Efficient intracellular delivery of siRNA with a safe multitargeted lipid-based nanoplatform

Nanomedicine (Lond). 2013 Sep;8(9):1397-413. doi: 10.2217/nnm.12.174. Epub 2013 Feb 8.

Abstract

Aim: The design of novel F3-targeted liposomes with adequate features for systemic administration, to enable efficient intracellular delivery of siRNA toward both cancer and endothelial cells from angiogenic blood vessels.

Materials & methods: Cellular association studies were performed by flow cytometry. Gene silencing was evaluated with eGFP-overexpressing cells, by flow cytometry and real-time reverse-transcription PCR. Safety and immunogenicity was assessed in CD1 mice.

Results: A strong improvement on siRNA internalization by the target cells was achieved, which was correlated with effective downregulation of eGFP. In addition, the F3-targeted liposomes were nonimmunogenic, even in a multiadministration schedule.

Conclusion: Overall, the developed F3-targeted nanocarrier constitutes a valuable tool for the specific and safe systemic delivery of siRNA to solid tumors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line, Tumor
  • Endothelial Cells / metabolism
  • Flow Cytometry
  • Gene Silencing*
  • Gene Transfer Techniques*
  • Green Fluorescent Proteins
  • Liposomes / administration & dosage
  • Liposomes / chemistry
  • Mice
  • Nanoparticles / administration & dosage
  • Nanoparticles / chemistry
  • Neoplasms / genetics*
  • Neoplasms / therapy
  • RNA, Small Interfering / administration & dosage*
  • RNA, Small Interfering / genetics

Substances

  • Liposomes
  • RNA, Small Interfering
  • Green Fluorescent Proteins