In the current study, ibuprofen (ibu) which is a non-steroidal anti-inflammatory drug (NSAID) was radiolabeled with(99m)Tc using two different methods: stannous chloride method (direct route) and technetium-99m tricarbonyl [Tc-99m(CO)(3)](+)route. Thus, it's aimed to investigate the radiolabeling potential of ibu for inflammation detection and to monitor if there is any difference inin vivodistribution depending on the radiolabeling route. Quality control studies of both radiolabeled ibu were performed by radiochromatographic methods (Thin Layer Liquid Radio Chromatography and High Performance Liquid Radio Chromatography). Radiolabeling yields of(99m)Tc-ibu and(99m)Tc(CO)(3)-ibu were determined as 99.05 +/- 0.83% and 91.79 +/- 3.30% (n = 5), respectively. Experimental lipophilicities of both radiolabeled ibu were determined. The biological behavior of both radiolabeled ibu was investigated in healthy Albino Wistar male rats byin vivobiodistribution studies. It was seen that both radiolabeled ibuprofen showed renal excretion while organ uptakes of(99m)Tc-ibu and(99m)Tc(CO)(3)-ibu differ against time.