Enhancing the Therapeutic Delivery of Oligonucleotides by Chemical Modification and Nanoparticle Encapsulation

Molecules. 2017 Oct 13;22(10):1724. doi: 10.3390/molecules22101724.

Abstract

Oligonucleotide (ON) drugs, including small interfering RNA (siRNA), microRNA (miRNA) and antisense oligonucleotides, are promising therapeutic agents. However, their low membrane permeability and sensitivity to nucleases present challenges to in vivo delivery. Chemical modifications of the ON offer a potential solution to improve the stability and efficacy of ON drugs. Combined with nanoparticle encapsulation, delivery at the site of action and gene silencing activity of chemically modified ON drugs can be further enhanced. In the present review, several types of ON drugs, selection of chemical modification, and nanoparticle-based delivery systems to deliver these ON drugs are discussed.

Keywords: antisense; miRNA; nanocarriers; oligonucleotide; siRNA.

Publication types

  • Review

MeSH terms

  • Gene Silencing
  • Gene Transfer Techniques
  • Humans
  • MicroRNAs / chemistry
  • MicroRNAs / therapeutic use*
  • Nanoparticles / chemistry
  • Nanoparticles / therapeutic use*
  • Oligonucleotides, Antisense / chemistry
  • Oligonucleotides, Antisense / genetics
  • Oligonucleotides, Antisense / therapeutic use*
  • RNA, Small Interfering / chemistry
  • RNA, Small Interfering / therapeutic use*

Substances

  • MicroRNAs
  • Oligonucleotides, Antisense
  • RNA, Small Interfering