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Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach
The aim of this study was to optimize the formulation of meloxicam (MEL)-containing human serum albumin (HSA) nanoparticles for nose-to-brain via a quality by design (QbD) approach. Liquid and dried formulations of nanoparticles containing Tween 80 and without the surfactant were investigated. Vario...
Autores principales: | , , , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7076499/ https://www.ncbi.nlm.nih.gov/pubmed/31991767 http://dx.doi.org/10.3390/pharmaceutics12020097 |
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author | Katona, Gábor Balogh, György Tibor Dargó, Gergő Gáspár, Róbert Márki, Árpád Ducza, Eszter Sztojkov-Ivanov, Anita Tömösi, Ferenc Kecskeméti, Gábor Janáky, Tamás Kiss, Tamás Ambrus, Rita Pallagi, Edina Szabó-Révész, Piroska Csóka, Ildikó |
author_facet | Katona, Gábor Balogh, György Tibor Dargó, Gergő Gáspár, Róbert Márki, Árpád Ducza, Eszter Sztojkov-Ivanov, Anita Tömösi, Ferenc Kecskeméti, Gábor Janáky, Tamás Kiss, Tamás Ambrus, Rita Pallagi, Edina Szabó-Révész, Piroska Csóka, Ildikó |
author_sort | Katona, Gábor |
collection | PubMed |
description | The aim of this study was to optimize the formulation of meloxicam (MEL)-containing human serum albumin (HSA) nanoparticles for nose-to-brain via a quality by design (QbD) approach. Liquid and dried formulations of nanoparticles containing Tween 80 and without the surfactant were investigated. Various properties, such as the Z-average, zeta potential, encapsulation efficacy (EE), conjugation of MEL and HSA, physical stability, in vitro dissolution, in vitro permeability, and in vivo plasma and brain distribution of MEL were characterized. From a stability point of view, a solid product (Mel-HSA-Tween) is recommended for further development since it met the desired critical parameters (176 ± 0.3 nm Z-average, 0.205 ± 0.01 PdI, −14.1 ± 0.7 mV zeta potential) after 6 months of storage. In vitro examination showed a significantly increased drug dissolution and permeability of MEL-containing nanoparticles, especially in the case of applying Tween 80. The in vivo studies confirmed both the trans-epithelial and axonal transport of nanoparticles, and a significantly higher cerebral concentration of MEL was detected with nose-to-brain delivery, in comparison with intravenous or per os administration. These results indicate intranasal the administration of optimized MEL-containing HSA formulations as a potentially applicable “value-added” product for the treatment of neuroinflammation. |
format | Online Article Text |
id | pubmed-7076499 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-70764992020-03-20 Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach Katona, Gábor Balogh, György Tibor Dargó, Gergő Gáspár, Róbert Márki, Árpád Ducza, Eszter Sztojkov-Ivanov, Anita Tömösi, Ferenc Kecskeméti, Gábor Janáky, Tamás Kiss, Tamás Ambrus, Rita Pallagi, Edina Szabó-Révész, Piroska Csóka, Ildikó Pharmaceutics Article The aim of this study was to optimize the formulation of meloxicam (MEL)-containing human serum albumin (HSA) nanoparticles for nose-to-brain via a quality by design (QbD) approach. Liquid and dried formulations of nanoparticles containing Tween 80 and without the surfactant were investigated. Various properties, such as the Z-average, zeta potential, encapsulation efficacy (EE), conjugation of MEL and HSA, physical stability, in vitro dissolution, in vitro permeability, and in vivo plasma and brain distribution of MEL were characterized. From a stability point of view, a solid product (Mel-HSA-Tween) is recommended for further development since it met the desired critical parameters (176 ± 0.3 nm Z-average, 0.205 ± 0.01 PdI, −14.1 ± 0.7 mV zeta potential) after 6 months of storage. In vitro examination showed a significantly increased drug dissolution and permeability of MEL-containing nanoparticles, especially in the case of applying Tween 80. The in vivo studies confirmed both the trans-epithelial and axonal transport of nanoparticles, and a significantly higher cerebral concentration of MEL was detected with nose-to-brain delivery, in comparison with intravenous or per os administration. These results indicate intranasal the administration of optimized MEL-containing HSA formulations as a potentially applicable “value-added” product for the treatment of neuroinflammation. MDPI 2020-01-25 /pmc/articles/PMC7076499/ /pubmed/31991767 http://dx.doi.org/10.3390/pharmaceutics12020097 Text en © 2020 by the authors. 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/). |
spellingShingle | Article Katona, Gábor Balogh, György Tibor Dargó, Gergő Gáspár, Róbert Márki, Árpád Ducza, Eszter Sztojkov-Ivanov, Anita Tömösi, Ferenc Kecskeméti, Gábor Janáky, Tamás Kiss, Tamás Ambrus, Rita Pallagi, Edina Szabó-Révész, Piroska Csóka, Ildikó Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach |
title | Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach |
title_full | Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach |
title_fullStr | Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach |
title_full_unstemmed | Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach |
title_short | Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach |
title_sort | development of meloxicam-human serum albumin nanoparticles for nose-to-brain delivery via application of a quality by design approach |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7076499/ https://www.ncbi.nlm.nih.gov/pubmed/31991767 http://dx.doi.org/10.3390/pharmaceutics12020097 |
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