N-acetylaminogalactosyl-decorated biodegradable PLGA-TPGS copolymer nanoparticles containing emodin for the active targeting therapy of liver cancer

AbstractPrimary liver cancer (PLC) is one of the most common malignant tumours and has the third highest mortality rate worldwide. An active liver-targeting drug delivery system via the asialoglycoprotein receptors expressed in the hepatic parenchyma cells of mammals has become a research focus for the treatment of PLC. N-acetylaminogalactosyl-poly(lactide-co-glycolide)-succinyl-D-α-tocopherol polyethylene glycol 1000 succinate (GalNAc-PLGA-sTPGS) was synthesized to achieve active liver-targeting properties. Emodin (EMO)-loaded GalNAc-PLGA-sTPGS nanoparticles (EGPTN) were prepared with EMO which was selected for its potential antitumour efficacy. The in vitro cellular uptake, mechanism, cytotoxicity, and apoptosis of HepG2 cells were analyzed. The in vivo therapeutic effects of EGPTN were assessed in a PLC mouse model. The results showed that GalNAc-PLGA-sTPGS was successfully synthesized. The cellular uptake assay demonstrated that coumarin 6-loaded GalNAc-PLGA-sTPGS nanoparticles had superior active liv...