Cyclodextrin based nanosponges for pulmonar delivery, a case with Budenoside

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Budesonide (BUD) is a glucocorticosteroid used for treating chronic obstructive pulmonary disease. However, its low solubility and poor bioavailability pose challenges. To overcome these issues, the group of prof. Francesco Trotta (UNITO, Italy) developed biocompatible β-cyclodextrin-based nanosponges (βCD-NS) to enhance drug delivery, tested in collaboration with prof. Shahiwala (Dubai).

BUD was loaded onto five types of βCD-NS at various ratios. The most effective formulation, BUD-βCD-NS, was achieved using 1:3 BUD:βCD-NS ratio with 1,1′-carbonyldiimidazole (CDI) as a crosslinking agent, exhibiting high encapsulation efficiency (approximately 80%). The optimized formulations underwent comprehensive characterization, including FTIR, TGA, WAC, SEM, XRD, particle size, zeta potential, encapsulation efficiency, in vitro and in vivo release studies, acute toxicity study, solid-state analysis, and aerosol performance evaluation.

Both in vitro and in vivo studies demonstrated sustained drug release and absorption over 12 hours for BUD-βCD-NS compared to pure BUD, which showed rapid release in the initial 2 hours. Safety assessments through acute toxicity and in vitro cytotoxicity studies on alveolar cells confirmed the safety of BUD-βCD-NS. Various aerosol parameters indicated the potential of BUD-βCD-NS for formulating dry powder inhalers (DPI).

In summary, this study provides valuable insights into the future development of βCD-NS as efficient drug delivery systems, ensuring controlled release of therapeutic agents for pulmonary diseases.


Salem, Y. Y., Hoti, G., Sammour, R. M., Caldera, F., Cecone, C., Matencio, A., Shahiwala, A.F. & Trotta, F. (2023). Preparation and Evaluation of β-Cyclodextrin-based Nanosponges loaded with Budesonide for Pulmonary Delivery. International Journal of Pharmaceutics 647, 123529.

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