二氧化硅介孔微球的制备、孔结构表征及其载药性能研究
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摘要
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 min 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.
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 min 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.
引文
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[2]Letchmanan K,Shen S C,Ng W K,et al. Enhanced dissolution and stability of artemisinin by nano-confinement in ordered mesoporous SBA-15 particles[J]. Journal of Microencapsulation,2015,32(4):390-400.
[3]Li J,Xu L,Yang B,et al. Facile synthesis of functionalized ionic surfactant templated mesoporous silica for incorporation of poorly water-soluble drug[J]. International Journal of Pharmaceutics,2015,492(1):191-198.
[4]Zhang K,Xu,LL,Jiang JG,et al. Facile large-scale synthesis of monodisperse mesoporous silica nanospheres with tunable pore structure[J]. Journal of the American Chemical Society,2013,135(7):2427-2430.
[5]Wang YQ,Zheng CM,Liu ZJ,et al. Fabrication of highly ordered mesoporous silica with the assistance of phosphate[J]. New Journal of Chemistry,2015,39(10):7763-7767.