赣南医科大学学报

目的：优化转铁蛋白修饰的木犀草素（Luteolin,LUT）功能性脂质体的制备工艺，并考察其对Hep3B细胞的影响。方法：采用薄膜分散法制备转铁蛋白修饰的木犀草素脂质体（Transferrin-modified luteolin-loaded liposomes,TF-LUT@LIP），以包封率为指标，通过单因素考察和响应面优化法优选最佳制备工艺，并通过CCK-8法和细胞摄取试验考察其对Hep3B细胞活性及摄取情况的影响。结果：最佳处方制备工艺条件为：胆脂比为1∶6.906，药脂比为1∶21.267，超声破碎功率为38%（总功率为650 W），水化温度为50℃，响应面法优化后的木犀草素脂质体平均包封率为96.94%；且当靶向分子投入量为3%时，所制备的TF-LUT@LIP包封率达（95.31±0.03）%，平均粒径为（184.53±0.61） nm，电位为（-23.800±0.500） mV，形态圆整，稳定性良好；TF-LUT@LIP对Hep3B细胞的抑制作用强于游离LUT，并呈浓度依赖性，且与非靶向脂质体相比，TF-LUT@LIP的摄取行为更明显。结论：按照最优制备工艺制备的TF-LUT@LIP包封率高、形态规整、粒径均匀，且对Hep3B细胞的抑制作用明显，细胞摄取行为良好。

Objective : To optimize the preparation process of transferrin modified functional liposomes of magnolol and to investigate their effects on Hep3B cells. Methods : Transferrin-modified luteolin-loaded liposomes(TF-LUT@LIP) was synthesized using the thin-film dispersion method. The encapsulation efficiency served as the evaluation criterion. Optimal preparation conditions were determined through single-factor experiments and response surface optimization. The effects on Hep3B cell viability and uptake were assessed via CCK-8 assays and cellular uptake experiments. Results : The optimal formulation preparation conditions are as follows: bile-to-lipid ratio of 1∶6. 906, drug-to-lipid ratio of 1∶21. 267, ultrasonication power of 38%(total power 650 W), and hydration temperature of 50 ℃. The response surface methodologyoptimized luteolin liposomes achieved an average encapsulation efficiency of 96. 94%. When the target molecule loading was 3%, the prepared TF-LUT@LIP exhibited(95. 31±0. 03)%, an average particle size of(184. 53±0. 61) nm, a zeta potential of （-23. 800±0. 500） mV, and excellent stability. TF-LUT@LIP exhibited stronger concentration-dependent inhibitory effects on Hep3B cells than free luteolin(LUT). Compared to non-targeted liposomes, TF-LUT@LIP demonstrated significantly enhanced uptake behavior. Conclusion : TF-LUT@LIP prepared via the optimal synthesis process exhibits high encapsulation efficiency, uniform morphology, and consistent particle size distribution. It demonstrates significant inhibitory effects on Hep3B cells and exhibits favorable cellular uptake behavior.