| Summary: | 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.
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