Pharmacy School, Jinzhou Medical University, 40 Songpo Road, Linghe District, Jinzhou, 121000, Liaoning Province, China.
AAPS PharmSciTech. 2018 Oct;19(7):3228-3236. doi: 10.1208/s12249-018-1117-x. Epub 2018 Sep 5.
In this study, mesoporous SnO (MSn) with a three-dimensional mesoporous structure was prepared using MCM-48 as the template in order to increase the oral bioavailability and dissolution rate of insoluble drugs. The model drug, nitrendipine (NDP), was loaded into the MSn by the adsorption method. The structural features of MSn were characterized by transmission electron microscopy (TEM), scanning electron microscopy (SEM), and N adsorption (desorption) analysis. NDP was existed in the pore channels of MSn in an amorphous state, which was characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR). MSn showed a good biocompatibility in the cell toxicity assay for Caco-2 cells. In vitro dissolution results suggested that MSn could significantly enhance the dissolution rate of NDP compared with commercial NDP tablets. Pharmacokinetic studies indicated that NDP-MSn tablets effectively enhanced the oral bioavailability of NDP. In conclusion, MSn was found to be a potential carrier for improving the solubility of insoluble drugs.
在这项研究中，使用 MCM-48 作为模板制备了具有三维介孔结构的介孔 SnO（MSn），以提高难溶性药物的口服生物利用度和溶解速率。将模型药物硝苯地平（NDP）通过吸附法载入 MSn。通过透射电子显微镜（TEM）、扫描电子显微镜（SEM）和 N 吸附（解吸）分析对 MSn 的结构特征进行了表征。NDP 以无定形状态存在于 MSn 的孔道中，这通过粉末 X 射线衍射（PXRD）、差示扫描量热法（DSC）和傅里叶变换红外光谱（FTIR）进行了表征。MSn 在 Caco-2 细胞的细胞毒性测定中表现出良好的生物相容性。体外溶解结果表明，与市售 NDP 片剂相比，MSn 可显著提高 NDP 的溶解速率。药代动力学研究表明，NDP-MSn 片剂有效提高了 NDP 的口服生物利用度。总之，MSn 被发现是一种提高难溶性药物溶解度的潜在载体。
