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具有可控双峰介孔的pH敏感型聚甲基丙烯酸-二氧化硅杂化纳米粒子的“接枝到”合成及布洛芬负载性能

"Graft to" Synthesis and Ibuprofen-Loading Performance of pH-Sensitive PMAA-Silica Hybrid Nanoparticles with Controlled Bimodal Mesopores.

作者信息

Han Jing, Sun Jihong, Bai Shiyang, Panezai Hamida, Jin Xiaoqi, Wu Xia

机构信息

Beijing Key Laboratory for Green Catalysis and Separation, Department of Chemistry and Chemical Engineering, Beijing University of Technology, Beijing 100124, People's Republic of China.

Beijing Key Laboratory for Green Catalysis and Separation, Department of Chemistry and Chemical Engineering, Beijing University of Technology, Beijing 100124, People's Republic of China.

出版信息

J Pharm Sci. 2015 Dec;104(12):4299-4306. doi: 10.1002/jps.24668. Epub 2015 Oct 26.

Abstract

Bimodal mesoporous silicas (BMMs) have been proved to be a good drug-loaded carrier. However, it did not provide stimuli sensitivity or controlled release performance yet. In the present work, a "smart" mesoporous silica-based pH-dependent [poly(methacrylic acid)]-silica hybrid nanoparticles (P/NN-BMMs) drug delivery system was developed and evaluated with ibuprofen (IBU) as a model drug. P/NN-BMMs were prepared by coating poly(methacrylic acid) (PMAA) onto amino-modified surface of BMMs via the "graft to" strategy. The structure and texture of resultant hybrid nanoparticles were determined with X-ray diffraction, scanning electron microscopy, transmission electron microscopy, Fourier transform infrared, thermogravimetric analysis, N2 sorption isotherms, and elemental analysis. The PMAA acts as a molecular switch to achieve controlled drug release and the amount of grafted-PMAA can remarkably affect its performance. The drug-loading rate is decreased markedly with the increasing of the amount of grafted-PMAA, meanwhile, the drug-loading kinetics on P/NN-BMMs fits Korsmeyer-Peppas model. In addition, the drug-release amount from drug-loaded P/NN-BMMs is pH dependent, showing an increasing tendency with the increase of pH value.

摘要

双峰介孔二氧化硅(BMMs)已被证明是一种良好的载药载体。然而,它尚未具备刺激敏感性或控释性能。在本研究中,开发了一种基于介孔二氧化硅的“智能”pH依赖性[聚(甲基丙烯酸)]-二氧化硅杂化纳米颗粒(P/NN-BMMs)药物递送系统,并以布洛芬(IBU)作为模型药物进行了评估。通过“接枝到”策略将聚(甲基丙烯酸)(PMAA)包覆在BMMs的氨基修饰表面上制备了P/NN-BMMs。通过X射线衍射、扫描电子显微镜、透射电子显微镜、傅里叶变换红外光谱、热重分析、N2吸附等温线和元素分析确定了所得杂化纳米颗粒的结构和织构。PMAA作为分子开关实现药物的控释,接枝的PMAA量可显著影响其性能。随着接枝PMAA量的增加,载药率显著降低,同时,P/NN-BMMs上的载药动力学符合Korsmeyer-Peppas模型。此外,载药P/NN-BMMs的药物释放量取决于pH值,随pH值的增加呈上升趋势。

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