Formulation and evaluation of Amlodipine transdermal patch for the treatment of Hypertension and Angina as a transdermal Drug delivery system.

Abstract

Hypertension and angina pectoris are the leading cardiovascular disorders affecting the millions of peoples and it require continuous long-term pharmacological management. Amlodipine is a long-acting calcium channel blocker and it is widely used to treatment of these conditions for its effectiveness in reducing blood pressure and improving coronary blood flow. Oral administration of Amlodipine is associated with first-pass hepatic metabolism, fluctuations in the plasma drug concentration, and need for repeated dosing, which may decrease patient compliance. To overcome these limitations, the present study is used to formulate and evaluate an Amlodipine transdermal patches as a novel drug delivery system. The transdermal patches are prepared by the solvent casting method using suitable film-forming polymers (Chitosan, Sodium alginate, and Ethyl cellulose), plasticisers, and permeation enhancers which is used to obtain the flexible, smooth, and uniform patches capable of delivering the drug at a controlled rate through the skin. The prepared formulation is evaluated for the various physicochemical and mechanical properties, which includes physical appearance, thickness, weight variation, folding endurance, surface pH, moisture content, moisture uptake, tensile strength, percentage elongation, and drug content uniformity, percentage cumulative drug release. The compatibility between the Active pharmaceutical ingredient and the excipients were assessed to ensure the formulation of stability .Therefore In vitro drug release studies and ex vivo drug for skin permeation studies were carried out to evaluate the release profile and the permeation enhance characteristics of the formulated transdermal patches. Stability studies were also performed under the accelerated storage conditions to determine the integrity and the shelf life of the formulations. The results of evaluation indicates the formulated patches exhibits satisfactory mechanical strength, uniform drug distribution, acceptable physicochemical characteristics, and sustained drug releases over an extended period of time. The optimized formulation exhibited effective skin permeation and maintains its stability throughout the study period. The transdermal delivery of Amlodipine has the potential to improve the bioavailability by passing first-pass metabolism, to minimize the dose-related adverse drug effects, reduce dosage frequency, and enhance patient compliance.