Centre for Novel Drug Delivery Systems, Department of Pharmaceutical Sciences and Technology, Institute of Chemical Technology, Matunga, Mumbai, 400019, India.
AAPS PharmSciTech. 2017 Oct;18(7):2764-2773. doi: 10.1208/s12249-017-0761-x. Epub 2017 Mar 28.
The aim of present investigation was the preparation of dodecylamine template-based hexagonal mesoporous silica (HMS) as a carrier for poorly water-soluble drug (fenofibrate). HMS material has distinctive characteristics such as easy synthesis, high surface area and wormhole pores. These characteristics are highly admirable to make use of it as a carrier in drug delivery system. HMS was prepared by pH and temperature-independent process. Fenofibrate was loaded into the HMS by solvent immersion method using organic solvent. The BET surface area of HMS was evaluated by nitrogen adsorption/desorption analysis. HMS and drug-loaded HMS were characterized by differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD), Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), transmission electron microscopy (TEM) and contact angle study. The HMS-based system was also evaluated for in vitro and in vivo study as compared to plain drug. The BET surface area of HMS was found 974 m/g with a narrow pore size average of 2.6 nm. The DSC and XRD study confirmed the amorphization of drug within the HMS. SEM and TEM study showed morphological features of HMS as well as revealed the wormhole porous structure. Contact angle study showed improvement in aqueous wetting property of drug within the HMS (contact angle 46°). The In vitro drug release study showed a remarkable dissolution enhancement in HMS-based system as compared to plain drug. In vivo pharmacodynamic study (hyperlipidaemia model) exhibited HMS-based formulation was significantly improved the bioavailability of fenofibrate. Thus, HMS has admirable properties; makes it a potential carrier for delivery system of poorly water-soluble drugs.
本研究的目的是制备十二胺模板的六方介孔硅（HMS）作为载体用于负载疏水性药物（非诺贝特）。HMS 材料具有易合成、高比表面积和蠕虫状孔等独特的特性。这些特性使其非常适合用作药物传递系统中的载体。通过 pH 和温度独立的过程制备 HMS。采用有机溶剂浸渍法将非诺贝特负载到 HMS 中。通过氮气吸附/解吸分析评估 HMS 的 BET 比表面积。采用差示扫描量热法（DSC）、X 射线粉末衍射（XRPD）、傅里叶变换红外光谱（FTIR）、扫描电子显微镜（SEM）、透射电子显微镜（TEM）和接触角研究对 HMS 和载药 HMS 进行了表征。与普通药物相比，还对基于 HMS 的系统进行了体外和体内研究评价。HMS 的 BET 比表面积为 974 m/g，平均孔径较小，为 2.6 nm。DSC 和 XRD 研究证实了药物在 HMS 中的无定形化。SEM 和 TEM 研究显示了 HMS 的形态特征，并揭示了蠕虫状多孔结构。接触角研究表明，药物在 HMS 中的润湿性得到了改善（接触角为 46°）。体外药物释放研究表明，与普通药物相比，基于 HMS 的系统具有显著的溶解增强作用。体内药效学研究（高脂血症模型）表明，基于 HMS 的配方显著提高了非诺贝特的生物利用度。因此，HMS 具有令人钦佩的特性；使其成为疏水性药物传递系统的潜在载体。
