Wang Xin, Li Chang, Fan Na, Li Jing, Zhang Haotian, Shang Lei, He Zhonggui, Sun Jin
Wuya college of Innovation, Shenyang Pharmaceutical University, No.103, Wenhua Road, Shenyang 110016, China.
School of Life Science and Biopharmaceutics, Shenyang Pharmaceutical University, No.103, Wenhua Road, Shenyang 110016, China.
Asian J Pharm Sci. 2019 Jul;14(4):405-412. doi: 10.1016/j.ajps.2018.04.002. Epub 2018 Jul 1.
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.
在本论文中,合成了氨基官能化的手性介孔二氧化硅纳米茧(A-CMSN),并研究了其对难溶性药物吲哚美辛(IMC)的负载和释放情况。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态,其表面有卷曲的通道,这与另一种具有直通道的二维六方介孔二氧化硅纳米颗粒(MCM-41)有很大不同。通过氢键负载到两种二氧化硅载体中后,结晶态的IMC转变为无定形形式,从而提高了药物的溶出度。并且A-CMSN对IMC的负载能力高于MCM-41,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,负载IMC的A-CMSN在整个释放实验中呈现出明显更快的释放,而负载IMC的MCM-41在最初5小时释放速度比IMC快,之后则呈现出可控的缓慢释放,这与介孔二氧化硅纳米颗粒以及这两种载体不同的通道介观结构密切相关。A-CMSN具有带有卷曲二维六方通道的纳米茧形态,其通道长度比MCM-41短,因此IMC分子可以很容易地摆脱A-CMSN的束缚,进而被溶解介质包围。