Abstract The purpose of this study was to optimize the preparation conditions of podophyllotoxin liposomes (PPT-Lips), and to investigate their effects on PC3 cells. PPT-Lips were prepared by using a thin-film dispersion method. In order to achieve maximum drug encapsulation efficiency (EE), the process and formulation variables were optimized by response surface methodology (RSM). The optimum preparation conditions were cholesterol to lecithin ratio of 3.6:40 (w/w), lipid to drug ratio of 15.8:1 (w/w), and the ultrasonic intensity of 35% (total power of 400 W). The experimental EE of PPT-Lips was 90.425%, which was consistent with the theoretically predicted value. The characterization studies showed that PPT-Lips were well-dispersible spherical particles with an average size of 106 nm and a zeta potential of –10.1 mV. A gradual and time-dependent pattern of PPT from liposomes was found in in vitro drug release with a cumulative release amount up to 70.3% in 24 h. Results of cell viability experiments on PC3 cells demonstrated that PPT-Lips exhibited more effective anticancer activity in comparison with free PPT. Therefore, PPT-Lips represent an efficient and promising drug delivery system for PPT.

中文翻译：

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响应面法优化负载鬼臼毒素脂质体的条件及其对PC3细胞的活性

摘要 本研究旨在优化鬼臼毒素脂质体（PPT-Lips）的制备条件，并研究其对PC3细胞的影响。PPT-Lips 是通过使用薄膜分散法制备的。为了实现最大的药物包封效率 (EE)，通过响应面方法 (RSM) 优化了工艺和配方变量。最佳制备条件为胆固醇与卵磷脂的比例为3.6：40（w/w），脂类与药物的比例为15.8：1（w/w），超声强度为35%（总功率400 W）。PPT-Lips的实验EE为90.425%，与理论预测值一致。表征研究表明，PPT-Lips 是一种分散性良好的球形颗粒，平均粒径为 106 nm，zeta 电位为 –10.1 mV。在体外药物释放中发现了脂质体 PPT 的逐渐和时间依赖性模式，24 小时内累积释放量高达 70.3%。PC3 细胞的细胞活力实验结果表明，与游离 PPT 相比，PPT-Lips 表现出更有效的抗癌活性。因此，PPT-Lips 代表了一种高效且有前景的 PPT 给药系统。