Characterization of amphiphilic dendrimer modified PEG-PLA nanoparticles prepared by a double emulsion-solvent evaporation method  

两亲性树枝状分子改造的PEG-PLA纳米粒的制备及其表征（英文）

作　　者：李欣[1] 庞宁[1] 李骥[1] 齐宪荣[1] 

机构地区：[1]北京大学医学部药学院药剂学系分子药剂学与新释药系统北京市重点实验室,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》2017年第7期521-527,共7页中国药学（英文版）

基　　金：National Natural Science Foundation of China(Grant No.81473156,81673365,81273454);Doctoral Foundation of the Ministry of Education(Grant No.20130001110055);National Key Basic Research Program(Grant No.2013CB932501)

摘　　要：Drug delivery by nanocarriers requires characterizations of suitable particle size, high drug loading and safety. In this work, we prepared an amphiphilic dendrimer modified PEG-PLA mixed nanoparticles（NPs） by a double emulsion-solvent evaporation（DESE） method. The particle size and drug encapsulation efficacy（EE） were compared to evaluate and optimize the preparation parameters. The mixed NPs had average size ranging from（102±1） nm to（137±5） nm, and the zeta potential turned to positive with incorporation of the amphiphilic dendrimer. The NPs showed different EE of docetaxel（DTX） and paclitaxel（PTX） with higher affinity to more lipophilic PTX. The blank mixed NPs showed little cytotoxicity, and the DTX-loaded NPs could effectively facilitate the antiproliferation activity on PC-3 cells. The NPs could be used as an effective drug delivery system, and its anti-tumor effect is worthy of further study.递送药物的纳米载体需要合适的粒度,高的药物负载效率以及良好的安全性。聚乙二醇-聚(D,L-丙交酯)(PEG-PLA)共聚物因其良好的生物相容性,载药能力和长循环时间,被广泛用于药物递送,而将脂质等其他材料掺入到PEG-PLA纳米粒体系中可以进一步改善其特性。我们通过双重乳液–溶剂蒸发法制备了两亲树枝状聚合物修饰的PEG-PLA混合纳米颗粒,通过比较粒径和药物包封率对制备参数进行评价和优化。使用不同的制备参数,混合纳米粒的平均尺寸分别分布在(102±1)nm和(137±5)nm,掺入两亲树枝状分子后,ζ电位转化为阳性。该纳米粒对紫杉醇的包封率高于多西紫杉醇。空白混合纳米粒没有显示出细胞毒性,而多西紫杉醇负载的纳米粒可有效促进抗肿瘤细胞增殖活性。该纳米粒可望成为有效的药物输送系统。

关 键 词：PEG-PLA nanoparticles DOCETAXEL PACLITAXEL Double emulsion-solvent evaporation method Amphiphilic dendrimer 

分 类 号：R943[医药卫生—药剂学]