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3D 立方介孔硅微球的简便合成及其可控孔径在改善难溶性药物传递中的应用。

Facile synthesis of 3D cubic mesoporous silica microspheres with a controllable pore size and their application for improved delivery of a water-insoluble drug.

机构信息

Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, Liaoning Province 110016, PR China.

出版信息

J Colloid Interface Sci. 2011 Nov 1;363(1):410-7. doi: 10.1016/j.jcis.2011.07.022. Epub 2011 Jul 21.

Abstract

A facile and simplified method was developed for the synthesis of 3D cubic mesoporous SBA-16 with both a spherical morphology and controllable pore size. The addition of CTAB during the synthesis allowed not only good control over the macroscopic morphology but also a significant reduction in the synthesis time. Notably, the pore size can simultaneously be adjusted by simply controlling the heating temperature. The pharmaceutical performance of the resulting SBA-16 for the delivery of the water-insoluble drug indomethacin (IMC), a non-steroidal anti-inflammatory agent used as a model drug, was systematically studied using nitrogen adsorption, powder X-ray diffraction, differential scanning calorimetry, infrared spectrometry and in vitro dissolution investigations. It was found that IMC could be effectively loaded into mesoporous SBA-16 via the solvent deposition method. An altered physical state and a marked improvement in the dissolution rate were observed for IMC after being loaded into SBA-16 microspheres. In particular, SBA-16 microspheres with the largest pore size (9.0 nm) and highly open and accessible pore networks exhibited the fastest drug release profile. We envisage that the improved drug delivery profiles obtained using SBA-16 as described in our work will offer an interesting option for the formulation of poorly water-soluble drugs.

摘要

本文开发了一种简便、简化的方法,用于合成具有球形形貌和可控孔径的 3D 立方介孔 SBA-16。在合成过程中添加 CTAB 不仅可以很好地控制宏观形貌,还可以显著缩短合成时间。值得注意的是,只需控制加热温度即可同时调整孔径。通过氮气吸附、粉末 X 射线衍射、差示扫描量热法、红外光谱和体外溶解研究,系统地研究了所得 SBA-16 作为模型药物的难溶性药物吲哚美辛(IMC)的药物传递性能。结果表明,IMC 可以通过溶剂沉积法有效地负载到介孔 SBA-16 中。负载到 SBA-16 微球后,IMC 的物理状态发生变化,溶解速率显著提高。特别是具有最大孔径(9.0nm)和高度开放且可及的孔网络的 SBA-16 微球表现出最快的药物释放曲线。我们设想,使用本文所述 SBA-16 获得的改善的药物递送曲线将为难溶性药物的配方提供一个有趣的选择。

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