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An Investigation into Alternative Sugars as Potential Carriers for a Dry Powder Formulation of Budesonide and Formoterol

Ali Nokhodchi, Mohammed N. Momin, Azher Iqbal

Abstract


Delivery of two drugs in one dry powder inhaler (DPI) is expected to play an increasing and more effective role in the management of asthma and chronic obstructive pulmonary disease. In this study we investigated five sugars as possible carriers of both budesonide, an anti-inflammatory glucocorticoid, and formoterol, a long-acting agonist, in one DPI formulation. Most DPI formulations utilise lactose as a carrier in the drug-carrier blends; however, it cannot be used for compounds that react with its reducing group, such as budesonide, formoterol, or peptide/protein-based drugs. Therefore, alternative carriers such as sorbitol, mannitol, dextrose and xylitol were selected for this study in addition to lactose, which was used as a reference. A formulation comprising 5% w/w budesonide and 0.3% w/w formoterol was prepared with each sugar. The carriers were sieved to obtain 63-90 µm fractions and physicochemically characterised via true density, powder flow, particle size and surface morphology analyses. The dispersion and deaggregation of the two drugs from the five formulations were assessed after aerosolisation at 58-68 L min-1 via a device-metered Airmax inhaler into a Multi-Stage Liquid Impinger. The findings show that the deposition efficiencies of the five formulations were influenced by the particle size distribution, surface morphology and flowability of the respective carriers, and that mannitol showed the greatest potential as an alternative carrier to lactose. Mannitol produced the highest fine particle fraction values of 72.4% and 27.5% for budesonide and formoterol, respectively, and this performance was largely attributable to the relatively high percentage of fine particles (< 10.50 µm) compared to the other carriers.

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