Inhalable Nano-Dimpled Microspheres Containing Budesonide-PLGA for Improved Aerodynamic Performance

Introduction: Dry powder inhalations are an attractive pharmaceutical dosage form. They are environmentally friendly, portable, and physicochemical stable compared to other inhalation forms like pressurized metered-dose inhalers and nebulizers. Sufficient drug deposition of DPIs into the deep lung is required to enhance the therapeutic activity. Nanoscale surface roughness in microparticles could improve aerosolization and aerodynamic performance. This study aimed to prepare microspheres with nanoscale dimples and confirm the effect of roughness on inhalation efficiency.

Methods: The dimpled-surface on microspheres (MSs) was achieved by oil in water (O/W) emulsion-solvent evaporation by controlling the stirring rate. The physicochemical properties of MSs were characterized. Also, in vitro aerodynamic performance of MSs was evaluated by particle image velocimetry and computational fluid dynamics.

Results: The particle image velocimetry results showed that dimpled-surface MSs had better aerosolization, about 20% decreased X-axial velocity, and a variable angle, which could improve the aerodynamic performance. Furthermore, it was confirmed that the dimpled surface of MSs could cause movement away from the bronchial surface, which helps the MSs travel into the deep lung using computational fluid dynamics.

Conclusion: The dimpled-surface MSs showed a higher fine particle fraction value compared to smooth-surface MSs in the Andersen Cascade Impactor, and surface roughness like dimples on microspheres could improve aerosolization and lung deposition.

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Materials

Budesonide (BUD) was provided by INIST (Hwaseong-si, Korea). Poly (D, L lactic-co-glycolic acid) (PLGA) 503H was supplied by Evonik, Ltd. (Essen, Germany). Polyvinyl alcohol 500 (PVA 500) was purchased from the OCI Company, Ltd (Seoul, Korea). InhaLac 230 was provided by the Masung & CO Ltd. (Seoul, Korea). Methanol, dichloromethane (DCM), and acetonitrile (ACN) were high-performance liquid chromatography (HPLC) grades and purchased from Honeywell Burdick & Jackson Ltd. (Muskegon, MI, USA). Other chemicals were analytical grade and used as received. All experiments were carried out using Milli-Q distilled water.

Han CS, Kang JH, Kim YJ, Kim DW, Park CW. Inhalable Nano-Dimpled Microspheres Containing Budesonide-PLGA for Improved Aerodynamic Performance. Int J Nanomedicine. 2022;17:3405-3419
https://doi.org/10.2147/IJN.S372582

See the overview The Inhalac family by Meggle