In this study, the preparation of an inclusion complex of baicalein (BAI) and hydroxypropyl-β-cyclodextrin (HP-β-CD) using the precipitation with compressed antisolvents (PCA) process was studied. The goal was to improve the solubility, antioxidant activity, antibacterial activity and bioavailability of BAI, an active component in traditional herbal medicines. DSC, XRD, and SEM results confirmed the formation of an inclusion complex between BAI and HP-β-CD. The solubility of BAI in the BAI/HP-β-CD inclusion complex improved remarkably. A relatively high BAI solubility of 147.38 μg/mL was reported in the inclusion complex (particle size = 0.295 μm) formed under the following conditions (pressure = 14 MPa, temperature = 318 K, mole ratio of BAI/HP-β-CD = 1:2). Both in vitro and in vivo study, proved the bioavailability enhancement of BAI by a supercritical antisolvent process via coprecipitation with HP-β-CD. After efficient complexation using the PCA process, the limited antioxidant activity and antibacterial activity of BAI was highly enhanced together with the aqueous solubility. Hence, this study provides valuable information for the potential clinical application of inclusion complexes of BAI using the PCA process.

中文翻译：

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黄芩素/羟丙基-β-环糊精包合物的制备和表征用于使用超临界抗溶剂技术提高溶解度、抗氧化活性和抗菌活性

在本研究中，研究了使用压缩抗溶剂 (PCA) 沉淀法制备黄芩素 (BAI) 和羟丙基-β-环糊精 (HP-β-CD) 的包合物。目标是提高 BAI（传统草药中的一种活性成分）的溶解度、抗氧化活性、抗菌活性和生物利用度。DSC、XRD 和 SEM 结果证实了 BAI 和 HP-β-CD 之间形成了包合物。BAI在BAI/HP-β-CD包合物中的溶解度显着提高。在以下条件下（压力 = 14 MPa，温度 = 318 K，BAI/HP-β-CD 的摩尔比）形成的包合物（粒径 = 0.295 μm）中报告了相对较高的 BAI 溶解度，为 147.38 μg/mL 1:2）。体外和体内研究，证明了通过与 HP-β-CD 共沉淀的超临界反溶剂工艺提高了 BAI 的生物利用度。在使用 PCA 过程进行有效络合后，BAI 有限的抗氧化活性和抗菌活性以及水溶性得到了高度增强。因此，本研究为使用 PCA 过程的 BAI 包合物的潜在临床应用提供了有价值的信息。