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裸露型和氨基修饰的介孔二氧化硅@聚(乙烯亚胺)干凝胶作为吲哚美辛载体的比较:氨基修饰的优越性

Comparison of bare and amino modified mesoporous silica@poly(ethyleneimine)s xerogel as indomethacin carrier: Superiority of amino modification.

作者信息

Li Jing, Xu Lu, Wang Hongyu, Yang Baixue, Liu Hongzhuo, Pan Weisan, Li Sanming

机构信息

School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China.

School of Pharmacy, Shenyang Pharmaceutical University, Shenyang, China.

出版信息

Mater Sci Eng C Mater Biol Appl. 2016 Feb;59:710-716. doi: 10.1016/j.msec.2015.10.072. Epub 2015 Oct 26.

Abstract

The purpose of this study was to facilely develop amino modified mesoporous silica xerogel synthesized using biomimetic method (B-AMSX) and to investigate its potential ability to be a drug carrier for loading poorly water-soluble drug indomethacin (IMC). For comparison, mesoporous silica xerogel without amino modification (B-MSX) was also synthesized using the same method. The changes of characteristics before and after IMC loading were systemically studied using fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), small angle X-ray scattering (SAXS) and nitrogen adsorption/desorption analysis. The results showed that B-MSX and B-AMSX were spherical nanoparticles with mesoporous structure. Compared with B-MSX, IMC loading capacity of B-AMSX was higher because more drug molecules can be loaded through stronger hydrogen bonding force. DSC and SAXS analysis confirmed the amorphous state of IMC after being loaded into B-MSX and B-AMSX. The in vitro drug release study revealed that B-MSX and B-AMSX improved IMC release significantly, and B-AMSX released IMC a little faster than B-MSX because of larger pore diameter of IMC-AMSX. B-MSX and B-AMSX degraded gradually in dissolution medium evidenced by color reaction and absorbance value, and B-AMSX degraded slower than B-MSX due to amino modification. In conclusion, B-AMSX with superiority of higher loading capacity and enhanced dissolution release can be considered to be a good candidate as drug carrier for IMC.

摘要

本研究的目的是简便地制备采用仿生方法合成的氨基修饰介孔二氧化硅干凝胶(B-AMSX),并研究其作为载药载体负载难溶性药物吲哚美辛(IMC)的潜在能力。为作比较,还采用相同方法合成了未进行氨基修饰的介孔二氧化硅干凝胶(B-MSX)。使用傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)、小角X射线散射(SAXS)和氮气吸附/脱附分析系统研究了负载IMC前后的特性变化。结果表明,B-MSX和B-AMSX均为具有介孔结构的球形纳米颗粒。与B-MSX相比,B-AMSX对IMC的负载能力更高,因为通过更强的氢键力可以负载更多的药物分子。DSC和SAXS分析证实了IMC负载到B-MSX和B-AMSX后呈无定形状态。体外药物释放研究表明,B-MSX和B-AMSX显著改善了IMC的释放,并且由于IMC-AMSX的孔径较大,B-AMSX释放IMC的速度比B-MSX略快。通过显色反应和吸光度值证明,B-MSX和B-AMSX在溶解介质中逐渐降解,并且由于氨基修饰,B-AMSX的降解速度比B-MSX慢。总之,具有更高负载能力和增强溶解释放优势的B-AMSX可被认为是IMC药物载体的良好候选者。

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