Design, Development and Characterization of S-Smedds of Budesonide For The Treatment of Eosinophilic Esophagitis

Abstract

Eosinophilic Esophagitis (EoE) is a chronic gastrointestinal disease which is cause by a Th2-mediated response to allergen sensitization, which leads to the activation and infiltration of eosinophils in the esophageal mucosa. Current therapies for EoE include off-label drugs for which patients often have to prepare their own formulations or inhaled budesonide and fluticasone, which can cause unwanted systemic side effects. The aim of this project is to develop, characterize and evaluate orodispersible tablets of budesonide as an effective treatment for EoE. Orodispersible tablets of budesonide were formulated by preparing liquid-SMEDDS which is proposed to increase the solubility of the budesonide. The prepared liquid-SMEDDS of budesonide showed high stability, monodispersed and small particle size. The optimized liquid-SMEDDS had a mean size of 125 nm, a PDI of 0.347 and a zeta potential of -53.6 mV. The liquid-SMEDDS were adsorbed onto a carrier to form solid-SMEDDS that can be compressed into orodispersible tablets to increase patience compliance. The solubility of the solid-SMEDDS was compared to the solubility of pure budesonide in 6.8 pH phosphate buffer. The results indicated that incorporating budesonide into liquid-SMEDDS significantly improved its solubility in 6.8 pH buffer. The formulated orodispersible tablets of budesonide had an average drug release of 81.1% and an average drug content of 96.1%. The incorporation of budesonide into liquid-SMEDDS and formulation into solid oral dosage form increased its solubility and allowed for fast disintegration and a high dissolution rate.