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Published on: April 6, 2017
Nano-Spray-Drying of Cyclodextrin/Ibuprofen Complexes with Aerosolization-Enhancing Additives for Pulmonary Drug
Anett Motzwickler-Németh1, Endre Körmendi1, Árpád Farkas2
1Institute of Pharmaceutical Technology and Regulatory Affairs, Faculty of Pharmacy, University of Szeged, 6720 Szeged, Hungary.
Cyclodextrins enhance ibuprofen solubility for lung delivery, improving cystic fibrosis treatment. Nano-spray drying created effective drug-carrier complexes with optimal aerodynamic properties for enhanced drug release.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Materials Science
Background:
- Poorly water-soluble drugs require enhanced delivery systems.
- Pulmonary drug delivery offers reduced dosage and side effects, beneficial for conditions like cystic fibrosis.
- Cyclodextrins (CDs) are effective carriers for improving drug solubility.
Purpose of the Study:
- To prepare and characterize cyclodextrin/ibuprofen (CD/IBU) complexes using nano-spray drying.
- To evaluate the aerodynamic properties and in vitro performance of these complexes for pulmonary delivery.
- To compare the efficacy of sulfobutylether-β-cyclodextrin (SBECD) and (2-Hydroxy-3-N,N,N-trimethylamino)propyl-beta-cyclodextrin chloride (QABCD) as carriers.
Main Methods:
- Nano-spray drying technique for complex preparation.
- Characterization using particle size analysis, SEM, XRPD, DSC, and FT-IR.
- In vitro evaluation via Andersen Cascade Impactor, dissolution, and diffusion tests, complemented by in silico simulations.
Main Results:
- Optimized formulations achieved approximately 50% fine particle fraction, indicating good aerosolization potential.
- Rapid in vitro drug release was observed for all formulations.
- QABCD-based formulations showed reduced membrane diffusion compared to SBECD due to electrostatic interactions.
Conclusions:
- Nano-spray drying is a viable method for preparing CD/IBU complexes for pulmonary delivery.
- Formulations exhibited favorable aerodynamic properties and rapid drug release.
- The choice of cyclodextrin (SBECD vs. QABCD) influences drug diffusion due to interactions, impacting overall delivery efficacy.
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