Kafkas Üniversitesi Veteriner Fakültesi Dergisi 2018 , Vol 24 , Issue 3
Radiosynthesis and Biodistribution of 99mTc-Trimethoprim: A Novel Radiolabeled Antibiotic for Bacterial Infection Imaging Using Experimental Animals
Hasan DEMİROĞLU1, Gökçen TOPAL2, Yasemin PARLAK2, Fikriye Gül GÜMÜŞER2, Elgin Uluer TÜRKÖZ3, Volkan TEKİN4, Buket ATEŞ1, Perihan ÜNAK4, Uğur AVCIBAŞI1
1Department of Chemistry, Faculty of Art and Science, Manisa Celal Bayar University, TR-45140 Manisa - TURKEY
2Department of Nuclear Medicine, Manisa Celal Bayar University, Faculty of Medicine, TR-45140 Manisa - TURKEY
3Department of Histology and Embryology, Manisa Celal Bayar University, Faculty of Medicine, TR-45140 Manisa - TURKEY
4Institute of Nuclear Sciences, Ege University, Department of Nuclear Applications, TR-35100 Bornova, Izmir - TURKEY
DOI : 10.9775/kvfd.2017.19052 In the present article, we focused on the radiolabeling and evaluation of 99mTc–TMH complex as a potential candidate for infection imaging in vivo. For this; Trimethoprim (TMH) used to treat bacterial infections was investigated to label with 99mTc. Labeling was performed using thin (II) chloride as a reducing agent at room temperature for 1 h and radiochemical analysis involved thin layer radiochromatography (TLRC) and high pressure liquid radiochromatograpy (HPLRC) methods. The stability of labeled antibiotic was checked in the presence of rat blood serum at 37ºC up to 180 min. The maximum radiolabeling yield was found to be 96±2% and remained constant at more than 85±1% even in rat serum for 180 min after radiolabeling. Static image of 99mTc-TMH in male rats demonstrated that important radiation signals are present in the infected site at first glance in 30 min. After 30 min the uptake of the 99mTc-TMH as ID/g% in the infected muscle (INM) and normal muscle (NM) of the rats were 7.5±1.5% and 5.00±1.2%, respectively. In the INM/NM ratio a desirable behavior was observed as the values for the INM/ NM increased up to 10.6. 99mTc-TMH prepared with high yield is able to localize well in the bacterially infected muscle of the rats. As a result, 99mTc-TMH may be developed as a radiopharmaceutical agent to distinguish infection from inflammation by nuclear imaging. Keywords : Trimethoprim, 99mTc, Infection imaging agent, S. aureus