由CPVA-g-PSSS功能接枝微球构建pH依赖型5-ASA结肠定位释药体系  

Construction of Colon-specific Drug Delivery System with pH-dependency 5-ASA Using Grafted CPVA-g-PSSS Microspheres

作　　者：门吉英[1] 高保娇[1] 么兰[1] 张妍妍[1] 

机构地区：[1]中北大学化学工程系,山西太原030051

出　　处：《过程工程学报》2012年第4期660-664,共5页The Chinese Journal of Process Engineering

基　　金：山西省青年科学基金资助项目(编号:20110210215)

摘　　要：采用铈盐-羟基氧化还原引发体系,在交联聚乙烯醇(CPVA)微球表面引发接枝聚合对苯乙烯磺酸钠(SSS),制备了接枝聚阴离子的功能接枝微球CPVA-g-PSSS,研究了其对5-氨基水杨酸(5-ASA)的吸附(载药)性能、机理和释放行为.结果表明,在酸性介质中,受强静电相互作用驱动,CPVA-g-PSSS对5-ASA分子表现出很强的吸附能力,吸附容量达39.1mg/g,可实现有效载药.载药微球的释药行为具有强烈的pH值依赖性,在pH=1的介质中基本不释药,而在pH=7.4的介质中发生突释,释放率可达86%,表现出良好的结肠定位释放行为.The graft-polymerization of sodium 4-styrene sulfonate（SSS） was performed on the surface of crosslinked polyvinyl alcohol（CPVA） microspheres with cerium salt-hydroxyl group redox initiation system,the grafted CPVA-g-PSSS microspheres with strong anionic polyelectrolyte PSSS were obtained.On this basis,the adsorption property of the microspheres for 5-amino salicylic acid（5-ASA）,namely drug carrying ability,was investigated and the adsorption mechanism analyzed.The in vitro release behavior of the drug-carried microspheres was also examined.The experimental results show that the grafted CPVA-g-PSSS microspheres exhibit very strong adsorption ability for 5-ASA by driving of electrostatic interaction in the acidic medium.Their adsorption capacity can reach 39.1 mg/g,displaying a high efficiency of drug-loading.Their in vitro release behavior is highly pH-dependent.In the medium of pH=1,the drug is not released,while in that of pH=7.4,the burst release occurs,displaying an excellent colon-specific drug delivery behavior.

关 键 词：对苯乙烯磺酸钠 交联聚乙烯醇微球 接枝聚合 5-氨基水杨酸 pH依赖性 结肠定位释放 

分 类 号：O631[理学—高分子化学]