Bridging small interfering RNA with giant therapeutic outcomes using nanometric liposomes

J Control Release. 2015 Dec 28;220(Pt A):368-387. doi: 10.1016/j.jconrel.2015.10.050. Epub 2015 Oct 31.


The scope of RNAi based therapeutics is unquestionable. However, if we dissect the current trend of clinical trials for afore mentioned drug class, some stark trends appear: 1) naked siRNA only exerts influence in topical mode whilst systemic delivery requires a carrier and 2) even after two decades of extensive efforts, not even a single siRNA containing product is commercially available. It was therefore felt that a perspective simplifying the unique intricacies of working with a merger of siRNA and liposomes from a pharmaceutical viewpoint could draw the attention of a wider array of interested researchers. We begin from the beginning and attempt to conduit the gap between theoretical logic and experimental/actual constraints. This, in turn could stimulate the next generation of investigators, gearing them to tackle the conundrum, which is siRNA delivery.

Keywords: Cationic lipids; Clinical trials; Endosomal escape; Lipoplexes; Liposomes; siRNA; siRNA delivery; siRNA selection.

Publication types

  • Review

MeSH terms

  • Animals
  • Endosomes / metabolism
  • Gene Expression Regulation
  • Gene Transfer Techniques*
  • Humans
  • Lipids / chemistry*
  • Lipids / immunology
  • Liposomes
  • Nanoparticles*
  • RNA Interference*
  • RNA Stability
  • RNA, Small Interfering / chemistry
  • RNA, Small Interfering / genetics*
  • RNA, Small Interfering / immunology
  • RNA, Small Interfering / metabolism
  • RNAi Therapeutics / methods*


  • Lipids
  • Liposomes
  • RNA, Small Interfering