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工程科学与技术:2016,48(3):202-208
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聚天冬氨酸苄酯修饰的泊洛沙姆纳米粒制备和表征
(1.四川大学化工学院制药与生物工程系;2.四川大学华西药学院药物化学系)
Preparation and characterization of the PBLA-POLO-PBLA nanoparticles
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投稿时间:2015-08-26    修订日期:2015-11-19
中文摘要: 本研究的目的是通过泊洛沙姆188引发L-天冬氨酸-β-苄酯-N-羧酸酐(BLA-NCA)开环聚合,合成一种新型的药物载体材料PBLA-POLO-PBLA嵌段共聚物。利用核磁共振(1H-NMR)、傅里叶变换红外光谱法(FTIR)和凝胶渗透色谱(GPC)对合成的聚合物结构和分子量进行表征;运用CCK-8法研究了聚合物材料对A549的细胞毒性。采用乳化溶剂蒸发法制备伐昔洛韦(VACV)聚合物纳米粒并对其理化性质进行了研究。动态光散射粒度仪(DLS)和透射电子显微镜(TEM)结果显示该载药纳米粒的尺寸为200nm左右, 具有圆球形态并且分散性能良好。用高效液相色谱法测得其载药量为4.36%,以透析法观察到载药纳米粒在磷酸缓释溶液中96h时释放达到70.22%,具有明显缓释作用。因此,PBLA-POLO-PBLA嵌段共聚物在纳米载药系统中作为药物载体有着良好的应用前景。
Abstract:The aim of the present study was designing a novel drug carrier system composed of the block copolymer PBLA-POLO-PBLA via ring-opening polymerization of the β-benzyl-Lasparate N-carboxyanhydride (BLA-NCA) monomer which was initiated by poloxamer 188. The polymers were characterized and confirmed by 1H-NMR, Fourier transform infrared assay (FTIR) and gel permeation chromatography (GPC). Then, studying with A549 cells to evaluate the material`s cytotoxicity showed that the copolymer was nontoxic. PBLA-POLO-PBLA nanoparticles loaded with Valaciclovir (VACV) were prepared by the emulsion-solvent evaporation method, and the physicochemical properties were also investigated afterwards. The transmission electron microscope (TEM) showed that the VACV-loaded nanoparticles had a sub-micron size with a spherical shape. The VACV-loaded nanoparticles (with a loading efficiency of 4.36%) showed a sustained release of VACV molecules (with 70.22% release in 96 h) which was determined by HPLC at 251 nm. These results suggested that PBLA-POLO-PBLA block copolymer was a promising nano-carrier in nanoparticle drug delivery systems.
文章编号:201500841     中图分类号:    文献标志码:
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Author NameAffiliationE-mail
Ma Li-fang  mlfang11@126.com 
ZHANG Ting   
GUO Li   
LI Yao   
WANG Xiao-jiao   
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引用文本:
马丽芳,张婷,郭丽,李瑶,王晓姣.聚天冬氨酸苄酯修饰的泊洛沙姆纳米粒制备和表征[J].工程科学与技术,2016,48(3):202-208.
Ma Li-fang,ZHANG Ting,GUO Li,LI Yao,WANG Xiao-jiao.Preparation and characterization of the PBLA-POLO-PBLA nanoparticles[J].Advanced Engineering Sciences,2016,48(3):202-208.