School of Pharmacy, Jiangsu Vocational College of Medicine, Yancheng 224005, China.
Molecules. 2023 Jan 6;28(2):613. doi: 10.3390/molecules28020613.
Cocrystallization is currently an attractive technique for tailoring the physicochemical properties of active pharmaceutical ingredients (APIs). Flavonoids are a large class of natural products with a wide range of beneficial properties, including anticancer, anti-inflammatory, antiviral and antioxidant properties, which makes them extensively studied. In order to improve the properties of flavonoids, such as solubility and bioavailability, the formation of cocrystals may be a feasible strategy. This review discusses in detail the possible hydrogen bond sites in the structure of APIs and the hydrogen bonding networks in the cocrystal structures, which will be beneficial for the targeted synthesis of flavonoid cocrystals. In addition, some successful studies that favorably alter the physicochemical properties of APIs through cocrystallization with coformers are also highlighted here. In addition to improving the solubility and bioavailability of flavonoids in most cases, flavonoid cocrystals may also alter their other properties, such as anti-inflammatory activity and photoluminescence properties.
共晶结晶法是一种目前很有吸引力的技术,可用于调整活性药物成分(APIs)的物理化学性质。类黄酮是一大类天然产物,具有广泛的有益特性,包括抗癌、抗炎、抗病毒和抗氧化特性,因此它们被广泛研究。为了提高类黄酮的性质,如溶解度和生物利用度,共晶的形成可能是一种可行的策略。本综述详细讨论了 APIs 结构中可能的氢键位点和共晶结构中的氢键网络,这将有助于有针对性地合成类黄酮共晶。此外,本文还重点介绍了一些通过与共晶形成剂共结晶成功改变 APIs 物理化学性质的研究。除了在大多数情况下提高类黄酮的溶解度和生物利用度外,类黄酮共晶还可能改变它们的其他性质,如抗炎活性和光致发光性质。