Intranasal Zolmitriptan-Loaded Bilosomes with Extended Nasal Mucociliary Transit Time for Direct Nose to Brain Delivery

This study aimed at delivering intranasal zolmitriptan directly to the brain through preparation of bilosomes incorporated into a mucoadhesive in situ gel with extended nasal mucociliary transit time. Zolmitriptan-loaded bilosomes were constructed through a thin film hydration method applying Box–Be...

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Autores principales:	Mai M. El Taweel, Mona H. Aboul-Einien, Mohammed A. Kassem, Nermeen A. Elkasabgy
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	zolmitriptan intranasal bilosomes sodium deoxycholate mucoadhesive gel brain targeting Pharmacy and materia medica RS1-441
Acceso en línea:	https://doaj.org/article/7e513cabd195458a9dad2f155cc647cc
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spelling	oai:doaj.org-article:7e513cabd195458a9dad2f155cc647cc2021-11-25T18:40:58ZIntranasal Zolmitriptan-Loaded Bilosomes with Extended Nasal Mucociliary Transit Time for Direct Nose to Brain Delivery10.3390/pharmaceutics131118281999-4923https://doaj.org/article/7e513cabd195458a9dad2f155cc647cc2021-11-01T00:00:00Zhttps://www.mdpi.com/1999-4923/13/11/1828https://doaj.org/toc/1999-4923This study aimed at delivering intranasal zolmitriptan directly to the brain through preparation of bilosomes incorporated into a mucoadhesive in situ gel with extended nasal mucociliary transit time. Zolmitriptan-loaded bilosomes were constructed through a thin film hydration method applying Box–Behnken design. The independent variables were amount of sodium deoxycholate and the amount and molar ratio of cholesterol/Span<sup>®</sup> 40 mixture. Bilosomes were assessed for their entrapment efficiency, particle size and in vitro release. The optimal bilosomes were loaded into mucoadhesive in situ gel consisting of poloxamer 407 and hydroxypropyl methylcellulose. The systemic and brain kinetics of Zolmitriptan were evaluated in rats by comparing intranasal administration of prepared gel to an IV solution. Statistical analysis suggested an optimized bilosomal formulation composition of sodium deoxycholate (5 mg) with an amount and molar ratio of cholesterol/Span<sup>®</sup> 40 mixture of 255 mg and 1:7.7, respectively. The mucoadhesive in situ gel containing bilosomal formulation had a sol-gel temperature of 34.03 °C and an extended mucociliary transit time of 22.36 min. The gelling system possessed enhanced brain bioavailability compared to bilosomal dispersion (1176.98 vs. 835.77%, respectively) following intranasal administration. The gel revealed successful brain targeting with improved drug targeting efficiency and direct transport percentage indices. The intranasal delivery of mucoadhesive in situ gel containing zolmitriptan-loaded bilosomes offered direct nose-to-brain drug targeting with enhanced brain bioavailability.Mai M. El TaweelMona H. Aboul-EinienMohammed A. KassemNermeen A. ElkasabgyMDPI AGarticlezolmitriptanintranasalbilosomessodium deoxycholatemucoadhesive gelbrain targetingPharmacy and materia medicaRS1-441ENPharmaceutics, Vol 13, Iss 1828, p 1828 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	zolmitriptan intranasal bilosomes sodium deoxycholate mucoadhesive gel brain targeting Pharmacy and materia medica RS1-441
spellingShingle	zolmitriptan intranasal bilosomes sodium deoxycholate mucoadhesive gel brain targeting Pharmacy and materia medica RS1-441 Mai M. El Taweel Mona H. Aboul-Einien Mohammed A. Kassem Nermeen A. Elkasabgy Intranasal Zolmitriptan-Loaded Bilosomes with Extended Nasal Mucociliary Transit Time for Direct Nose to Brain Delivery
description	This study aimed at delivering intranasal zolmitriptan directly to the brain through preparation of bilosomes incorporated into a mucoadhesive in situ gel with extended nasal mucociliary transit time. Zolmitriptan-loaded bilosomes were constructed through a thin film hydration method applying Box–Behnken design. The independent variables were amount of sodium deoxycholate and the amount and molar ratio of cholesterol/Span<sup>®</sup> 40 mixture. Bilosomes were assessed for their entrapment efficiency, particle size and in vitro release. The optimal bilosomes were loaded into mucoadhesive in situ gel consisting of poloxamer 407 and hydroxypropyl methylcellulose. The systemic and brain kinetics of Zolmitriptan were evaluated in rats by comparing intranasal administration of prepared gel to an IV solution. Statistical analysis suggested an optimized bilosomal formulation composition of sodium deoxycholate (5 mg) with an amount and molar ratio of cholesterol/Span<sup>®</sup> 40 mixture of 255 mg and 1:7.7, respectively. The mucoadhesive in situ gel containing bilosomal formulation had a sol-gel temperature of 34.03 °C and an extended mucociliary transit time of 22.36 min. The gelling system possessed enhanced brain bioavailability compared to bilosomal dispersion (1176.98 vs. 835.77%, respectively) following intranasal administration. The gel revealed successful brain targeting with improved drug targeting efficiency and direct transport percentage indices. The intranasal delivery of mucoadhesive in situ gel containing zolmitriptan-loaded bilosomes offered direct nose-to-brain drug targeting with enhanced brain bioavailability.
format	article
author	Mai M. El Taweel Mona H. Aboul-Einien Mohammed A. Kassem Nermeen A. Elkasabgy
author_facet	Mai M. El Taweel Mona H. Aboul-Einien Mohammed A. Kassem Nermeen A. Elkasabgy
author_sort	Mai M. El Taweel
title	Intranasal Zolmitriptan-Loaded Bilosomes with Extended Nasal Mucociliary Transit Time for Direct Nose to Brain Delivery
title_short	Intranasal Zolmitriptan-Loaded Bilosomes with Extended Nasal Mucociliary Transit Time for Direct Nose to Brain Delivery
title_full	Intranasal Zolmitriptan-Loaded Bilosomes with Extended Nasal Mucociliary Transit Time for Direct Nose to Brain Delivery
title_fullStr	Intranasal Zolmitriptan-Loaded Bilosomes with Extended Nasal Mucociliary Transit Time for Direct Nose to Brain Delivery
title_full_unstemmed	Intranasal Zolmitriptan-Loaded Bilosomes with Extended Nasal Mucociliary Transit Time for Direct Nose to Brain Delivery
title_sort	intranasal zolmitriptan-loaded bilosomes with extended nasal mucociliary transit time for direct nose to brain delivery
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/7e513cabd195458a9dad2f155cc647cc
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Intranasal Zolmitriptan-Loaded Bilosomes with Extended Nasal Mucociliary Transit Time for Direct Nose to Brain Delivery

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