Engineered lipid nanoparticles enable therapeutic gene silencing of GTSE1 for the treatment of liver fibrosis

J Control Release. 2024 Oct:374:337-348. doi: 10.1016/j.jconrel.2024.08.012. Epub 2024 Aug 22.

Abstract

Liver fibrosis is characterized by abnormal accumulation of extracellular matrix proteins, disrupting normal liver function. Despite its significant health impact, effective treatments remain limited. Here, we present the development of engineered lipid nanoparticles (LNPs) for targeted RNA therapeutic delivery in the liver. We investigated the therapeutic potential of modulating the G2 and S-phase expressed 1 (GTSE1) protein for treating liver fibrosis. Through screening, we identified P138Y LNP as a potent candidate with superior delivery efficiency and lower toxicity. Using these engineered LNPs, we successfully delivered siGTSE1 to hepatocytes, significantly reducing collagen accumulation and restoring liver function in a fibrosis animal model. Additionally, GTSE1 downregulation altered miRNA expression and upregulated hepatocyte nuclear factor 4 alpha (HNF4α). These findings suggest that therapeutic gene silencing of GTSE1 is a promising strategy for treating liver fibrosis by regenerating liver phenotypes and functions.

Keywords: GTSE1; Gene silencing; Gene therapy; Lipid nanoparticles; Liver fibrosis; Targeted delivery.

MeSH terms

  • Animals
  • Gene Silencing*
  • Hepatocyte Nuclear Factor 4 / genetics
  • Hepatocyte Nuclear Factor 4 / metabolism
  • Hepatocytes / metabolism
  • Humans
  • Lipids / chemistry
  • Liposomes
  • Liver / metabolism
  • Liver / pathology
  • Liver Cirrhosis* / genetics
  • Liver Cirrhosis* / therapy
  • Male
  • Mice, Inbred C57BL
  • MicroRNAs / administration & dosage
  • MicroRNAs / genetics
  • Nanoparticles*
  • RNA, Small Interfering / administration & dosage
  • RNA, Small Interfering / genetics

Substances

  • Hepatocyte Nuclear Factor 4
  • MicroRNAs
  • RNA, Small Interfering
  • Lipids
  • Lipid Nanoparticles
  • Liposomes