Karimzadeh Mahmonir, Rashidi Ladan, Ganji Fariba
a Chemical Engineering Department , Payam Noor University , Tehran , Iran.
b Faculty of Food Industry and Agriculture , Standard Research Institute, Iranian National Standards Organization , Karaj , Iran.
Drug Dev Ind Pharm. 2017 Apr;43(4):628-636. doi: 10.1080/03639045.2016.1275668. Epub 2017 Jan 8.
Rivastigmine hydrogen tartrate (RT) is a molecule with both hydrophilic and hydrophobic properties used for the treatment of the Alzheimer's disease. In this work, the larger pore size of mesoporous silica nanoparticles (P1-MSN) was synthesized and then, P1-MSN were functionalized by succinic anhydride (S-P1-MSN) and 3-aminopropyltriethoxysilane (APTES) (AP-CO-P1-MSN) using the grafting and co-condensation methods, respectively. A new method was used for the functionalization of P1-MSN by succinic anhydride at room temperature. Nanoparticles were characterized by special instrumental analysis and loaded by RT. Maximum entrapment efficiency and RT loading percentage into P1-MSN, AP-CO-P1-MSN and S-P1-MSN were respectively obtained as 21.26 and 25.5%, 41.5 and 49.8%, and 11.9 and 14.28% for 24 h. In the simulated gastric and body fluids, the release rate of RT-loaded AP-CO-P1-MSN (AP-CO-P1-MSN-RT) was lower than that of other RT-loaded nanoparticles. In oral pathway, the sustained release of RT was observed in AP-CO-P1-MSN-RT. Moreover, no cytotoxicity effect was observed for P1-MSN, but the cells treated by AP-CO-P1-MSN showed a reduction in SY5Y cell viability due to easy entrance of these nanoparticles and their accumulation in different parts of the cell as observed by TEM.
酒石酸氢卡巴拉汀（RT）是一种兼具亲水性和疏水性的分子，用于治疗阿尔茨海默病。在本研究中，合成了孔径较大的介孔二氧化硅纳米颗粒（P1-MSN），然后分别采用接枝法和共缩合法，用琥珀酸酐（S-P1-MSN）和3-氨丙基三乙氧基硅烷（APTES）（AP-CO-P1-MSN）对P1-MSN进行功能化修饰。采用一种新方法在室温下用琥珀酸酐对P1-MSN进行功能化修饰。通过特殊仪器分析对纳米颗粒进行表征，并负载RT。24小时内，RT在P1-MSN、AP-CO-P1-MSN和S-P1-MSN中的最大包封率和负载率分别为21.26%和25.5%、41.5%和49.8%、11.9%和14.28%。在模拟胃液和体液中，负载RT的AP-CO-P1-MSN（AP-CO-P1-MSN-RT）的释放速率低于其他负载RT的纳米颗粒。在口服途径中，观察到AP-CO-P1-MSN-RT中RT的缓释。此外，未观察到P1-MSN的细胞毒性作用，但经AP-CO-P1-MSN处理的细胞显示SY5Y细胞活力降低，这是由于这些纳米颗粒易于进入细胞并如通过透射电镜观察到的那样在细胞的不同部位积累。
