Effect of drying methods on swelling, erosion and drug release from chitosan-naproxen sodium complexes

AAPS PharmSciTech. 2008;9(1):1-12. doi: 10.1208/s12249-007-9001-0. Epub 2007 Dec 29.

Abstract

The purpose of this research was to explore theapplication of ionic interactions between naproxen sodium (NS) and chitosan (CH) in complexes (NSC) prepared by tray drying (TD) and spray drying (SD) methods. Drug-polymer ratio (1:1) in the NSC was optimized on the basis of dialysis studies. The particulate systems of NSC were prepared by tray drying (TD) and spray drying (SD) methods. Release retarding polymers were added to the NSC and to the physical mixtures containing NS-CH and their effects on water uptake, matrix erosion and drug release at different pH were compared. Spray dried complexes (SDC) were spherical, free flowing, light and fine amorphous particles in contrast to the crystalline, hard, tenacious, irregularly shaped, denser tray dried complexes (TDC) with poor flowability. Differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and Fourier transform infrared (FTIR) patterns confirm the conversion of crystalline to high energy amorphous phase suitable for ionic interactions in NSC. Presence of release retarding polymers, kappa carrageenan and hydroxypropylmethylcellulose (HPMC) in the NSC compacts retarded the drug release and improved the matrix integrity. Carrageenan matrices exhibited more retardation than HPMC tablets. FTIR patterns, erosion, swelling and drug release from matrices support ionic interactions between NS and CH in NSC. The reasons for retarded drug release from the chitosan matrices at acidic pH include poor solubility of drug at acidic pH, formation of a rate limiting polymer gel barrier along the periphery of matrices and the ionic interactions between oppositely charged moieties.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Absorption
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Chitosan / chemistry*
  • Desiccation / methods*
  • Diffusion
  • Drug Carriers / chemistry*
  • Hydrogen-Ion Concentration
  • Materials Testing
  • Naproxen / administration & dosage
  • Naproxen / chemistry*
  • Particle Size
  • Powders

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Drug Carriers
  • Powders
  • Naproxen
  • Chitosan