磁性介孔氧化锆载药体系的制备及其抗肺癌活性研究  

Study on the preparation and activity on anti-lung cancer of magnetic ZrO2 nanoparticles as drug delivery system

作　　者：彭延波 叶昌邦 陶灿 邓淑君 林洁柔 许汇成 卢焕俊 刘冰 赵平 PENG Yanbo;YE Changbang;TAO Can;DENG Shujun;LIN Jierou;XU Huicheng;LU Huanjun;LIU Bing;ZHAO Ping(School of Chemistry and Chemical Engineering,Guangdong Pharmaceutical University,Zhongshan,528458,China;School of Pharmacy,Guangdong Pharmaceutical University,Guangzhou 510006,China)

机构地区：[1]广东药科大学医药化工学院,广东中山528458 [2]广东药科大学药学院,广东广州510006

出　　处：《广东药科大学学报》2020年第2期205-209,共5页Journal of Guangdong Pharmaceutical University

基　　金：广东省特色创新项目(2017KTSCX103);广东省大学生创新创业训练计划(S201910573037)。

摘　　要：目的建立安全有效的抗肿瘤药物运载和控释方法。方法采用化学包埋法,以超顺磁性Fe 3O 4纳米粒子为磁核、ZrO 2为壳层制备了MnO 2封堵的磁性氧化锆纳米微球,差量法研究该纳米微球对化疗药物道诺霉素的运载情况,并通过MTT法对其抗肺癌活性进行评价。结果成功制备了磁性介孔氧化锆纳米微球并实现对道诺霉素的高效运载;载体浓度高达100μg/mL时,对A549细胞无明显生物毒性;载药纳米微球在8 mmmol/L谷胱苷肽中的缓释率较同浓度其他溶质高出8~10倍,显示出灵敏的谷胱苷肽刺激响应性;此外,载药纳米微球(IC 50为0.40 mmol/L)具有比自由道诺霉素(IC 50为0.68 mmol/L)更高的体外抗肺癌活性。结论二氧化锰封堵的磁性介孔氧化锆纳米体系在抗肿瘤药物的运载方面具有较大的应用潜力。Objective To establish a safe and efficient system for the drug delivery of anticancer drugs.Methods Superparamagnetic Fe3O4 nanoparticles were used as the core and ZrO2 was used as the shell,the magnetic zirconia nano-system blocked by MnO2 were prepared by chemical embedding method.The loading efficiency of the system to the chemotherapy drug daunomycin was studied by differential method,and its antitumor activity was evaluated by MTT method.Results The magnetic mesoporous zirconia nano system was successfully constructed and the efficient delivery of donomicin was realized.When the concentration of carrier was up to 100μg/ml,there was no obvious biological toxicity to A549 cells.The release rate of the system in 8 mmol/L GSH was 8-10 times higher than that in other solutes of the same concentration,and it suggested the sensitive GSH stimulation response.In addition,the carrier system(IC 500.48 mmol/L)had higher anti-lung cancer activity in vitro than that of free daunomycin(IC 50 is 0.6 mmol/L).Conclusion The manganese dioxide blocked magnetic zirconia nano-system has great applications potential in the delivery of antitumor drugs.

关 键 词：氧化锆 二氧化锰 载药体系 谷胱苷肽刺激响应性 抗肿瘤活性 

分 类 号：R914[医药卫生—药物化学]