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

Authors :
Csilla Bartos
Rita Ambrus
Anita Kovács
Róbert Gáspár
Anita Sztojkov-Ivanov
Árpád Márki
Tamás Janáky
Ferenc Tömösi
Gábor Kecskeméti
Piroska Szabó-Révész
Source :
Molecules, Vol 23, Iss 4, p 784 (2018)
Publication Year :
2018
Publisher :
MDPI AG, 2018.

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.

Details

Language :
English
ISSN :
14203049
Volume :
23
Issue :
4
Database :
Directory of Open Access Journals
Journal :
Molecules
Publication Type :
Academic Journal
Accession number :
edsdoj.bf9200aca0b945e2acd063f7c038ad76
Document Type :
article
Full Text :
https://doi.org/10.3390/molecules23040784