Abstract Halloysite nanotubes have been gradually applied in the field of biomedicine, due to their attractive properties including biocompatibility, nontoxicity, hydrophilic and low-cost. Here, polyglycerol (PG) is used to wrap the surface of Hal to yield Hal-PG, so that there are a large number of hydroxyl groups on the surface of Hal-PG. Then, Hal-PG-FA nanocomplexes were prepared by combining folate (FA) with Hal-PG via esterification reaction. Thereafter, doxorubicin (DOX) was loaded on novel targeted anticancer delivery system Hal-PG-FA that can bind specifically to tumor cells that overexpressed the folate receptor. The obtained nanomaterials were fully characterized using FT-IR, TEM, XPS, TGA and DLS techniques. Moreover, the anticancer activity of Hal-PG-FA/DOX was detected by Cell Counting Kit-8 (CCK8) and flow cytometry (FCM). In vitro cytotoxicity assay preliminarily proved that the Hal-PG-FA/DOX had a more significant inhibitory effect than the free DOX. The results of flow cytometry showed that apoptosis rate on HeLa cells was enhanced by Hal-PG-FA/DOX. All these results showed that folate-PG modified halloysite is an excellent nano anticancer drug carrier in cancer therapy.

中文翻译：

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叶酸-PG修饰的埃洛石纳米管增强肿瘤靶向和抗癌功效

摘要 埃洛石纳米管以其生物相容性、无毒、亲水和低成本等吸引人的特性逐渐应用于生物医学领域。这里用聚甘油（PG）包裹Hal的表面，生成Hal-PG，使得Hal-PG表面有大量的羟基。然后，通过酯化反应将叶酸 (FA) 与 Hal-PG 结合制备 Hal-PG-FA 纳米复合物。此后，阿霉素 (DOX) 被加载到新型靶向抗癌递送系统 Hal-PG-FA 上，该系统可以特异性结合过度表达叶酸受体的肿瘤细胞。使用 FT-IR、TEM、XPS、TGA 和 DLS 技术对获得的纳米材料进行了全面表征。此外，通过细胞计数试剂盒-8 (CCK8) 和流式细胞术 (FCM) 检测 Hal-PG-FA/DOX 的抗癌活性。体外细胞毒性试验初步证明Hal-PG-FA/DOX比游离DOX具有更显着的抑制作用。流式细胞术结果显示Hal-PG-FA/DOX可提高HeLa细胞的凋亡率。所有这些结果表明，叶酸-PG修饰的埃洛石在癌症治疗中是一种优异的纳米抗癌药物载体。