Transdermal delivery of angiotensin II receptor blockers (ARBs), angiotensin-converting enzyme inhibitors (ACEIs) and others for management of hypertension

Abstract

Context: Angiotensin II receptor blockers (ARBs), angiotensin-converting enzyme inhibitors (ACEIs) are some of the most commonly prescribed medications for hypertension. Objective: Most of all conventional dosage forms of ARBs and ACEIs undergo extensive first-pass metabolism, which significantly reduces bioavailability. Majority of ARBs and ACEIs are inherently short acting due to a rapid elimination half-life. In addition, oral dosage forms of ARBs and ACEIs have many high incidences of adverse effects due to variable absorption profiles, higher frequency of administration and poor patient compliance. Methods: Many attempts have been made globally at the laboratory level to investigate the skin permeation and to develop transdermal therapeutic systems of various ARBs, ACEIs and other anti-hypertensives, to circumvent the drawbacks associated with their conventional dosage form. Results: This manuscript presents an outline of the transdermal research specifically in the area of ARBs, ACEIs and other anti-hypertensives reported in various pharmaceutical journals. Conclusion: The transdermal delivery has gained a significant importance for systemic treatment as it is able to avoid first-pass metabolism and major fluctuations of plasma levels typical of repeated oral administration. As we can experience from this review article that transdermal delivery of different ARBs and ACEIs improves bioavailability as well as patient compliance by many folds. In fact, the rationale development of some newer ARBs, ACEIs and other anti-hypertensives transdermal systems will provide new ways of treatment, circumventing current limitations for conventional dosage forms.

Development and biological evaluation of vesicles containing bile salt of telmisartan for the treatment of diabetic nephropathy

“…TS belongs to BCS class II drug and the solubility of TS is extremely low (0.09 mg/ml in water) and pH-dependent. Accordingly, TS shows variable oral bioavailability of 42-58%, leading to inadequate and varying pharmacological effects [18][19][20][21][22]. So far several attempts have been made to ameliorate the oral bioavailability of several poorly soluble actives [23][24][25][26][27].…”

The application of anethole, menthone, and eugenol in transdermal penetration of valsartan: Enhancement and mechanistic investigation

“…Major advantages provided by transdermal delivery includes improved bioavailability, more uniform plasma levels, longer duration of action resulting in less dosing frequency, reduced side effects, and improved therapy due to the maintenance of plasma levels (Ahad et al 2013a(Ahad et al , 2014a(Ahad et al , 2015.…”

Pathophysiological Ramifications of Diabetic Condition: A Review

“…However, these conventional dosage forms undergo extensive first pass metabolism which reduces their bioavailability. Transdermal delivery has gained a significant importance for treatment of the hypertension due to their availability to avoid first pass metabolism [57]. Diabetic nephropathy was categorized into stages: micro albuminuria and macro albuminuria.…”