有序介孔硅胶提高难溶性药物白藜芦醇的溶出速率

本研究的目的是制备有序介孔硅胶并考察其作为难溶性药物载体的体外药物释放特点。以十六烷基三甲基溴化铵为模板合成了有序介孔硅胶, 以白藜芦醇为模型药物, 采用扫描电镜、透射电镜、N₂吸附-脱附、X-射线衍射和红外光谱对载药前后的有序介孔硅胶进行表征, 并考察药物体外释放行为。结果表明, 合成的有序介孔硅胶比表面积大、粒度均匀, 具有有序六方孔道结构, 载药后药物以无定形态或分子态存在, 释放速率明显提高。有序介孔硅胶有望成为新型的难溶性药物载体。

Improving the dissolution rate of poorly water-soluble resveratrol by the ordered mesoporous silica

The aim of this study is to synthesize the ordered mesoporous silica (OMS) as drug carrier to improve release property of insoluble drug and investigate the dissolution profile of insoluble drug from the porous carrier.  The OMS was obtained by using cetyltrimethyl ammonium bromide as the template and resveratrol was selected as the model drug.  The resveratrol-loaded OMS (Res-OMS) were characterized by scanning electron microscopy (SEM), transmission electron microscopy (TEM), N₂ adsorption-desorption,  X-ray diffraction (XRD) and FT-IR spectroscopy.  In vitro drug release behavior was also investigated.  It was found that the synthesized OMS showed a large surface area, a narrow pore size distribution and an important mesoporosity associated to hexagonally organized channels.  Compared with physical mixture and crystalline powder, resveratrol was in amorphous or molecular form after loading into OMS.  The release rate of resveratrol from drug-loaded OMS was significantly increased suggesting the great potential application of OMS for the formulation of poorly soluble drugs.