Tadalafil-Loaded Limonene-Based Orodispersible Tablets: Formulation, in vitro Characterization and in vivo Appraisal of Gastroprotective Activity

Mohammed M Mehanna,1,2 Amina Tarek Mneimneh,2 Souraya Domiati,3 Ahmed N Allam4 1Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; 2Department of Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, Beirut, Lebanon; 3Department of Pha...

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Autores principales: Mehanna MM, Mneimneh AT, Domiati S, Allam AN
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Publicado: Dove Medical Press 2020
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spelling oai:doaj.org-article:922ebb991d1e434cacf2454d06eafa1c2021-12-02T10:39:29ZTadalafil-Loaded Limonene-Based Orodispersible Tablets: Formulation, in vitro Characterization and in vivo Appraisal of Gastroprotective Activity1178-2013https://doaj.org/article/922ebb991d1e434cacf2454d06eafa1c2020-12-01T00:00:00Zhttps://www.dovepress.com/tadalafil-loaded-limonene-based-orodispersible-tablets-formulation-in--peer-reviewed-article-IJNhttps://doaj.org/toc/1178-2013Mohammed M Mehanna,1,2 Amina Tarek Mneimneh,2 Souraya Domiati,3 Ahmed N Allam4 1Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; 2Department of Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, Beirut, Lebanon; 3Department of Pharmacology and Therapeutics, Faculty of Pharmacy, Beirut Arab University, Beirut, Lebanon; 4Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, EgyptCorrespondence: Mohammed M MehannaDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, Beirut, LebanonTel +961 71708661Email mmhanna@bau.edu.lbBackground: Gastric ulcer is a prevalent disease with various etiologies, including non-steroidal anti-inflammatory drugs and alcohol consumption. This study aimed to explore the dual gastric protection effect of tadalafil and limonene as a self-nanoemulsifying system (SNES)-based orodispersible tablets.Methods: Tadalafil-loaded limonene-based SNES was prepared, and the optimum formula was characterized in terms of particle size (PS), polydispersity index (PDI), and zeta potential (ZP) then loaded on various porous carriers to formulate lyophilized orodispersible tablets (ODTs). The ODTs were evaluated via determining hardness, friability, content uniformity, wetting, and disintegration time. The selected ODT was examined for its gastric ulcer protective effect against alcohol-induced ulcers in rat model. Ulcer score and ulcer index were computed for rats stomachs that were inspected macroscopically and histopathologically.Results: The prepared SNES had droplet size of 104 nm, polydispersity index of 0.2, and zeta potential of − 15.4 mV. From the different ODTs formulated, the formula with superior wetting time: 23.67 s, outstanding disintegration time: 28 s, accepted hardness value: 3.11 kg/cm2 and friability: 0.6% was designated. A significant gastroprotective effect of the unloaded and tadalafil-loaded ODTs was recognized compared to the omeprazole pre-treated group. Moreover, the histopathological analysis displayed very mild inflammation in the limonene-based ODTs group and intact structure in the tadalafil-loaded pre-treated animals.Conclusion: Limonene gastroprotective effect functioned along with tadalafil in the form of SNES-incorporated ODTs could serve as a promising revenue for better efficacy in gastric ulcer prevention.Keywords: gastric ulcer, gastroprotection, limonene, orodispersible tablets, self-nanoemulsifying system, tadalafilMehanna MMMneimneh ATDomiati SAllam ANDove Medical Pressarticlegastric ulcergastroprotectionlimoneneorodispersible tabletsself-nanoemulsifying systemtadalafilMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol Volume 15, Pp 10099-10112 (2020)
institution DOAJ
collection DOAJ
language EN
topic gastric ulcer
gastroprotection
limonene
orodispersible tablets
self-nanoemulsifying system
tadalafil
Medicine (General)
R5-920
spellingShingle gastric ulcer
gastroprotection
limonene
orodispersible tablets
self-nanoemulsifying system
tadalafil
Medicine (General)
R5-920
Mehanna MM
Mneimneh AT
Domiati S
Allam AN
Tadalafil-Loaded Limonene-Based Orodispersible Tablets: Formulation, in vitro Characterization and in vivo Appraisal of Gastroprotective Activity
