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Amino functionalized chiral mesoporous silica nanoparticles for improved loading and release of poorly water-soluble drug

机译:氨基官能化的手性介孔二氧化硅纳米粒子用于改善难溶性药物的负载和释放

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摘要

In the present paper, chiral mesoporous silica nano-cocoon (A-CMSN) functionalized with amino group was synthesized, and its loading and release of indomethacin (IMC), a poorly soluble drug, was studied. Due to the use of chiral anionic surfactants as a template, A-CMSN possessed 2D hexagonal nano-cocoon morphology with curled channels on its surface, which was quite different from another 2D hexagonal mesoporous silica nanoparticles (MCM-41) with straightway channels. After being loaded into the two silica carriers by hydrogen bond, crystalline IMC converted to amorphous form, leading to the improved drug dissolution. And IMC loading capacity of A-CMSN was higher than MCM-41 because curled loading process originating from curvature chiral channels can hold more drug molecules. Compared with IMC, IMC loaded A-CMSN presented obviously fast release throughout the release experiment, while IMC loaded MCM-41 released faster than IMC at the initial 5 h then showed controlled slow release afterwards, which was closely related to the mesoporous silica nanoparticles and different channel mesostructures of these two carriers. A-CMSN possessed nano-cocoon morphology with curled 2D hexagonal channel and its channel length was shorter than MCM-41, therefore IMC molecules can easily get rid of the constraint of A-CMSN then to be surrounded by dissolution medium.
机译:本文合成了被氨基官能化的手性介孔二氧化硅纳米茧(A-CMSN),并研究了难溶性药物吲哚美辛(IMC)的负载和释放。由于使用手性阴离子表面活性剂作为模板,A-CMSN具有二维六方纳米茧形貌,表面上有卷曲的通道,这与另一种具有直通道的六方六方介孔二氧化硅纳米颗粒(MCM-41)完全不同。通过氢键加载到两个二氧化硅载体中后,结晶的IMC转变为无定形形式,从而改善了药物的溶出度。 A-CMSN的IMC负载能力高于MCM-41,这是因为源自曲率手性通道的卷曲负载过程可以容纳更多的药物分子。与IMC相比,IMC负载的A-CMSN在整个释放实验中均表现出明显的快速释放,而IMC负载的MCM-41在最初5h内的释放速度要比IMC快,然后表现出受控的缓慢释放,这与介孔二氧化硅纳米粒子和这两个载波的不同通道介观结构。 A-CMSN具有纳米茧形的二维卷曲六边形通道,其通道长度比MCM-41短,因此IMC分子可以轻松摆脱A-CMSN的约束,然后被溶蚀介质包围。

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