论文部分内容阅读
目的 :制备含有二硫键的环形RGD肽(cyclic RGD peptide,c RGD)修饰长循环阿霉素主动靶向脂质体,对其理化性质、靶向性和对Hela细胞的影响进行评价。方法:用DSPE-PEG-NHS耦联c RGD,插入采用p H法制备的磁性长循环阿霉素脂质体中制备主动靶向脂质体;利用透射电镜、紫外分光光度计和质谱仪进行表征;流式细胞术和免疫荧光验证其靶向性;MTT和流式细胞术验证其对Hela细胞的影响。结果:制备的主动靶向脂质体粒径在100~180 nm之间,包封率达到72%,免疫荧光及流式细胞术均显示其对Hela细胞具有一定靶向性,且能显著诱导Hela细胞凋亡。结论:本研究制备的c RGD靶向阿霉素脂质体具有一定靶向性,能显著提高其杀伤肿瘤细胞的作用。这种具有靶向及穿透功能的脂质体载体可能为肿瘤治疗提供一个新方法。
OBJECTIVE: To prepare long-acting doxorubicin active cyclic liposomes by cyclic RGD peptide (c RGD) containing disulfide bond, and to evaluate its physical and chemical properties, targeting ability and effect on Hela cells. METHODS: C RGD was coupled with DSPE-PEG-NHS and inserted into magnetic long circulating doxorubicin liposomes prepared by p H method to prepare active targeting liposomes. Transmission electron microscopy, ultraviolet spectrophotometer and mass spectrometer Characterization; flow cytometry and immunofluorescence to verify its targeting; MTT and flow cytometry to verify the impact of Hela cells. Results: The size of active targeting liposomes was between 100 and 180 nm with an entrapment efficiency of 72%. Both immunofluorescence and flow cytometry showed that the targeting liposomes had certain targeting ability to Hela cells and could be induced significantly Hela cell apoptosis. CONCLUSION: Targeted doxorubicin liposomes prepared in this study have some targeting properties, which can significantly improve the killing effect of tumor cells. This targeting and penetrating liposome carrier may provide a new approach to cancer therapy.