PEG修饰介孔硅纳米粒子负载丹参素的体外控制释放研究  

Study on in vitro controlled release of danshensu based on PEG modified of mesoporous silica nanoparticles

作　　者：袁宁宁[1] 谢鹏波[1] 侯慧玉[1] 王婕[1] 林坚涛[2] 王冠海[2] 

机构地区：[1]广州工程技术职业学院,广东广州510075 [2]广东医学院,广东东莞523808

出　　处：《中草药》2016年第14期2441-2446,共6页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金青年基金项目(81402563);广东医学院博士启动项目(XB1303;XB1387)

摘　　要：目的设计制备一系列PEG修饰的介孔硅纳米粒子(MSNs-PEG),用于负载丹参素的药物传输载体。方法通过与硅烷偶联剂共水解缩合的方法,在介孔硅纳米粒子(MSNs)中引入数量可控的叠氮基,然后通过点击化学的方法,在MSNs表面引入数量可控的PEG链段,并通过傅里叶转换红外线光谱(FTIR)、X射线粉末衍射(XRD)、Zeta电位和透射电子显微镜(TEM)等方法表征MSNs-PEG,通过MTT法对MSNs-PEG载体的安全性进行初步评价,体外释放实验考察MSNs-PEG负载丹参素的释放规律。结果 PEG能够有效、可控地接枝到MSNs上,使MSNs-PEG具有良好的水分散性和稳定性。通过负载丹参素实验发现,MSNs-PEG对丹参素的负载率较高,其载药量和包封率分别为6.8%和22.8%。体外释放规律发现,PEG的接枝改变了药物的释放规律,能够有效延长丹参素的释放时间;随着PEG接枝量(质量分数)的提高,能够有效控制丹参素的释放速率。结论点击化学法能够有效地控制PEG接枝量(质量分数),并有效地控制丹参素的释放速度,方法简单易行。Objective To prepare a series of polyethylene（PEG）-modified mesoporous silica nanoparticles（MSNs-PEG） used for danshensu delivery carrier. Methods By the co-hydrolysis method with silica coupling agent, the content of the azide groups was controlled into MSNs. The structures of MSNs-PEG were characterized by FTIR, XRD, and TEM analyses. The results showed that PEG chains have been grafted on the surface of MSNs. The safety of MSNs-PEG carrier was preliminarily evaluated by MTT, the release rule of MSNs-PEG was investigated by in vitro release experiment. Results PEG can be effectively and controlled grafted onto MSNs. The MSNs-PEG have the good stability in aqueous solution. The loading rate of MSNs-PEG was higher in the experimental results of danshensu. The drug loading and entrapment efficiency were 6.8 % and 22.8 %. The graft of PEG could change the release of the drug, which could effectively prolong the time of drug release. And with the increase of the amount of PEG（mass fraction）, the release time of danshensu could be prolonged effectively. Conclusion The click chemistry method is easy to control the PEG graft content, and effectively controls the release rate of danshensu.

关 键 词：介孔硅纳米粒子 PEG修饰 丹参素 体外释药 叠氮基 点击化学 安全性 

分 类 号：R283.6[医药卫生—中药学]