Galangin-loaded, liver targeting liposomes: Optimization and hepatoprotective efficacy

Abstract

The aim of this study was to develop liver targeting galangin-loaded liposomes (Galangin-Liposomes) and evaluate their oral bioavailability. Box Behnken design was applied to optimize the formulation of Galangin-Liposomes by assessing encapsulation efficiency. The optimized Galangin-Liposomes were characterized by zeta potential, encapsulation efficiency, morphology, stability and in vitro release. Meanwhile, in vivo pharmacokinetics and tissue distributions were studied. Morphology of the selected Galangin-Liposomes revealed spherical and uniformly distributed nanoparticles with size of 74.67 ± 7.09 nm and encapsulation efficiency of 92.36 ± 2.71%. The formulation also significantly increased the extent of galangin release in vitro as well as its oral bioavailability (470.12%) in vivo. Furthermore, the tissue distribution studies further showed that the Galangin-Liposomes were enriched in the liver and exhibited better hepatoprotective effects in CCl4-intoxicated mice compared with the free galangin (p < 0.01). Collectively, these results indicated that the liposomes could serve as an effective delivery system to achieve improved oral bioavailability and liver targeting of galangin.