Limnell T, Riikonen J, Salonen J, Kaukonen A M, Laitinen L, Hirvonen J, Lehto V-P
Drug Discovery and Development Technology Center, University of Helsinki, FI-00014 Helsinki, Finland.
Int J Pharm. 2007 Oct 1;343(1-2):141-7. doi: 10.1016/j.ijpharm.2007.05.010. Epub 2007 May 16.
Six different types of mesoporous silicon microparticles were prepared to evaluate the effect of surface treatment and pore sizes on their properties as drug carriers. The studied porous silicon particles were as-anodized, thermally carbonized (TCPSi) and thermally oxidized (TOPSi) in addition to three novel ones: annealed TCPSi, annealed TOPSi and thermally hydrocarbonized porous silicon (THCPSi). Drug dissolution at pH 5.5 and physical and chemical stabilities after 3 months of storage were used as experimental models to investigate the loaded particles. Loading degrees of ibuprofen in the particles were determined by several methods before and after storage, and the results were in good agreement with each other. Loading improved the dissolution rate of ibuprofen in all the studied cases, while the hydrophilic TCPSi material resulted in the fastest dissolution and the most stable mesoporous microparticles. The release profiles of ibuprofen did not change markedly during storage. The effect of storage on the loading degrees of the other PSi microparticles than the unstable (easily oxidized) as-anodized porous silicon was not notable.
制备了六种不同类型的介孔硅微粒，以评估表面处理和孔径对其作为药物载体性能的影响。除了三种新型的介孔硅微粒：退火热碳化硅（annealed TCPSi）、退火热氧化硅（annealed TOPSi）和热烃化多孔硅（THCPSi）之外，所研究的多孔硅颗粒还包括阳极氧化态、热碳化（TCPSi）和热氧化（TOPSi）态的。以pH 5.5条件下的药物溶出以及储存3个月后的物理和化学稳定性作为实验模型来研究负载颗粒。通过多种方法测定了储存前后颗粒中布洛芬的负载度，结果相互吻合。在所有研究的情况下，负载均提高了布洛芬的溶出速率，而亲水性的TCPSi材料导致了最快的溶出和最稳定的介孔微粒。布洛芬的释放曲线在储存期间没有明显变化。储存对除不稳定的（易氧化的）阳极氧化多孔硅之外的其他PSi微粒负载度的影响并不显著。
