Hepatic Stellate Cell Membrane-Camouflaged Nanoparticles for Targeted Delivery of an Antifibrotic Agent to Hepatic Stellate Cells with Enhanced Antifibrosis Efficacy

Nano Lett. 2024 Dec 11;24(49):15827-15836. doi: 10.1021/acs.nanolett.4c04820. Epub 2024 Nov 25.

Abstract

Liver fibrosis is characterized by the excessive accumulation of extracellular matrix proteins primarily produced by activated hepatic stellate cells (HSCs). The activation of HSCs plays a pivotal role in driving the progression of liver fibrosis. Achieving specific targeted delivery of antifibrotic agents toward activated HSCs remains a formidable challenge. Here, we developed an HSC membrane-camouflaged nanosystem, named HSC-PLGA-BAY, for the precise delivery of the antifibrosis agent BAY 11-7082 to activated HSCs in the treatment of liver fibrosis. The designed HSC-PLGA-BAY nanosystem exhibited selective targeting toward activated HSCs, with internalization mediated by homologous cell adhesion molecules from the HSC membrane, namely integrins and N-cadherin. Furthermore, our findings demonstrate that treatment with HSC-PGA-BAY significantly increased apoptosis of activated HSCs and ameliorated liver fibrosis progression in a bile duct ligation (BDL)-induced fibrotic mice model. Collectively, the HSCs-targeted therapeutic platform holds promising potential as an effective strategy for liver fibrosis treatment.

Keywords: active targeting; biomimetic nanoparticle; hepatic stellate cell; hepatic stellate cell membrane; liver fibrosis.

MeSH terms

  • Animals
  • Antifibrotic Agents / chemistry
  • Antifibrotic Agents / pharmacology
  • Apoptosis / drug effects
  • Cell Membrane / drug effects
  • Cell Membrane / metabolism
  • Drug Delivery Systems
  • Hepatic Stellate Cells* / drug effects
  • Hepatic Stellate Cells* / metabolism
  • Hepatic Stellate Cells* / pathology
  • Humans
  • Liver Cirrhosis* / drug therapy
  • Liver Cirrhosis* / pathology
  • Mice
  • Nanoparticles* / chemistry
  • Polylactic Acid-Polyglycolic Acid Copolymer / chemistry

Substances

  • Antifibrotic Agents
  • Polylactic Acid-Polyglycolic Acid Copolymer