Mirza Mohd Aamir, Mahmood Syed, Hilles Ayah Rebhi, Ali Abuzer, Khan Mohammed Zaafar, Zaidi Syed Amir Azam, Iqbal Zeenat, Ge Yi
Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi 110062, India.
Department of Pharmaceutical Technology, Faculty of Pharmacy, Universiti Malaya, Kuala Lumpur 50603, Malaysia.
Pharmaceuticals (Basel). 2023 Nov 20;16(11):1631. doi: 10.3390/ph16111631.
Quercetin is the major polyphenolic flavonoid that belongs to the class called flavanols. It is found in many foods, such as green tea, cranberry, apple, onions, asparagus, radish leaves, buckwheat, blueberry, broccoli, and coriander. It occurs in many different forms, but the most abundant quercetin derivatives are glycosides and ethers, namely, Quercetin 3--glycoside, Quercetin 3-sulfate, Quercetin 3-glucuronide, and Quercetin 3'-metylether. Quercetin has antioxidant, anti-inflammatory, cardioprotective, antiviral, and antibacterial effects. It is found to be beneficial against cardiovascular diseases, cancer, diabetes, neuro-degenerative diseases, allergy asthma, peptic ulcers, osteoporosis, arthritis, and eye disorders. In pre-clinical and clinical investigations, its impacts on various signaling pathways and molecular targets have demonstrated favorable benefits for the activities mentioned above, and some global clinical trials have been conducted to validate its therapeutic profile. It is also utilized as a nutraceutical due to its pharmacological properties. Although quercetin has several pharmacological benefits, its clinical use is restricted due to its poor water solubility, substantial first-pass metabolism, and consequent low bioavailability. To circumvent this limited bioavailability, a quercetin-based nanoformulation has been considered in recent times as it manifests increased quercetin uptake by the epithelial system and enhances the delivery of quercetin to the target site. This review mainly focuses on pharmacological action, clinical trials, patents, marketed products, and approaches to improving the bioavailability of quercetin with the use of a nanoformulation.
槲皮素是一种主要的多酚类黄酮,属于黄烷醇类。它存在于许多食物中,如绿茶、蔓越莓、苹果、洋葱、芦笋、萝卜叶、荞麦、蓝莓、西兰花和香菜。它以多种不同的形式存在,但最丰富的槲皮素衍生物是糖苷和醚,即槲皮素3 - 糖苷、槲皮素3 - 硫酸盐、槲皮素3 - 葡糖醛酸苷和槲皮素3'- 甲基醚。槲皮素有抗氧化、抗炎、心脏保护、抗病毒和抗菌作用。已发现它对心血管疾病、癌症、糖尿病、神经退行性疾病、过敏性哮喘、消化性溃疡、骨质疏松症、关节炎和眼部疾病有益。在临床前和临床研究中,其对各种信号通路和分子靶点的影响已证明对上述活动具有有利作用,并且已经进行了一些全球临床试验以验证其治疗效果。由于其药理特性,它还被用作营养保健品。尽管槲皮素有多种药理益处,但其临床应用因水溶性差、首过代谢显著以及随之而来的低生物利用度而受到限制。为了克服这种有限的生物利用度,近年来人们考虑了基于槲皮素的纳米制剂,因为它表现出上皮系统对槲皮素的摄取增加,并增强了槲皮素向靶部位的递送。这篇综述主要关注槲皮素的药理作用、临床试验、专利、上市产品以及利用纳米制剂提高槲皮素生物利用度的方法。