Development and Evaluation of Transdermal Patches of Azelnidipine

Objective: Azelnidipine, a long-acting dihydropyridine based calcium channel blocker, on oral administration, the drug undergoes extensive first pass metabolism. Delivery of azelnidipine (AZP) via transdermal route would minimize some of the deficiencies associated with the oral delivery and increase the bioavailability of the drug. In the present study, is to investigate the development and evaluation transdermal patches of azelnidipine for controlled release medication and to increase bioavailability by avoiding hepatic first-pass metabolism and degradation of drug in GIT fluids. Methods: The drug and excipients compatibility studied by FTIR. The transdermal patches were prepared by solvent casting method using different amounts and combination of hydroxyl propyl methyl cellulose (HPMC E15), Eudragit RL100 (ERL) and Eudragit RS100 (ERS). Ex-vivo skin permeation studies were performed on rat abdominal skin using Franz diffusion cell. Diffused drug was quantified by Uv-Spectrophotometer at 281nm. Results: The patches were found to be smooth in appearance, uniform in thickness, The Formulations were shown subjected to physicochemical studies such as drug content, weight variation, thickness, moisture absorption, moisture loss, water vapor transmission rate (WVTR) and folding endurance. Conclusions: Azelnidipine is a new DHP basis calcium channel blocker; transdermal route is very safe and convenient for patients who are unable to take oral administration of tablet. And its combination of HPMC, Eudragit RL100 and RS 100 shown better compatibility and controlled release for 24hrs.