Systemic delivery of β-blockers via transdermal route for hypertension

Abstract

Hypertension is the most common cardiovascular disease worldwide. Moreover, management of hypertension requires long-term treatment that may result in poor patient compliance with conventional dosage forms due to greater frequency of drug administration. Although there is availability of a plethora of therapeutically effective antihypertensive molecules, inadequate patient welfare is observed; this arguably presents an opportunity to deliver antihypertensive agents through a different route. Ever since the transdermal drug delivery came into existence, it has offered great advantages including non-invasiveness, prolonged therapeutic effect, reduced side effects, improved bioavailability, better patient compliance and easy termination of drug therapy. Attempts were made to develop the transdermal therapeutic system for various antihypertensive agents, including β-blockers, an important antihypertensive class. β-blockers are potent, highly effective in the management of hypertension and other heart ailments by blocking the effects of normal amounts of adrenaline in the heart and blood vessels. The shortcomings associated with β-blockers such as more frequent dose administration, extensive first pass metabolism and variable bioavailability, make them an ideal candidate for transdermal therapeutic systems. The present article gives a brief view of different β-blockers formulated as transdermal therapeutic system in detail to enhance the bioavailability as well as to improve patient compliance. Constant improvement in this field holds promise for the long-term success in technologically advanced transdermal dosage forms being commercialized sooner rather than later.

Terminalia Arjuna Transdermal Matrix Formulation Containing Different Polymer Components

“…TMS has been showing an increased interest than other delivery methods, one of which is to avoid the metabolism of the first pass effect on the liver and able to deliver the drug in a controlled manner directly to the blood vessels. Transdermal administration can give local therapeutic effect as well as a systemic effect [1][2][3]. TMS imparts a leading advantage beyond injectables and oral routes by elevating patient compliance, minimize dosing frequency, painless, and cost effective.…”

Comparative Evaluation of Selected Polymers and Plasticizer on Transdermal Drug Delivery System

“…Major advantages of transdermal drug delivery: the constant level of drug is maintained within the therapeutic window during the whole period of the administration; the pre-systemic first-pass effect can be avoided which can result in higher bioavailability and fewer adverse effects than in the case of oral administration; the drug administration can be stopped instantly in situations where drug input is no longer desirable; it allows a reduced frequency of dosing which is particularly favourable for compounds with short biological half-life [10][11][12][13][14].…”

The formulation of carvedilol transdermal patch with resin gum as rate control

“…However, its bioavailability in humans is merely around 20% because it undergoes the first-pass metabolism that converts it into its inactive form and, thereby, provides no therapeutic effect. Due to the low oral bioavailability, it requires a repeated administration that may reduce medication compliance (Ahad et al, 2015).…”