In this study, we have surface-functionalized PEGylated-nanoliposomal doxorubicin (DOX) with anti-EpCAM (epithelial cell adhesion molecule) aptamer via post-insertion of anti-EpCAM aptamer-conjugated DSPE-mPEG2000 into Caelyx® (ED-lip). The size, charge, release profile, and cytotoxicity and cellular uptake of formulation were determined. The characterization of the ED-lip demonstrated the slightly increase in size and PDI along with the decrease in zeta potential which indicated that post-insertion efficiently done. The results of flow cytometry and fluorescent microscopy have shown that ED-lip enhanced the rate of cell uptake on C26 cell line compared to Caelyx®. The ED-lip also had more cytotoxic effects than Caelyx® which indicated the efficacy of anti-EpCAM aptamer as targeting ligand. The pharmacokinetic and tissue biodistribution of formulations in mice bearing C26 tumors demonstrated that ED-lip did not affect the distribution profile of DOX compared to Caelyx® in animal model. In addition, ED-lip effectively improved the tumor accumulation of DOX and promoted survival of animals compared to Caelyx®. These results suggest that the functionalization of Caelyx® with anti-EpCAM aptamer is promising in cancer treatment and merits further investigation.

中文翻译：

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抗Epcam适体（Syl3c）功能化脂质体用于阿霉素的靶向递送：携带C26结肠癌的小鼠的体内和体外抗肿瘤研究。

在这项研究中，我们通过将抗EpCAM适体偶联的DSPE-mPEG2000后插入Caelyx®（ED-lip）中，将具有抗EpCAM（上皮细胞粘附分子）适体的表面官能化的聚乙二醇化纳米脂质体阿霉素（DOX）。确定了制剂的大小，电荷，释放曲线，细胞毒性和细胞摄取。ED唇的特征表明，大小和PDI略有增加，同时zeta电位降低，这表明插入后可以高效完成。流式细胞仪和荧光显微镜的结果表明，与Caelyx®相比，ED-lip增强了C26细胞系细胞的摄取速率。ED-lip还具有比Caelyx®更多的细胞毒性作用，这表明抗EpCAM适体作为靶向配体的功效。制剂在患有C26肿瘤的小鼠中的药代动力学和组织生物分布证明，与动物模型中的Caelyx®相比，ED-lip不会影响DOX的分布。此外，与Caelyx®相比，ED-lip有效地改善了DOX的肿瘤积累并促进了动物的存活。这些结果表明，用抗EpCAM适体对Caelyx®的功能化在癌症治疗中很有前途，值得进一步研究。