氨基化修饰介孔二氧化硅用于疏水性药物的负载和释放

摘要

为了提高介孔二氧化硅（MSN）对疏水性药物的负载能力，在合成二氧化硅后对其表面进行氨基化修饰。以二氧化硅粒子对盐酸非索非那定（FXD）的负载量作为评价标准，在最适宜制备工艺条件，MSN和氨基化修饰二氧化硅（MSN-NH₂）对FXD的最大负载效率分别为28.1 mg/g和39.3 mg/g。通过FXD累计释放实验表明， MSN-NH₂-3和MSN在32 h的累计释放量分别达到59.3% 和67.7%，说明氨基化修饰二氧化硅可以增强药物缓释能力。采用Korsmeyer-Peppas 方程拟合分析二氧化硅对FXD的累计释放数据，MSN-NH₂-3的释放动力学参数（k=13.41）小于MSN（k=19.64），实验结果表明氨基化使二氧化硅对FXD的负载效率提高了11.2 mg/g，32 h FXD累计释放降低了8.4%。

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	颜建民
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关键词：介孔二氧化硅；氨基化修饰；疏水性药物；药物负载和释放

Abstract：

In order to increase drug loading capacity, the surface of MSN was functionalized with amine groups by treatment with APTS. Under the best preparation conditions, the FXD loading efficiency of MSN and MSN-NH₂ was 28.1 mg/g and 39.3 mg/g. In this experiment, we studied the in vitro release properties of samples and found that the amounts of released FXD from MSN was about 67.7% for 32 h, whereas the released FXD from MSN-NH₂-3 was around 59.3% for 32 h. FXD release data of MSN and MSN-NH₂-3 was fitted with the Korsmeyer-Peppas model. The drug release kinetics constant of MSN-NH₂-3 (k=13.41) is less than MSN(k=19.64). These results demonstrated that the FXD loading capacity of MSN-NH₂ was increased by 11.2 mg/g and the FXD cumulative release capability of MSN-NH₂ was decreased by 8.4%.

Keywords： mesoporous silica； amino modification； hydrophobic drug； drug loading and release

Received 2015-02-05;

Fund:

国家自然科学基金（21676180，21076143）；天津市科技支撑重点项目（15ZCZDSF00160）；天津市应用基础研究计划（13JCYBJC20100）；天津市科技兴海计划（KJXH2014-05）。

Corresponding Authors: 张裕卿,E-mail:zhangyuqing@tju.edu.cn。 Email: zhangyuqing@tju.edu.cn

About author: 颜建民(1988-),男,硕士研究生,主要从事小尺度功能材料制备及其在药物传输中应用的研究。

引用本文:

颜建民, 张裕卿.氨基化修饰介孔二氧化硅用于疏水性药物的负载和释放[J]. 化学工业与工程, 2017,34(3): 43-49

Yan Jianmin, Zhang Yuqing.Preparation of Amino Group Modified Mesoporous Silica Nano-particles and Its Application in Hydrophobic Drug Loading and Release[J]. Chemcial Industry and Engineering, 2017,34(3): 43-49

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