To overcome the lack of selectivity and nonspecific biodistribution of drugs in the body, targeted delivery of chemotherapeutic agents with aptamers is a very effective method. In this strategy, aptamers could be specifically identified and attach to targeted molecules on the cancerous cells and deliver the chemotherapeutic agents to desired tissue with minimal or no damage to the normal cells. In this study, we designed anti-epithelial cell adhesion molecule (EpCAM) RNA aptamer conjugated PEGylated liposomal doxorubicin (ER-lip) to investigate its in vitro and in vivo anticancer abilities. Data showed that EpCAM aptamer was able to enhance cell uptake and cytotoxic effects of Dox in C26 cell line. The biodistribution study indicated that ER-lip enhanced the tumor accumulation of Dox compared to Caelyx. Also, double staining of isolated tumor cells with anti-CD44-PE-cy5 and anti-EpCAM Cy-7 antibodies indicated that tumor cells expressed a high level of EpCAM⁺ CD44⁺ cells (p ≤ .001) compared to cultured C26 cell line. in vivo results showed that ER-lip promoted survival and reduced tumor growth rate in animal model compared to Caelyx. In conclusion, these results suggested that the ER-lip could be served as promising formulation for the treatment of cancers with the high expression of EpCAM.

中文翻译：

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抗上皮细胞粘附分子 RNA 适体偶联脂质体阿霉素作为结肠癌肿瘤模型小鼠的有效靶向治疗

为了克服药物在体内缺乏选择性和非特异性生物分布的问题，靶向递送具有适体的化学治疗剂是一种非常有效的方法。在这种策略中，适体可以被特异性识别并附着在癌细胞上的靶向分子上，并将化学治疗剂递送至所需组织，而对正常细胞的损伤最小或没有。在这项研究中，我们设计了抗上皮细胞粘附分子 (EpCAM) RNA 适体缀合的聚乙二醇化脂质体阿霉素 (ER-lip) 来研究其体外和体内抗癌能力。数据显示，EpCAM 适体能够增强 Dox 在 C26 细胞系中的细胞摄取和细胞毒作用。生物分布研究表明，与 Caelyx 相比，ER-lip 增强了 Dox 的肿瘤积累。还，⁺ CD44 ⁺细胞 ( p  ≤ .001) 与培养的 C26 细胞系相比。体内结果表明，与 Caelyx 相比，ER-lip 在动物模型中促进了存活并降低了肿瘤生长率。总之，这些结果表明，ER-lip 可作为治疗具有高表达 EpCAM 的癌症的有前景的制剂。