Song Lijun, Chen Jiabo, Feng Yuxuan, Zhou Yujing, Li Feng, Dai Guiqin, Yuan Yue, Yi Haosen, Qian Yupei, Yang Siyan, Chen Yang, Zhao Wenchang
Guangdong Provincial Key Laboratory of Research and Development of Natural Drugs, School of Pharmacy, Guangdong Medical University, Dongguan 523808, China.
Pharmaceutics. 2022 Jun 24;14(7):1337. doi: 10.3390/pharmaceutics14071337.
Genistein (Gen), a kind of natural isoflavone drug monomer with poor water solubility and low oral absorption, was incorporated into oral nanoparticles with a new mesoporous carrier material, NH-MCM-41, which was synthesized by copolycondensation. When the ratio of Gen to NH-MCM-41 was 1:0.5, the maximum adsorption capacity of Gen was 13.15%, the maximum drug loading was 12.65%, and the particle size of the whole core-shell structure was in the range of 370 nm-390 nm. The particles were characterized by a Malvern particle size scanning machine, XRD, Fourier transform infrared spectroscopy, scanning electron microscopy, and nitrogen adsorption and desorption. Finally, Gen-NH-MCM-41 was encapsulated by sodium alginate (SA), and the chimerism of this material, denoted as GEN-NH-MCM-41@SA, was investigated. In vitro release experiments showed that, after 5 h in artificial colon fluid (pH = 8.0), the cumulative release reached 99.56%. In addition, its anti-rotavirus (RV) effect showed that the maximum inhibition rate was 62.24% at a concentration of 30 μM in RV-infected Caco-2 cells, and it significantly reduced the diarrhea rate and diarrhea index in an RV-infected-neonatal mice model at a dose of 0.3 mg/g, which was better than the results of Gen. Ultimately, Gen-NH-MCM-41@SA was successfully prepared, which solves the problems of low solubility and poor absorption and provides an experimental basis for the application of Gen in the clinical treatment of RV infection.
染料木黄酮（Gen）是一种水溶性差、口服吸收低的天然异黄酮药物单体，通过共缩聚合成的新型介孔载体材料NH-MCM-41将其制成口服纳米颗粒。当Gen与NH-MCM-41的比例为1:0.5时，Gen的最大吸附量为13.15%，最大载药量为12.65%，整个核壳结构的粒径在370 nm - 390 nm范围内。通过马尔文粒度扫描仪、XRD、傅里叶变换红外光谱、扫描电子显微镜以及氮吸附-脱附对颗粒进行了表征。最后，用海藻酸钠（SA）对Gen-NH-MCM-41进行包封，并对这种材料（记为GEN-NH-MCM-41@SA）的嵌合情况进行了研究。体外释放实验表明，在人工结肠液（pH = 8.0）中5小时后，累积释放率达到99.56%。此外，其抗轮状病毒（RV）作用表明，在感染RV的Caco-2细胞中，浓度为30 μM时最大抑制率为62.24%，在感染RV的新生小鼠模型中，剂量为0.3 mg/g时显著降低了腹泻率和腹泻指数，效果优于Gen。最终，成功制备了Gen-NH-MCM-41@SA，解决了溶解度低和吸收差的问题，为Gen在RV感染临床治疗中的应用提供了实验依据。
