Investigation of absorption routes of meloxicam and its salt form from intranasal delivery systems

Csilla Bartos, Rita Ambrus, Anita Kovács, R. Gáspár, Anita Sztojkov-Ivanov, A. Márki, T. Janáky, Ferenc T m si, Gábor Kecskeméti, P. Szabó-Révész

Research output: Contribution to journalArticle

1 Citation (Scopus)

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.

Original languageEnglish
Article number784
JournalMolecules
Volume23
Issue number4
DOIs
Publication statusPublished - Jan 1 2018

Fingerprint

meloxicam
Nose
sprayers
Brain
delivery
Salts
routes
salts
brain
Axonal Transport
Blood
Plasmas
blood
drugs
Pharmaceutical Preparations
formulations
Pain Management
pain
Potassium
Dissolution

Keywords

  • Absolute bioavailability for brain
  • Dissolution rate
  • In vitro diffusion
  • Intranasal formulation
  • Meloxicam potassium monohydrate
  • Nanosized meloxicam
  • Plasma drug-content

ASJC Scopus subject areas

  • Organic Chemistry

Cite this

Investigation of absorption routes of meloxicam and its salt form from intranasal delivery systems. / Bartos, Csilla; Ambrus, Rita; Kovács, Anita; Gáspár, R.; Sztojkov-Ivanov, Anita; Márki, A.; Janáky, T.; T m si, Ferenc; Kecskeméti, Gábor; Szabó-Révész, P.

In: Molecules, Vol. 23, No. 4, 784, 01.01.2018.

Research output: Contribution to journalArticle

Bartos, Csilla ; Ambrus, Rita ; Kovács, Anita ; Gáspár, R. ; Sztojkov-Ivanov, Anita ; Márki, A. ; Janáky, T. ; T m si, Ferenc ; Kecskeméti, Gábor ; Szabó-Révész, P. / Investigation of absorption routes of meloxicam and its salt form from intranasal delivery systems. In: Molecules. 2018 ; Vol. 23, No. 4.
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