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

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 properti...

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Autores principales: Bartos, Csilla, Ambrus, Rita, Kovács, Anita, Gáspár, Róbert, Sztojkov-Ivanov, Anita, Márki, Árpád, Janáky, Tamás, Tömösi, Ferenc, Kecskeméti, Gábor, Szabó-Révész, Piroska
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017030/
https://www.ncbi.nlm.nih.gov/pubmed/29597330
http://dx.doi.org/10.3390/molecules23040784
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author Bartos, Csilla
Ambrus, Rita
Kovács, Anita
Gáspár, Róbert
Sztojkov-Ivanov, Anita
Márki, Árpád
Janáky, Tamás
Tömösi, Ferenc
Kecskeméti, Gábor
Szabó-Révész, Piroska
author_facet Bartos, Csilla
Ambrus, Rita
Kovács, Anita
Gáspár, Róbert
Sztojkov-Ivanov, Anita
Márki, Árpád
Janáky, Tamás
Tömösi, Ferenc
Kecskeméti, Gábor
Szabó-Révész, Piroska
author_sort Bartos, Csilla
collection PubMed
description 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.
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spelling pubmed-60170302018-11-13 Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems Bartos, Csilla Ambrus, Rita Kovács, Anita Gáspár, Róbert Sztojkov-Ivanov, Anita Márki, Árpád Janáky, Tamás Tömösi, Ferenc Kecskeméti, Gábor Szabó-Révész, Piroska Molecules Article 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. MDPI 2018-03-28 /pmc/articles/PMC6017030/ /pubmed/29597330 http://dx.doi.org/10.3390/molecules23040784 Text en © 2018 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
Bartos, Csilla
Ambrus, Rita
Kovács, Anita
Gáspár, Róbert
Sztojkov-Ivanov, Anita
Márki, Árpád
Janáky, Tamás
Tömösi, Ferenc
Kecskeméti, Gábor
Szabó-Révész, Piroska
Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems
title Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems
title_full Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems
title_fullStr Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems
title_full_unstemmed Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems
title_short Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems
title_sort investigation of absorption routes of meloxicam and its salt form from intranasal delivery systems
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017030/
https://www.ncbi.nlm.nih.gov/pubmed/29597330
http://dx.doi.org/10.3390/molecules23040784
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