A Slowly Self-Emulsifying Delivery System of Sesamin With Improved Biopharmaceutical Properties

This study is the first attempt to develop a novel slowly self-emulsifying drug delivery system (SL-SEDDS) of sesamin (SES) for improved biopharmaceutical properties. Firstly, SES-loaded self-emulsifying drug delivery system (SEDDS/SES) comprising krill oil, medium-chain triglyceride, Tween 80, and propylene glycol with 1.5 w/w% SES loading was prepared and optimized using a pseudo-ternary phase diagram. Then, SES-loaded SL-SEDDS (SL-SEDDS/SES) was produced by mixing the optimized SEDDS/SES with varying Geleol (solid lipid) contents. The resulting formulations were evaluated in terms of their physicochemical properties and pharmacokinetics. The self-emulsifying potency of SL-SEDDS/SES remained largely unaffected by the presence of Geleol. The dissolution behavior of SES in SL-SEDDS/SES improved relative to that of crystalline SES, with sustained release that was dependent on Geleol content. Notably, SL-SEDDS/SES containing 20 w/w% Geleol content (SL-SEDDS/SES-20) performed favorable sustained release with 65% dissolved SES at 6 h. After oral administration of SES samples (20 mg-SES/kg) in rats, SL-SEDDS/SES-20 showed 7.9-fold higher area under the curve of plasma concentration-time profile than that of crystalline SES. Additionally, it reduced the peak systemic exposure observed with SEDDS/SES, with a 22% lower C_max and a prolonged mean residence time (MRT) of 5.3 h. These findings suggest that SL-SEDDS is a promising dosage form for enhancing the biopharmaceutical properties of SES and potentially other lipophilic nutraceuticals.