Tripling the Bioavailability of Rosuvastatin Calcium Through Development and Optimization of an In-Situ Forming Nanovesicular System
In situ forming nanovesicular systems (IFNs) were prepared and optimized to improve Rosuvastatin calcium (RC) oral bioavailability through increasing its solubility and dissolution rate. The IFN was composed of Tween<sup>®</sup> 80 (T80), cetyl alcohol (CA), in addition to manni...
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| Format: | Article |
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MDPI AG
2019-06-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/11/6/275 |
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| author | Ibrahim Elsayed Rania Moataz El-Dahmy Ahmed Hassen Elshafeey Nabaweya Abdelaziz Abd El Gawad Omaima Naim El Gazayerly |
| author_facet | Ibrahim Elsayed Rania Moataz El-Dahmy Ahmed Hassen Elshafeey Nabaweya Abdelaziz Abd El Gawad Omaima Naim El Gazayerly |
| author_sort | Ibrahim Elsayed |
| collection | DOAJ |
| description | In situ forming nanovesicular systems (IFNs) were prepared and optimized to improve Rosuvastatin calcium (RC) oral bioavailability through increasing its solubility and dissolution rate. The IFN was composed of Tween<sup>®</sup> 80 (T80), cetyl alcohol (CA), in addition to mannitol or Aerosil 200. A single simple step was adopted for preparation, then the prepared formulations were investigated by analyzing their particle size (PS), polydispersity index (PDI), Zeta potential (ZP), entrapment efficiency (EE), and flowability properties. D-optimal design was applied to choose the optimized formulations. The maximum desirability values were 0.754 and 0.478 for the optimized formulations containing 0.05 g CA, 0.18 g T80, and 0.5 g mannitol (OFM) or Aerosil (OFA), respectively. In vitro drug release from the optimized formulations showed a significantly faster dissolution rate when compared to the market product. In vivo performance of the optimized formulations in rabbits was investigated after filling them into enteric-coated capsules. Ultimately, OFA formulation achieved a 3 times increase in RC oral bioavailability in comparison with the market product, supporting the hypothesis of considering IFNs as promising nanocarriers able to boost the bioavailability of BCS class II drugs. |
| first_indexed | 2024-04-14T03:30:21Z |
| format | Article |
| id | doaj.art-a5aee300bcb64397aeed966a0de42198 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-04-14T03:30:21Z |
| publishDate | 2019-06-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-a5aee300bcb64397aeed966a0de421982022-12-22T02:15:00ZengMDPI AGPharmaceutics1999-49232019-06-0111627510.3390/pharmaceutics11060275pharmaceutics11060275Tripling the Bioavailability of Rosuvastatin Calcium Through Development and Optimization of an In-Situ Forming Nanovesicular SystemIbrahim Elsayed0Rania Moataz El-Dahmy1Ahmed Hassen Elshafeey2Nabaweya Abdelaziz Abd El Gawad3Omaima Naim El Gazayerly4Department of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo 11562, EgyptDepartment of Pharmaceutics, Faculty of Pharmacy, October 6 University, Cairo 12585, EgyptDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo 11562, EgyptDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo 11562, EgyptDepartment of Pharmaceutics and Industrial Pharmacy, Faculty of Pharmacy, Cairo University, Cairo 11562, EgyptIn situ forming nanovesicular systems (IFNs) were prepared and optimized to improve Rosuvastatin calcium (RC) oral bioavailability through increasing its solubility and dissolution rate. The IFN was composed of Tween<sup>®</sup> 80 (T80), cetyl alcohol (CA), in addition to mannitol or Aerosil 200. A single simple step was adopted for preparation, then the prepared formulations were investigated by analyzing their particle size (PS), polydispersity index (PDI), Zeta potential (ZP), entrapment efficiency (EE), and flowability properties. D-optimal design was applied to choose the optimized formulations. The maximum desirability values were 0.754 and 0.478 for the optimized formulations containing 0.05 g CA, 0.18 g T80, and 0.5 g mannitol (OFM) or Aerosil (OFA), respectively. In vitro drug release from the optimized formulations showed a significantly faster dissolution rate when compared to the market product. In vivo performance of the optimized formulations in rabbits was investigated after filling them into enteric-coated capsules. Ultimately, OFA formulation achieved a 3 times increase in RC oral bioavailability in comparison with the market product, supporting the hypothesis of considering IFNs as promising nanocarriers able to boost the bioavailability of BCS class II drugs.https://www.mdpi.com/1999-4923/11/6/275in situRosuvastatin calciumbioavailability enhancementmannitol and Aerosil |
| spellingShingle | Ibrahim Elsayed Rania Moataz El-Dahmy Ahmed Hassen Elshafeey Nabaweya Abdelaziz Abd El Gawad Omaima Naim El Gazayerly Tripling the Bioavailability of Rosuvastatin Calcium Through Development and Optimization of an In-Situ Forming Nanovesicular System Pharmaceutics in situ Rosuvastatin calcium bioavailability enhancement mannitol and Aerosil |
| title | Tripling the Bioavailability of Rosuvastatin Calcium Through Development and Optimization of an In-Situ Forming Nanovesicular System |
| title_full | Tripling the Bioavailability of Rosuvastatin Calcium Through Development and Optimization of an In-Situ Forming Nanovesicular System |
| title_fullStr | Tripling the Bioavailability of Rosuvastatin Calcium Through Development and Optimization of an In-Situ Forming Nanovesicular System |
| title_full_unstemmed | Tripling the Bioavailability of Rosuvastatin Calcium Through Development and Optimization of an In-Situ Forming Nanovesicular System |
| title_short | Tripling the Bioavailability of Rosuvastatin Calcium Through Development and Optimization of an In-Situ Forming Nanovesicular System |
| title_sort | tripling the bioavailability of rosuvastatin calcium through development and optimization of an in situ forming nanovesicular system |
| topic | in situ Rosuvastatin calcium bioavailability enhancement mannitol and Aerosil |
| url | https://www.mdpi.com/1999-4923/11/6/275 |
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