Incorporation of Naked Peptide Nucleic Acids into Liposomes Leads to Fast and Efficient Delivery

Bioconjug Chem. 2015 Aug 19;26(8):1533-41. doi: 10.1021/acs.bioconjchem.5b00156. Epub 2015 Jul 30.

Abstract

The delivery of peptide nucleic acids (PNAs) to cells is a very challenging task. We report here that a liposomal formulation composed of egg PC/cholesterol/DSPE-PEG2000 can be loaded, according to different encapsulation techniques, with PNA or fluorescent PNA oligomers. PNA loaded liposomes efficiently and quickly promote the uptake of a PNA targeting the microRNA miR-210 in human erythroleukemic K562 cells. By using this innovative delivery system for PNA, down-regulation of miR-210 is achieved at a low PNA concentration.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Down-Regulation
  • Drug Delivery Systems*
  • Gene Expression Regulation, Neoplastic
  • Humans
  • K562 Cells
  • Liposomes*
  • MicroRNAs / antagonists & inhibitors*
  • MicroRNAs / genetics
  • Oligonucleotides, Antisense / administration & dosage*
  • Peptide Nucleic Acids / administration & dosage*
  • Peptide Nucleic Acids / chemistry*
  • Peptide Nucleic Acids / pharmacology
  • Phosphatidylethanolamines / chemistry
  • Polyethylene Glycols / chemistry

Substances

  • 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-N-methoxy-poly(ethylene glycol 2000)
  • Liposomes
  • MIRN210 microRNA, human
  • MicroRNAs
  • Oligonucleotides, Antisense
  • Peptide Nucleic Acids
  • Phosphatidylethanolamines
  • Polyethylene Glycols