木犀草素功能性脂质体制备处方工艺优化及其对Hep3B细胞的影响OA
Optimization of the preparation process for functional liposomes containing luteolin and their effects on Hep3B cells
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 methodology-optimized 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.
娄思思;李风叶;杨海龙
赣南医科大学创新与转化医学研究院,江西 赣州 341000赣南医科大学创新与转化医学研究院,江西 赣州 341000赣南医科大学创新与转化医学研究院,江西 赣州 341000
医药卫生
木犀草素转铁蛋白脂质体响应面优化Hep3B细胞
LuteolinTransferrinLiposomesResponse surface optimizationHep3B cells
《赣南医科大学学报》 2026 (5)
421-428,8
江西省国际科技合作项目(20232BBH80011)赣州市科技计划项目(2024RC05)
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