Enhanced Bioavailability of Nimodipine from Bioadhesive Buccal Bilayered Patches in Human Volunteers

Abstract

Aims:The objective of the present study was to develop a bioadhesive bilayered buccal patch of Nimodipine (15 mg) using Eudragit Rs 100 as secondary layer and a primary layer with Hydroxy propyl methyl cellulose and Hydroxy propyl cellulose JF. Methodology: Bilayered buccal patches were prepared by solvent casting technique. The absence of physiochemical interactions between NMDP and the polymer were investigated by differential scanning calorimetry (DSC). Bilayered buccal patches of NMDP were evaluated for in vitro drug permeation through porcine buccal membrane, in vitro drug release, moisture absorption, surface pH, mechanical properties and in vitro bioadhesion. Results:The results indicated that suitable bioadhesive bilayered buccal patches with desired permeability could be prepared. The bioavailability study was performed in healthy humans in a crossover experimental design. Bioavailability studies revealed that nimodipine possessed good buccal absorption. The relative bioavailability of the optimized buccal patch was found to be 205% in comparison to 30 mg marketed oral tablet. The formulation CC3 showed 68.84 ± 1.4% release and 46.85 ± 5.1% of drug permeated