Improving Inhalation Performance with Particle Agglomeration via Combining Mechanical Dry Coating and Ultrasonic Vibration
Agglomerate formulations for dry powder inhalation (DPI) formed with fine particles are versatile means for the highly efficient delivery of budesonide. However, uncontrolled agglomeration induces high deposition in the upper airway, causing local side effects due to high mechanical strength, worse deagglomeration, and poor fine-particle delivery. In the present study, fine lactose was mechanically dry-coated prior to particle agglomeration, and the agglomerates were then spheroidized via ultrasonic vibration to improve their aerosol performance.
The results showed that the agglomerate produced with the surface-enriched hydrophobic magnesium stearate and ultrasonic vibration demonstrated improved aerosolization properties, benefiting from their lower mechanical strength, less interactive cohesive force, and improved fine powder dispersion behavior. After dispersion utilizing a Turbuhaler® with a pharmaceutical cascade impactor test, a fine particle fraction (FPF) of 71.1 ± 1.3% and an artificial throat deposition of 19.3 ± 0.4% were achieved, suggesting the potential to improve the therapeutic outcomes of budesonide with less localized infections of the mouth and pharynx.
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Materials
The budesonide (purity: 98%) used in this study was purchased from Humanwell Healthcare (Group) Co., Ltd., (Yichang, China). Lactose (purity: 99%) was received as Inhalac 300 from DFE Pharma (Borculo, The Netherlands); the magnesium stearate (MgSt, purity: 99%) was acquired from PETER GREVEN (Venlo, The Netherlands), and all the materials used were of pharmaceutical grade.
Zhang, Q.; Wang, Z.; Shi, K.; Zhou, H.; Wei, X.; Hall, P. Improving Inhalation Performance with Particle Agglomeration via Combining Mechanical Dry Coating and Ultrasonic Vibration. Pharmaceutics 2024, 16, 68. https://doi.org/10.3390/pharmaceutics16010068
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