Cross-linked chitosan microspheres: preparation and evaluation as a matrix for the controlled release of pharmaceuticals

J Pharm Pharmacol. 1992 Apr;44(4):283-6. doi: 10.1111/j.2042-7158.1992.tb03607.x.

Abstract

Chitosan microspheres having good spherical geometry and a smooth surface were prepared by the glutaraldehyde cross-linking of an aqueous acetic acid dispersion of chitosan in paraffin oil using dioctyl sulphosuccinate as the stabilizing agent. Microspheres having different degrees of swelling were made by varying the cross-linking density. Microspheres were prepared by incorporating theophylline, aspirin or griseofulvin. Drug incorporation efficiencies exceeding 80% could be achieved for these drugs. In-vitro release studies of these drugs were carried out in simulated gastric and intestinal fluids at 37 degrees C. It was observed that the drug release rates were influenced by the cross-linking density, particle size and initial drug loading in the microspheres.

MeSH terms

  • Aspirin / administration & dosage
  • Aspirin / chemistry
  • Body Fluids / chemistry
  • Chitin / analogs & derivatives*
  • Chitin / chemistry
  • Chitosan
  • Cross-Linking Reagents
  • Delayed-Action Preparations*
  • Griseofulvin / administration & dosage
  • Griseofulvin / chemistry
  • Microscopy, Electron, Scanning
  • Microspheres
  • Particle Size
  • Theophylline / administration & dosage
  • Theophylline / chemistry

Substances

  • Cross-Linking Reagents
  • Delayed-Action Preparations
  • Chitin
  • Griseofulvin
  • Chitosan
  • Theophylline
  • Aspirin