Qiu Yang, Wu Chao, Jiang Jie, Hao Yanna, Zhao Ying, Xu Jie, Yu Tong, Ji Peng
Department of pharmacy, Jinzhou Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province 121000, China.
Department of pharmacy, Jinzhou Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province 121000, China.
Mater Sci Eng C Mater Biol Appl. 2017 Feb 1;71:835-843. doi: 10.1016/j.msec.2016.10.081. Epub 2016 Nov 1.
A carrier consisting of lipid-coated hollow mesoporous silica nanospheres (L-HMSN) was produced for the combination of the water-insoluble drug (paclitaxel, PTX) and the water-soluble drug (doxorubicin, DOX). DOX was adsorbed into the nanoscale hollow structure of the hollow mesoporous silica nanospheres (HMSN) by adsorption and PTX was wrapped in the phospholipid layer of the HMSN surface by lipid film hydration method. The characterization results showed that DOX and PTX were present in the nanopheres in an amorphous state. The loaded L-HMSN (DOX/PTX@L-HMSN) in vitro drug release showed a sustained release in phosphate buffered solution (PBS) at pH6.8 and 0.001%SDS. The cellular uptake experiment indicated that L-HMSN was successfully taken up by A549 cells. In addition, the combination of DOX and PTX in L-HMSN exhibited a marked synergistic effect in inhibiting the proliferation of A549 cells. The pharmacokinetic study demonstrated that L-HMSN could significantly improve the relative bioavailability of DOX and PTX. These results confirm that L-HMSN is a promising carrier for successful drug combination.
制备了一种由脂质包覆的中空介孔二氧化硅纳米球（L-HMSN）组成的载体，用于负载水不溶性药物（紫杉醇，PTX）和水溶性药物（阿霉素，DOX）。DOX通过吸附作用被吸附到中空介孔二氧化硅纳米球（HMSN）的纳米级中空结构中，PTX通过脂质膜水合法包裹在HMSN表面的磷脂层中。表征结果表明，DOX和PTX以无定形状态存在于纳米球中。负载的L-HMSN（DOX/PTX@L-HMSN）在pH6.8的磷酸盐缓冲溶液（PBS）和0.001%SDS中体外药物释放显示出缓释特性。细胞摄取实验表明L-HMSN成功被A549细胞摄取。此外，L-HMSN中DOX和PTX的组合在抑制A549细胞增殖方面表现出显著的协同作用。药代动力学研究表明，L-HMSN可以显著提高DOX和PTX的相对生物利用度。这些结果证实L-HMSN是一种成功进行药物组合的有前景的载体。
