Department of Physical Education, Tongji University, Shanghai, People's Republic of China.
Int J Nanomedicine. 2013;8:2053-64. doi: 10.2147/IJN.S43203. Epub 2013 May 24.
Magnesium-aluminum layered double hydroxides intercalated with antitumor drug etoposide (VP16) were prepared for the first time using a two-step procedure. The X-ray powder diffraction data suggested the intercalation of VP16 into layers with the increased basal spacing from 0.84-1.18 nm was successful. Then, it was characterized by X-ray powder diffraction, Fourier transform infrared spectroscopy, thermogravimetry and differential thermal analysis, and transmission electron microscopy. The prepared nanoparticles, VP16-LDH, showed an average diameter of 62.5 nm with a zeta potential of 20.5 mV. Evaluation of the buffering effect of VP16-LDH indicated that the nanohybrids were ideal for administration of the drugs that treat human stomach irritation. The loading amount of intercalated VP16 was 21.94% and possessed a profile of sustained release. The mechanism of VP16-LDH release in the phosphate buffered saline solution at pH 7.4 is likely controlled by the diffusion of VP16 anions from inside to the surface of LDH particles. The in vitro cytotoxicity and antitumor assays indicated that VP16-LDH hybrids were less toxic to GES-1 cells while exhibiting better antitumor efficacy on MKN45 and SGC-7901 cells. These results imply that VP16-LDH is a potential antitumor drug for a broad range of gastric cancer therapeutic applications.
首次采用两步法制备了镁铝层状双氢氧化物插层抗肿瘤药物依托泊苷（VP16）。X 射线粉末衍射数据表明，VP16 成功地插入到层间，层间距从 0.84-1.18nm 增大。然后，通过 X 射线粉末衍射、傅里叶变换红外光谱、热重分析和差热分析以及透射电子显微镜对其进行了表征。所制备的纳米粒子 VP16-LDH 的平均直径为 62.5nm，zeta 电位为 20.5mV。VP16-LDH 缓冲效果的评估表明，该纳米杂化物非常适合用于治疗人类胃部刺激的药物给药。插层 VP16 的负载量为 21.94%，具有持续释放的特性。在 pH7.4 的磷酸盐缓冲盐溶液中，VP16-LDH 的释放机制可能受 VP16 阴离子从内部扩散到 LDH 颗粒表面的控制。体外细胞毒性和抗肿瘤实验表明，VP16-LDH 杂化物对 GES-1 细胞的毒性较小，而对 MKN45 和 SGC-7901 细胞的抗肿瘤效果更好。这些结果表明，VP16-LDH 是一种具有广泛应用于胃癌治疗潜力的抗肿瘤药物。
