单分散性介孔二氧化硅的制备及靶向性评价

目的:为了制备可稳定分散的介孔二氧化硅纳米材料,并将其用于尾静脉注射的纳米制剂。方法:本文采用Stober法,以十六烷基三甲基溴化铵(CTAB)为模板剂,正硅酸乙酯(TEOS)为硅源,通过酸液萃取法去除模板,制备出分散性良好的MSN纳米粒。通过FTIR、扫描电子显微镜及透射电镜等仪器,进行结构和形貌的表征。结果:单因素实验结果可知MSN的最佳制备工艺为:CTAB/TEOS质量比为1∶5,pH 10,反应温度70~80℃,搅拌速率为500 r·min-1。MSN负载DOX,表现出高负载率;体外释放实验表明DOX在中性条件下释放缓慢,弱酸性条件下释放迅速;体内实验表明MSN具有良好的靶向性。结论:通过优化后的制备工艺,MSN可稳定分散,该制剂制备方法简单,具有pH敏感性,良好的靶向性,有利于达到肿瘤靶向给药的要求,介孔二氧化硅在靶向传递系统的应用具有广阔前景。

Evaluation of preparation and targeting evaluation of monodisperse mesoporous silica

OBJECTIVE To prepare stable and dispersible mesoporous silica nanomaterials and use them in nano-preparations for tail vein injection.METHODS In this paper,MSN nanoparticles with good dispersibility were prepared by Stober method,using cetyltrimethylammonium bromide (CTAB) as template and tetraethyl orthosilicate (TEOS) as silicon source.The structure and morphology were characterized by FTIR,scanning electron microscope and transmission electron microscope.RESULTS The results of single factor experiment showed that the optimum preparation process of MSN was as follows:mass ratio of CTAB/TEOS 1:5,pH 10,reaction temperature 70-80℃ and stirring rate 500 r·min^-1.MSN loaded DOX,showed high loading rate;in vitro release test showed that DOX was released slowly in neutral condition and rapid in weak acid condition;in vivo experiment showed that MSN had good targeting ability.CONCLUSION Through the optimized preparation process,MSN can be stably dispersed.The preparation method of the preparation is simple,sensitive to pH and has good targeting,which is beneficial to meet the requirements of tumor targeted administration.This property is beneficial to meet the requirements of targeted drug delivery,and has broad prospects for application in targeted delivery systems.