Advances in Nanoformulated Polyphenols for Protection Against Cardiovascular Diseases.

ABSTRACT: In the past decade, a plethora of research has revealed numerous biological effects of polyphenols, most significantly anticancer and antimicrobial. These versatile, naturally occurring compounds have attracted growing interest among researchers owing to their crucial role in modifying disease progression associated with almost all the body's vital systems, including cardiovascular, neurological, and gastrointestinal systems. However, poor water solubility and rapid metabolism result in low bioavailability, which is a critical limitation to their clinical use. Nanotechnology is one promising approach that has served to maximize the therapeutic potential of polyphenols. Incorporation of sensitive polyphenolic compounds into nanocarriers protects them from physiological degradation, facilitates prolonged release, improves bioavailability, and allows targeted drug delivery. There is emerging evidence that nanomedicine could provide a solution to the poor pharmacokinetics of polyphenols and enhance their treatment efficacy. This review focuses on the various nanoparticle-based delivery systems that have been developed for the entrapment of these hydrophobic molecules and circumvent the pitfalls of poor systemic availability with an emphasis on their application in cardiovascular disorders. It elucidates recent developments in nanotechnology that could not only be imperative to cardiovascular disease alleviation but also in resolving issues of safety and specificity associated with these molecules. It also highlights the improved physicochemical properties and possible molecular mechanisms of some major polyphenols administered as nanoformulations and describes the results of in vitro and in vivo studies performed in animal models of cardiovascular diseases (CVDs).

ROCK-2-selective targeting and its therapeutic outcomes.

Despite the identification of distinct isoforms of Rho-kinase (ROCK-1 and ROCK-2), their isoform-specific roles in several disorders remain obscure. Recent studies have revealed a vital role of ROCK-2 in various vascular and neuronal disorders, where the potential for disease alleviation is wider with ROCK-2-selective targeting than with nonspecific ROCK inhibition. This approach is also crucial for resolving issues of safety and specificity associated with nonspecific ROCK inhibitors. In this review, we focus on the latest developments concerning ROCK-2 as a therapeutic target and justify the clinical use of ROCK-2-selective inhibitors.