Poly(amidoamine)-based dendrimer/siRNA complexation studied by computer simulations: effects of pH and generation on dendrimer structure and siRNA binding

Macromol Biosci. 2012 Feb;12(2):225-40. doi: 10.1002/mabi.201100276. Epub 2011 Dec 6.

Abstract

In this work we report, compare and discuss the results obtained from fully atomistic molecular dynamics simulations of generations 4, 5, and 6 of PAMAM-based dendrimers having NH(3) and triethanolamine as cores, forming complexes with a short interfering RNA (siRNA) at different pH values and at physiological ionic strength. By employing a detailed analysis we demonstrate how features such as molecular size, structural details, and protonation level of this category of dendrimers affect the dendrimer/siRNA complexation. Properties like the conformational flexibility of the dendrimer, the effective charge distribution of the assembly, and the level of intra- and intermolecular hydrogen bonding between the two molecular entities are all found to play a significant role in the mutual interactions between the nucleic acid and the hyperbranched molecules. All these features are of key importance in the multifaceted mechanism of dendrimer/gene complexation, and their understanding can provide valuable insight toward the design of more efficient nucleic acid nanocarriers.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biocompatible Materials / chemistry*
  • Computer Simulation
  • Dendrimers / chemistry*
  • Drug Carriers / chemistry
  • Ethanolamines / chemistry
  • Hydrogen Bonding
  • Hydrogen-Ion Concentration
  • Models, Molecular*
  • Nanostructures / chemistry*
  • Osmolar Concentration
  • Polyamines / chemistry
  • Protons*
  • RNA, Small Interfering / chemistry*
  • Static Electricity
  • Thermodynamics

Substances

  • Biocompatible Materials
  • Dendrimers
  • Drug Carriers
  • Ethanolamines
  • PAMAM Starburst
  • Polyamines
  • Protons
  • RNA, Small Interfering
  • triethanolamine