Division of Pharmaceutical Technology, Faculty of Pharmacy, University of Helsinki, FI-00014, Finland.
Int J Pharm. 2011 Jul 29;414(1-2):148-56. doi: 10.1016/j.ijpharm.2011.05.021. Epub 2011 May 12.
Mesoporous materials have an ability to enhance dissolution properties of poorly soluble drugs. In this study, different mesoporous silicon (thermally oxidized and thermally carbonized) and non-ordered mesoporous silica (Syloid AL-1 and 244) microparticles were compared as drug carriers for a hydrophobic drug, itraconazole (ITZ). Different surface chemistries pore volumes, surface areas, and particle sizes were selected to evaluate the structural effect of the particles on the drug loading degree and on the dissolution behavior of the drug at pH 1.2. The results showed that the loaded ITZ was apparently in amorphous form, and that the loading process did not change the chemical structure/morphology of the particles' surface. Incorporation of ITZ in both microparticles enhanced the solubility and dissolution rate of the drug, compared to the pure crystalline drug. Importantly, the physicochemical properties of the particles and the loading procedure were shown to have an effect on the drug loading efficiency and drug release kinetics. After storage under stressed conditions (3 months at 40 °C and 70% RH), the loaded silica gel particles showed practically similar dissolution profiles as before the storage. This was not the case with the loaded mesoporous silicon particles due to the almost complete chemical degradation of ITZ after storage.
介孔材料具有提高难溶性药物溶解性能的能力。在这项研究中，比较了不同的介孔硅（热氧化和热碳化）和无定形介孔硅（Syloid AL-1 和 244）微球作为疏水性药物伊曲康唑（ITZ）的药物载体。选择了不同的表面化学、孔体积、比表面积和粒径来评估颗粒的结构效应对药物载药量和药物在 pH 值为 1.2 时的溶解行为的影响。结果表明，负载的 ITZ 明显呈无定形形式，负载过程没有改变颗粒表面的化学结构/形态。与纯结晶药物相比，将 ITZ 掺入两种微球中均增强了药物的溶解度和溶解速率。重要的是，颗粒的物理化学性质和负载程序对药物载药量和药物释放动力学有影响。在应激条件下（在 40°C 和 70%RH 下储存 3 个月）后，负载硅胶颗粒的溶解曲线与储存前基本相似。对于负载的介孔硅颗粒则不是这样，因为储存后 ITZ 几乎完全化学降解。
