Preparation of spray dried amorphous solid dispersion of diosmin in soluplus with improved hepato-renoprotective activity: In vitro anti-oxidant and in-vivo safety studies

Abstract

In the current study, spray drying technique was utilized to prepare dissolution enhanced solid dispersion of a poorly soluble flavonoid, diosmin (DSM) with an excellent solubilizer, soluplus (SOL). Three formulae (F1–F3) of DSM-SOL solid dispersion powders were prepared in different ratio (1:0.5, 1:1 and 1:2, w/w) with a range of particle size (1.4–2.8 μm), PDI (0.257–0.349), ZP (−11.1 to −12.5 mV), content (67–82%) and yield (44–73%). Based on particle characterization, DSC, FTIR, PXRD, SEM and in-vitro studies, the spray dried solid dispersion (F3) formulae was optimized. The optimized formulae (F3) was additionally assessed for its in-vitro antioxidant activity and in-vivo protective effects against thioacetamide (TAA)-induced kidney and liver damage in rats. Results clearly indicate that pure DSM and F3 formulae significantly protected the renal and hepatic damage caused by TAA toxin. In addition, F3 formulae was found more protective than DSM as indicated by histopathological, and biochemical findings.