Bi Yanping, Wu Chaonan, Xin Ming, Bi Shuyan, Yan Chengxin, Hao Jifu, Li Fei, Li Shou
School of Pharmaceutical Sciences, Taishan Medical University, No. 619, Changcheng Road, Tai'an, 271016, PR China.
School of Pharmaceutical Sciences, Taishan Medical University, No. 619, Changcheng Road, Tai'an, 271016, PR China.
Int J Pharm. 2016 Mar 16;500(1-2):77-84. doi: 10.1016/j.ijpharm.2016.01.027. Epub 2016 Jan 16.
Mesoporous silica microspheres (MSMs) with a pore-size larger than 10nm and a large pore-volume have attracted considerable attention for their application in delivering poorly water-soluble drugs. Here we developed a simple method for large-scale synthesis of MSMs using sodium silicate as silica precursor. The novelty of this approach lies in the use of sucrose solution to achieve large size and volume of nanopores. The highest values of pore size and pore volume are 13.2 nm and 1.97 cm(3)/g, respectively. Importantly, the method is reliable and easily upscalable. The blank and drug-loaded MSMs were characterized by differential scanning calorimetry (DSC) and X-ray powder diffraction (XRPD). Ibuprofen and resveratrol were successfully loaded into the nanopores of MSMs in amorphous and nanocrystalline form and showed high drug-loadings and enhanced dissolution rates. This kind of MSMs appears to be a promising candidate as a new oral drug delivery vehicle providing a rapid drug release.
孔径大于10nm且孔体积大的介孔二氧化硅微球(MSMs)因其在递送难溶性药物方面的应用而备受关注。在此,我们开发了一种以硅酸钠为硅源大规模合成MSMs的简单方法。该方法的新颖之处在于使用蔗糖溶液来实现大尺寸和大体积的纳米孔。孔径和孔体积的最高值分别为13.2nm和1.97cm³/g。重要的是,该方法可靠且易于放大。通过差示扫描量热法(DSC)和X射线粉末衍射(XRPD)对空白和载药MSMs进行了表征。布洛芬和白藜芦醇成功以无定形和纳米晶形式负载到MSMs的纳米孔中,并显示出高载药量和提高的溶解速率。这种MSMs似乎是一种有前途的新型口服药物递送载体,可实现药物的快速释放。