Helper Lipid-Enhanced mRNA Delivery for Treating Metabolic Dysfunction-Associated Fatty Liver Disease

Nano Lett. 2024 Jun 5;24(22):6743-6752. doi: 10.1021/acs.nanolett.4c01458. Epub 2024 May 23.

Abstract

Lipid nanoparticles (LNPs) represent the forefront of mRNA delivery platforms, yet achieving precise delivery to specific cells remains a challenge. The current targeting strategies complicate the formulation and impede the regulatory approval process. Here, through a straightforward regulation of helper lipids within LNPs, we introduce an engineered LNP designed for targeted delivery of mRNA into hepatocytes for metabolic dysfunction-associated fatty liver disease (MAFLD) treatment. The optimized LNP, supplied with POPC as the helper lipid, exhibits a 2.49-fold increase in mRNA transfection efficiency in hepatocytes compared to that of FDA-approved LNPs. CTP:phosphocholine cytidylyltransferase α mRNA is selected for delivery to hepatocytes through the optimized LNP system for self-calibration of phosphatidylcholine levels to prevent lipid droplet expansion in MAFLD. This strategy effectively regulates lipid homeostasis, while demonstrating proven biosafety. Our results present a mRNA therapy for MAFLD and open a new avenue for discovering potent lipids enabling mRNA delivery to specific cells.

Keywords: MAFLD; helper lipid; hepatocyte-selective; lipid nanoparticle; mRNA delivery.

MeSH terms

  • Animals
  • Choline-Phosphate Cytidylyltransferase / genetics
  • Choline-Phosphate Cytidylyltransferase / metabolism
  • Fatty Liver / genetics
  • Fatty Liver / metabolism
  • Fatty Liver / therapy
  • Gene Transfer Techniques
  • Hepatocytes* / metabolism
  • Humans
  • Lipids / chemistry
  • Liposomes
  • Mice
  • Nanoparticles* / chemistry
  • Phosphatidylcholines* / chemistry
  • RNA, Messenger* / genetics
  • RNA, Messenger* / metabolism
  • Transfection / methods

Substances

  • RNA, Messenger
  • Phosphatidylcholines
  • Choline-Phosphate Cytidylyltransferase
  • Lipids
  • Lipid Nanoparticles
  • 1-palmitoyl-2-oleoylphosphatidylcholine
  • Liposomes