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Transformation of Meloxicam Containing Nanosuspension into Surfactant-Free Solid Compositions to Increase the Product Stability and Drug Bioavailability for Rapid Analgesia

Authors Bartos C, Ambrus R, Katona G, Sovány T, Gáspár R, Márki Á, Ducza E, Ivanov A, Tömösi F, Janáky T, Szabó-Révész P

Received 4 July 2019

Accepted for publication 13 November 2019

Published 28 November 2019 Volume 2019:13 Pages 4007—4020

DOI https://doi.org/10.2147/DDDT.S220876

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Melinda Thomas

Peer reviewer comments 3

Editor who approved publication: Professor Manfred Ogris


Csaba Bartos,1 Rita Ambrus,1 Gábor Katona,1 Tamás Sovány,1 Róbert Gáspár,2 Árpád Márki,3 Eszter Ducza,4 Anita Ivanov,4 Ferenc Tömösi,5 Tamás Janáky,5 Piroska Szabó-Révész1

1Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Szeged, Hungary; 2Faculty of Medicine, Department of Pharmacology and Pharmacotherapy, University of Szeged, Szeged, Hungary; 3Faculty of Medicine, Department of Medical Physics and Informatics, University of Szeged, Szeged, Hungary; 4Faculty of Pharmacy, Department of Pharmacodynamics and Biopharmacy, University of Szeged, Szeged, Hungary; 5Interdisciplinary Excellence Centre, Department of Medical Chemistry, University of Szeged, Szeged, Hungary

Correspondence: Piroska Szabó-Révész
Faculty of Pharmacy, Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u 6, Szeged H-6720, Hungary
Tel +36 62 545 5722
Fax +36 62 545 571
Email revesz@pharm.u-szeged.hu

Purpose: The aim of this work was to study the influence of solidification of meloxicam (Mel) containing nanosuspension (nanoMel) on the physical stability and drug bioavailability of the products. The nanoMel sample had poly(vinyl alcohol) (PVA) as a protective polymer, but no surfactant as a further stabilizing agent because the final aim was to produce surfactant-free solid phase products as well.
Methods: The solidified samples produced by fluidization and lyophilization (fluidMel, lyoMel) were examined for particle size, crystallinity, and in vitro release of Mel compared to similar parameters of nanoMel. The products were subjected to an animal experiment using per oral administration to verify their bioavailability.
Results: Mel containing (1%) nanoMel sample was produced by wet milling process using an optimized amount of PVA (0.5%) which resulted in 130 nm as mean particle size and a significant reduction in the degree of crystallinity (13.43%) of Mel. The fluidization technique using microcrystalline cellulose (MCC) as carrier resulted in a quick conversion and no significant change in the critical product parameters. The process of lyophilization required a longer operation time, which resulted in the amorphization of the crystalline carrier (trehalose) and the recrystallization of Mel increased its particle size and crystallinity. The fluidMel and lyoMel samples had nearly five-fold higher relative bioavailability than nanoMel application by oral administration. The correlation between in vitro and in vivo studies showed that the fixed Mel nanoparticles on the surface of solid carriers (MCC, trehalose) in both the artificial gastric juice and the stomach of the animals rapidly reached saturation concentration leading to faster dissolution and rapid absorption.
Conclusion: The solidification of the nanosuspension not only increased the stability of the Mel nanoparticles but also allowed the preparation of surfactant-free compositions with excellent bioavailability which may be an important consideration for certain groups of patients to achieve rapid analgesia.

Keywords: solidification, fluidization, lyophilization, surfactant-free product, rapid drug absorption, IVIV correlation

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