RGD序列修饰的PEG化脂质体对肿瘤细胞靶向作用的初步研究

The preliminary study on RGD modied PEGylated liposomes in targeting tumor cells

目的本研究中,我们构建了一个RGD修饰的封装香豆素-6的聚乙二醇化脂质体(RGD-PLS-C6),通过细胞实验探讨其对过表达整合素α5β1胃癌细胞的靶向效果。方法通过酰胺化反应将RGD偶联到聚乙二醇链的末端,检测制备好脂质体的特征和稳定性。利用流式细胞术和激光共聚焦显微镜分析RGD-PLS-C6的肿瘤靶向作用。结果在胃癌细胞中,RGD-PLS-C6结合到胃癌细胞的荧光强度明显高于PLS-C6;而在正常对照细胞中两者的荧光强度均比较弱,荧光强度与PLS-C6处理的胃癌细胞无明显差异。结论实验表明RGD-PLS可作为运输荧光染料的靶向载体,具有一定的应用前景。

Objective In this study we developed a RGD modied PEGylated liposomes-eneapsulated coumarin-6 （RGD-PLS-C6） system and investigated the targeting effect on gastric cancer cells with overexpression of integrin α5β1. Methods RGD was covalently conjugated to the distal end of DSPE-PEG2000-NH2 lipid by amide bound. The characteristics and stability of prepared liposomes were measured. The targeting effects of RGD were detected by using flow cytometry and confocal microscopy. Results The fluorescence intensity in gastric cancer ceils treated with RGD-PLS-C6 was obviously higher than that of those ceils treated with PLS-C6 ; however, the fluorescence intensity of normal cells treated with RGD-PLS-C6 and PLS-C6 was weak, as well as that of the gastric cancer cells treated with PLS-C6. Conclusions The experimental data suggested that RGD-PLS might be a fluorescent dye delivery system for targeting of gastric carcinoma and worth wide application.