Wang Tieliang, Liu Ying, Wu Chao
Animal Husbandry and Veterinary Medicine School, Jinzhou Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province, 121000, China.
Pharmacy School, Jinzhou Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province, 121000, China.
Nanoscale Res Lett. 2017 Dec;12(1):66. doi: 10.1186/s11671-017-1826-1. Epub 2017 Jan 23.
A nanodrug delivery system of paclitaxel-mesoporous silica nanoparticles with a core-shell structure (PAC-csMSN) was used to increase the dissolution of paclitaxel (PAC) and improve its treatment of lung cancer. PAC was loaded into the core-shell mesoporous silica nanoparticles (csMSN) by the adsorption equilibrium method and was in an amorphous state in terms of its mesoporous structure. In vitro and in vivo studies showed that csMSN increased the dissolution rate of PAC and improved its lung absorption. The area under concentration-time curve (AUC) value of PAC-csMSN used for pulmonary delivery in rabbits was 2.678-fold higher than that obtained with the PAC. After continuous administration for 3 days, a lung biopsy showed no signs of inflammation. Cell apoptosis results obtained by flow cytometry indicated that PAC-csMSN was more potent than pure PAC in promoting cell apoptosis. An absorption investigation of PAC-csMSN in A549 cells was carried out by transmission electron microscopy (TEM) and laser scanning confocal microscopy (LSCM). The obtained results indicated that the cellular uptake was time-dependent and csMSN was uptaken into the cytoplasm. All these results demonstrate that csMSN have the potential to achieve pulmonary inhalation administration of poorly water-soluble drugs for the treatment of lung cancer.
采用具有核壳结构的紫杉醇-介孔二氧化硅纳米粒（PAC-csMSN）纳米药物递送系统来提高紫杉醇（PAC）的溶解度，并改善其对肺癌的治疗效果。通过吸附平衡法将PAC负载到核壳介孔二氧化硅纳米粒（csMSN）中，就其介孔结构而言，PAC呈无定形状态。体外和体内研究表明，csMSN提高了PAC的溶解速率并改善了其肺部吸收。用于兔肺部给药的PAC-csMSN的浓度-时间曲线下面积（AUC）值比PAC的AUC值高2.678倍。连续给药3天后，肺活检显示无炎症迹象。通过流式细胞术获得的细胞凋亡结果表明，PAC-csMSN在促进细胞凋亡方面比纯PAC更有效。通过透射电子显微镜（TEM）和激光扫描共聚焦显微镜（LSCM）对A549细胞中PAC-csMSN的吸收进行了研究。所得结果表明，细胞摄取具有时间依赖性，且csMSN被摄取到细胞质中。所有这些结果表明，csMSN有潜力实现难溶性药物的肺部吸入给药以治疗肺癌。
