Development of a Lipid-encapsulated TGFβRI-siRNA Drug for Liver Fibrosis Induced by Schistosoma mansoni

PLoS Negl Trop Dis. 2024 Sep 12;18(9):e0012502. doi: 10.1371/journal.pntd.0012502. eCollection 2024 Sep.

Abstract

Schistosoma mansoni infection leads to chronic schistosomiasis and severe hepatic fibrosis. We designed a liver-targeted lipid nanoparticle (LNP) carrying siRNA against type I TGF-β receptor (TGFβRI) mRNA to treat schistosomiasis-induced liver fibrosis in BALB/c mice. Knockdown of TGFβRI by LNP-siTGFβRI reduced LX-2 cell activation in vitro and alleviated liver fibrosis in S. mansoni-infected mice. αSMA and Col1a1 fibrotic markers in the liver tissues of infected mice were significantly suppressed in the treatment groups. In the serum of the LNP-siTGFβRI-treated groups, cytokines IFNγ, IL-1α, IL-6, IL-12, RANTES (CCL5), and TNFα increased, while GM-CSF, IL-2, IL-4, IL-10, IL-13, and KC (CXCL1) decreased compared to the control. Cell proportions were significantly altered in S. mansoni-infected mice, with increased CD56d NK cells and decreased CD19+ B cells and CD4+ T cells compared to naïve mice. Following LNP-siTGFβRI treatment, CD56d NK cells were downregulated, while B and memory Th cell populations were upregulated. The density of fibrotic regions significantly decreased with LNP-siTGFβRI treatment in a dose-dependent manner, and no systemic toxicity was observed in the major organs. This targeted siRNA delivery strategy effectively reduced granulomatous lesions in schistosomiasis-induced liver fibrosis without detectable side effects.

MeSH terms

  • Animals
  • Cytokines / metabolism
  • Female
  • Humans
  • Lipids
  • Liver / parasitology
  • Liver / pathology
  • Liver Cirrhosis* / parasitology
  • Mice
  • Mice, Inbred BALB C
  • Nanoparticles / administration & dosage
  • RNA, Small Interfering* / administration & dosage
  • RNA, Small Interfering* / genetics
  • Schistosoma mansoni* / genetics
  • Schistosomiasis mansoni*

Substances

  • Cytokines
  • Lipids
  • RNA, Small Interfering

Grants and funding

This study was supported by a grant MOST 111-2320-B-038-055 from the Ministry of Science and Technology, Taipei, Taiwan to Po-Ching Cheng; and in part by grants: the LEO Foundation (LF-OC-20-000370) project to Edwin En-Te Hwu; and Intelligent Drug Delivery and Sensing Using Microcontainers and Nanomechanics (IDUN2) to Edwin En-Te Hwu. The funders had no role in study design, data collection and analysis, decision to publish, or preparation of the manuscript.