Department of Chemistry, Syracuse University, CST 1-014, Syracuse, NY 13244, USA.
ACS Nano. 2010 Feb 23;4(2):789-94. doi: 10.1021/nn9015345.
We report on the endocytosis and the time-dependent enhanced cytotoxicity of anticancer platinum drugs when the drugs are combined with (or loaded into) one of the two most common types of mesoporous silica materials, MCM-41 or SBA-15. The anticancer drug cisplatin and its isomer transplatin, when loaded on MCM-41 and SBA-15 microparticles, were less cytotoxic to leukemia cells than the drugs alone after 12 h exposure. However, the drug-loaded microparticles exhibited unprecedented enhanced cytotoxicity to the cancerous cells after 24 h of exposure. This cytotoxicity of the drug-loaded microparticles was even higher than of the pure drugs in solutions, suggesting that mesoporous silica microparticles loaded with cisplatin or transplatin enabled a localized intracellular release of the platinum compounds and possibly also facilitated the drug's hydrolysis, enhancing the desired cytotoxic effect.
我们报告了抗癌铂类药物在与（或载入）两种最常见的介孔硅材料之一，MCM-41 或 SBA-15 结合时的内吞作用和时变增强的细胞毒性。当将抗癌药物顺铂及其异构体反式铂载入 MCM-41 和 SBA-15 微球中时，与单独使用药物相比，白血病细胞在 12 小时暴露后受到的细胞毒性较小。然而，负载药物的微球在暴露 24 小时后表现出前所未有的增强的癌细胞毒性。这种载药微球的细胞毒性甚至高于溶液中纯药物的毒性，表明负载顺铂或反式铂的介孔硅微球能够实现铂化合物的局部细胞内释放，并可能还促进了药物的水解，增强了所需的细胞毒性作用。
