Effects of local structural transformation of lipid-like compounds on delivery of messenger RNA

Sci Rep. 2016 Feb 26:6:22137. doi: 10.1038/srep22137.

Abstract

Lipid-like nanoparticles (LLNs) have shown great potential for RNA delivery. Lipid-like compounds are key components in LLNs. In this study, we investigated the effects of local structural transformation of lipid-like compounds on delivery of messenger RNA. Our results showed that position change of functional groups on lipid-like compounds can dramatically improve delivery efficiency. We then optimized formulation ratios of TNT-b10 LLNs, a lead material, increasing delivery efficiency over 2-fold. More importantly, pegylated TNT-b10 LLNs is stable for over four weeks and is over 10-fold more efficient than that of its counterpart TNT-a10 LLNs. Additionally, the optimal formulation O-TNT-b10 LLNs is capable of delivering mRNA encoding luciferase in vivo. These results provide useful insights into the design of next generation LLNs for mRNA delivery.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • Drug Carriers / administration & dosage*
  • Humans
  • Lipids / chemistry
  • Luciferases / administration & dosage*
  • Luciferases / genetics*
  • Nanoparticles / administration & dosage
  • RNA, Messenger / administration & dosage*
  • RNA, Messenger / genetics*

Substances

  • Drug Carriers
  • Lipids
  • RNA, Messenger
  • Luciferases