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Open AccessArticle

Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach

1
Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, H-6720 Szeged, Hungary
2
Department of Chemical and Environmental Process Engineering, Budapest University of Technology and Economics, H-1111 Budapest, Hungary
3
Faculty of Pharmacy, Department of Pharmacodynamics and Biopharmacy, University of Szeged, H-6720 Szeged, Hungary
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Faculty of Medicine, Department of Pharmacology and Pharmacotherapy, University of Szeged, H-6720 Szeged, Hungary
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Faculty of Medicine, Department of Medical Physics and Informatics, University of Szeged, H-6720 Szeged, Hungary
6
Interdisciplinary Excellence Centre, Department of Medical Chemistry, University of Szeged, H-6720 Szeged, Hungary
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(2), 97; https://doi.org/10.3390/pharmaceutics12020097
Received: 10 December 2019 / Revised: 19 January 2020 / Accepted: 21 January 2020 / Published: 25 January 2020
(This article belongs to the Special Issue Intranasal Drug Delivery Systems)
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. View Full-Text
Keywords: meloxicam; HSA nanoparticles; nose-to-brain delivery; quality by design; physical stability; in vivo animal studies; rapid equilibrium dialysis; PAMPA meloxicam; HSA nanoparticles; nose-to-brain delivery; quality by design; physical stability; in vivo animal studies; rapid equilibrium dialysis; PAMPA
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Katona, G.; Balogh, G.T.; Dargó, G.; Gáspár, R.; Márki, Á.; Ducza, E.; Sztojkov-Ivanov, A.; Tömösi, F.; Kecskeméti, G.; Janáky, T.; Kiss, T.; Ambrus, R.; Pallagi, E.; Szabó-Révész, P.; Csóka, I. Development of Meloxicam-Human Serum Albumin Nanoparticles for Nose-to-Brain Delivery via Application of a Quality by Design Approach. Pharmaceutics 2020, 12, 97.

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