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穿膜肽GGPFV修饰的柔红霉素/薯蓣皂苷脂质体的处方优化及细胞毒性研究
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| 篇名： | 穿膜肽GGPFV修饰的柔红霉素/薯蓣皂苷脂质体的处方优化及细胞毒性研究 |
| TITLE： | Formulation Optimization and Cytotoxicity Study of GGPFV-modified Daunorubicin/dioscin Liposomes |
| 摘要： | 目的：制备穿膜肽GGPFV修饰的柔红霉素/薯蓣皂苷脂质体，对其处方进行优化，并初步评价其对乳腺癌细胞的体外毒性。方法：采用薄膜分散法和硫酸铵水化法，将柔红霉素和薯蓣皂苷包载其中，在表面以聚乙二醇-二硬脂酰基磷脂酰乙醇胺2000（DSPE-PEG2000）-GGPFV修饰，制备GGPFV修饰的柔红霉素/薯蓣皂苷脂质体。以包封率为指标，采用Box-Behnken响应面法优化处方中水化体积、胆固醇用量和柔红霉素用量；测定按最优处方制备的3批脂质体的包封率。比较柔红霉素/薯蓣皂苷脂质体、GGPFV修饰的柔红霉素/薯蓣皂苷脂质体和空白脂质体作用后对人乳腺癌MDA-MB-435S细胞存活率的影响。结果：最优处方为水化体积5mL、胆固醇4mg、蛋黄卵磷脂22mg、柔红霉素0.55mg、薯蓣皂苷0.85mg、DSPE-PEG20003.5mg、DSPE-PEG2000-GGP-FV2mg。所制3批脂质体中，柔红霉素的包封率为（96.21±1.54）％，薯蓣皂苷的包封率为（95.39±2.48）％。体外细胞毒性试验显示，GGPFV修饰的柔红霉素/薯蓣皂苷脂质体对MDA-MB-435S细胞的抑制作用显著强于柔红霉素/薯蓣皂苷脂质体（P＜0.05），膜材无细胞毒性。结论：成功制得GGPFV修饰的柔红霉素/薯蓣皂苷脂质体，其对人乳腺癌MDA-MB-435S细胞的体外抑制作用明显增强。 |
| ABSTRACT： | OBJECTIVE：To prepare GGPFV-modified Daunorubicin/dioscin liposomes ，and to optimize their formulation and to preliminarily evaluate their cytotoxicity to breast cancer cells in vitro . METHODS ：Daunorubicin and diosgenin were wrapped by thin film dispersion method and ammonium sulfate hydration method ；the surface was modified with DSPE-PEG2000-GGPFV to prepare GGPFV-modified Daunorubicin/dioscin liposomes. Taking encapsulation rate as index ，Box-Behnken response surface methodology was used to optimize the film hydration volume ，cholesterol amount and daunorubicin amount in the formulation. The entrapment efficiency of 3 batches of liposomes prepared according to the optimal formulation was determined. The effects of Daunorubicin/dioscin liposomes ，GGPFV-modified Daunorubicin/dioscin liposomes and blank liposomes on the survival rate of human breast cancer MDA-MB- 435S cells were compared. RESULTS ：The optimal formulation was as film hydration volume of 5 mL，cholesterol of 4 mg，yolk lecithin of 22 mg，daunorubicin of 0.55 mg，dioscin of 0.85 mg，DSPE-PEG2000 of 3.5 mg， DSPE-PEG2000-GGPFV of 2 mg. The encapsulation rate of daunorubicin was （96.21±1.54）％ and that of dioscin was （95.39± 2.48）％ in the 3 batches of liposomes prepared. The in vitro cytotoxicity tests showed that the inhibition effect of GGPFV-modified Daunorubicin/dioscin liposome on MDA-MB-435S cells was significantly stronger than that of Daunorubicin/dioscin liposome （P＜ 0.05）. There was no cytotoxicity in the membrane. CONCLUSIONS ：GGPFV-modified Daunorubicin/dioscin liposomes are successfully prepared ，and its inhibitory effect on human breast cancer MDA-MB- 435S cells in vitro was significantly enhanced. |
| 期刊： | 2020年第31卷第21期 |
| 作者： | 姚雪敏，荆鸣，蔡馥伊，孔亮，李学涛 |
| AUTHORS： | YAO Xuemin ，JING Ming，CAI Fuyi，KONG Liang，LI Xuetao |
| 关键字： | 脂质体；GGPFV；柔红霉素；薯蓣皂苷；处方优化；Box-Behnken响应面法；细胞毒性 |
| KEYWORDS： | Liposome；GGPFV；Daunorubicin；Dioscin；Formulation optimization ；Box-Behnken design response surface |
| 阅读数： | 279 次 |
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