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论文摘要

甘草次酸修饰的聚天冬氨酸苄酯纳米粒制备及表征

Preparation and Evaluation of Glycyrrhetinic Acid-modified Poly(β-benzyl-L-asparate) Nanoparticles

作者:马丽芳(四川大学 化学工程学院);马鹏里(四川大学 化学工程学院);张婷(四川大学 化学工程学院);曾星(四川大学 化学工程学院)

Author:Ma Lifang(College of Chem. Eng.,Sichuan Univ.);Ma Pengli(College of Chem. Eng.,Sichuan Univ.);Zhang Ting(College of Chem. Eng.,Sichuan Univ.);Zeng Xing(College of Chem. Eng.,Sichuan Univ.)

收稿日期:2014-08-05          年卷(期)页码:2015,47(3):187-192

期刊名称:工程科学与技术

Journal Name:Advanced Engineering Sciences

关键字:甘草次酸;聚天冬氨酸苄酯;纳米粒;紫杉醇

Key words:glycyrrhetinic acid; PBLA; nanoparticles; paclitaxel

基金项目:

中文摘要

用甘草次酸 (GA) 修饰可生物降解的聚天冬氨酸苄酯 (PBLA),将其制备成纳米粒,考察其作为药物载体的可行性。首先将GA氨基化,以引发L-天冬氨酸-β-苄酯-N-羧酸酐 (BLA-NCA) 开环聚合,合成不同分子量的材料GA-NH-PBLA,通过1H-NMR、FT-IR对其结构进行表征,GPC显示3种材料的分子量为1 565、3 560、5 550。采用MTT法以人肝癌细胞 (HepG2) 为对象,评价其作为药物载体的安全性,结果实验表明该材料无细胞毒性。采用乳化-溶剂挥发法制备包载紫杉醇(PTX)的纳米粒,并考察了不同分子量材料GA-NH-PBLA对纳米粒粒径,包封率及载药量的影响。结果显示:分子量为5 550的材料,制得的纳米粒粒径约100 nm,粒径分布均匀,球形度良好,具有良好的缓释作用,表明分子量大的材料更适合作为药物载体。

英文摘要

Three kinds of GA-NH-PBLA with different molecular weight were synthesized by the ring opening polymerization of N-carbobenzoxy-L-aspartic acid benzyl ester (BLA-NCA) initiated by GA-NH2. Their structures were characterized by1H-NMR, FT-IR.The molecule weights were measured by GPC.The cytotoxicity of GA-NH-PBLA was investigated to evaluate the security by MTT assay against human hepatoma cells (HepG2). Result demonstrated that the material had no significant cytotoxicity. The material was processed into NPs loaded paclitaxel (PTX) via emulsion solvent evaporation method, the influence of different weights on the particle size, encapsulation efficiency and loading capacity was investigated, and the release in vitro was evaluated in vitro release study. Results showed that NPs formed from the polymer of 5 550 were spherical in shape with about 100 nm in size and the NPs had a good sustained release effect in PBS buffer solution. The study indicated that the material with high molecular weight was more suitable for being used as drug carrier.

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