Browsing by Author "Asikoglu, M"

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    Gamma scintigraphy and biodistribution of 99mTc-cefotaxime sodium in preclinical models of bacterial infection and sterile inflammation
    Ilem-Ozdemir, D; Asikoglu, M; Ozkilic, H; Yilmaz, F; Hosgor-Limoncu, M; Ayhan, S
    Tc-99m-cefotaxime sodium (Tc-99m-CEF) was developed and standardized under varying conditions of reducing and antioxidant agent concentration, pH, radioactivity dose, and reducing agent type. Labeling studies were performed by changing the selected parameters one by one, and optimum labeling conditions were determined. After observing the conditions for maximum labeling efficiency and stability, lyophilized freeze dry kits were prepared accordingly. Simple method for radiolabeling of CEF with Tc-99m has been developed and standardized. Labeling efficiency of Tc-99m-CEF was assessed by both radio thin-layer chromatography and radio high-performance liquid chromatography and found higher than 90%. The labeled compound was found to be stable in saline and human serum up to 24h. Two different freeze dry kits were developed and evaluated. Based on the data obtained from this study, both products were stable for 6months with high labeling efficiency. The prepared cold kit was found sterile and pyrogen free. The bacterial infection and sterile inflammation imaging capacity of Tc-99m-CEF was evaluated. Based on the in vivo studies, Tc-99m-CEF has higher uptake in infected and inflamed thigh muscle than healthy thigh muscle.
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    99mTc-Doxycycline hyclate: a new radiolabeled antibiotic for bacterial infection imaging
    Ilem-Özdemir, D; Asikoglu, M; Ozkilic, H; Yilmaz, F; Hosgor-Limoncu, M; Ayhan, S
    Radiolabeled antibiotics are promising radiopharmaceuticals for the precise diagnosis and detection of infectious lesions. Doxycycline Hyclate (DOX) was chosen to investigate new Tc-99m-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 Tc-99m with high radiochemical purity, and the labeled compound was stable in human serum. Kits were sterile, pyrogen-free, and stable up to 6months. 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 5h. 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 Tc-99m-DOX was found 0.230.06 for infected thigh muscle. According to the imaging, biodistribution, and histopathological studies, the promising characteristics of Tc-99m-DOX make the new radiopharmaceutical valuable to examine for future studies. Copyright (c) 2013 John Wiley & Sons, Ltd.
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    Radiolabeling and in vitro evaluation of a new 5-fluorouracil derivative with cell culture studies
    Ilem-Ozdemir, D; Atlihan-Gundogdu, E; Ekinci, M; Halay, E; Ay, K; Karayildirim, T; Asikoglu, M
    The clinical impact and accessibility of Tc-99m tracers for cancer diagnosis would be greatly enhanced by the availability of a new, simple, and easy labeling process and radiopharmaceuticals. 5-Fluorouracil is an antitumor drug, which has played an important role for the treatment of breast carcinoma. In the present study, a new derivative of 5-Fluorouracil was synthesized as (1-[{1 '-(1 ''-deoxy-2 '',3 '':4 '',5 ''-di-O-isopropylidene-beta-D-fructopyranose-1 ''-yl)-1 ' H-1 ',2 ', 3 '-triazol-4 '-yl}methyl]-5-fluorouracil) (E) and radiolabeled with Tc-99m. It was analyzed by radio thin layer chromatography for quality control and stability. The radiolabeled complex was subjected to in vitro cell-binding studies to determine healthy and cancer cell affinity using HaCaT and MCF-7 cells, respectively. In addition, in vitro cytotoxicity studies of compound E were performed with HaCaT and MCF-5 cells. The radiochemical purity of the [Tc-99m]TcE was found to be higher than 90% at room temperature up to 6 hours. The radiolabeled complex showed higher specific binding to MCF-7 cells than HaCaT cells. IC50 values of E were found 31.5 +/- 3.4 mu M and 20.7 +/- 2.77 mu M for MCF-7 and HaCaT cells, respectively. The results demonstrated the potential of a new radiolabeled E with Tc-99m has selective for breast cancer cells.