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甲基丙烯酸缩水甘油酯有机桥接介孔硅 SBA-15 的制备及表征作为布洛芬和美沙拉嗪的控释载体。

Preparation and characterization of glycidyl methacrylate organo bridges grafted mesoporous silica SBA-15 as ibuprofen and mesalamine carrier for controlled release.

机构信息

Institute of Chemistry, University of Campinas, UNICAMP, P.O. Box 6154, 13084-971 Campinas, SP, Brazil; Interdisciplinary Research Centre in Biomedical Materials (IRCBM), COMSATS Institute of Information Technology, Lahore, Pakistan.

Interdisciplinary Research Centre in Biomedical Materials (IRCBM), COMSATS Institute of Information Technology, Lahore, Pakistan.

出版信息

Mater Sci Eng C Mater Biol Appl. 2016 Feb;59:970-979. doi: 10.1016/j.msec.2015.11.005. Epub 2015 Nov 4.

Abstract

Mesoporous silica SBA-15 was synthesized and functionalized with bridged polysilsesquioxane monomers obtained by the reaction of 3-aminopropyltriethoxy silane with glycidyl methacrylate in 2:1 ratio. The synthesized mesoporous silica materials were characterized by elemental analysis, infrared spectroscopy, nuclear magnetic resonance spectroscopy, nitrogen adsorption, X-ray diffraction, thermogravimetry and scanning electron microscopy. The nuclear magnetic resonance in the solid state is in agreement with the sequence of carbon distributed in the attached organic chains, as expected for organically functionalized mesoporous silica. After functionalization with organic bridges the BET surface area was reduced from 1311.80 to 494.2m(2)g(-1) and pore volume was reduced from 1.98 to 0.89cm(3)g(-1), when compared to original precursor silica. Modification of the silica surface with organic bridges resulted in high loading capacity and controlled release of ibuprofen and mesalamine in biological fluids. The Korsmeyer-Peppas model better fits the release data indicating Fickian diffusion and zero order kinetics for synthesized mesoporous silica. The drug release rate from the modified silica was slow in simulated gastric fluid, (pH1.2) where less than 10% of mesalamine and ibuprofen were released in initial 8h, while comparatively high release rates were observed in simulated intestinal (pH6.8) and simulated body fluids (pH7.2). The preferential release of mesalamine at intestinal pH suggests that the modified silica could be a simple, efficient, inexpensive and convenient carrier for colon targeted drugs, such a mesalamine and also as a controlled drug release system.

摘要

介孔硅 SBA-15 是通过 3-氨丙基三乙氧基硅烷与缩水甘油甲基丙烯酸酯以 2:1 的比例反应合成的桥联聚硅倍半氧烷单体功能化的。合成的介孔硅材料通过元素分析、红外光谱、核磁共振光谱、氮气吸附、X 射线衍射、热重分析和扫描电子显微镜进行了表征。固态核磁共振与预期的有机官能化介孔硅中分布的碳的序列一致。与原始前体硅相比,用有机桥接官能化后,BET 表面积从 1311.80 降至 494.2m(2)g(-1),孔体积从 1.98 降至 0.89cm(3)g(-1)。介孔硅表面的有机桥接修饰导致布洛芬和柳氮磺胺吡啶在生物流体中的高载药量和控制释放。Korsmeyer-Peppas 模型更适合释放数据,表明合成介孔硅的扩散为 Fickian 扩散,动力学为零级。在模拟胃液 (pH1.2) 中,改性硅释放的柳氮磺胺吡啶和布洛芬均小于初始 8 小时内的 10%,而在模拟肠液 (pH6.8) 和模拟体液 (pH7.2) 中观察到较高的释放速率。在肠道 pH 下柳氮磺胺吡啶的优先释放表明,改性硅可能是一种简单、高效、廉价和方便的结肠靶向药物载体,如柳氮磺胺吡啶,也可以作为一种控制药物释放系统。

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