Development of Mucoadhesive Buccal Film for Rizatriptan: In Vitro and In Vivo Evaluation
The reduced therapeutic efficacy of rizatriptan in migraine treatment is primarily due to low oral bioavailability and extensive first pass metabolism. The purpose of this investigation was to optimize the thin mucoadhesive buccal film of rizatriptan and assess the practicability of its development...
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| Format: | Article |
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MDPI AG
2021-05-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/5/728 |
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| author | Anroop B. Nair Jigar Shah Shery Jacob Bandar E. Al-Dhubiab Vimal Patel Nagaraja Sreeharsha Pottathil Shinu |
| author_facet | Anroop B. Nair Jigar Shah Shery Jacob Bandar E. Al-Dhubiab Vimal Patel Nagaraja Sreeharsha Pottathil Shinu |
| author_sort | Anroop B. Nair |
| collection | DOAJ |
| description | The reduced therapeutic efficacy of rizatriptan in migraine treatment is primarily due to low oral bioavailability and extensive first pass metabolism. The purpose of this investigation was to optimize the thin mucoadhesive buccal film of rizatriptan and assess the practicability of its development as a potential substitute for conventional migraine treatment. Buccal films (FR1–FR10) were fabricated by a conventional solvent casting method utilizing a combination of polymers (Proloc, hydroxypropyl methylcellulose and Eudragit RS 100). Drug-loaded buccal films (F1–F4) were examined for mechanical, mucoadhesive, swelling and release characteristics. In vivo pharmacokinetics parameters of selected buccal film (F1) in rabbits were compared to oral administration. Films F1–F4 displayed optimal physicomechanical properties including mucoadhesive strength, which can prolong the buccal residence time. A biphasic, complete and higher drug release was seen in films F1 and F4, which followed Weibull model kinetics. The optimized film, F1, exhibited significantly higher (<i>p</i> < 0.005) rizatriptan buccal flux (71.94 ± 8.26 µg/cm<sup>2</sup>/h) with a short lag time. Film features suggested the drug particles were in an amorphous form, compatible with the polymers used and had an appropriate surface morphology suitable for buccal application. Pharmacokinetic data indicated a significantly higher rizatriptan plasma level (<i>p</i> < 0.005) and C<sub>max</sub> (<i>p</i> < 0.0001) upon buccal film application as compared to oral solution. The observed AUC<sub>0–12h</sub> (994.86 ± 95.79 ng.h/mL) in buccal treatment was two-fold higher (<i>p</i> < 0.0001) than the control, and the relative bioavailability judged was 245%. This investigation demonstrates the prospective of buccal films as a viable and alternative approach for effective rizatriptan delivery. |
| first_indexed | 2024-03-10T11:22:53Z |
| format | Article |
| id | doaj.art-61e7a4be3e5d4932a24fe90ac3620d86 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T11:22:53Z |
| publishDate | 2021-05-01 |
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| series | Pharmaceutics |
| spelling | doaj.art-61e7a4be3e5d4932a24fe90ac3620d862023-11-21T19:52:11ZengMDPI AGPharmaceutics1999-49232021-05-0113572810.3390/pharmaceutics13050728Development of Mucoadhesive Buccal Film for Rizatriptan: In Vitro and In Vivo EvaluationAnroop B. Nair0Jigar Shah1Shery Jacob2Bandar E. Al-Dhubiab3Vimal Patel4Nagaraja Sreeharsha5Pottathil Shinu6Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi ArabiaDepartment of Pharmaceutics, Institute of Pharmacy, Nirma University, Ahmedabad 382481, IndiaDepartment of Pharmaceutical Sciences, College of Pharmacy, Gulf Medical University, Ajman 4184, United Arab EmiratesDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi ArabiaDepartment of Pharmaceutics, Institute of Pharmacy, Nirma University, Ahmedabad 382481, IndiaDepartment of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi ArabiaDepartment of Biomedical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Ahsa 31982, Saudi ArabiaThe reduced therapeutic efficacy of rizatriptan in migraine treatment is primarily due to low oral bioavailability and extensive first pass metabolism. The purpose of this investigation was to optimize the thin mucoadhesive buccal film of rizatriptan and assess the practicability of its development as a potential substitute for conventional migraine treatment. Buccal films (FR1–FR10) were fabricated by a conventional solvent casting method utilizing a combination of polymers (Proloc, hydroxypropyl methylcellulose and Eudragit RS 100). Drug-loaded buccal films (F1–F4) were examined for mechanical, mucoadhesive, swelling and release characteristics. In vivo pharmacokinetics parameters of selected buccal film (F1) in rabbits were compared to oral administration. Films F1–F4 displayed optimal physicomechanical properties including mucoadhesive strength, which can prolong the buccal residence time. A biphasic, complete and higher drug release was seen in films F1 and F4, which followed Weibull model kinetics. The optimized film, F1, exhibited significantly higher (<i>p</i> < 0.005) rizatriptan buccal flux (71.94 ± 8.26 µg/cm<sup>2</sup>/h) with a short lag time. Film features suggested the drug particles were in an amorphous form, compatible with the polymers used and had an appropriate surface morphology suitable for buccal application. Pharmacokinetic data indicated a significantly higher rizatriptan plasma level (<i>p</i> < 0.005) and C<sub>max</sub> (<i>p</i> < 0.0001) upon buccal film application as compared to oral solution. The observed AUC<sub>0–12h</sub> (994.86 ± 95.79 ng.h/mL) in buccal treatment was two-fold higher (<i>p</i> < 0.0001) than the control, and the relative bioavailability judged was 245%. This investigation demonstrates the prospective of buccal films as a viable and alternative approach for effective rizatriptan delivery.https://www.mdpi.com/1999-4923/13/5/728migraineProlocEudragitphysicomechanicalreleasein vivo |
| spellingShingle | Anroop B. Nair Jigar Shah Shery Jacob Bandar E. Al-Dhubiab Vimal Patel Nagaraja Sreeharsha Pottathil Shinu Development of Mucoadhesive Buccal Film for Rizatriptan: In Vitro and In Vivo Evaluation Pharmaceutics migraine Proloc Eudragit physicomechanical release in vivo |
| title | Development of Mucoadhesive Buccal Film for Rizatriptan: In Vitro and In Vivo Evaluation |
| title_full | Development of Mucoadhesive Buccal Film for Rizatriptan: In Vitro and In Vivo Evaluation |
| title_fullStr | Development of Mucoadhesive Buccal Film for Rizatriptan: In Vitro and In Vivo Evaluation |
| title_full_unstemmed | Development of Mucoadhesive Buccal Film for Rizatriptan: In Vitro and In Vivo Evaluation |
| title_short | Development of Mucoadhesive Buccal Film for Rizatriptan: In Vitro and In Vivo Evaluation |
| title_sort | development of mucoadhesive buccal film for rizatriptan in vitro and in vivo evaluation |
| topic | migraine Proloc Eudragit physicomechanical release in vivo |
| url | https://www.mdpi.com/1999-4923/13/5/728 |
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