In this study, we propose doxorubicin (DOX) loaded oligonucleotides (ONTs) attached to gold nanoparticles (AuNPs) as a drug delivery system for cancer chemotherapy. DOX is one of the representative cancer chemotherapy agents and is widely used by many researchers as a chemotherapy agent in the drug delivery system. Due to the advantages of AuNPs such as simple steps in synthesis, high surface-area-to-volume ratio, and biocompatibility, we utilized AuNPs as drug delivery vehicle. AuNPs were synthesized by chemical reduction to be 13 nm diameter. The G-C rich oligonucleotides were used both for drug loading sites and AuNPs capping agents.

80% of DOX in solution could be bound to ONTs on AuNPs to became DOX-loaded AuNPs coated with ONTs (Doxorubicin-Oligomer-AuNP, DOA), and about 28% of loaded DOX was released from the as-prepared DOA. Confocal microscopy observation showed that DOA was well transported into cells, and finally the DOX was released into the cell nucleus. The drug's efficacies such as in vitro cytotoxicity and in vivo tumor growth inhibition were demonstrated with SW480 colon cancer cell line and a xenograft mouse model. MTT assay was performed to see the cytotoxicity effect on SW480 cells treated with DOA for 24 h, and the cell viability was determined to be 41.77% (p < 0.001). When DOA was administered regularly to a tumor bearing mouse, the tumor growth inhibition degree was examined by measuring the tumor size. The treatment-control (T/C) ratio was found to be 0.69. Thus, our results suggest the use of DOAs as promising drug delivery systems for colorectal cancer therapy.

在这项研究中，我们建议将附有阿霉素（DOX）的寡核苷酸（ONT）附着到金纳米颗粒（AuNPs）上，作为癌症化学疗法的药物递送系统。DOX是代表性的癌症化学治疗剂之一，被许多研究人员广泛用作药物输送系统中的化学治疗剂。由于AuNPs的优点，例如合成步骤简单，高表面积/体积比和生物相容性，我们将AuNPs用作药物传递载体。通过化学还原合成到13nm直径的AuNP。富含GC的寡核苷酸可用于载药位点和AuNPs封端剂。

溶液中80％的DOX可以与AuNPs上的ONT结合，从而成为用ONT（阿霉素-低聚物-AuNP，DOA）涂覆的DOX负载的AuNP，并且约28％的负载DOX从制备的DOA中释放出来。共聚焦显微镜观察表明，DOA可以很好地转运到细胞中，最后DOX释放到细胞核中。该药物的功效，例如体外细胞毒性和体内用SW480结肠癌细胞系和异种移植小鼠模型证明了肿瘤的生长抑制。进行MTT测定以观察对用DOA处理24小时的SW480细胞的细胞毒性作用，并且确定细胞存活率为41.77％（p ＜0.001）。当定期将DOA给药于荷瘤小鼠时，通过测量肿瘤大小来检查肿瘤生长抑制程度。发现处理控制（T / C）比为0.69。因此，我们的结果表明，DOA可以用作大肠癌治疗的有希望的药物递送系统。