title: Sulindac loaded alginate beads for a mucoprotective and controlled drug release.
abstract: 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 (0.9 mm needle: 1.28 to 1.44 mm; 0.45 mm needle: 1.04 to 1.07 mm) 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.
authors.affiliation: Faculty of Pharmacy, Department of Pharmaceutical Technology, Hacettepe University, 06100 Sihhiye, Ankara, Turkey.
authors.forename: Betül Arica
authors.initials: BA
authors.lastname: Yegin
authors.forename: Brice
authors.initials: B
authors.lastname: Moulari
authors.forename: N Tugba
authors.initials: NT
authors.lastname: Durlu-Kandilci
authors.forename: Petek
authors.initials: P
authors.lastname: Korkusuz
authors.forename: Yann
authors.initials: Y
authors.lastname: Pellequer
authors.forename: Alf
authors.initials: A
authors.lastname: Lamprecht
mesh_terms: D000464:Alginates; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage; D003692:Delayed-Action Preparations / Q000737:chemistry*; D005260:Female; D051379:Mice; D008855:Microscopy, Electron, Scanning; D008863:Microspheres; D013467:Sulindac / Q000008:administration & dosage*
chemical_list: D000464:Alginates; D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D013467:Sulindac