Bakr, F., Soliman, M., Elsabbagh, H. (2022). Formulation and In-Vitro, Ex-Vivo, and In-Vivo Evaluation of Mucoadhesive Buccal Tablets Containing Labetalol Hydrochloride for Enhancement of Systemic Bioavailability. Journal of Advanced Pharmacy Research, 6(1), 15-27. doi: 10.21608/aprh.2021.97253.1142
Fatma Bakr; Moetaza Soliman; Hassan Elsabbagh. "Formulation and In-Vitro, Ex-Vivo, and In-Vivo Evaluation of Mucoadhesive Buccal Tablets Containing Labetalol Hydrochloride for Enhancement of Systemic Bioavailability". Journal of Advanced Pharmacy Research, 6, 1, 2022, 15-27. doi: 10.21608/aprh.2021.97253.1142
Bakr, F., Soliman, M., Elsabbagh, H. (2022). 'Formulation and In-Vitro, Ex-Vivo, and In-Vivo Evaluation of Mucoadhesive Buccal Tablets Containing Labetalol Hydrochloride for Enhancement of Systemic Bioavailability', Journal of Advanced Pharmacy Research, 6(1), pp. 15-27. doi: 10.21608/aprh.2021.97253.1142
Bakr, F., Soliman, M., Elsabbagh, H. Formulation and In-Vitro, Ex-Vivo, and In-Vivo Evaluation of Mucoadhesive Buccal Tablets Containing Labetalol Hydrochloride for Enhancement of Systemic Bioavailability. Journal of Advanced Pharmacy Research, 2022; 6(1): 15-27. doi: 10.21608/aprh.2021.97253.1142
Formulation and In-Vitro, Ex-Vivo, and In-Vivo Evaluation of Mucoadhesive Buccal Tablets Containing Labetalol Hydrochloride for Enhancement of Systemic Bioavailability
1Department of Pharmaceutics, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt
2Department of Clinical Pharmacy and Pharmacy Practice, Faculty of Pharmacy, Mansoura University, Mansoura, Egypt
Abstract
Objective: Labetalol hydrochloride is an alpha/beta adrenoceptor blocker that undergoes comprehensive first pass-metabolism resulting in a low oral bioavailability. This study aimed to formulate and evaluate mucoadhesive buccal formulations of labetalol hydrochloride for enhancement of its bioavailability. Methods: Using various concentrations of hydroxypropyl methylcellulose (HPMC), carbopol-934, and sodium alginate, ten formulations of mucoadhesive buccal tablets containing labetalol hydrochloride were prepared. The produced tablets were evaluated to test physical and mucoadhesive properties as well as in-vitro drug release properties. Ex-vivo evaluations of the tablets were examined using chicken pouch membrane. Formulations that offered best results in in-vitro and ex-vivo evaluations were selected for running in-vivo comparative bioavailability study using New Zealand rabbits and adopted HPLC method to assess the buccal bioavailability of labetalol hydrochloride in relation to its oral bioavailability from commercial tablets. Results: It was found that drug release and mucoadhesive properties depended on the type and proportion of different polymers. Sodium alginate-containing formulations showed higher release rates and ex-vivo permeation rates compared to carbopol-containing formulations. Increasing the proportion of HPMC resulted in more swelling, better mucoahesion forces and times but more delayed permeation and release rates. A strong correlation was detected between in-vivo drug release and ex-vivo transmucosal permeation of labetalol hydrochloride. The relative bioavailability of labetalol hydrochloride from the selected mucoadhesive buccal tablets F1 and F6 were 2.76 and 1.60, respectively. Conclusion: The produced mucoadhesive buccal tablets were successful in improving the systemic bioavailability of labetalol hydrochloride in rabbits. Clinical applications of formulations F1 and F6 are recommended.
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