Fluorocarbon Modified Low-Molecular-Weight Polyethylenimine for siRNA Delivery

Bioconjug Chem. 2016 Aug 17;27(8):1784-8. doi: 10.1021/acs.bioconjchem.6b00216. Epub 2016 Jul 29.

Abstract

We report the synthesis and study of fluorocarbon (FC) modified polyethylenimine (PEI) for the purpose of siRNA delivery. Low-molecular-weight PEI (Mn = 600) was functionalized with fluorocarbon epoxides of varying length. All FC-modified samples with greater than 2.0 equiv of FC epoxide per PEI induced potent gene silencing in vitro. Compared to hydrocarbon (HC) analogues, the FC vectors showed greater general silencing efficacy, higher cell uptake, and reduced association with serum components. Collectively, the data suggest that modification of polyamines with FCs is a promising approach for the discovery of novel vectors for siRNA delivery.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Drug Carriers / chemistry*
  • Fluorocarbons / chemistry*
  • Gene Silencing
  • HEK293 Cells
  • Humans
  • Mice
  • Models, Molecular
  • Molecular Weight
  • NIH 3T3 Cells
  • Nucleic Acid Conformation
  • Polyethyleneimine / chemistry*
  • RNA, Small Interfering / chemistry*
  • RNA, Small Interfering / genetics

Substances

  • Drug Carriers
  • Fluorocarbons
  • RNA, Small Interfering
  • Polyethyleneimine