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Double-nano silica xerogel contributes to establish nifedipine delivery system with superior delivery effect
Microporous and Mesoporous Materials ( IF 4.8 ) Pub Date : 2020-01-02 , DOI: 10.1016/j.micromeso.2019.109996
Ping Zhang , Qiankun Jiang , Yue Zheng , Jing Li

To further explore the wonder of nano technology in drug delivery system, the combination of micelles and mesoporous silica was conducted for delivering poorly water soluble nifedipine (NFP). Double-nano silica xerogel (DN-SX) with both micelles and nanopores was prepared and silica xerogel with only nanopores (SN-SX) was made for comparison. Characteristics of DN-SX and SN-SX, including morphology, porous structure and crystalline state were investigated and pharmaceutical performances of drug loaded carriers were studied. The micelles in DN-SX contributed to achieve larger mesopores and enhanced NFP dissolution better than SN-SX. How responses of drug release amount and reduced drug release amount reacted as changing each influencing factor was elucidated by Box–Behnken experimental design. With the DN-SX obtained by optimization, in vivo pharmacokinetic study result demonstrated that the relative bioavailability of NFP loaded DN-SX and NFP loaded SN-SX were 216.84% and 161.14%, respectively. Therefore, the optimized DN-SX with double-nano structure was of great value for designing poorly water soluble drug delivery system.



中文翻译:

双纳米二氧化硅干凝胶有助于建立硝苯地平输送系统,并具有出色的输送效果

为了进一步探索纳米技术在药物输送系统中的应用,胶束和中孔二氧化硅的组合用于输送水溶性差的硝苯地平(NFP)。制备具有胶束和纳米孔的双纳米二氧化硅干凝胶(DN-SX),并制备仅具有纳米孔的二氧化硅干凝胶(SN-SX)进行比较。研究了DN-SX和SN-SX的形态,多孔结构和结晶状态,并研究了载药载体的药理性能。DN-SX中的胶束比SN-SX更好地实现了更大的中孔并增强了NFP的溶解性。Box–Behnken实验设计阐明了随着各种影响因素的变化,药物释放量和减少的药物释放量如何反应。通过优化获得的DN-SX,体内药代动力学研究结果表明,NFP负载的DN-SX和NFP负载的SN-SX的相对生物利用度分别为216.84%和161.14%。因此,优化的具有双纳米结构的DN-SX对于设计水溶性差的药物递送系统具有重要的价值。

更新日期:2020-01-02
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