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...
| Main Authors: | , , , , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2018-03-01
|
| Series: | Molecules |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1420-3049/23/4/784 |
| _version_ | 1819265010071764992 |
|---|---|
| author | Csilla Bartos Rita Ambrus Anita Kovács Róbert Gáspár Anita Sztojkov-Ivanov Árpád Márki Tamás Janáky Ferenc Tömösi Gábor Kecskeméti Piroska Szabó-Révész |
| author_facet | Csilla Bartos Rita Ambrus Anita Kovács Róbert Gáspár Anita Sztojkov-Ivanov Árpád Márki Tamás Janáky Ferenc Tömösi Gábor Kecskeméti Piroska Szabó-Révész |
| author_sort | Csilla Bartos |
| collection | DOAJ |
| 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. |
| first_indexed | 2024-12-23T20:38:34Z |
| format | Article |
| id | doaj.art-bf9200aca0b945e2acd063f7c038ad76 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-12-23T20:38:34Z |
| publishDate | 2018-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-bf9200aca0b945e2acd063f7c038ad762022-12-21T17:32:00ZengMDPI AGMolecules1420-30492018-03-0123478410.3390/molecules23040784molecules23040784Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery SystemsCsilla Bartos0Rita Ambrus1Anita Kovács2Róbert Gáspár3Anita Sztojkov-Ivanov4Árpád Márki5Tamás Janáky6Ferenc Tömösi7Gábor Kecskeméti8Piroska Szabó-Révész9Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u. 6, H-6720 Szeged, HungaryInstitute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u. 6, H-6720 Szeged, HungaryInstitute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u. 6, H-6720 Szeged, HungaryDepartment of Pharmacodynamics and Biopharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, HungaryDepartment of Pharmacodynamics and Biopharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, HungaryDepartment of Pharmacodynamics and Biopharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, HungaryDepartment of Medical Chemistry, University of Szeged, Dóm tér 8, H-6720 Szeged, HungaryDepartment of Medical Chemistry, University of Szeged, Dóm tér 8, H-6720 Szeged, HungaryDepartment of Medical Chemistry, University of Szeged, Dóm tér 8, H-6720 Szeged, HungaryInstitute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u. 6, H-6720 Szeged, HungaryThe 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.http://www.mdpi.com/1420-3049/23/4/784nanosized meloxicammeloxicam potassium monohydrateintranasal formulationdissolution ratein vitro diffusionplasma drug-contentabsolute bioavailability for brain |
| spellingShingle | Csilla Bartos Rita Ambrus Anita Kovács Róbert Gáspár Anita Sztojkov-Ivanov Árpád Márki Tamás Janáky Ferenc Tömösi Gábor Kecskeméti Piroska Szabó-Révész Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems Molecules nanosized meloxicam meloxicam potassium monohydrate intranasal formulation dissolution rate in vitro diffusion plasma drug-content absolute bioavailability for brain |
| 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 | nanosized meloxicam meloxicam potassium monohydrate intranasal formulation dissolution rate in vitro diffusion plasma drug-content absolute bioavailability for brain |
| url | http://www.mdpi.com/1420-3049/23/4/784 |
| work_keys_str_mv | AT csillabartos investigationofabsorptionroutesofmeloxicamanditssaltformfromintranasaldeliverysystems AT ritaambrus investigationofabsorptionroutesofmeloxicamanditssaltformfromintranasaldeliverysystems AT anitakovacs investigationofabsorptionroutesofmeloxicamanditssaltformfromintranasaldeliverysystems AT robertgaspar investigationofabsorptionroutesofmeloxicamanditssaltformfromintranasaldeliverysystems AT anitasztojkovivanov investigationofabsorptionroutesofmeloxicamanditssaltformfromintranasaldeliverysystems AT arpadmarki investigationofabsorptionroutesofmeloxicamanditssaltformfromintranasaldeliverysystems AT tamasjanaky investigationofabsorptionroutesofmeloxicamanditssaltformfromintranasaldeliverysystems AT ferenctomosi investigationofabsorptionroutesofmeloxicamanditssaltformfromintranasaldeliverysystems AT gaborkecskemeti investigationofabsorptionroutesofmeloxicamanditssaltformfromintranasaldeliverysystems AT piroskaszaborevesz investigationofabsorptionroutesofmeloxicamanditssaltformfromintranasaldeliverysystems |