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目的:构建用于治疗脑部肿瘤的复方柔红霉素氯喹脂质体,对其理化性质进行表征并考察其对脑胶质瘤细胞及脑胶质瘤干细胞的抑制效应。方法:以柔红霉素为抗肿瘤药、氯喹为抗耐药调节剂,制备复方柔红霉素氯喹脂质体,并对该脂质体进行理化表征;在脑胶质瘤细胞及脑胶质瘤干细胞上考察其抑制效应。结果:构建的复方柔红霉素氯喹脂质体经HPLC检测,对柔红霉素和氯喹的包封情况良好,经透射电镜和原子力显微镜观察形态为圆形球囊状,经粒径仪测定粒径约为95 nm,粒径均一,分散情况良好,电位略呈负电性。在体外细胞毒实验中,复方柔红霉素氯喹脂质体对脑胶质瘤细胞及脑胶质瘤干细胞呈现明显增强的抑制效果。结论:本研究成功构建了复方柔红霉素氯喹脂质体,这种联合给药的长循环脂质体可望有效增强化疗药物对脑胶质瘤细胞和脑胶质瘤干细胞的生长抑制作用。
OBJECTIVE: To construct the compound daunorubicin-chloroquine liposome for the treatment of brain tumors and to characterize its physicochemical properties and investigate its inhibitory effect on glioma cells and glioma stem cells. Methods: Daunorubicin as anticancer drug and chloroquine as anti-resistance modifier were used to prepare compound daunorubicin-chloroquine liposomes. The liposomes were identified by physical and chemical methods. In glioma cells and brain glue Tumor stem cells were investigated for their inhibitory effect. Results: The results showed that the encapsulated daunorubicin and chloroquine were well encapsulated by HPLC. The encapsulated daunorubicin and chloroquine were in good shape. The shape of the liposome was observed as circular balloon by transmission electron microscopy and atomic force microscopy. Particle size of about 95 nm, uniform particle size, good dispersion, the potential is slightly negative. In vitro cytotoxicity experiments, compound daunorubicin chloroquine liposomes glioma cells and glioma stem cells showed significantly enhanced inhibitory effect. CONCLUSION: The compound daunorubicin-chloroquine liposome has been successfully constructed in this study. The long-circulating liposomes combined with it are expected to enhance the growth inhibitory effect of chemotherapeutic drugs on glioma cells and glioma stem cells .