Miniaturized chromatographic systems for radiochemical purity evaluation of 131I-Ferulic acid as a new candidate in nuclear medicine applications

Recently, the anticancer activity of ferulic acid (FA) which is a caffeic acid derivative has been reported. Therefore, in this study FA was radiocaped with 131I− to explore its potential as a tumor targeting agent. The radiolabeling process was carried out via electrophilic substitution reaction. The factors affecting labeling yield were optimized and the radiochemical purity (RCP) was assessed by various analytical techniques including paper chromatography (PC), thin layer chromatography (TLC), instant thin layer chromatography (ITLC), paper electrophoresis (PE) and high-performance liquid chromatography (HPLC). The RCP assay was extended to the utilization of miniaturized techniques including miniaturized PC (mini-PC), mini-TLC and mini-column chromatography (silica, sephadex-G25). Validation of mini-TLC, as one of 131I-FA RCP assay methods, was done according to ICH guidelines. Biodistribution studies of 131I-FA were performed on Ehrlich solid tumor bearing mice at various time points (5, 30, 60, 120 and 240 min), post injection. The radiolabeling yield of 131I-FA was 96.23 ± 0.45% and the miniaturized chromatographic systems showed high efficacy in RCP evaluation comparable to the conventional ones. Mini-TLC was proved to be specific, accurate, precise and linear. The tumor uptake of 131I-FA in solid tumor bearing mice was 4.35 ± 0.41 ID/g at 60 min with 2.79 as a tumor/muscle ratio. Consequently, 131I-FA could be used as a tumor targeting agent for nuclear medicine applications and the fast reaction monitoring could be achieved using miniaturized chromatographic techniques.