cRGD靶向阿霉素脂质体制备及其对Hela细胞的影响

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。

Preparation of cRGD modified doxorubicin liposomals and the targeting effects on Hela cells

Objective:To prepare doxorubicin liposomals modified with PEG and cRGD,and study physicochemical properties of liposomals along with targeting effects on Hela cells. Methods:Using pH gradient method to prepare the liposomes modified with cRGD. The characteristics were observed with TEM and UV spectrophotometer. The targeting effect was determined by immunofluorescence and flow cytometry on Hela cells,and cell apoptosis was measured by MTT assay and flow cytometry. Results:The particle size of liposomes was between 100-180 nm,and encapsulation ratio detected by UV spectrophotometer was 72%. The result of immunofluorescence and flow cytometry showed targeting effect of liposomes on Hela cells,which was significantly better than that of control group. Conclusion:These doxorubicin liposomes with high encapsulation ratio and small particle size exhibited an effect of cell targeting and cell penetrating,which might be a novel approach for specific and efficient intracellular drug delivery.