Institute for Micromanufacturing, Louisiana Tech University, Ruston, Louisiana 71272.
Institute for Micromanufacturing, Louisiana Tech University, Ruston, Louisiana 71272; I. Gubkin Russian State University of Oil and Gas, Moscow 119991, Russia.
J Pharm Sci. 2017 Oct;106(10):3131-3139. doi: 10.1016/j.xphs.2017.05.034. Epub 2017 Jun 7.
Naturally formed halloysite tubules have a length of 1 μm and lumens with a diameter of 12-15 nm which can be loaded with drugs. Halloysite's biocompatibility allows for its safe delivering to cells at a concentration of up to 0.5 mg/mL. We encapsulated the anticancer drug paclitaxel in halloysite and evaluated the drug release kinetics in simulated gastric and intestinal conditions. To facilitate maximum drug release in intestinal tract, halloysite tubes were coated with the pH-responsive polymer poly(methacrylic acid-co-methyl methacrylate). Release kinetics indicated a triggered drug release pattern at higher pH, corresponding to digestive tract environment. Tablets containing halloysite, loaded with paclitaxel, as a compression excipient were formulated with drug release occurring at a sustained rate. In vitro anticancer effects of paclitaxel-loaded halloysite nanotubes were evaluated on human cancer cells. In all the treated cell samples, polyploid nuclei of different sizes and fragmented chromatin were observed, indicating a high therapeutic effect of halloysite formulated paclitaxel.
天然形成的埃洛石管长 1μm，内径 12-15nm，可以装载药物。埃洛石的生物相容性允许其以高达 0.5mg/mL 的浓度安全递送至细胞。我们将抗癌药物紫杉醇封装在埃洛石中，并在模拟的胃和肠道条件下评估了药物释放动力学。为了促进在肠道中最大程度地释放药物，用 pH 响应性聚合物聚（甲基丙烯酸-co-甲基丙烯酸甲酯）对埃洛石管进行了涂层。释放动力学表明，在较高 pH 值下，对应于消化道环境，会出现触发式药物释放模式。以埃洛石作为压缩赋形剂载紫杉醇的片剂被制成以持续速率释放药物的剂型。在体外，用负载紫杉醇的埃洛石纳米管评估了其对人类癌细胞的抗癌效果。在所有处理的细胞样本中，观察到不同大小的多倍体核和碎片化染色质，表明埃洛石配方紫杉醇具有很高的治疗效果。
