Galactosylated chitosan-functionalized liposome for targeted delivery of <i>Coreopsis tinctoria</i> flavonoids: Protective effect in acute liver injury

Acute liver injury (ALI) is a syndrome characterized by rapid deterioration of liver function, rapid progression, and high mortality. In this study, a liver-targeted drug delivery system, galactosylated chitosan modified Coreopsis tinctoria flavonoid liposome (GC-CTF-Lip) was constructed. The targeted ligand was synthesized by the amidation reaction between chitosan and lactobionic acid, and its structure was identified. The modification conditions of GC on liposomes were optimized and characterization of liposomes was studied. The liver-targeting ability of GC-CTF-Lip was evaluated through in vivo and in vitro experiments. A mouse model of ALI induced by CCl4 was established to evaluate the hepatoprotective effect of GC-CTF-Lip. The results confirmed that lactobionic acid was successfully grafted onto chitosan. Finally, GC-CTF-Lip with particle size of 236.32 ± 0.60 nm and encapsulation efficiency of 68.67 ± 0.58% was obtained. GC-CTF-Lip improved the uptake efficiency of CTF in hepatocytes in vitro and exhibited excellent liver enrichment in vivo. Serum ALT/AST levels were significantly decreased, and the histological liver injury was alleviated. It exhibited a trend of liver enrichment and a hepatoprotective effect. This liver-targeted nanodrug delivery system can achieve active accumulation of drugs at the lesion site, providing a potential strategy for the prevention of ALI.