Mucoadhesive Budesonide Formulation for the Treatment of Eosinophilic Esophagitis

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.

Semisolid Dosage

“…Last but not least, the article that does not deal with dermal application describes a ''Mucoadhesive Budesonide Formulation for the Treatment of Eosinophilic Esophagitis (EE)" [12]. The authors present results from a study that revealed a standardized budesonide oral formulation intended to improve the resistance time of the drug on the esophageal mucosa for EE treatment.…”

Comment on Casiraghi et al. “Mucoadhesive Budesonide Formulation for the Treatment of Eosinophilic Esophagitis” 2020, 12, 211

“…In their article, Casiraghi, A. et al claim that [ 1 ] “the compounding procedures (in order to compound oral viscous budesonide-author’s addition) are empirical and the composition is not supported by real physicochemical and technological characterization”. Indeed, Casiraghi et al analyzed a few relevant aspects of the formulation of oral viscous budesonide in their article, such as rheological properties, syringeability, mucoadhesiveness, and in vitro penetration of budesonide in porcine esophageal tissue.…”

Formulations of Topical Steroids in Eosinophilic Esophagitis—Current Treatment and Emerging Possibilities

“…A key consideration in therapy with topical corticosteroids is the time that the drug remains in contact with the mucosa, as this duration is directly associated with histological improvement [ 46 ]. Therefore, various modifications of compounded OVB have been developed to improve the local effects of steroid delivery, and these have been subjected to randomised placebo-controlled trials [ 78 , 79 , 80 ].…”