Physico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres

Nasal drug delivery has many beneficial properties, such as avoiding the first pass metabolism and rapid onset of action. However, the limited residence time on the mucosa and limited absorption of certain molecules make the use of various excipients necessary to achieve high bioavailability. The ap...

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Autores principales:	Patrícia Varga, Rita Ambrus, Piroska Szabó-Révész, Dávid Kókai, Katalin Burián, Zsolt Bella, Ferenc Fenyvesi, Csilla Bartos
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	alpha-cyclodextrin hydroxypropyl-β-cyclodextrin meloxicam potassium nano spray drying nasal drug delivery Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/a636b8b967564a81af59f22f546de9bf
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spelling	oai:doaj.org-article:a636b8b967564a81af59f22f546de9bf2021-11-25T18:41:26ZPhysico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres10.3390/pharmaceutics131118831999-4923https://doaj.org/article/a636b8b967564a81af59f22f546de9bf2021-11-01T00:00:00Zhttps://www.mdpi.com/1999-4923/13/11/1883https://doaj.org/toc/1999-4923Nasal drug delivery has many beneficial properties, such as avoiding the first pass metabolism and rapid onset of action. However, the limited residence time on the mucosa and limited absorption of certain molecules make the use of various excipients necessary to achieve high bioavailability. The application of mucoadhesive polymers can increase the contact time with the nasal mucosa, and permeation enhancers can enhance the absorption of the drug. We aimed to produce nanoparticles containing meloxicam potassium (MEL-P) by spray drying intended for nasal application. Various cyclodextrins (hydroxypropyl-β-cyclodextrin, α-cyclodextrin) and biocompatible polymers (hyaluronic acid, poly(vinylalcohol)) were used as excipients to increase the permeation of the drug and to prepare mucoadhesive products. Physico-chemical, in vitro and ex vivo biopharmaceutical characterization of the formulations were performed. As a result of spray drying, mucoadhesive nanospheres (average particle size <1 µm) were prepared which contained amorphous MEL-P. Cyclodextrin-MEL-P complexes were formed and the applied excipients increased the in vitro and ex vivo permeability of MEL-P. The highest amount of MEL-P permeated from the α-cyclodextrin-based poly(vinylalcohol)-containing samples in vitro (209 μg/cm<sup>2</sup>) and ex vivo (1.47 μg/mm<sup>2</sup>) as well. After further optimization, the resulting formulations may be promising for eliciting a rapid analgesic effect through the nasal route.Patrícia VargaRita AmbrusPiroska Szabó-RévészDávid KókaiKatalin BuriánZsolt BellaFerenc FenyvesiCsilla BartosMDPI AGarticlealpha-cyclodextrinhydroxypropyl-β-cyclodextrinmeloxicam potassiumnano spray dryingnasal drug deliveryPharmacy and materia medicaRS1-441ENPharmaceutics, Vol 13, Iss 1883, p 1883 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	alpha-cyclodextrin hydroxypropyl-β-cyclodextrin meloxicam potassium nano spray drying nasal drug delivery Pharmacy and materia medica RS1-441
spellingShingle	alpha-cyclodextrin hydroxypropyl-β-cyclodextrin meloxicam potassium nano spray drying nasal drug delivery Pharmacy and materia medica RS1-441 Patrícia Varga Rita Ambrus Piroska Szabó-Révész Dávid Kókai Katalin Burián Zsolt Bella Ferenc Fenyvesi Csilla Bartos Physico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres
description	Nasal drug delivery has many beneficial properties, such as avoiding the first pass metabolism and rapid onset of action. However, the limited residence time on the mucosa and limited absorption of certain molecules make the use of various excipients necessary to achieve high bioavailability. The application of mucoadhesive polymers can increase the contact time with the nasal mucosa, and permeation enhancers can enhance the absorption of the drug. We aimed to produce nanoparticles containing meloxicam potassium (MEL-P) by spray drying intended for nasal application. Various cyclodextrins (hydroxypropyl-β-cyclodextrin, α-cyclodextrin) and biocompatible polymers (hyaluronic acid, poly(vinylalcohol)) were used as excipients to increase the permeation of the drug and to prepare mucoadhesive products. Physico-chemical, in vitro and ex vivo biopharmaceutical characterization of the formulations were performed. As a result of spray drying, mucoadhesive nanospheres (average particle size <1 µm) were prepared which contained amorphous MEL-P. Cyclodextrin-MEL-P complexes were formed and the applied excipients increased the in vitro and ex vivo permeability of MEL-P. The highest amount of MEL-P permeated from the α-cyclodextrin-based poly(vinylalcohol)-containing samples in vitro (209 μg/cm<sup>2</sup>) and ex vivo (1.47 μg/mm<sup>2</sup>) as well. After further optimization, the resulting formulations may be promising for eliciting a rapid analgesic effect through the nasal route.
format	article
author	Patrícia Varga Rita Ambrus Piroska Szabó-Révész Dávid Kókai Katalin Burián Zsolt Bella Ferenc Fenyvesi Csilla Bartos
author_facet	Patrícia Varga Rita Ambrus Piroska Szabó-Révész Dávid Kókai Katalin Burián Zsolt Bella Ferenc Fenyvesi Csilla Bartos
author_sort	Patrícia Varga
title	Physico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres
title_short	Physico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres
title_full	Physico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres
title_fullStr	Physico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres
title_full_unstemmed	Physico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres
title_sort	physico-chemical, in vitro and ex vivo characterization of meloxicam potassium-cyclodextrin nanospheres
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/a636b8b967564a81af59f22f546de9bf
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Physico-Chemical, In Vitro and Ex Vivo Characterization of Meloxicam Potassium-Cyclodextrin Nanospheres

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