Microfluidic assembly of lipid nanoparticles for delivery of antisense oligonucleotides

Curr Pharm Biotechnol. 2014;15(9):823-8. doi: 10.2174/1389201015666141020155417.

Abstract

Microfluidically (MF) synthesized lipid nanoparticles (LNPs) for antisense oligonucleotides (ODN) delivery have been shown to be superior to those prepared by bulk mixing (BM). In this study, a 5-inlet MF chip was used to synthesize LNPs loaded with LOR-2501, an antisense ODN targeting the ribonucleotide reductase R1 subunit. The size distribution of ODN- LNPs was measured by dynamic light scattering. The cytotoxicity of ODN- LNPs was determined by MTS assay. Gene silencing activity of ODN- LNPs was investigated by qRT-PCR and by Western blot. Results showed that MF synthesis produced ODN-LNPs that have lower average size and polydispersity values. The highest antisense activity was shown by LNs synthesized by the MF T2 chip, with downregulation of R1 mRNA by 32.5%. In conclusion, given their simplicity, affordability and reproducibility, MF is an attractive method for synthesis of LNs for ODN delivery.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Survival / drug effects
  • Fatty Acids, Monounsaturated / chemistry*
  • Flow Cytometry
  • Humans
  • KB Cells
  • Microfluidics
  • Microscopy, Confocal
  • Nanoparticles / chemistry*
  • Oligonucleotides, Antisense / administration & dosage*
  • Oligonucleotides, Antisense / chemistry
  • Quaternary Ammonium Compounds / chemistry*
  • RNA, Messenger / metabolism
  • Ribonucleoside Diphosphate Reductase
  • Tumor Suppressor Proteins / genetics
  • Tumor Suppressor Proteins / metabolism

Substances

  • Fatty Acids, Monounsaturated
  • Oligonucleotides, Antisense
  • Quaternary Ammonium Compounds
  • RNA, Messenger
  • Tumor Suppressor Proteins
  • RRM1 protein, human
  • Ribonucleoside Diphosphate Reductase
  • 1,2-dioleoyloxy-3-(trimethylammonium)propane