Highly efficient nanomedicines assembled via polymer-drug multiple interactions: Tissue-selective delivery carriers

J Control Release. 2011 Jun 10;152(2):317-24. doi: 10.1016/j.jconrel.2011.03.013. Epub 2011 Mar 22.

Abstract

This study presents the construction and evaluation of highly efficient nanomedicines via self-assembly directed by multiple non-covalent interactions between carrier polymer and cargo molecules, including hydrophobic, host-guest recognition, hydrogen bonding and electrostatic forces. β-Cyclodextrin conjugated polyethyleneimine (PEI-CD) was employed as the model carrier material, while indomethacin (IND), a nonsteroidal anti-inflammatory drug, was used as the drug model. Spontaneous assembly of PEI-CD and IND led to core-shell structured nanoparticles with a positive surface and pH-triggering behavior as well as high drug loading capacity. These nano-assemblies can function as gastro-OFF/intestinal-ON delivery systems to selectively transport payload to enteric sites, thereby dramatically increasing the oral bioavailability of the loaded therapeutic, which can also serve as multifunctional nano-platforms for multiple delivery of various therapeutics. In addition, the strategy employed herein may provide new insights into the design of novel nanocarriers by self-assembling.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage*
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Drug Delivery Systems / methods*
  • Gastrointestinal Tract / metabolism
  • Indomethacin / administration & dosage*
  • Indomethacin / chemistry
  • Indomethacin / pharmacokinetics
  • Male
  • Nanomedicine
  • Nanoparticles / chemistry*
  • Polyethyleneimine / chemical synthesis
  • Polyethyleneimine / chemistry*
  • Rats
  • Rats, Sprague-Dawley
  • beta-Cyclodextrins / chemical synthesis
  • beta-Cyclodextrins / chemistry*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • beta-Cyclodextrins
  • Polyethyleneimine
  • betadex
  • Indomethacin