Enhanced oral bioavailability, reduced irritation and increased hypolipidemic activity of self-assembled capsaicin prodrug nanoparticles

Abstract

The study was aimed at formulating self-assembled capsaicin prodrug nanoparticles (Cap-SSVE NPs) with improved bioavailability, increased antihyperlipidemic activity and less gastrointestinal mucosa irritations. The in vitro release profile of the developed Cap-SSVE NPs was stable in HCl solution (pH 1.2) and distilled water, but very susceptible in PBS (pH 6.8 and 7.4). The relative oral bioavailability of Cap-SSVE NPs was 3.2 folds higher than free capsaicin, with an extended Tmax (0.25–1 h). The Cap-SSVE NPs decreased certain lipid profile indices of both the liver tissue (Total lipids and TG) and the blood sample (TC, TG, LDL and TBA) with elevated levels of HDL in high fat diet induced hyperlipidemic rats. The nanoparticles also predominantly accumulated in the liver with reduced irritations in the gastrointestinal mucosa. Collectively, the formulated Cap-SSVE NPs showed an enhanced bioavailability, increased hypolipidemic effects and reduced mucosa irritations.

Keywords

• Capsaicin
• Prodrug
• Self-assembling
• Bioavailability
• Gastrointestinal irritation
• Antihyperlipidemic effect