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.
作者
季珂
韩华
韩冰
梁绿圆
祝侠丽
关延彬
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)
出处
《中草药》
CAS
CSCD
北大核心
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)。
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
curcumin
transferrin
liposome
anti-tumor activity
thin film dispersion method
targeting
