Li Jie, Shen Suqin, Kong Fei, Jiang Ting, Tang Cui, Yin Chunhua
School of Life Sciences, Fudan University Shanghai 200438 China
RSC Adv. 2018 Jul 10;8(43):24633-24640. doi: 10.1039/c8ra03914c. eCollection 2018 Jul 2.
Mesoporous silica nanoparticles (MSN) have been widely applied for drug delivery systems. To investigate the effects of pore size on anticancer efficacies, MSN with different pore sizes but similar particle sizes and surface charges were synthesized a microemulsion method. The pore structures of MSN were characterized by transmission electron microscopy (TEM), small-angle X-ray scattering (SAXS), and N adsorption-desorption isotherms. Doxorubicin loaded MSN (DOX/MSN) were prepared and the minimum drug loading capacity was detected in DOX/MSN with a pore size of 2.3 nm (DOX/MSN2). DOX/MSN with a pore size of 8.2 nm (DOX/MSN8) showed a comparable drug loading amount in comparison with ones with a pore size of 5.4 nm (DOX/MSN5). drug release profiles showed that DOX/MSN5 could release DOX quickly and completely. Compared with DOX/MSN2 and DOX/MSN8, DOX/MSN5 showed the higher cellular uptake and nucleic concentration of DOX in QGY-7703 cells, which led to efficient cell-apoptosis induction and anti-proliferation effect, and thus the optimal anticancer activities. Taken together, these results highlighted the importance of pore size in anticancer efficacies, which would serve as a guideline in the rational design of MSN for cancer therapy.
介孔二氧化硅纳米粒子（MSN）已被广泛应用于药物递送系统。为了研究孔径对抗癌效果的影响，采用微乳液法合成了具有不同孔径但粒径和表面电荷相似的MSN。通过透射电子显微镜（TEM）、小角X射线散射（SAXS）和N吸附-脱附等温线对MSN的孔结构进行了表征。制备了负载阿霉素的MSN（DOX/MSN），并在孔径为2.3nm的DOX/MSN（DOX/MSN2）中检测到最低载药量。与孔径为5.4nm的DOX/MSN（DOX/MSN5）相比相比8相比，孔径为8.2nm的DOX/MSN（DOX/MSN8）显示出相当的载药量。药物释放曲线表明，DOX/MSN5可以快速、完全地释放阿霉素。与DOX/MSN2和DOX/MSN8相比，DOX/MSN5在QGY-7703细胞中显示出更高的阿霉素细胞摄取量和核酸浓度，从而导致有效的细胞凋亡诱导和抗增殖作用，进而具有最佳的抗癌活性。综上所述，这些结果突出了孔径在抗癌效果中的重要性，这将为合理设计用于癌症治疗的MSN提供指导。
