转铁蛋白修饰的姜黄素脂质体的制备及体外抗肿瘤活性  

Preparation and anti-tumor activity in vitro of transferrin modified curcumin liposomes

作　　者：季珂 韩华 韩冰 梁绿圆 祝侠丽[1] 关延彬[1] JI Ke;HAN Hua;HAN Bing;LIANG Lyu-yuan;ZHU Xia-li;GUAN Yan-bin(School of Pharmacy,Henan University of TCM,Zhengzhou 450040,China;School of Pediatrics,Henan University of TCM,Zhengzhou 450040,China)

机构地区：[1]河南中医药大学药学院,河南郑州450040 [2]河南中医药大学儿科医学院,河南郑州450040

出　　处：《中草药》2022年第18期5649-5656,共8页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(81803740);河南省科技攻关项目(182102310096);河南省高等学校重点科研项目(18B360002);河南省中医药科学研究专项课题(20-21ZY2150);河南省高校国家级大学生创新创业训练计划项目(202110471009)。

摘　　要：目的 制备转铁蛋白(transferrin,Tf)修饰的姜黄素(curcumin,Cur)脂质体(Tf-Cur-Lip),并研究其理化性质和体外抗肿瘤活性。方法 采用薄膜分散法制备Tf-Cur-Lip,对其形态、粒径、多分散性指数、包封率、载药量、体外释放等进行表征;以人前列腺癌DU154细胞为模型进行细胞抑制率实验与细胞摄取实验。结果 所制得的Tf-Cur-Lip呈类球形,大小分布均匀,平均粒径为(68.27±0.36)nm,多分散指数为0.194±0.050,平均包封率与载药量分别为(98.13±0.38)%与(2.94±0.38)%。体外释放研究表明,Tf-Cur-Lip相比游离姜黄素具有一定缓释效果。MTT实验结果表明Tf-Cur-Lip对DU145细胞的抑制作用显著高于游离姜黄素,与非靶向姜黄素脂质体(Cur-Lip)相比,转铁蛋白的修饰明显增加了DU145细胞对脂质体的摄取效率。结论 成功制备了Tf-Cur-Lip,该脂质体能够提高肿瘤靶向性,具有一定的抗肿瘤活性。Objective To prepare transferrin(Tf) modified curcumin(Cur) liposomes(Tf-Cur-Lip) and evaluate its physicochemical properties and antitumor activity in vitro. Methods The Tf-Cur-Lip was prepared by thin film dispersion method, followed by characterization of the morphology, particle size, polydispersity index(PDI), encapsulation efficiency, drug loading amount and in vitro release. The anti-proliferative effect and cellular uptake of Tf-Cur-Lip were studied in DU145 cells. Results The prepared Tf-Cur-Lip showed spherical morphology, and the average particle size was(68.27 ± 0.36) nm and uniform distribution with narrow PDI was(0.194 ± 0.050). The encapsulation efficiency and drug loading amount were(98.13 ± 0.38)% and(2.94±0.38)%,respectively. The in vitro release studies showed that Tf-Cur-Lip has a sustained-release property compared with free Cur. MTT assay showed that the inhibitory effect of Tf-Cur-Lip on DU145 cells was significantly higher than that of free Cur. Tf-Cur-Lip showed significantly increased cellular uptake than curcumin-loaded liposomes(Cur-Lip) in DU145 cells. Conclusion Tf-Cur-Lip were successfully prepared, which can improve tumor targeting capability with enhanced anti-tumor activity.

关 键 词：姜黄素 转铁蛋白 脂质体 抗肿瘤活性 薄膜分散法 靶向性 

分 类 号：R283.6[医药卫生—中药学]