labeling; D011854:Radiochemistry; D011877:Radionuclide Imaging; D051381:Rats; D017208:Rats, Wistar; D013667:Technetium
chemical_list: D000900:Anti-Bacterial Agents; D013667:Technetium; D004318:Doxycycline
keywords: 99m-technetium; doxycycline hyclate; infection imaging; radiolabeled antibiotic