天冬酰胺酶纳米微球体外活性和稳定性  

Studies on in vitro Activity and Stability of Asparaginase Loaded in Nanospheres

作　　者：晏子俊[1] 李万玉[1] 胡雪原[1] 何丹[1] 谢江川[1] 张景勍[1] YAN Zijun;LI Wanyu;HU Xueyuan;HE Dan;XIE Jiangchuan;ZHANG Jingqing(Engineering Research Center in University,Chongqing Medical University,Chongqing 400016, China)

机构地区：[1]重庆医科大学药物高校工程研究中心,重庆400016

出　　处：《食品与生物技术学报》2017年第12期1258-1263,共6页Journal of Food Science and Biotechnology

基　　金：国家自然科学基金项目(30973645);重庆市首批高等学校优秀人才资助计划项目(渝教人(2009)2号文件)

摘　　要：制备自组装天冬酰胺酶(Asparaginase,AAS)透明质酸-聚乙二醇(Hyaluronic acid-graftpoly(ethylene glycol),HA-g-PEG)/羟丙基-β-环糊精(Hydroxypropyl-beta-cyclodextrin,HPCD)纳米微球(self-assembly HA-g-PEG/HPCD hollow nanospheres loaded with AAS,AHHPs),并对AHHPs的体外活性及稳定性进行初步研究。制备并测定AHHPs的透射电镜、粒径、Zeta电位和包封率。再分别从最适温度、最适pH、热稳定性、贮存稳定性、酸碱稳定性、抗胰蛋白酶水解能力和血浆稳定性初步考察AHHPs的体外活性和稳定性。测得AHHPs的平均粒径为(367.43±2.72)nm,Zeta电位为(-15.70±1.25)mV,平均包封率为(66.03±3.81)%。AHHPs的最适温度为50℃,最适pH值为7.0;游离AAS的最适温度为60℃,最适pH值为7.5。体外稳定性的结果显示,同样条件下,AHHPs的体外稳定性明显比游离AAS的好。因此AHHPs能有效提高AAS的体外活性和体外稳定性。To prepare self-assembly hyaluronic acid- graft-poly （ethylene glycol）,（HA- g-PEG） / hydroxypropyl- beta-cyclodextrin（HPCD） hollow nanospheres loaded with AAS （AHHPs）, and then investigate the in vitro activity and stability difference between AHHPs and free AAS. AHHPs was prepared and the transmission electron microscopy, size, zeta potential, entrapment efficiency were detected. We investigated the in vitro activity and stability of AHRPs and free AN by measuring the optimum temperature, optimum pH, thermal stability, storage stability, pH stabilities, trypsin stabilities and plasma stabilities. The average particle size was （367.43±2.72） nm, zeta potential was （-15.70 ± 1.25） mV, and the entrapment efficiency of UHPHD was （66.03 ±3.81）% . The optimum temperature and optimum pH of the AHHPs were 50 ： and 7.0,respectively; the optimum temperature and optimum pH of free AAS were 60 Eand 7.5, respectively. The results of stability experiments showed that the stabilities of AHHPs were significantly superior to the free AAS. AHHPs can improve the activity of AAS and significantly enhance the stabilities of AAS in vitro.

关 键 词：天冬酰胺酶 纳米微球 体外活性 体外稳定性 

分 类 号：O629.8[理学—有机化学] TB383.1[理学—化学]