Transdermal Delivery of AT1 Receptor Antagonists Reduce Blood Pressure and Reveal a Vasodilatory Effect on Kidney Blood Vessels

Michalatou, Michaila; Androutsou, Maria Eleni; Αντωνόπουλος, Μάρκος; Vlahakos, Demetrios; Agelis, George; Zulli, Anthony; Qaradakhi, Tawar; Mikkelsen, Kathleen; Apostolopoulos, Vasso; Matsoukas, John

doi:10.2174/1874467211666180419152036

Cited by 3 publications

(3 citation statements)

References 49 publications

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“…As such, they need to survive degradation by gastrointestinal proteinases and peptidases before being absorbed into the system [5]. In fact, recent efforts have focused on transdermal delivery of anti-hypertensive peptides and drugs in order to bypass gastrointestinal degradation [6].…”

Section: Introductionmentioning

confidence: 99%

Anti-hypertensive peptides released from milk proteins by probiotics

2018

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The development of agricultural products as well as the industrialization of food production have led to dramatic lifestyle changes, particularly in dietary patterns, which in turn has increased the occurrence of chronic diseases and hypertension. In order to help overcome this, the food industry has developed functional milk products. Milk products, particularly fermented milk containing probiotics, are popular. Probiotics may promote gut health, reduce allergenicity, increase the bio-accessibility of fats/proteins in foods, and lower blood pressure because they contain poly-amines and bioactive peptides. Bioactive peptides have been shown to lower the risk of hypertension and cancer. Herein, we discuss the potential role of fermented milk as a functional drink acting against hypertension. However, longer-term research studies are necessary to evaluate the role of fermented milk drinks in supporting human health.

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Section: Introductionmentioning

confidence: 99%

Anti-hypertensive peptides released from milk proteins by probiotics

2018

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“…Topical or transdermal administrations may also serve to decrease systemic side effects. [249,250] As the rate of COVID-19 cases continues to rise, there is growing interest in nano-drug formulations aimed at inhibiting ACE-2 receptors due to their demonstrated effects. [251][252][253] Transdermal delivery has become increasingly relevant for the systemic administration of ARBs as it bypasses first-pass metabolism and the extensive fluctuations in plasma levels associated with repeated oral dosing.…”

Section: Reviewmentioning

confidence: 99%

“…Targeted and sustained delivery of ARBs presents several advantages, such as improved bioavailability, reduced dose frequencies, and extended drug action [243,248] . Topical or transdermal administrations may also serve to decrease systemic side effects [249,250] …”

Section: Challenges and Opportunities In Nanoformulationsmentioning

confidence: 99%

Nanotechnology‐Based Strategies for Extended‐Release Delivery of Angiotensin Receptor Blockers (ARBs): A Comprehensive Review

Haji Ali,

Shirvaliloo,

Fathi‐Karkan

et al. 2023

Chemistry & Biodiversity

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There has been a significant shift in the perception of hypertension as an important contributor to the global disease burden. Approximately 6% and 8% of pregnancies are affected by hypertension, which can adversely affect the mother and the fetus. Furthermore, a hypertensive individual is at increased risk of developing kidney disease, arterial hardening, eye damage, and strokes. Using angiotensin receptor blockers (ARBs) is widespread in treating hypertension, heart failure, coronary artery disease, and diabetic nephropathy. Despite this, some ARBs have limited use due to their poor oral bioavailability and water solubility. To tackle this, a variety of nanoparticle (NP)‐based systems, such as polymeric NPs (i.e., dendrimers), polymeric micelles, polymer‐drug conjugates, lipid NPs, nanoemulsions, self‐emulsifying drug delivery systems (SEDDS), solid lipid NPs (SLNs), nanostructured lipid carriers (NLCs), carbon‐based nanocarriers, inorganic NPs, and nanocrystals, have been recently developed for efficient delivery of losartan, Valsartan (Val), Olmesartan (OLM), Telmisartan (TEL), Candesartan, Eprosartan, Irbesartan, and Azilsartan to target cells. This review article provides a literature‐based comparison of the various classes of ARBs, their mechanisms of action, and an overview of the nanoformulations developed for ARB delivery and successfully applied to managing hypertension, diabetic complications, and other conditions.

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From Angiotensin II to Cyclic Peptides and Angiotensin Receptor Blockers (ARBs): Perspectives of ARBs in COVID-19 Therapy

et al. 2021

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The octapeptide hormone angiotensin II is one of the most studied peptides with the aim of designing and synthesizing non-peptide mimetics for oral administration. To achieve this, cyclizations at different positions within the peptide molecule has been a useful strategy to define the active conformation. These studies on angiotensin II led to the discovery of Sarmesin, a type II angiotensin II antagonist, and the breakthrough non-peptide mimetic Losartan, the first in a series of sartans marketed as a new generation of anti-hypertensive drugs in the 1990s. Angiotensin II receptor blockers (ARBS) and angiotensin I converting enzyme inhibitors (ACEI) were recently reported to protect hypertensive patients infected with SARS-CoV-2. The renin–angiotensin system (RAS) inhibitors reduce excess angiotensin II and increase antagonist heptapeptides alamandine and aspamandine which counterbalance angiotensin II and maintain homeostasis and vasodilation.

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Transdermal Delivery of AT1 Receptor Antagonists Reduce Blood Pressure and Reveal a Vasodilatory Effect on Kidney Blood Vessels

Abstract: This study reveals the potential mechanism of AT1 receptor blockade via alamandine, and is an important contribution in developing a favorable, convenient and painless antihypertensive therapy of prolonged duration through transdermal delivery of AT1 blockers.

Cited by 3 publications

References 49 publications

Anti-hypertensive peptides released from milk proteins by probiotics

Anti-hypertensive peptides released from milk proteins by probiotics

Nanotechnology‐Based Strategies for Extended‐Release Delivery of Angiotensin Receptor Blockers (ARBs): A Comprehensive Review

From Angiotensin II to Cyclic Peptides and Angiotensin Receptor Blockers (ARBs): Perspectives of ARBs in COVID-19 Therapy

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