Quercetin loaded liposomes modified with galactosylated chitosan prevent LPS/D-GalN induced acute liver injury

Abstract

Quercetin (Que) has been proved to have various biological activities, including anti-oxidation, anti-inflammation and anti-virus, showing great potential in liver protection. However, its water insolubility leads to low bioavailability. Therefore, the development of a suitable drug delivery fashion is imminent. In recent years, liposomes have been widely used in the fields of drug delivery and gene transfer thanks to the cell membrane like structure, easy surface-modification and high encapsulation efficiency. Herein, we fabricated Que loaded anionic liposomes. Galactosylated chitosan (GC) was simply attached to the surfaces of liposomes through electrostatic adsorption to achieve targeted delivery by binding to asialoglycoprotein receptor (ASGPR). The results showed that Que loaded liposomes modified with GC (GC-Que-Lipo) could enrich the liver in mice through tail vein injection. Liposomes could achieve sustained drug release and GC-Que-Lipo promoted M2 polarization of macrophages. More importantly, it could maintain low content of AST, ALT, ALP and high level of GSH while reducing lipid oxidation, thereby protecting the liver from damage in acute liver injury model. In general, we expect to be able to acquire targeted and efficient delivery of quercetin through a facile approach, thus fulfill the prevention and treatment of liver diseases.