Formulation and Evaluation of Spray-Dried Esomeprazole Magnesium Microspheres

Abstract

Purpose: To prepare and evaluate in vitro mucoadhesive esomeprazole magnesium microspheres for the treatment of Zollinger Ellison syndrome.Methods: The microspheres were prepared by spray drying technique using locust bean and xanthan gums as polymers. Esomeprazole magnesium was entrapped in the microspheres at various polymer/cross-linking ratios. Glutaraldehyde was used to cross-link the gums. The microspheres wereevaluated for their micromeritic properties and in vitro release. as well as by Fourier transform infrared (FTIR), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM).Results: The microspheres were discrete, spherical, and showed good drug entrapment efficiency (60.5 - 92.3 %). FTIR and DSC results indicate that the drug was compatible with the polymers used. Amongst all the formulations, F6 (drug:locust bean gum:xanthan gum, 1:2:2) showed the most suitable sustained release properties with 99.8 % of drug released at the end of 12 h.Conclusion: Microspheres prepared using locust bean and xanthan gums can be used as a sustained release delivery system for esomeprazole magnesium.Keywords: Spray drying, Microspheres, Esomeprazole magnesium, Sustained release