Amphiphilic cholic-acid-modified dextran sulfate and its application for the controlled delivery of superoxide dismutase

Macromol Biosci. 2012 Apr;12(4):515-24. doi: 10.1002/mabi.201100367.

Abstract

A novel amphiphilic and biodegradable polyelectrolyte DS-CA is prepared by the esterification of DS with CA. DS-CA can self-assemble into stable nanoparticles in water. SOD can effectively associate with DS-CA at pH = 5.0 by virtue of electrostatic and hydrophobic interactions. SOD release from the complex nanoparticles is slow at pH = 1.2. The release at pH = 7.4 PBS shows an extended behavior and is tunable by changing the weight ratio of SOD to DS-CA as well as the CA substitution degree. Increasing the CA substitution degree of DS-CA can significantly enhance the cellular uptake of the loaded SOD. This study demonstrates that the amphiphilic DS-CA provides a promising strategy for oral delivery of protein/peptide drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Survival / drug effects
  • Cholic Acid / chemistry*
  • Delayed-Action Preparations / chemical synthesis*
  • Delayed-Action Preparations / pharmacology
  • Dextran Sulfate / chemistry*
  • Endocytosis / drug effects
  • HEK293 Cells
  • Humans
  • Hydrogen-Ion Concentration
  • Hydrophobic and Hydrophilic Interactions
  • Magnetic Resonance Spectroscopy
  • Microscopy, Electron, Transmission
  • Nanoparticles
  • Particle Size
  • Static Electricity
  • Superoxide Dismutase / chemistry*
  • Superoxide Dismutase / pharmacology
  • Surface-Active Agents / chemical synthesis*
  • Surface-Active Agents / pharmacology
  • Water

Substances

  • Delayed-Action Preparations
  • Surface-Active Agents
  • Water
  • Dextran Sulfate
  • Superoxide Dismutase
  • Cholic Acid