(99m)Tc-radiolabeled Levofloxacin and micelles as infection and inflammation imaging agents

Silindir-Gunay, Mine; Ozer, Asuman Yekta

Easy and early detection of infection and inflammation is essential for early and effective treatment. In this study, PEGylated micelles were designed and both micelles and Levofloxacin were radiolabeled with (99m)TcO(4)(-) to develop potential radiotracers for detection of infection/inflammation. Radiolabeling efficiency, in vitro stability and bacterial binding of (99m)Tc-Levofloxacin and (99m)Tc-micelles were compared. The aim of this study is to formulate and compare (99m)Tc-Levofloxacin and (99m)Tc-micelles as infection and inflammation agents having different mechanisms for the accumulation at infection and inflammation site. PEGylated micelles were designed with a particle size of 80 ± 0.7 nm and proper characterization properties. High radiolabeling efficiency was achieved for (99m)Tc-Levofloxacin (96%) and (99m)Tc-micelles (87%). The radiolabeling efficiency was remained stable with some insignificant alterations for both radiotracers at 25 °C for 24 h. Although in vitro bacterial binding of (99m)Tc-levofloxacine was higher than (99m)Tc-micelles, (99m)Tc-micelles may also be evaluated potential agent due to long circulation and passive accumulation mechanisms at infection/inflammation site. Both radiopharmaceutical agents exhibit potential results in design, characterization, radiolabeling efficiency and in vitro bacterial binding point of view.