Microencapsulation of sodium alendronate reduces drug mucosal damage in rats

Drug Deliv. 2010 May;17(4):231-7. doi: 10.3109/10717541003667830.

Abstract

Sodium alendronate is an effective treatment for osteoporosis, but its oral administration is associated with adverse gastrointestinal effects. The aim of this work was to evaluate gastroresistant sodium alendronate-loaded microparticles prepared by spray-drying using Eudragit S100 or a blend of Eudragit S100/Methocel E4M. Both formulations presented high encapsulation efficiencies, mean diameters below 17 microm, and similar collapsed shape. Dissolution experiments showed good gastro-resistance for the microparticles at pH 1.2. At pH 6.8, the blended microparticles retarded the drug release. In vivo studies showed that the formulations were able to protect the rat stomachs against ulcer formation by sodium alendronate. In conclusion, the microparticles seems to be promising oral carriers for sodium alendronate.

Publication types

  • Comparative Study

MeSH terms

  • Alendronate / adverse effects*
  • Alendronate / chemical synthesis
  • Alendronate / pharmacokinetics
  • Animals
  • Drug Compounding
  • Female
  • Gastric Mucosa / drug effects*
  • Gastric Mucosa / metabolism
  • Gastric Mucosa / pathology
  • Intestinal Mucosa / drug effects*
  • Intestinal Mucosa / metabolism
  • Intestinal Mucosa / pathology
  • Rats
  • Rats, Wistar

Substances

  • Alendronate