Formulation, Optimization and Evaluation of Dexrabeprazole Mucoadhesive Buccal Patch to Overcome First-Pass Metabolism

Abstract

Objectives: The study aimed to develop, optimize, and evaluate dexrabeprazole buccal patches to overcome limitations of conventional oral administration by enhancing bioavailability and providing sustained drug release.

Methods: Dexrabeprazole buccal patches were formulated using Hydroxypropyl Methylcellulose (HPMC K4M) and Carbopol 934P as polymers. A 3² factorial design was employed to optimize key formulation variables. Preformulation compatibility was confirmed by FTIR and DSC. Prepared patches were evaluated for physicochemical properties, mucoadhesion, swelling index, in-vitro drug release, ex-vivo permeation, and stability as per ICH guidelines. Statistical models (ANOVA and polynomial equations) and response surface methodology were applied to identify the optimized batch.

Results: All formulations showed acceptable physicochemical characteristics (thickness 0.22 ± 0.03 mm, surface pH 6.7 ± 0.1, folding endurance >250). Among them, batch F9 emerged as optimized, exhibiting cumulative drug release of 93.5% at 8 h, mucoadhesive strength of 6.1 ± 0.4 N, and swelling index of 58.79 ± 1.5%. Statistical validation revealed close agreement between predicted and experimental values, with relative error <2%. Stability testing confirmed no significant changes over 3 months, with drug content maintained at 98.61% under long-term and 97.92% under accelerated conditions.

Conclusion: The optimized dexrabeprazole buccal patch (F9) demonstrated favorable mechanical strength, sustained release, and stability, highlighting its potential to bypass first-pass metabolism, enhance bioavailability, and reduce dosing frequency in clinical use. Future in vivo studies are warranted to establish pharmacokinetic advantages and therapeutic efficacy for translation into clinical application.