description Mohammed M Mehanna,1,2 Amina Tarek Mneimneh,2 Souraya Domiati,3 Ahmed N Allam4 1Department of Industrial Pharmacy, Faculty of Pharmacy, Alexandria University, Alexandria, Egypt; 2Department of Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, Beirut, Lebanon; 3Department of Pharmacology and Therapeutics, Faculty of Pharmacy, Beirut Arab University, Beirut, Lebanon; 4Department of Pharmaceutics, Faculty of Pharmacy, Alexandria University, Alexandria, EgyptCorrespondence: Mohammed M MehannaDepartment of Pharmaceutical Technology, Faculty of Pharmacy, Beirut Arab University, Beirut, LebanonTel +961 71708661Email mmhanna@bau.edu.lbBackground: Gastric ulcer is a prevalent disease with various etiologies, including non-steroidal anti-inflammatory drugs and alcohol consumption. This study aimed to explore the dual gastric protection effect of tadalafil and limonene as a self-nanoemulsifying system (SNES)-based orodispersible tablets.Methods: Tadalafil-loaded limonene-based SNES was prepared, and the optimum formula was characterized in terms of particle size (PS), polydispersity index (PDI), and zeta potential (ZP) then loaded on various porous carriers to formulate lyophilized orodispersible tablets (ODTs). The ODTs were evaluated via determining hardness, friability, content uniformity, wetting, and disintegration time. The selected ODT was examined for its gastric ulcer protective effect against alcohol-induced ulcers in rat model. Ulcer score and ulcer index were computed for rats stomachs that were inspected macroscopically and histopathologically.Results: The prepared SNES had droplet size of 104 nm, polydispersity index of 0.2, and zeta potential of − 15.4 mV. From the different ODTs formulated, the formula with superior wetting time: 23.67 s, outstanding disintegration time: 28 s, accepted hardness value: 3.11 kg/cm2 and friability: 0.6% was designated. A significant gastroprotective effect of the unloaded and tadalafil-loaded ODTs was recognized compared to the omeprazole pre-treated group. Moreover, the histopathological analysis displayed very mild inflammation in the limonene-based ODTs group and intact structure in the tadalafil-loaded pre-treated animals.Conclusion: Limonene gastroprotective effect functioned along with tadalafil in the form of SNES-incorporated ODTs could serve as a promising revenue for better efficacy in gastric ulcer prevention.Keywords: gastric ulcer, gastroprotection, limonene, orodispersible tablets, self-nanoemulsifying system, tadalafil
format article
author Mehanna MM
Mneimneh AT
Domiati S
Allam AN
author_facet Mehanna MM
Mneimneh AT
Domiati S
Allam AN
author_sort Mehanna MM
title Tadalafil-Loaded Limonene-Based Orodispersible Tablets: Formulation, in vitro Characterization and in vivo Appraisal of Gastroprotective Activity
title_short Tadalafil-Loaded Limonene-Based Orodispersible Tablets: Formulation, in vitro Characterization and in vivo Appraisal of Gastroprotective Activity
title_full Tadalafil-Loaded Limonene-Based Orodispersible Tablets: Formulation, in vitro Characterization and in vivo Appraisal of Gastroprotective Activity
title_fullStr Tadalafil-Loaded Limonene-Based Orodispersible Tablets: Formulation, in vitro Characterization and in vivo Appraisal of Gastroprotective Activity
title_full_unstemmed Tadalafil-Loaded Limonene-Based Orodispersible Tablets: Formulation, in vitro Characterization and in vivo Appraisal of Gastroprotective Activity
title_sort tadalafil-loaded limonene-based orodispersible tablets: formulation, in vitro characterization and in vivo appraisal of gastroprotective activity
publisher Dove Medical Press
publishDate 2020
url https://doaj.org/article/922ebb991d1e434cacf2454d06eafa1c
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AT mneimnehat tadalafilloadedlimonenebasedorodispersibletabletsformulationinvitrocharacterizationandinvivoappraisalofgastroprotectiveactivity
AT domiatis tadalafilloadedlimonenebasedorodispersibletabletsformulationinvitrocharacterizationandinvivoappraisalofgastroprotectiveactivity
AT allaman tadalafilloadedlimonenebasedorodispersibletabletsformulationinvitrocharacterizationandinvivoappraisalofgastroprotectiveactivity
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