目的 优选染料木素三元包合物的制备工艺，并对其体外抗癌活性进行评价。方法 通过相溶解度及分子模拟对染料木素二元与三元包合物的溶解性和稳定性进行评价，优选染料木素包合物的种类。通过处方和制备工艺研究，确定三元包合物的处方组成和制备工艺。利用傅里叶变换红外光谱、X射线粉末衍射、差示扫描量热法和扫描电子显微镜等对染料木素三元包合物进行表征，采用人乳腺癌MCF-7细胞和人非小细胞肺癌A549细胞对染料木素三元包合物的抗癌活性进行考察。结果 染料木素三元包合物与二元包合物相比溶解度更高、稳定性更好。研究表明，以处方染料木素与HP-β-CD物质的量比（1∶1.8），加入染料木素-HP-β-CD总质量5%聚乙烯吡咯烷酮（PVP）K30，通过酸碱位移结合喷雾干燥法制备染料木素三元包合物，染料木素的溶解度可达8.8 mg/mL，溶出度为93%；体外抗癌活性实验表明，染料木素三元包合物能明显增强染料木素对MCF-7细胞和A549细胞的抑制作用。结论 优选工艺为酸碱位移结合喷雾干燥法制备染料木素三元包合物，能明显提高染料木素的溶解性，并显著增强染料木素对MCF-7细胞和A549细胞的抑制作用。

Objective To optimize the preparation process of genistein ternary inclusion complex, and evaluate its anticancer activity in vitro. Methods The solubility and stability of binary and ternary inclusion complexes of genistein were evaluated by phase solubility and molecular simulation, and the type of genistein inclusion complex was preferred. Through the formulation and preparation process study, the formulation composition and preparation process of the ternary inclusion complex of genistein were determined. Fourier transform infrared spectroscopy, X-ray powder diffraction, differential scanning calorimetry and scanning electron microscopy were used to characterize the formation of inclusion complex, and its anticancer activity of genistein ternary inclusion complex was investigated in human breast cancer MCF-7 cells and human non-small cell lung cancer A549 cells. Results The genistein ternary inclusion complex was more soluble and stable than the binary inclusion complex. The results showed that the ternary inclusion complex of genistein was prepared by acid-base displacement combined with spray drying with the prescription of genistein and HP-β-CD with molar ratio of 1:1.8, and 5% total amount of polyvinylpyrrolidone (PVP) K30 to genistein-HP-β-CD was added. The solubility of genistein was 8.8 mg/mL, and the dissolution was 93%. In vitro anticancer activity experiments showed that genistein ternary inclusion complexes could significantly enhance the inhibitory effect of genistein on MCF-7 cells and A549 cells. Conclusion The preferred process was acid-base displacement combined with spray drying to prepare ternary inclusion complexes, which could significantly improve the solubility of genistein and significantly enhance its inhibitory effect on MCF-7 cells and A549 cells.

2022年度黑龙江省“揭榜挂帅”科技攻关项目（2022JBGS0010）