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新型核壳结构双介孔二氧化硅纳米球的合成及其在提高难溶性药物溶出速率中的应用。

Synthesis of novel core-shell structured dual-mesoporous silica nanospheres and their application for enhancing the dissolution rate of poorly water-soluble drugs.

作者信息

Wu Chao, Sun Xiaohu, Zhao Zongzhe, Zhao Ying, Hao Yanna, Liu Ying, Gao Yu

机构信息

Department of Pharmaceutics, Liaoning Medical University, 40 Songpo Road, Linghe District, Jinzhou, Liaoning Province 121001, China.

Management Center for Experiments, Bohai University, 19 Keji Road, Songshan District, Jinzhou, Liaoning Province 121000, China.

出版信息

Mater Sci Eng C Mater Biol Appl. 2014 Nov;44:262-7. doi: 10.1016/j.msec.2014.08.040. Epub 2014 Aug 21.

Abstract

Novel core-shell dual-mesoporous silica nanospheres (DMSS) with a tunable pore size were synthesized successfully using a styrene monomer as a channel template for the core and cetyltrimethyl ammonium bromide (CTAB) as a channel template for the shell in order to improve the dissolution rate of poorly water-soluble drugs. Simvastatin was used as a model drug and loaded into DMSS and the mesoporous core without the shell (MSC) by the solvent evaporation method. The drug loading efficiency of DMSS and MSC were determined by thermogravimetric analysis (TGA) and ultraviolet spectroscopy (UV). Characterization, using scanning electron microscopy (SEM), transmission electron microscopy (TEM), nitrogen adsorption, powder X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR) showed that simvastatin adsorbed in DMSS and MSC was in an amorphous state, and in vitro release test results demonstrated that both DMSS and MSC increased the water solubility and dissolution rate of simvastatin. The shell structure of DMSS was able to regulate the release of simvastatin compared with MSC. It is worth noting that DMSS has significant potential as a carrier for improving the dissolution of poorly water-soluble drugs and reducing the rapid release.

摘要

成功合成了具有可调孔径的新型核壳双介孔二氧化硅纳米球(DMSS),以苯乙烯单体作为核的通道模板,十六烷基三甲基溴化铵(CTAB)作为壳的通道模板,以提高难溶性药物的溶解速率。以辛伐他汀为模型药物,通过溶剂蒸发法将其载入DMSS和无壳介孔核(MSC)中。通过热重分析(TGA)和紫外光谱(UV)测定了DMSS和MSC的载药效率。利用扫描电子显微镜(SEM)、透射电子显微镜(TEM)、氮吸附、粉末X射线衍射(XRD)、差示扫描量热法(DSC)和傅里叶变换红外光谱(FTIR)进行表征,结果表明,吸附在DMSS和MSC中的辛伐他汀呈无定形状态,体外释放试验结果表明,DMSS和MSC均提高了辛伐他汀的水溶性和溶解速率。与MSC相比,DMSS的壳结构能够调节辛伐他汀的释放。值得注意的是,DMSS作为改善难溶性药物溶解和减少快速释放的载体具有巨大潜力。

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