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, cilt.24, ss.371-382, 2007 (SCI İndekslerine Giren Dergi) identifier identifier identifier

  • Cilt numarası: 24 Konu: 4
  • Basım Tarihi: 2007
  • Doi Numarası: 10.1080/02652040701298153
  • Dergi Adı: JOURNAL OF MICROENCAPSULATION
  • Sayfa Sayıları: ss.371-382

Özet

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.