DESIGN, DEVELOPMENT, AND EVALUATION OF TRANSDERMAL PATCHES CONTAINING MEMANTINE HYDROCHLORIDE

Abstract

Objective: This study aimed to develop an effective transdermal drug delivery system of memantine hydrochloride (MH), an anti-Alzheimer's drug, to improve patient compliance and optimize drug therapy in patients with dementia who often have difficulties adhering to oral medication schedules. Methods: Various transdermal patches of MH were prepared using the box-Behnken design of experiments with different polymer combinations. The fabricated patches were evaluated for properties like thickness, folding endurance, drug content uniformity, in vitro drug release, and diffusion studies. An optimal formulation was selected based on the results and further studied for pharmacokinetic parameters in rabbits. The results were compared to conventional tablets containing the same polymer combination. Results: Formulation B2 containing Hydroxy Propyl Methyl Cellulose (HPMC) 137.5 mg, Ethyl Cellulose (EC) 400 mg, and xanthan gum 300 mg had a flux of 212.24 μg/cm2/h, the permeability of 2.32 cm/h, and 27.95% release at 8h, with first-order and non-Fickian drug release kinetics. It was non-irritating, and in vitro release studies showed sustained release for up to 48 h. In vivo studies in rabbits also indicated superior drug absorption and sustained release from the patches compared to tablets. Conclusion: The optimized transdermal patch formulation had the potential to provide a prolonged release of MH for over 2 d and reduce the frequency of dosing. However, further studies are warranted to confirm the efficacy, safety, and pharmacokinetics of the patches in human models before clinical use.