Physicochemical and toxicological characterization of sucrose-bound polynuclear iron oxyhydroxide formulations

Abstract

Intravenous iron formulations comprising of iron/iron–oxyhydroxide–carbohydrate complex are an established therapy for the treatment of iron deficiency anemia. These preparations should be subjected to exhaustive physicochemical and toxicological studies in order to establish their safety and efficacy. Following Venofer® (innovator iron–sucrose formulation), various iron sucrose similar have entered into the market with equivalent physicochemical and toxicological profile. This report describes the physicochemical and toxicological studies of a novel iron sucrose injection (IS-Claris). IS-Claris and Venofer® were subjected to various physicochemical studies such as elemental and chemical analysis; X-ray diffraction; particle size and distribution; labile iron detection, Mossbauer and Raman spectroscopy. The presence of iron oxides in IS-Claris and Venofer® could be confirmed by the major peaks at 24.65° (2θ) and 38.2° (2θ). The iron sucrose samples demonstrated similar reduction peaks of Fe(III) to Fe in their respective polarograms. The average diameter of the core of IS-Claris and Venofer® was estimated to be 2.92 ± 0.01 and 2.77 ± 0.63 nm, respectively. The Mossbauer spectra of IS-Claris and Venofer® showed a doublet with an isomer shift δ = 0.43 ± 0.01 mm/s. Moreover, the other physicochemical specifications of IS-Claris were comparable to Venofer®. The toxicological studies demonstrated that IS-Claris safety profile is equivalent to Venofer®. It could be concluded that IS-Claris could be used as a potential alternative to Venofer® with similar clinical implications.