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Interest of cyclodextrins in spray-dried microparticles formulation for sustained pulmonary delivery of budesonide.
Dufour, Gilles; Bigazzi, William; Wong, Nelson; Boschini, Frederic; de Tullio, Pascal; Piel, Geraldine; Cataldo, Didier; Evrard, Brigitte.
Afiliación
  • Dufour G; Laboratory of Pharmaceutical Technology and Biopharmacy, Department of Pharmacy, Center for Interdisciplinary Research on Medicines (CIRM), University of Liege, 4000 Liège, Belgium. Electronic address: gilles.dufour@ulg.ac.be.
  • Bigazzi W; Laboratory of Pharmaceutical Technology and Biopharmacy, Department of Pharmacy, Center for Interdisciplinary Research on Medicines (CIRM), University of Liege, 4000 Liège, Belgium.
  • Wong N; Laboratory of Pharmaceutical Technology and Biopharmacy, Department of Pharmacy, Center for Interdisciplinary Research on Medicines (CIRM), University of Liege, 4000 Liège, Belgium.
  • Boschini F; APTIS, Chemistry Institute B6a, University of Liege, 4000 Liège, Belgium.
  • de Tullio P; Laboratory of Medicinal Chemistry, Department of Pharmacy, Center for Interdisciplinary Research on Medicines (CIRM), University of Liege, 4000 Liège, Belgium.
  • Piel G; Laboratory of Pharmaceutical Technology and Biopharmacy, Department of Pharmacy, Center for Interdisciplinary Research on Medicines (CIRM), University of Liege, 4000 Liège, Belgium.
  • Cataldo D; Laboratory of Tumour and Development Biology, Groupe Interdisciplinaire de Génoprotéomique Appliquée (GIGA-Research), University of Liege, 4000 Liège, Belgium.
  • Evrard B; Laboratory of Pharmaceutical Technology and Biopharmacy, Department of Pharmacy, Center for Interdisciplinary Research on Medicines (CIRM), University of Liege, 4000 Liège, Belgium.
Int J Pharm ; 495(2): 869-78, 2015 Nov 30.
Article en En | MEDLINE | ID: mdl-26410753
To achieve an efficient lung delivery and efficacy, both active ingredient aerosolisation properties and permeability through the lung need to be optimized. To overcome these challenges, the present studies aim to develop cyclodextrin-based spray-dried microparticles containing a therapeutic corticosteroid (budesonide) that could be used to control airway inflammation associated with asthma. The complexation between budesonide and hydroxypropyl-ß-cyclodextrin (HPBCD) has been investigated. Production of inhalation powders was carried out using a bi-fluid nozzle spray dryer and was optimized based on a design of experiments. Spray-dried microparticles display a specific "deflated-ball like shape" associated with an appropriate size for inhalation. Aerodynamic assessment show that the fine particle fraction was increased compared to a classical lactose-based budesonide formulation (44.05 vs 26.24%). Moreover, the budesonide permeability out of the lung was shown to be reduced in the presence of cyclodextrin complexes. The interest of this sustained budesonide release was evaluated in a mouse model of asthma. The anti-inflammatory effect was compared to a non-complexed budesonide formulation at the same concentration and attests the higher anti-inflammatory activity reach with the cyclodextrin-based formulation. This strategy could therefore be of particular interest for improving lung targeting while decreasing systemic side effects associated with high doses of corticosteroids. In conclusion, this works reports that cyclodextrins could be used in powder for inhalation, both for their abilities to improve active ingredient aerosolisation properties and further to their dissolution in lung fluid, to decrease permeability out of the lungs leading to an optimized activity profile.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Portadores de Fármacos / Budesonida / Beta-Ciclodextrinas / Pulmón Límite: Animals / Humans / Male Idioma: En Revista: Int J Pharm Año: 2015 Tipo del documento: Article Pais de publicación: Países Bajos
Texto completo
Añadir a Mi BVS
Imprimir
XML
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Portadores de Fármacos / Budesonida / Beta-Ciclodextrinas / Pulmón Límite: Animals / Humans / Male Idioma: En Revista: Int J Pharm Año: 2015 Tipo del documento: Article Pais de publicación: Países Bajos