LAUSR

Tilianin (TIL) may prevent and treat myocardial ischemia reperfusion injuries. However, its oral administration is hampered by its low bioavailability. The present study aimed to formulate lipid-polymer hybrid nanoparticles (LPHNs) as carriers for the sustained release and oral bioavailability enhancement of TIL in vitro and in vivo. A nanodrug delivery system of TIL-loaded LPHNs (TIL-LPHNs) was constructed. TIL-LPHNs were prepared via a self-assembly method, and their particle size, polymer dispersity index (PDI), zeta potential, encapsulation efficiency (EE) and morphology were investigated. In addition, pharmacokinetic studies were performed in vivo. The TIL-LPHN formulation produced a spherical, homogeneous, smooth surface and multi-lamellar structured nanoparticles. The particle size and distribution profile of TIL-LPHNs had a mean particle diameter of 54.6 ± 5.3 nm and PDI of 0.112 ± 0.017. The zeta potential was -33.4 ± 4.7 mV. The EE of TIL-LPHNs was 86.6 ± 3.6%, which was determined with the dialysis method. The TIL-LPHNs significantly enhanced the oral bioavailability of TIL with a 3.7-fold increase in the area under the concentration-time curve in comparison with the TIL solution. These findings support the potential use of LPHNs in improving the stability and bioavailability of TIL via oral administration.