Comparison Between Conventional and Supersaturable Self-nanoemulsion Loaded with Nebivolol: Preparation and In-vitro/Ex-vivo Evaluation
Nebivolol (NBH) is a third-generation B1-blocker with high selectivity and vasodilation activity. Nevertheless, nebivolol exhibits low oral bioavailability, which may adversely affect its efficacy. Recently, supersaturable self-nanoemulsion (Su-SNE) is an advanced SNE approach that can address low...
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| Format: | Article |
| Language: | English |
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College of Pharmacy University of Baghdad
2020-06-01
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| Series: | Iraqi Journal of Pharmaceutical Sciences |
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| Online Access: | https://bijps.uobaghdad.edu.iq/index.php/bijps/article/view/1038 |
| _version_ | 1811265956933009408 |
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| author | Lubna A. Sabri Ahmed A. Hussein |
| author_facet | Lubna A. Sabri Ahmed A. Hussein |
| author_sort | Lubna A. Sabri |
| collection | DOAJ |
| description |
Nebivolol (NBH) is a third-generation B1-blocker with high selectivity and vasodilation activity. Nevertheless, nebivolol exhibits low oral bioavailability, which may adversely affect its efficacy. Recently, supersaturable self-nanoemulsion (Su-SNE) is an advanced SNE approach that can address low bioavailability The study aims to prepare nebivolol-loaded Su-SNE by reduction the amount of the prepared conventional SNE to half. Besides, an appropriate polymer type and concentration to prevent NBH precipitation upon oral administration have investigated.. A conventional self-nanoemulsion (formula A) was prepared by dissolving NBH in 500 mg vehicle mixture of imwitor®988: cremophor-EL: propylene glycol. Then, eight Su-SNE formulas with the absence or presence of four different polymers were prepared and evaluated. In-vitro precipitation assay was performed to assess the precipitation inhibition capacity of polymers. The ex-vivo permeation through rat intestinal mucosa was also conducted for determination of permeability parameters. Results revealed that (Su-SNA formula SAS1) containing 5% soluplus could effectively retard the nebivolol precipitation. There was no statistical difference between formula A and SAS1; both maintained a higher apparent NBH concentration for approximately 240 min in 0.1N HCl. The permeation rate of conventional (formula A) and soluplus-based Su-SNE (formula SAS1) was significantly improved, and the permeation enhancement ratio was found 2.7 and 3.2, respectively, as compared with non-formulated NBH. Consequently, it is concluded that developing soluplus-based nebivolol SNE is a promising alternative approach. It can enhance nebivolol stability and permeability with half the amount of conventional SNE components.
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| first_indexed | 2024-04-12T20:33:19Z |
| format | Article |
| id | doaj.art-f608ac6eacde4ce9a287c1127e2bd0c2 |
| institution | Directory Open Access Journal |
| issn | 2521-3512 1683-3597 |
| language | English |
| last_indexed | 2024-04-12T20:33:19Z |
| publishDate | 2020-06-01 |
| publisher | College of Pharmacy University of Baghdad |
| record_format | Article |
| series | Iraqi Journal of Pharmaceutical Sciences |
| spelling | doaj.art-f608ac6eacde4ce9a287c1127e2bd0c22022-12-22T03:17:40ZengCollege of Pharmacy University of BaghdadIraqi Journal of Pharmaceutical Sciences2521-35121683-35972020-06-0129110.31351/vol29iss1pp216-2251038Comparison Between Conventional and Supersaturable Self-nanoemulsion Loaded with Nebivolol: Preparation and In-vitro/Ex-vivo EvaluationLubna A. Sabri0Ahmed A. HusseinCollege of Pharmacy/University of Baghdad Nebivolol (NBH) is a third-generation B1-blocker with high selectivity and vasodilation activity. Nevertheless, nebivolol exhibits low oral bioavailability, which may adversely affect its efficacy. Recently, supersaturable self-nanoemulsion (Su-SNE) is an advanced SNE approach that can address low bioavailability The study aims to prepare nebivolol-loaded Su-SNE by reduction the amount of the prepared conventional SNE to half. Besides, an appropriate polymer type and concentration to prevent NBH precipitation upon oral administration have investigated.. A conventional self-nanoemulsion (formula A) was prepared by dissolving NBH in 500 mg vehicle mixture of imwitor®988: cremophor-EL: propylene glycol. Then, eight Su-SNE formulas with the absence or presence of four different polymers were prepared and evaluated. In-vitro precipitation assay was performed to assess the precipitation inhibition capacity of polymers. The ex-vivo permeation through rat intestinal mucosa was also conducted for determination of permeability parameters. Results revealed that (Su-SNA formula SAS1) containing 5% soluplus could effectively retard the nebivolol precipitation. There was no statistical difference between formula A and SAS1; both maintained a higher apparent NBH concentration for approximately 240 min in 0.1N HCl. The permeation rate of conventional (formula A) and soluplus-based Su-SNE (formula SAS1) was significantly improved, and the permeation enhancement ratio was found 2.7 and 3.2, respectively, as compared with non-formulated NBH. Consequently, it is concluded that developing soluplus-based nebivolol SNE is a promising alternative approach. It can enhance nebivolol stability and permeability with half the amount of conventional SNE components. https://bijps.uobaghdad.edu.iq/index.php/bijps/article/view/1038imwitor 988; non-sink condition; permeation enhancement; supersaturable self-nanoemulsion; soluplus. |
| spellingShingle | Lubna A. Sabri Ahmed A. Hussein Comparison Between Conventional and Supersaturable Self-nanoemulsion Loaded with Nebivolol: Preparation and In-vitro/Ex-vivo Evaluation Iraqi Journal of Pharmaceutical Sciences imwitor 988; non-sink condition; permeation enhancement; supersaturable self-nanoemulsion; soluplus. |
| title | Comparison Between Conventional and Supersaturable Self-nanoemulsion Loaded with Nebivolol: Preparation and In-vitro/Ex-vivo Evaluation |
| title_full | Comparison Between Conventional and Supersaturable Self-nanoemulsion Loaded with Nebivolol: Preparation and In-vitro/Ex-vivo Evaluation |
| title_fullStr | Comparison Between Conventional and Supersaturable Self-nanoemulsion Loaded with Nebivolol: Preparation and In-vitro/Ex-vivo Evaluation |
| title_full_unstemmed | Comparison Between Conventional and Supersaturable Self-nanoemulsion Loaded with Nebivolol: Preparation and In-vitro/Ex-vivo Evaluation |
| title_short | Comparison Between Conventional and Supersaturable Self-nanoemulsion Loaded with Nebivolol: Preparation and In-vitro/Ex-vivo Evaluation |
| title_sort | comparison between conventional and supersaturable self nanoemulsion loaded with nebivolol preparation and in vitro ex vivo evaluation |
| topic | imwitor 988; non-sink condition; permeation enhancement; supersaturable self-nanoemulsion; soluplus. |
| url | https://bijps.uobaghdad.edu.iq/index.php/bijps/article/view/1038 |
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