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首页> 外文期刊>Nanoscale Research Letters >Anti-Epcam Aptamer (Syl3c)-Functionalized Liposome for Targeted Delivery Of Doxorubicin: In Vitro And In Vivo Antitumor Studies in Mice Bearing C26 Colon Carcinoma
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Anti-Epcam Aptamer (Syl3c)-Functionalized Liposome for Targeted Delivery Of Doxorubicin: In Vitro And In Vivo Antitumor Studies in Mice Bearing C26 Colon Carcinoma

机译:抗EPCAM适体(SYL3C) - 用于靶向递送多柔比星的功能化脂质体:体外和体内抗肿瘤研究轴承C26结肠癌

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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-mPEG_(2000)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.
机译:在该研究中,我们通过将抗EPCAM适体 - 缀合的DSPE-MPEG_(2000)的后插入到Caelyx中,用抗EPCAM(上皮细胞粘附分子)适体具有表面官能化的聚乙基化纳米脂素多柔比蛋白(DOX)。 (Ed-Lip)。测定了大小,充电,释放曲线和细胞毒性和细胞摄取。 ED-唇唇的表征证明了尺寸和PDI略微增加,以及Zeta电位的降低,表明插入后的能力。流式细胞术和荧光显微镜的结果表明,与Caelyx相比,Ed-Lip提高了C26细胞系上的细胞摄取率。 Ed-唇还具有比Caelyx更多的细胞毒性效果?这表明抗EPCAM适体作为靶向配体的疗效。轴承C26肿瘤的小鼠配方的药代动力学和组织生物分布表明,与Caelyx相比,Ed-唇唇不影响DOX的分布曲线?在动物模型中。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caelyx的功能化?抗EPCAM适体在癌症治疗中具有很大的进一步调查。

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