葡萄糖受体靶向的钆喷酸葡胺长循环脂质体的肿瘤细胞靶向研究

Glucose-Receptor targeting Long-circulating Gd-DTPA liposomes targeting to Tumor cell

目的:制备葡萄糖受体靶向的钆喷酸葡胺(Gd-DTPA)长循环脂质体,并研究其对高表达葡萄糖受体肿瘤细胞的靶向性。方法:合成新型含葡萄糖表面活性剂(N-棕榈酰葡萄糖胺),利用逆向蒸发法制备Gd-DTPA脂质体、PEG修饰Gd-DTPA脂质体、葡萄糖修饰Gd-DTPA脂质体以及葡萄糖PEG修饰Gd-DTPA脂质体。将4种脂质体分别与前列腺癌细胞一起培养,用MRI检测前列腺癌细胞摄取的Gd-DTPA浓度。结果:成功合成新型含葡萄糖表面活性剂(N-棕榈酰葡萄糖胺),以及制备4种Gd-DTPA脂质体。前列腺癌细胞对4种脂质体都有摄取,每种脂质体MRI检测的SE-T1W信号值分别为Gd-DT-PA脂质体362、PEG修饰Gd-DTPA脂质体299、葡萄糖修饰Gd-DTPA脂质体397、葡萄糖PEG修饰Gd-DTPA脂质体377。结论:葡萄糖的修饰有利于脂质体对肿瘤细胞的靶向。

OBJECTIVE To repare glucose receptor targeting long cycle of Gd - DTPA liposomes and to study the targeting the tumor cells with high express glucose receptors. METHODS New surfactant containing glucose （N Palmitoyl effect on Glucosamine） was synthesized, and Gd-DTPA liposomes, PEG-modified Gd-DTPA liposomes, glucose-modified Gd-DTPA liposomes and glucose PEG-modified Gd-DTPA liposomes were prepared using reverse-phase evaporation. Four types of lipo somes were cultured with prostate cancer cells respectively, and then Gd DTPA concentrations of prostate cancer were detected by MRI. RESULTS A new glucose-containing surfactant （NPG） was synthesized, and the four Gd-DTPA liposomes were prepared successfully. These four liposomes could be taken by prostate cancer cells. SE-T1W signal values of each liposome by MRI detection were： Gd-DTPA liposomes362, PEG-modified Gd-DTPA liposomes299, glucose-modified Gd-DTPA liposomes 397, glucose PEG-modified Gd-DTPA liposomes377. CONCLUSION Targeting to tumor cells of Liposome can be improved by glucose modification.