Development and evaluation of transdermal drug delivery system of metoprolol

Abstract

Metoprolol (MP) is a potent ill-selective adrenergic blocking agent with proven antihypertensive activity. However, it undergoes extensive hepatic first-pass metabolism and has a short biological half-life, which necessitates frequent dosing to attain adequate therapeutic blood levels. To overcome this problem, the feasibility of systemic delivery of MT via the transdermal route was explored. In the present work, efforts have been made to prepare a transdermal drug delivery system of MT using various blends of polymers such as Eudragit RS 100, Hydroxy propyl methyl cellulose and Poly vinyl pyrrolidone using propylene glycol as a permeation enhancer. The prepared patches were evaluated for various physicochemical properties and In-vitro drug release studies. The releases were fitted to statistical treatment such as Zero order kinetics, Higuchi’s and Peppa’s plot. The optimized formulation from the In-vitro drug release study is used to carry out In-vitro skin permeation study using porcine ear skin, snake shed skin and rat skin. The In-vivo evaluation of formulation F 1 (1% Eudragit RS 100, 1.5%HPMC & 0.5% PVP) show better correlation with the In-vitro drug release which confirms the achievement of targets of the present study such as the controlled prolonged zero order release, reduced frequency of administration, greater therapeutic effect, overcome the side effects, simplify the treatment regimen and thus may improve patient compliance.