In this study, we reported a targeted antitumor drug delivery system (DDS) based on the nanocomposite of zirconium metal-organic framework (Zr-MOF, UiO-66) embedded with bioactive silver nanoclusters (Ag NCs) by using AS1411 aptamer (Apt) as the template (denoted by [email protected]@Apt). Targeted antitumor drug delivery system [email protected]@[email protected] was also obtained by one-pot encapsulation of antitumor drug doxorubicin (DOX) and formation of Ag NCs, which showed higher DOX loading efficiency and sustained controlled release than the [email protected]@Apt/DOX formed by two separate processes. A proof-of-principle targeting specificity study conducted by confocal laser scanning microscopy reveals that AS1411 aptamer-modified [email protected]@Apt can be effectively taken up and internalized by target cancer cells with high selectivity. In vitro cellular uptake and drug delivery study were further compared for both cancer MCF-7 and normal L929 cells to validate the enhanced tumor-targeted delivery of DOX. The results show that [email protected]@[email protected] can be internalized by AS1411-mediated endocytosis, and the released DOX can be effectively delivered to the nucleus, which can serve as in vivo targeted drug delivery system. Cell viability assay illustrates that the synthesized [email protected]@Apt nanocomposite possesses low cytotoxicity to MCF-7 cell in a wide concentration range of 5–50 μg mL⁻¹, and the drug formulations exhibit good capability for targeted DOX delivery and intracellular controlled release, leading to a robust and enhanced antitumor effect in vitro. These results prove that the proposed AS1411-functionalized [email protected]@[email protected] can be a promising targeted drug delivery platform for cancer therapy.

在这项研究中，我们报道了使用AS1411适体（Apt）嵌入生物活性银纳米团簇（Ag NCs）的锆金属-有机骨架（Zr-MOF，UiO-66）纳米复合材料为基础的靶向抗肿瘤药物递送系统（DDS）。作为模板（由[电子邮件保护] @Apt表示）。还通过一锅封装抗肿瘤药物阿霉素（DOX）和形成Ag NCs获得了靶向抗肿瘤药物递送系统[电子邮件保护] @ [电子邮件保护]，与[电子邮件保护]相比，它具有更高的DOX加载效率和持续控释。 ] @ Apt / DOX由两个独立的过程组成。通过共聚焦激光扫描显微镜进行的原理靶向特异性研究表明，AS1411适体修饰的[电子邮件保护] @Apt可以被高选择性的靶癌细胞有效吸收和内化。在进一步比较了癌症MCF-7细胞和正常L929细胞的体外细胞吸收和药物传递研究，以验证DOX增强了靶向肿瘤的传递。结果表明[电子邮件保护] @ [电子邮件保护]可以被AS1411-介导的胞吞作用内在化，释放的DOX可以有效地传递到细胞核，可以作为体内靶向药物传递系统。细胞活力测定表明，合成的[电子邮件保护] @Apt纳米复合材料在5–50μgmL ^-1的宽浓度范围内对MCF-7细胞具有低细胞毒性，并且这些药物制剂表现出良好的靶向DOX传递和细胞内控释的能力，从而在体外产生了强大且增强的抗肿瘤作用。这些结果证明，拟议的AS1411功能化[受电子邮件保护] @ [受电子邮件保护]可以成为有前途的针对癌症治疗的靶向药物递送平台。