二氧化硅介孔微球的制备、孔结构表征及其载药性能研究

Preparation,porosity characterization and drug releasing property of mesoporous silica microspheres

目的制备二氧化硅介孔微球,通过加入不同的致孔剂来改变微球的孔结构,用于负载难溶性药物并提高其溶出速度。方法以水玻璃为原料,通过乳化-固化法制备介孔微球;微球的孔结构用氮气吸附法进行表征;通过浸渍法将布洛芬沉积到微球的纳米孔内,并用液相色谱法测定其载药量和溶出速度。结果致孔剂的种类会影响微球的孔结构,其中以蔗糖作致孔剂所制备的微球具有最大的平均孔径和孔容;用该种微球负载布洛芬后,药物可在5 min内溶出89%,而原料药达到相同的释放率则需要150 min。结论以蔗糖溶液稀释水玻璃制得的微球具有良好的载药性能,有助于提高难溶性药物的溶出速度。

Objective：To prepare mesoporous silica microspheres （MSMs） and to modify their porosity by using different porogenic agent for drug loading and releasing. Methods： Prepare MSMs by emulsification-solidification method using water glass as silica precursor; characterize their porosity using nitrogen adsorption method; after drug loading of ibuprofen, the high performance liquid chromatography method was used to determine drug concentration. Results： The MSMs achieves the highest average pore size and pore volume when sucrose was used as as porogenic agent, the drug-loaded MSMs release 89% of ibuprofen in 5 rain while the raw material of ibuprofen takes 150 min to achieve the same amount of drug releasing. Conclusion： This kind of MSMs, showing high drug loading and rapid releasing, offers a promising alternative for formulating poorly water-soluble drugs.