穗花杉双黄酮PLGA纳米粒的制备、表征及其体外抗肿瘤活性  

Preparation,characterization,and in vitro antitumor activity of amentoflavone⁃PLGA nanoparticles

作　　者：庄子钰 张帅[1] 王渤达 陈拙拙 沈丽霞 赵永明[1] ZHUANG Ziyu;ZHANG Shuai;WANG Boda;CHEN Zhuozhuo;SHEN Lixia;ZHAO Yongming(School of Pharmaceutical Sciences,Hebei North University,Zhangjiakou 075000,China;Hebei Key Laboratory of Neuropharmacology)

机构地区：[1]河北北方学院药学院,张家口075000 [2]河北省神经药理学重点实验室

出　　处：《山西医科大学学报》2024年第11期1437-1442,共6页Journal of Shanxi Medical University

基　　金：张家口市重点研发计划项目(2221184D)。

摘　　要：目的 制备穗花杉双黄酮(amentoflavone,AF)聚乳酸-羟基乙酸共聚物[poly(lactic-co-glycolic acid),PLGA]纳米粒(AF-PLGA-NPs),对制备的AF-PLGA-NPs进行表征,并考察体外抗肿瘤活性。方法 以AF为模型药,PLGA为材料,采用纳米沉淀法制备AF-PLGA-NPs。以PLGA用量、水相/油相体积比和载体/药物比为自变量,包封率为评价指标,采用Box-Behnken设计-效应面法优化AF-PLGA-NPs处方。采用激光粒度仪和透射电镜对AF-PLGA-NPs的粒径、zeta电位、多分散指数(polydispersity index,PDI)及形态进行表征;MTT实验考察AF及AF-PLGA-NPs对Hep G2、A549和HT29细胞体外增殖抑制作用。结果 AF-PLGA-NPs最佳处方为:PLGA用量为13.1 mg,水相/油相比为8.2∶1,载体/药物比为14.7∶1,此时包封率为(55.2±1.06)%,粒径为(176.3±3.7)nm,zeta电位(-29.8±0.98)m V,PDI为0.16±0.01。透射电镜显示制备的纳米粒圆整规则,粒径分布均匀。与AF相比,AF-PLGA-NPs对Hep G2、A549和HT29细胞的IC_(50)值更低,表明AF-PLGA-NPs对肿瘤细胞具有更强的抑制作用。结论 AF-PLGA-NPs制备工艺简便可行,制成纳米粒后可提高AF的体外抗肿瘤活性。Objective To prepare and characterize the amentoflavone(AF)-poly(lactic-co-glycolic acid)(PLGA)nanoparticles(AF-PLGA-NPs),and evaluate their in vitro anti-tumor activity.Methods AF-PLGA-NPs were prepared by nanoprecipitation method,with AF as model drug and PLGA as polymer matrix.The formulation of AF-PLGA-NPs was optimized using a Box-Behnken design,with PLGA amount,water/oil ratio,and drug/carrier ratio as independent variables and encapsulation efficiency as the response vari-able.The particle size,the zeta potential,the polydispersity index,and the morphology of AF-PLGA-NPs were characterized by laser particle size analysis and transmission electron microscopy(TEM).The in vitro inhibitory effects of AF and AF-PLGA-NPs on prolifera-tion of HepG2,A549,and HT29 cells were evaluated by the MTT assay.Results The optimal formulation was as follows:PLGA 13.1 mg,water/oil ratio of 8.2∶1,carrier/drug ratio of 14.7∶1.The encapsulation efficiency was(55.2±1.06)%,the particle size was(176.3±3.7)nm,zeta potential was(-29.8±0.98)mV,and PDI was 0.16±0.01.The TEM images demonstrated that the nanoparticles exhibited a spherical morphology with a narrow size distribution.Compared to AF,AF-PLGA-NPs exhibited lower IC_(50) against HepG2,A549,and HT29 cells,indicating stronger inhibitory effect on tumor cells.Conclusion The preparation process of AF-PLGA-NPs is simple and feasible,and the prepared nanoparticles could significantly enhance the in vitro antitumor activity of AF.

关 键 词：穗花杉双黄酮 聚乳酸-羟基乙酸共聚物 纳米粒 BOX-BEHNKEN设计 表征 高效液相色谱法 

分 类 号：R917[医药卫生—药物分析学]