It is challenging but imperative to merge imaging agents and small molecule therapeutics into one nanoentity for diagnosis and treatment. Herein, we constructed polymeric nanoparticles for targeted delivery and combination chemotherapy, which formed through host–guest interactions among three elements: 1) β‐cyclodextrin polymer (poly‐β‐CD), as the backbone of nanoparticles; 2) two antitumor drugs—doxorubicin (DOX) and docetaxel (DTX); and 3) aptamers labeled with adamantane and fluorescein (Ad‐aptamer‐FAM), as recognition elements. First, polymeric nanoparticles, termed self‐assembled supramolecular nanoparticles (SSNPs), were formulated by combining hydrophobic DTX and DOX with poly‐β‐CD via host–guest interactions. Then, the surface of SSNPs modified the aptamer to acquire targeting ability; such nanoparticles were termed targeted self‐assembled supramolecular nanoparticles (T‐SSNPs). As evidenced by MTS assay data, T‐SSNPs exhibited significant selective cytotoxicity toward target cells. The results also indicated that combination drugs achieved a good synergistic effect with a combination index of 0.43. Thus, an effective and simple drug delivery system was constructed for targeted delivery and combination chemotherapy.

中文翻译：

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自组装的超分子纳米颗粒，用于靶向递送和联合化疗

将成像剂和小分子治疗剂合并为一个用于诊断和治疗的纳米实体是一项挑战，但势在必行。本文中，我们构建了用于靶向递送和联合化疗的聚合物纳米颗粒，它是通过三个要素之间的主客体相互作用形成的：1）β-环糊精聚合物（poly-β-CD），作为纳米颗粒的骨架；2）两种抗肿瘤药物-阿霉素（DOX）和多西他赛（DTX）；3）以金刚烷和荧光素（Ad-aptamer-FAM）标记的适体作为识别元素。首先，通过主客体相互作用将疏水性DTX和DOX与poly-β-CD结合在一起，配制了被称为自组装超分子纳米颗粒（SSNP）的聚合物纳米颗粒。然后，SSNPs的表面修饰适体以获得靶向能力。此类纳米颗粒称为靶向自组装超分子纳米颗粒（T-SSNPs）。MTS分析数据证明，T-SSNP对靶细胞表现出明显的选择性细胞毒性。结果还表明，组合药物达到了良好的协同作用，组合指数为0.43。因此，构建了有效且简单的药物递送系统用于靶向递送和联合化疗。