pH-Sensitive cationic copolymers of different macromolecular architecture as potential dexamethasone sodium phosphate delivery systems

J Pharm Sci. 2014 Aug;103(8):2406-13. doi: 10.1002/jps.24059. Epub 2014 Jun 24.

Abstract

This paper describes the synthesis and characterization of cationic copolymers with different macromolecular architecture and drug delivery properties of the corresponding dexamethasone sodium phosphate (DSP)-loaded systems. Copolyelectrolytes comprising poly[2-(acryloyloxy)ethyl] trimethylammonium chloride (PAETMAC) and poly(ethylene glycol) blocks as well as a tri-arm star-shaped PAETMAC were synthesized using cerium(IV) ion-mediated polymerization method. The obtained copolyelectrolytes and corresponding ionic associates with DSP have been characterized by (1)H NMR, Fourier Transform Infrared spectroscopy, and differential scanning calorimetry. The average diameter, size distribution, and ζ-potential of the copolymers and DSP-copolymer ionic associates were determined by dynamic light scattering, and particles were visualized by scanning electron microscopy and transmission electron microscopy. The biocompatibility and cytotoxicity of obtained copolymers were determined. In vitro drug release experiments were carried out to estimate the ability of the obtained nanoparticles for sustained release of DSP for a period of 24 h.

Keywords: controlled release; corticosteroids; drug delivery systems; nanoparticles; polyelectrolytes; polymer synthesis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Delayed-Action Preparations / chemistry*
  • Dexamethasone / administration & dosage
  • Dexamethasone / analogs & derivatives*
  • Glucocorticoids / administration & dosage*
  • Hep G2 Cells
  • Humans
  • Hydrogen-Ion Concentration
  • Nanoparticles / chemistry
  • Polyethylene Glycols / chemistry
  • Quaternary Ammonium Compounds / chemistry

Substances

  • Delayed-Action Preparations
  • Glucocorticoids
  • Quaternary Ammonium Compounds
  • dexamethasone 21-phosphate
  • Polyethylene Glycols
  • Dexamethasone