Department of Pharmaceutics, Shenyang Pharmaceutical University, Shenyang, PR China.
Eur J Pharm Biopharm. 2011 Nov;79(3):544-51. doi: 10.1016/j.ejpb.2011.07.001. Epub 2011 Jul 13.
In the present study, we exploited for the first time the potential of 3-D ordered macroporous (3DOM) silica as matrix for drug nanoparticles, in order to obtain proper control over drug particle size in the sub-micrometer range, enhance the dissolution rate, and reduce gastric damage. 3DOM silica matrix with 3-D spherical pores of 200 nm was successfully created and then loaded with IMC nanoparticles at various drug-silica ratios. A rapid release profile for IMC nanoparticle formulations was achieved in comparison with microsized IMC and a commercial capsule, which could be attributed to both increase in the specific surface area and decrease in the crystallinity of IMC, as well as the hydrophilic surface and the interconnected pore networks of 3DOM silica. Reduced gastric damage of IMC was demonstrated, and the protective effect may arise from the reduction in drug particle size as well as encapsulation effect of 3DOM silica.
在本研究中，我们首次利用 3-D 有序大孔（3DOM）硅作为药物纳米颗粒的基质，以便能够在亚微米范围内对药物颗粒大小进行适当控制，提高药物的溶解速率，并减少胃损伤。成功制备了具有 200nm 三维球形孔的 3DOM 硅基质，然后以不同的药物-硅比例负载 IMC 纳米颗粒。与微尺度 IMC 和商业胶囊相比，IMC 纳米颗粒制剂呈现快速释放特征，这归因于 IMC 的比表面积增加、结晶度降低，以及 3DOM 硅的亲水性表面和互联孔网络。证明 IMC 对胃损伤的减轻，其保护作用可能来自于药物粒径的减小以及 3DOM 硅的包封作用。
