Paediatric formulation: budesonide 0.1 mg/mL viscous oral solution for eosinophilic esophagitis using cyclodextrins

Ey, Caroline; Hosselet, Christel; Villon, Benjamin; Marçon, Fréderic

doi:10.1515/pthp-2018-0004

Cited by 1 publication

(1 citation statement)

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“…Frequently, they have been prepared by mixing a commercial sterile suspension of BU to be nebulized, which is indicated in the treatment of bronchial asthma and in infants and children with croup, with a thickening agent (e.g., sucralose) [19][20][21]. Alternatively, cellulose derivatives [22] or gums [23,24] have also been added. Hefner et al [25] compared the technological performances of different types of thickening agents like sucralose, xanthan gum or honey, demonstrating that the gum permitted a better residence time of the active pharmaceutical ingredients (API) on the esophageal mucosa.…”

Section: Introductionmentioning

confidence: 99%

Mucoadhesive Budesonide Formulation for the Treatment of Eosinophilic Esophagitis

et al. 2020

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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.

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