Sulindac loaded alginate beads for a mucoprotective and controlled drug release

Yegin B. A., Moulari B., Durlu-Kandilci N. T., Korkusuz P., Pellequer Y., Lamprecht A.

JOURNAL OF MICROENCAPSULATION, vol.24, no.4, pp.371-382, 2007 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 24 Issue: 4
  • Publication Date: 2007
  • Doi Number: 10.1080/02652040701298153
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.371-382
  • Hacettepe University Affiliated: Yes


Ionotropic gelation was used to entrap sulindac into calcium alginate beads as a potential drug carrier for the oral delivery of this anti-inflammatory drug. Beads were investigated in vitro for a possible sustained drug release and their use in vivo as a gastroprotective system for sulindac. Process parameters such as the polymer concentration, polymer/ drug ratio, and different needle diameter were analysed for their influences on the bead properties. Size augmented with increasing needle diameter ( 0.9mm needle: 1.28 to 1.44mm; 0.45mm needle: 1.04 to 1.07mm) due to changes in droplet size as well as droplet viscosity. Yields varied between 87% and 98% while sulindac encapsulation efficiencies of about 88% and 94% were slightly increasing with higher alginate concentrations. Drug release profiles exhibited a complete release for all formulations within 4 hours with a faster release for smaller beads. Sulindac loaded alginate beads led to a significant reduction of macroscopic histological damage in the stomach and duodenum in mice. Similarly, microscopic analyses of the mucosal damage demonstrated a significant mucoprotective effect of all bead formulation compared to the free drug. The present alginate formulations exhibit promising properties of a controlled release form for sulindac; meanwhile they provide a distinct tissue protection in the stomach and duodenum.