Optimization of prednisolone acetate-loaded chitosan microspheres using a 2(3) factorial design for preventing restenosis

Drug Deliv. 2010 Apr;17(3):178-86. doi: 10.3109/10717541003667780.

Abstract

Prednisolone acetate (PA)-loaded microspheres were prepared by the spray-drying technique using different polymer (1% and 2%) and drug concentrations (10% and 20%). To obtain the optimum formulation, a three-factor two-level (2(3)) design was employed. The independent variables were polymer molecular weight, polymer concentration, and theoretical drug loading. Responses were the particle size, percentage of encapsulation efficiency, and the t(50%) release. The best formulation was prepared with 20% of PA and 1% of chitosan with medium molecular weight showing relative good yield of production (48.0 + or - 6.7%) and encapsulation efficiency (45.7 + or - 0.3%), and released the drug at a constant rate in 11 days.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Arteries / physiology
  • Calorimetry, Differential Scanning
  • Chitosan / chemistry*
  • Desiccation
  • Drug Compounding
  • Graft Occlusion, Vascular / prevention & control*
  • Hyperplasia / prevention & control
  • Microscopy, Electron, Scanning
  • Microspheres
  • Particle Size
  • Prednisolone / administration & dosage
  • Prednisolone / analogs & derivatives*
  • Prednisolone / therapeutic use
  • Prodrugs / administration & dosage*
  • Prodrugs / therapeutic use*
  • Solubility
  • Stents

Substances

  • Prodrugs
  • prednisolone acetate
  • Chitosan
  • Prednisolone