Development of a Soluplus budesonide freeze-dried powder for nasal drug delivery |
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| Authors: | Michele Pozzoli Daniela Traini Paul M. Young Maria B. Sukkar |
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| Affiliation: | 1. Graduate School of Health – Pharmacy, University of Technology Sydney, Ultimo, New South Wales, Australia;2. Respiratory Technology, The Woolcock Institute of Medical Research and Discipline of Pharmacology, Sydney Medical School, University of Sydney, Glebe, New South Wales, Australia;3. Respiratory Technology, The Woolcock Institute of Medical Research and Discipline of Pharmacology, Sydney Medical School, University of Sydney, Glebe, New South Wales, Australia |
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| Abstract: | Objective: The aim of this work was to develop an amorphous solid dispersions/solutions (ASD) of a poorly soluble drug, budesonide (BUD) with a novel polymer Soluplus® (BASF, Germany) using a freeze-drying technique, in order to improve dissolution and absorption through the nasal route.Significance: The small volume of fluid present in the nasal cavity limits the absorption of a poorly soluble drug. Budesonide is a corticosteroid, practically insoluble and normally administered as a suspension-based nasal spray.Methods: The formulation was prepared through freeze-drying of polymer-drug solution. The formulation was assessed for its physicochemical (specific surface area, calorimetric analysis and X-ray powder diffraction), release properties and aerodynamic properties as well as transport in vitro using RPMI 2650 nasal cells, in order to elucidate the efficacy of the Soluplus–BUD formulation.Results: The freeze-dried Soluplus–BUD formulation (LYO) showed a porous structure with a specific surface area of 1.4334?±?0.0178 m2/g. The calorimetric analysis confirmed an interaction between BUD and Soluplus and X-ray powder diffraction the amorphous status of the drug. The freeze-dried formulation (LYO) showed faster release compared to both water-based suspension and dry powder commercial products. Furthermore, a LYO formulation, bulked with calcium carbonate (LYO-Ca), showed suitable aerodynamic characteristics for nasal drug delivery. The permeation across RPMI 2650 nasal cell model was higher compared to a commercial water-based BUD suspension.Conclusions: Soluplus has been shown to be a promising polymer for the formulation of BUD amorphous solid suspension/solution. This opens up opportunities to develop new formulations of poorly soluble drug for nasal delivery. |
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| Keywords: | Nasal powder RPMI 2650 soluplus budesonide deposition dissolution permeation freeze-drying solid solutions |
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