Intracellular siRNA delivery system using polyelectrolyte complex micelles prepared from VEGF siRNA-PEG conjugate and cationic fusogenic peptide

Soo Hyeon Lee, Sun Hwa Kim, Tae Gwan Park

Research output: Contribution to journalArticlepeer-review

121 Scopus citations

Abstract

To develop a small interfering RNA (siRNA) delivery system with low cytotoxicity and high transfection efficiency, siRNA was conjugated to poly(ethylene glycol) via a disulfide linkage (siRNA-PEG) to prepare polyelectrolyte complex micelles (PECMs) by condensing with a cationic fusogenic peptide (KALA). The siRNA-PEG conjugate exhibited enhanced resistance to degradation from nucleases. Anionic siRNA-PEG conjugate and cationic KALA, when mixed in an aqueous phase, spontaneously formed nano-sized PECMs (<200 nm) that have an inner core of charge neutralized siRNA/KALA complex surrounded by a PEG corona. Vascular endothelial growth factor (VEGF) siRNA was used to demonstrate VEGF sequence-specific gene inhibition in prostate carcinoma cells (PC-3 cells). The extent of gene silencing was gradually increased with increasing nitrogen to phosphate (N/P) ratio and the concentration of siRNA-PEG/KALA PECMs. These results suggest that the formulation of siRNA-PEG/KALA PECMs could be widely applied for intracellular delivery of various therapeutic siRNAs.

Original languageEnglish
Pages (from-to)511-516
Number of pages6
JournalBiochemical and Biophysical Research Communications
Volume357
Issue number2
DOIs
StatePublished - Jun 1 2007
Externally publishedYes

Funding

This work was supported by the grants from the Ministry of Science and Technology (National Research Laboratory Project) and the National Cancer Center, South Korea.

Keywords

  • Fusogenic peptide
  • PEG
  • Polyelectrolyte complex micelles
  • Vascular endothelial growth factor
  • siRNA delivery

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