In Vitro Regional Deposition of Nasal Sprays in an Idealized Nasal Inlet: Comparison with In Vivo Gamma Scintigraphy
- PMID: 36109462
- DOI: 10.1007/s11095-022-03388-7
In Vitro Regional Deposition of Nasal Sprays in an Idealized Nasal Inlet: Comparison with In Vivo Gamma Scintigraphy
Abstract
Purpose: To compare in vitro regional nasal deposition measurements using an idealized nasal airway geometry, the Alberta Idealized Nasal Inlet (AINI), with in vivo regional deposition for nasal drug products.
Materials and methods: One aqueous solution formulation (NasalCrom), one aqueous suspension formulation (Nasonex) and one nasal pressurized metered dose spray device (QNASL) were selected. Two spray orientation angles, 60° and 45° from the horizontal, were selected. A steady inhalation flow rate of 7.5 L/min was selected to simulate slow inhalation through a single nostril. After actuation, the AINI was disassembled. The mass of drug deposited in each region and a downstream filter, representing penetration of drug to the lungs, was determined using ultraviolet-visible (UV-Vis) spectrophotometry.
Results: No filter (lung) deposition was detected for NasalCrom or Nasonex. Filter deposition ranged from 6 to 11% for QNASL. For NasalCrom, 45% to 69% of the dose deposited in the AINI was deposited in the vestibule and 31% to 55% was deposited in the turbinates; for Nasonex, 66% to 74% (vestibule) and 26% to 34% (turbinates); for QNASL, 90% to 100% (vestibule) and 0% to 10% (turbinates). No statistically significant difference was observed between regional deposition in vivo and in vitro for any of the formulations, except that nasopharyngeal deposition with Nasonex differed by less than 1.56% from in vivo, which while statistically significant, is unlikely to be clinically significant.
Conclusions: The AINI was able to mimic regional in vivo deposition for nasal drug products, permitting differentiation between devices based on regional deposition.
Keywords: aerosols; in vitro-in vivo correlations; nasal sprays; regional deposition.
© 2022. The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.
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References
-
- Pharmacopiea U. Aerosols, nasal sprays, metered-dose inhalers, and dry powder inhalers. US Pharmacopeial [Internet]. 2006;30:2617–36. Available from: http://www.pharmacopeia.cn/v29240/usp29nf24s0_c601_viewall.html
-
- U.S. Department of Health and Human Services, Food and Drug Administration Center for Drug Evaluation and Research D of DI (HFD-240). Draft: Guidance for Industry Bioavailability and Bioequivalence Studies for Nasal Aerosol and Nasal Sprays for Local Action. 2003; Available from: http://www.fda.gov/cder/guidance/index.htm
-
- Newman SP, Pitcairn GR, Dalby RN. Drug Delivery to the Nasal Cavity: In Vitro and In Vivo Assessment. Critical Reviews in Therapeutic Drug Carrier Systems. 2004;21:46.
-
- Li Bv, Jin F, Lee SL, Bai T, Chowdhury, Badrul Caramenico HT, Conner DP. Bioequivalence for locally acting nasal spray and nasal aerosol products: Standard development and generic approval. The AAPS Journal. 2013;15:875–83.
-
- Below A, Bickmann D, Breitkreutz J. Assessing the performance of two dry powder inhalers in preschool children using an idealized pediatric upper airway model. International Journal of Pharmaceutics. Elsevier B.V.; 2013;444:169–74.
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