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Molecules 2018, 23(4), 784; https://doi.org/10.3390/molecules23040784

Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems

1
Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary
2
Department of Pharmacodynamics and Biopharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary
3
Department of Medical Chemistry, University of Szeged, Dóm tér 8, H-6720 Szeged, Hungary
*
Author to whom correspondence should be addressed.
Received: 12 March 2018 / Revised: 26 March 2018 / Accepted: 27 March 2018 / Published: 28 March 2018
(This article belongs to the Collection Poorly Soluble Drugs)
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Abstract

The aim of this article was to study the trans-epithelial absorption to reach the blood and to target the brain by axonal transport using nasal formulations with nanonized meloxicam (nano MEL spray) and its salt form known as meloxicam potassium monohydrate (MELP spray). The physicochemical properties and the mucoadhesivity of nasal formulations were controlled. In vitro and in vivo studies were carried out. These forms were first investigated in “nose-to-brain” relation. It was found that the in vitro study and in vivo study did not show any significant correlation. In vitro experiments demonstrated faster dissolution rate and higher diffusion of MELP from the spray compared with the nano MEL spray. The administration of the nano MEL spray resulted in faster absorption and constant plasma concentration of the drug after five minutes of administration as compared to MELP. The axonal transport of the drug was justified. MEL appeared in the brain tissues after the first five minutes of administration in the case of both spray forms, but its amount was too small in comparison with the total plasma concentration. The application of the nano MEL spray resulted in the same AUC in the brain as the intravenous injection. The “nose-to-blood” results predicted the nasal applicability of MEL and MELP in pain management. The “nose-to-brain” pathway requires further study. View Full-Text
Keywords: nanosized meloxicam; meloxicam potassium monohydrate; intranasal formulation; dissolution rate; in vitro diffusion; plasma drug-content; absolute bioavailability for brain nanosized meloxicam; meloxicam potassium monohydrate; intranasal formulation; dissolution rate; in vitro diffusion; plasma drug-content; absolute bioavailability for brain
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
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Bartos, C.; Ambrus, R.; Kovács, A.; Gáspár, R.; Sztojkov-Ivanov, A.; Márki, Á.; Janáky, T.; Tömösi, F.; Kecskeméti, G.; Szabó-Révész, P. Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems. Molecules 2018, 23, 784.

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