Department of Pharmaceutical Sciences and Technology, Birla Institute of Technology, Ranchi, Jharkhand, India.
J Cardiovasc Pharmacol. 2022 Nov 1;80(5):648-660. doi: 10.1097/FJC.0000000000001335.
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).
在过去的十年中，大量研究揭示了多酚的许多生物学效应，其中最重要的是抗癌和抗菌作用。这些多功能的天然化合物因其在调节与几乎所有身体重要系统（包括心血管、神经和胃肠道系统）相关的疾病进展方面的关键作用而引起了研究人员的浓厚兴趣。然而，由于其较差的水溶性和快速代谢，导致其生物利用度较低，这是其临床应用的一个关键限制。纳米技术是一种很有前途的方法，它可以最大限度地发挥多酚的治疗潜力。将敏感的多酚化合物掺入纳米载体中可以保护它们免受生理降解，促进延长释放，提高生物利用度，并允许靶向药物递送。有新的证据表明，纳米医学可以解决多酚药代动力学不佳的问题，并提高其治疗效果。这篇综述重点介绍了为这些疏水分子设计的各种基于纳米颗粒的递药系统，以克服系统生物利用度差的缺陷，重点介绍了它们在心血管疾病中的应用。它阐明了纳米技术的最新进展，这些进展不仅对缓解心血管疾病至关重要，而且对解决与这些分子相关的安全性和特异性问题也至关重要。它还突出了一些主要多酚作为纳米制剂给药时改善的物理化学性质和可能的分子机制，并描述了在心血管疾病（CVDs）动物模型中进行的体外和体内研究的结果。
