Towards a more desirable dry powder inhaler formulation: large spray-dried mannitol microspheres outperform small microspheres

Kaialy, Waseem, Hussain, Tariq, Alhalaweh, Amjad and Nokhodchi, Ali (2014) Towards a more desirable dry powder inhaler formulation: large spray-dried mannitol microspheres outperform small microspheres. Pharmaceutical Research, 31 (1). pp. 60-76. ISSN 0724-8741

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Abstract

Purpose: To investigate, for the first time, the performance of a dry powder inhaler (DPI, Aerolizer®) in the case of a model drug (i.e. albuterol sulphate) formulated with spray dried mannitol carrier particles with homogeneous shape and solid-state form but different sizes. Methods: Spray dried mannitol (SDM) particles were characterized in terms of size, surface area, morphology, water content, solid-state, density and electrostatic charge by a novel approach. DPI formulations composed of SDM and albuterol sulphate (AS) were prepared and evaluated in terms of drug content homogeneity and in vitro aerosolization performance. Results: All SDM particles generated similar fine particle fractions of AS. Formulations consisting of larger SDM particles demonstrated better drug content homogeneity, reduced amounts of drug loss and reduced oropharyngeal deposition. Comparing different SDM products demonstrated that SDM powders with relatively poorer flowability, wider size distributions and higher charge density generated DPI formulations with poorer drug content homogeneity and deposited higher amount of drug on the inhaler, mouthpiece adaptor and throat. DPI formulation total desirability increased linearly with the mean diameter of SDM. Conclusion: Particle shape and solid-state form of mannitol could dominate over carrier size, bulk density, flowability and charge in terms of determining the aerosolization behaviour of AS formulated with mannitol carrier, at least within the experimental protocols applied in the present study. © 2013 Springer Science+Business Media New York.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Subjects: Q Science > QD Chemistry
Depositing User: Tom Gittoes
Date Deposited: 17 Dec 2014 12:32
Last Modified: 17 Dec 2014 12:32
URI: http://sro.sussex.ac.uk/id/eprint/51714
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