A green approach for the sustained-intestinal delivery of red chili (Capsicum annum L) extracted capsaicinoids with enhanced bioavailability

Abstract

Intestinal delivery with enhanced bioavailability is of great significance for stomach irritating and pungent bioactive molecules. The present study reports the development of a pungency-masked food-grade microbeadlets for the sustained-intestinal delivery of red chili extracted capsaicinoids using fenugreek galactomannans. Capsaicinoids encapsulated microbeads (CapF) of about 250 to 400 µm were prepared by a gel-phase homogenization, fluid-bed granulation followed by galactomannan coating, and characterized by NMR, FTIR, DSC, PXRD, and SEM as stable, directly compressible, free flowing amorphous beadlets with a tap density of 0.64 ± 0.2 g/mL. Swelling studies, in vitro release kinetics and particle size analysis indicated the intestinal delivery of soluble capsaicinoids. Pharmacokinetic studies on Wistar rats revealed enhanced bioavailability (19-fold) of CapF when the area under plasma concentration verses time was compared with that of unformulated capsaicinoids. CapF was safe upon gastric mucosa irritation test and demonstrated significant (P < 0.05) anti-obesity effect in high fat diet-induced hypercholesteremic rats.