Stable and high-yielding intrinsic (59) Fe-radiolabeling of the intravenous iron preparations Monofer and Cosmofer

Abstract

Commercial iron supplements Monofer(®) and Cosmofer(®) were intrinsically radiolabeled with (59) Fe for the purpose of tracing iron absorption in vivo. Optimized procedures aimed at introducing (59) Fe into the macromolecular construct in a form that was as chemically equivalent to the matrix iron as possible. This was determined by challenging the labeled constructs with diethylenetriaminepentaacetic acid (DTPA) followed by separation by size-exclusion and measurements of radioactivity and iron in the eluted fractions. The final procedures were simple and involved heating aqueous dispersions of the supplements in the presence of [(59) Fe]FeCl3 for 24 h at 95 °C for Monofer, and 85 °C for Cosmofer, resulting in radiochemical yields greater than 94%. High performance size exclusion chromatography, UV-VIS spectroscopy, and dynamic light scattering were used to show that the supplements remained unchanged after radiolabeling, underscoring the applicability of the methodology for radiolabeling commercial iron preparations.

Keywords: Fe-59; cosmofer; intravenous iron therapy; intrinsic radiolabeling; iron supplements; monofer.