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      Systemic delivery of β-blockers via transdermal route for hypertension

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          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.

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          Most cited references107

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          Penetration enhancers.

          One long-standing approach for improving transdermal drug delivery uses penetration enhancers (also called sorption promoters or accelerants) which penetrate into skin to reversibly decrease the barrier resistance. Numerous compounds have been evaluated for penetration enhancing activity, including sulphoxides (such as dimethylsulphoxide, DMSO), Azones (e.g. laurocapram), pyrrolidones (for example 2-pyrrolidone, 2P), alcohols and alkanols (ethanol, or decanol), glycols (for example propylene glycol, PG, a common excipient in topically applied dosage forms), surfactants (also common in dosage forms) and terpenes. Many potential sites and modes of action have been identified for skin penetration enhancers; the intercellular lipid matrix in which the accelerants may disrupt the packing motif, the intracellular keratin domains or through increasing drug partitioning into the tissue by acting as a solvent for the permeant within the membrane. Further potential mechanisms of action, for example with the enhancers acting on desmosomal connections between corneocytes or altering metabolic activity within the skin, or exerting an influence on the thermodynamic activity/solubility of the drug in its vehicle are also feasible, and are also considered in this review.
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            Worldwide epidemic of hypertension.

            The World Health Report 2002 identified hypertension, or high blood pressure, as the third ranked factor for disability-adjusted life years. Hypertension is one of the primary risk factors for heart disease and stroke, the leading causes of death worldwide. Recent analyses have shown that as of the year 2000, there were 972 million people living with hypertension worldwide, and it is estimated that this number will escalate to more than 1.56 billion by the year 2025. Nearly two-thirds of hypertensives live in low- and middle-income countries, resulting in a huge economic burden. Awareness, prevention, treatment and control of hypertension is a significant public health measure. The World Hypertension League, through its national member societies, launched World Hypertension Day in 2005 and, due to its success throughout the world, it has been made an annual event. The 2006 World Hypertension Day was held on May 13; the theme of the day was "Treat to Goal", with a clear intent to ensure patient adherence and control of hypertension worldwide. In Canada, all stakeholders--professional societies, government, nongovernment organizations and industry--are working together to promote awareness of hypertension and to control it.
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              Definition and classification of hypertension: an update.

              Since the publication of a paper by the American Society of Hypertension, Inc. Writing Group in 2003, some refinements have occurred in the definition of hypertension. Blood pressure is now recognized as a biomarker for hypertension, and a distinction is made between the various stages of hypertension and global cardiovascular risk. This paper discusses the logic underlying the refinements in the definition of hypertension.
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                Author and article information

                Contributors
                Journal
                Saudi Pharm J
                Saudi Pharm J
                Saudi Pharmaceutical Journal : SPJ
                Elsevier
                1319-0164
                2213-7475
                03 January 2014
                November 2015
                03 January 2014
                : 23
                : 6
                : 587-602
                Affiliations
                [a ]Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia
                [b ]Department of Pharmaceutics, College of Pharmacy, Buraydah Private Colleges, P.O. Box 31, 717, Buraydah, Al-Qassim, Saudi Arabia
                [c ]Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard (Hamdard University), M. B. Road, New Delhi 110062, India
                Author notes
                [* ]Corresponding author. Tel.: +966 557124812. abdulahad20@ 123456yahoo.com aahad@ 123456ksu.edu.sa
                Article
                S1319-0164(13)00146-1
                10.1016/j.jsps.2013.12.019
                4669430
                26702253
                d66141f5-ca8c-4310-9692-fe0b4acc66e2
                © 2013 King Saud University. Production and hosting by Elsevier B.V. All rights reserved.

                This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

                History
                : 19 August 2013
                : 14 December 2013
                Categories
                Review

                antihypertensive agent,β-blockers,transdermal delivery,transdermal therapeutic system

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