载门冬酰胺酶的自组装聚乙二醇-透明质酸/二甲基-β-环糊精纳米粒体外稳定性的初步考察  

Preliminary Stability of Asparaginase-loaded Self-assembled Nanoparticles Based on PEG Grafted Hyaluronic Acid and Dimethyl-β-cyclodextrin

作　　者：谢江川[1] 何丹[1] 晏子俊[1] 周云莉 张景勍[1] 

机构地区：[1]重庆医科大学药物高校工程研究中心和生物化学与分子药理学重点实验室

出　　处：《中国医药工业杂志》2015年第7期716-721,共6页Chinese Journal of Pharmaceuticals

基　　金：国家自然科学基金(30973645)

摘　　要：采用聚乙二醇接枝透明质酸和二甲基-？-环糊精制备了含载门冬酰胺酶（1）的自组装纳米粒（THDCD）,并比较其与游离1在体外的活性及稳定性。测定了THDCD和1的最适温度、最适p H值,并对比了二者的酸碱稳定性、热稳定性、贮存稳定性、血浆稳定性、抗胰蛋白酶水解能力、抗部分金属离子及有机化合物影响的能力。结果表明,THDCD的最适温度和最适p H值为50℃和p H 6.5,而1为60℃和p H 7.5。THDCD的上述稳定性和抗性均优于1。本试验表明,THDCD在提高了1体外活性的同时,也显著增强了1的体外稳定性。Asparaginase （1）-loaded self-assembled nanoparticles （THDCD） with polyethylene glycol （PEG） grafted hyaluronic acid and dimethyl-β-cyclodextrin were prepared. The in vitro activity and stability of the product and free 1 were investigated and compared. The optimum temperature and optimum pH value for THDCD and 1 were determined and their acidic and basic stability, thermal stability, storage stability, plasma stability, resistance to trypsin and resistance to several metal ions and organic compounds were compared. The optimum temperature and optimum pH value for THDCD were 50 ℃ and pH 6.5, while for I were 60℃ and pH 7.5. The above stabilities and resistance abilities of THDCD were all superior to 1. The results showed that THDCD not only improved the activity but also significantly enhanced the stability of 1 in vitro.

关 键 词：门冬酰胺酶 自组装纳米粒 聚乙二醇接枝透明质酸 二甲基-β-环糊精 最适温度 最适PH值 稳定性 

分 类 号：R944.9[医药卫生—药剂学]