转铁蛋白修饰的姜黄素脂质体的制备及体外抗肿瘤活性

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。

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

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.