聚天冬氨酸苄酯修饰的泊洛沙姆纳米粒制备和表征  

Preparation and Characterization of the PBLA-POLO-PBLA Nanoparticles

作　　者：马丽芳[1] 张婷[1] 李瑶[1] 王晓姣[1] 蒙正宇 

机构地区：[1]四川大学化学工程学院,四川成都610065

出　　处：《四川大学学报（工程科学版）》2016年第3期202-208,共7页Journal of Sichuan University (Engineering Science Edition)

摘　　要：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（^1HNMR）、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）结果表明,该载药纳米粒的尺寸为200 nm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96 h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。A novel drug carrier system of block copolymer PBLA -POLO -PBLA was designed with the ring-opening ization of the β- benzyl-Lasparate N -carboxyanhydride （BLA -NCA） monomer which was initiated by poloxamer 188. The polymers were characterized and confirmed by ^1HNMR, Fourier transform infrared assay （FTIR） and gel permeation chromatography （GPC）. The material＇s cytotoxicity was evaluated with A549 cells and the result 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 rtanoparticles 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 is a promising nano-carrier in nanoparticle drug delivery systems.

关 键 词：泊洛沙姆 聚天冬氨酸苄酯 嵌段共聚物 纳米粒 载体 

分 类 号：R94[医药卫生—药剂学]