Effect of a novel siRNA delivery system, siRNA ternary complex, on melanoma lung metastasis

J Drug Target. 2024 Aug;32(7):848-854. doi: 10.1080/1061186X.2024.2362361. Epub 2024 Jun 5.

Abstract

In this study, we determined effects of an anionic siRNA delivery vector, siRNA ternary complex, which is constructed with biodegradable dendrigraft poly-L-lysine (DGL) and γ-polyglutamic acid (γ-PGA) on the melanoma cells and melanoma lung metastasis. The siRNA ternary complex showed high cellular uptake and silencing effect in melanoma cell line B16-F10/Luc cells. After intravenous administration of the siRNA ternary complex, high silencing effect was also observed in the lung of B16-F10/Luc melanoma metastasis model mice. Therefore, we applied vascular endothelial growth factor (VEGF)-siRNA on the siRNA ternary complex and determined the effect on the melanoma lung metastasis. The siRNA ternary complex containing VEGF-siRNA reduced VEGF protein levels significantly in in vitro and in vivo, and the complex successfully inhibited melanoma lung metastasis. This biodegradable and effective siRNA delivery vector, siRNA ternary complex, could be available for clinical trials.

Keywords: biodegradable polymer; drug delivery system; melanoma; nanoparticle; siRNA; ternary complex.

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Gene Silencing
  • Lung Neoplasms* / pathology
  • Lung Neoplasms* / secondary
  • Melanoma / genetics
  • Melanoma / pathology
  • Melanoma, Experimental* / pathology
  • Mice
  • Mice, Inbred C57BL
  • Polyglutamic Acid* / analogs & derivatives
  • Polyglutamic Acid* / chemistry
  • Polylysine* / chemistry
  • RNA, Small Interfering* / administration & dosage
  • RNA, Small Interfering* / pharmacology
  • Vascular Endothelial Growth Factor A* / genetics

Substances

  • RNA, Small Interfering
  • Polyglutamic Acid
  • Vascular Endothelial Growth Factor A
  • Polylysine
  • poly(gamma-glutamic acid)