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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 design and prepare a series of PEG-modified mesoporous silica nanoparticles (MSNs-PEG) for the drug delivery of Danshensu. Methods By co-hydrolyzing and condensing with silane coupling agent, a number of azide groups were introduced into mesoporous silica nanoparticles (MSNs), and then controlled by click chemistry to introduce a controlled number of PEG segments , And characterized by Fourier transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRD), Zeta potential and transmission electron microscopy (TEM) were used to characterize the safety of MSNs-PEG by MTT assay Evaluation, in vitro release test of MSNs-PEG-loaded danshensu release rule. Results PEG could effectively and controllably be grafted to MSNs, making MSNs-PEG have good water dispersibility and stability. Danshensu loading by the experiment found that, MSNs-PEG on Danshensu load was higher, the drug loading and encapsulation efficiency were 6.8% and 22.8%. The results of in vitro release showed that the grafting of PEG changed the release of drug and prolonged the release time of Danshensu effectively. With the grafting amount of PEG increased, the release rate of Danshensu could be controlled effectively. Conclusion The click chemical method can effectively control the grafting amount of PEG (mass fraction) and effectively control the release rate of danshensu. The method is simple and easy to operate.