Abstract
Eosinophilic esophagitis (EE) is a chronic immune/antigen-mediated esophageal inflammatory disease for which off-label topical corticosteroids (e.g., budesonide) are widely used in clinic. In general, thickening excipients are mixed with industrial products to improve the residence time of the drug on the esophageal mucosa. The compounding procedures are empirical and the composition is not supported by real physicochemical and technological characterization. The current study aimed to propose a standardized budesonide oral formulation intended to improve the resistance time of the drug on the esophageal mucosa for EE treatment. Different placebo and drug-loaded (0.025% w/w) formulations were prepared by changing the percentage of xanthan gum alone or in ratio 1:1 with guar gum. Both excipients were added in the composition for their mucoadhesive properties. The formulative space was rationalized based on the drug physicochemical stability and the main critical quality attributes of the formulation, e.g., rheological properties, syringeability, mucoadhesiveness and in vitro penetration of budesonide in porcine esophageal tissue. The obtained results demonstrated that gums allowed a prolonged residence time. However, the concentration of the mucoadhesive polymer has to be rationalized appropriately to permit the syringeability of the formulation and, therefore, easy dosing by the patient/caregiver.
Highlights
Eosinophilic esophagitis (EE) is a chronic immune/antigen-mediated esophageal inflammatory disease associated with esophageal dysfunction resulting from severe eosinophil-predominant inflammation [1,2]
Foods can be reintroduced in the diet sequentially in order to identify food triggers of esophageal eosinophilia and to establish a less restrictive, long-term, therapeutic diet for the effective disease management [3]
Off-label topical corticosteroids are frequently used in clinic: patients are trained to swallow asthma medicinal products designed initially to be inhaled or viscous oral formulations extemporaneously compounded in pharmacies
Summary
Eosinophilic esophagitis (EE) is a chronic immune/antigen-mediated esophageal inflammatory disease associated with esophageal dysfunction resulting from severe eosinophil-predominant inflammation [1,2]. The benefit-risk balance of such medicinal products may be affected by significant secondary side effects due to systemic drug absorption after pulmonary administration It may be affected by a low patient adherence, due to the complexity of the administration devices (e.g., metered-dose inhaler). The interest in developing topically applied therapeutics is increasing [11,12] In this context, off-label topical corticosteroids are frequently used in clinic: patients are trained to swallow asthma medicinal products designed initially to be inhaled or viscous oral formulations extemporaneously compounded in pharmacies. European regulatory authorities have authorized an orodispersible tablet loaded with BU indicated for the treatment of EE in adults older than 18 years of age This medicinal product is not suitable for pediatric patients since they require adjustments in strength and dosage form in comparison to adults [13,14,15]
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