Design, characterization and in vitro evaluation of stavudine-loaded microspheres

Pharm Dev Technol. 2011 Apr;16(2):146-51. doi: 10.3109/10837450903544559. Epub 2010 Jan 25.

Abstract

The aim of the present study was to prepare and evaluate microspheres of Eudragit containing an antiviral drug stavudine. Microspheres were prepared by O/O solvent evaporation method using acetone/liquid paraffin system. The prepared microspheres were characterized for their micromeretic properties and entrapment efficiency; as well by Fourier transformed infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), X-ray powder diffractometry (XRPD) and scanning electron microscopy (SEM) which revealed the crystalline nature of drug in a final state. The in vitro studies revealed the controlled release of drug from microspheres up to 12 h and the best fit release kinetics was achieved with a Higuchi plot and found to be diffusion controlled. The yields of preparation and entrapment efficiencies were very high with a larger particle size for all the formulations. Mean particle size, entrapment efficiency and production yield were highly influenced by the type of polymer and polymer concentration.

MeSH terms

  • Acquired Immunodeficiency Syndrome / drug therapy
  • Anti-HIV Agents / administration & dosage*
  • Calorimetry, Differential Scanning
  • Delayed-Action Preparations / chemistry*
  • Humans
  • Microscopy, Electron, Scanning
  • Microspheres*
  • Particle Size
  • Polymethacrylic Acids / chemistry*
  • Spectroscopy, Fourier Transform Infrared
  • Stavudine / administration & dosage*

Substances

  • Anti-HIV Agents
  • Delayed-Action Preparations
  • Polymethacrylic Acids
  • methylmethacrylate-methacrylic acid copolymer
  • Stavudine