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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| Format: | Article |
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Dove Medical Press
2020-12-01
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| Series: | International Journal of Nanomedicine |
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| Online Access: | https://www.dovepress.com/tadalafil-loaded-limonene-based-orodispersible-tablets-formulation-in--peer-reviewed-article-IJN |
| _version_ | 1818995270610845696 |
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| author | Mehanna MM Mneimneh AT Domiati S Allam AN |
| author_facet | Mehanna MM Mneimneh AT Domiati S Allam AN |
| author_sort | Mehanna MM |
| collection | DOAJ |
| 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 |
| first_indexed | 2024-12-20T21:11:11Z |
| format | Article |
| id | doaj.art-922ebb991d1e434cacf2454d06eafa1c |
| institution | Directory Open Access Journal |
| issn | 1178-2013 |
| language | English |
| last_indexed | 2024-12-20T21:11:11Z |
| publishDate | 2020-12-01 |
| publisher | Dove Medical Press |
| record_format | Article |
| series | International Journal of Nanomedicine |
| spelling | doaj.art-922ebb991d1e434cacf2454d06eafa1c2022-12-21T19:26:31ZengDove Medical PressInternational Journal of Nanomedicine1178-20132020-12-01Volume 15100991011260248Tadalafil-Loaded Limonene-Based Orodispersible Tablets: Formulation, in vitro Characterization and in vivo Appraisal of Gastroprotective ActivityMehanna MMMneimneh ATDomiati SAllam ANMohammed 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, tadalafilhttps://www.dovepress.com/tadalafil-loaded-limonene-based-orodispersible-tablets-formulation-in--peer-reviewed-article-IJNgastric ulcergastroprotectionlimoneneorodispersible tabletsself-nanoemulsifying systemtadalafil |
| spellingShingle | 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 International Journal of Nanomedicine gastric ulcer gastroprotection limonene orodispersible tablets self-nanoemulsifying system tadalafil |
| title | 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_short | 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 |
| topic | gastric ulcer gastroprotection limonene orodispersible tablets self-nanoemulsifying system tadalafil |
| url | https://www.dovepress.com/tadalafil-loaded-limonene-based-orodispersible-tablets-formulation-in--peer-reviewed-article-IJN |
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