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Nasal Powder Formulations: In-Vitro Characterisation of the Impact of Powders on Nasal Residence Time and Sensory Effects

Nasal drug delivery is still primarily associated with locally-effective drugs, but next-generation products utilising the benefits of nasal administration—such as easy access to a relatively permeable mucosa, the presence of immunocompetent cells, and a direct route to the brain—are under investiga...

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Autores principales: Trenkel, Marie, Scherließ, Regina
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8001606/
https://www.ncbi.nlm.nih.gov/pubmed/33805779
http://dx.doi.org/10.3390/pharmaceutics13030385
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author Trenkel, Marie
Scherließ, Regina
author_facet Trenkel, Marie
Scherließ, Regina
author_sort Trenkel, Marie
collection PubMed
description Nasal drug delivery is still primarily associated with locally-effective drugs, but next-generation products utilising the benefits of nasal administration—such as easy access to a relatively permeable mucosa, the presence of immunocompetent cells, and a direct route to the brain—are under investigation. Nasal powders offer the potential to improve the drugs’ effects by providing higher resistance against the mucociliary clearance, and thus prolonging the contact time of the drug with its target site. However, suitable and easy-to-use in-vitro setups tailored to the characterisation of this effect are missing. In this study, a selection of excipients for powder formulations were used to evaluate the applicability of different methods which investigate the influence on the contact time. The combination of the assessment of rheological properties, dynamic vapour sorption, and adhesiveness on agar–mucin plates was found to be a valuable predictive tool. For the additional assessment of the sensations associated with the close contact of powders and the mucosa, a slug mucosal irritation assay was conducted and adapted to powders. These methods are regarded as being especially useful for comparative screenings in early formulation development.
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spelling pubmed-80016062021-03-28 Nasal Powder Formulations: In-Vitro Characterisation of the Impact of Powders on Nasal Residence Time and Sensory Effects Trenkel, Marie Scherließ, Regina Pharmaceutics Article Nasal drug delivery is still primarily associated with locally-effective drugs, but next-generation products utilising the benefits of nasal administration—such as easy access to a relatively permeable mucosa, the presence of immunocompetent cells, and a direct route to the brain—are under investigation. Nasal powders offer the potential to improve the drugs’ effects by providing higher resistance against the mucociliary clearance, and thus prolonging the contact time of the drug with its target site. However, suitable and easy-to-use in-vitro setups tailored to the characterisation of this effect are missing. In this study, a selection of excipients for powder formulations were used to evaluate the applicability of different methods which investigate the influence on the contact time. The combination of the assessment of rheological properties, dynamic vapour sorption, and adhesiveness on agar–mucin plates was found to be a valuable predictive tool. For the additional assessment of the sensations associated with the close contact of powders and the mucosa, a slug mucosal irritation assay was conducted and adapted to powders. These methods are regarded as being especially useful for comparative screenings in early formulation development. MDPI 2021-03-13 /pmc/articles/PMC8001606/ /pubmed/33805779 http://dx.doi.org/10.3390/pharmaceutics13030385 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ).
spellingShingle Article
Trenkel, Marie
Scherließ, Regina
Nasal Powder Formulations: In-Vitro Characterisation of the Impact of Powders on Nasal Residence Time and Sensory Effects
title Nasal Powder Formulations: In-Vitro Characterisation of the Impact of Powders on Nasal Residence Time and Sensory Effects
title_full Nasal Powder Formulations: In-Vitro Characterisation of the Impact of Powders on Nasal Residence Time and Sensory Effects
title_fullStr Nasal Powder Formulations: In-Vitro Characterisation of the Impact of Powders on Nasal Residence Time and Sensory Effects
title_full_unstemmed Nasal Powder Formulations: In-Vitro Characterisation of the Impact of Powders on Nasal Residence Time and Sensory Effects
title_short Nasal Powder Formulations: In-Vitro Characterisation of the Impact of Powders on Nasal Residence Time and Sensory Effects
title_sort nasal powder formulations: in-vitro characterisation of the impact of powders on nasal residence time and sensory effects
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8001606/
https://www.ncbi.nlm.nih.gov/pubmed/33805779
http://dx.doi.org/10.3390/pharmaceutics13030385
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