姜黄素聚乙二醇-聚乳酸嵌段共聚物纳米粒的制备及其质量评价

目的制备姜黄素(Cur)聚乙二醇-聚乳酸嵌段共聚物(mPEG-PLA)纳米粒(Cur-mPEG-PLA-NPs),并考察其理化性质、体外释药特性及抗肿瘤活性。方法采用乳化溶剂挥发法制备Cur-mPEG-PLA-NPs,通过正交设计优化处方工艺。利用透射电子显微镜观察纳米粒形态;激光粒度仪考察其粒径和Zeta电位;超速离心法测定其包封率及载药量;透析法考察其体外释药特性;四甲基偶氮唑盐(MTT)法考察其对人肝癌细胞SMMC-7721的抑制作用。结果根据优化处方工艺制备的Cur-mPEG-PLA-NPs外观呈圆形或类圆形,平均粒径为(129.24±1.45)nm,包封率和载药量分别为(82.15±1.07)%和(4.03±0.11)%;体外释药符合Weibull方程;与原料药Cur比较,Cur-mPEG-PLA-NPs对SMMC-7721细胞具有更强的抑制作用(P<0.05)。结论乳化溶剂挥发法可成功制备Cur-mPEG-PLA-NPs,为Cur新剂型的研究开发提供了实验基础。

Preparation of curcumin-loaded mPEG-PLA nanoparticles and its quality evaluation

Objective To prepare curcumin-loaded methoxy polyethylene glycol-polylactic acid nanoparticles (Cur-mPEG-PLA- NPs), to characterize their physicochemical properties, and to study the in vitro release behavior and antitumor activity on hepatoma cells SMMC-7721. Methods The Cur-mPEG-PLA-NPs were prepared by emulsification-solvent evaporation method and the formulation was optimized through orthogonal test. The transmission electron microscope was used to observe the particle appearance, Zetasizer instrument was used to detect the diameter and Zeta potential, and ultracentrifugation was utilized to determine entrapment rate and drug-loading rate. Dynamic dialysis method was used to study the in vitro release behavior of the NPs. The antitumor activity on SMCC-7721 cells was determined by MTT method. Results The optimal NPs were round with the nanometric size of (129.24 ± 1.45) nm, high entrapment rate of (82.15 ± 1.07) %, and drug-loading rate of (4.03 ± 0.11) %. The in vitro release behavior showed the accordance with Weibull equation. Compared with free Cur, Cur-mPEG-PLA-NPs showed stronger cytotoxicity and inhibition on hepatoma cells SMMC-7721 (P < 0.05). Conclusion The emulsification-solvent evaporation method could be used to prepare Cur-mPEG-PLA-NPs, which could lay the foundation for the research on novel Cur preparations.