接枝微球CPVA-g-PSSS的制备及其对5-氟尿嘧啶载药及体外结肠定位释药特性研究  

PREPARATION OF GRAFTED MICROSPHERES CPVA-g-PSSS AND STUDIES ON THEIR CHARACTER OF DRUG CARRYING AND COLON-SPECIFIC DRUG DELIVERY FOR 5-FLUOROURACIL

作　　者：门吉英[1] 高保娇[1] 陈志萍[1] 

机构地区：[1]中北大学化学工程系,太原030051

出　　处：《高分子学报》2012年第9期943-951,共9页Acta Polymerica Sinica

基　　金：山西省青年科学基金(基金号20110210215)资助项目

摘　　要：在具有生物相容性的交联聚乙烯醇(CPVA)微球表面,采用铈盐-羟基氧化还原引发体系,实施了对苯乙烯磺酸钠(SSS)的表面引发接枝聚合,制得了接枝有聚阴离子的接枝微球CPVA-g-PSSS,采用红外光谱(FTIR)、扫描电子显微镜(SEM)及zeta电位测定等法,对接枝微球的化学结构及物理化学特性进行了表征.在此基础上重点考察分析了接枝微球CPVA-g-PSSS对5-氟尿嘧啶(5-FU)的吸附(载药)性能与吸附机理,考察探索了载药微球在不同pH介质中的释放行为.实验结果表明,羟基-铈盐氧化还原引发体系可有效地引发SSS在CPVA微球的表面接枝聚合,在适宜的反应条件下,可制得PSSS接枝度为16.1 g/100g的接枝微球CPVA-g-PSSS.在酸性介质中,受强静电相互作用的驱动,接枝微球CPVA-g-PSSS对5-FU分子表现出很强的吸附能力,吸附容量达105 mg/g,可实现有效载药.载药微球的释药行为具有强烈的pH依赖性,在pH=1的介质中,基本不释药;而在pH=7.4的介质中,则发生突释,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 surfaces of crosslinked polyvinyl alcohol（CPVA） microspheres using cerium salt-hydroxyl group redox initiation system,and the grafted microspheres CPVA-g-PSSS,on which the strong anionic polyelectrolyte PSSS was grafted,was obtained.The chemical structure and physicochemistry characters of CPVA-g-PSSS microspheres were adequately characterized by infrared spectrum（FTIR）,scanning electron microscope（SEM） and determination of zeta potential.On this basis,the adsorption property of CPVA-g-PSSS microspheres for 5-fluorouracil（5-FU）,namely the drug carrying ability,was mainly investigated and the adsorption mechanism was discussed.The in vitro release behavior of the drug-carried microspheres was also examined.The experimental results show that cerium salt-hydroxyl group redox initiation system can effectively initiate the graft polymerization of SSS on CPVA microspheres,and under the suitable conditions,the grafting degree of PSSS can reach 16.1 g/100g.In the acidic medium,the grafted microspheres CPVA-g-PSSS exhibit very strong adsorption ability for 5-FU by driving of electrostatic interaction.The adsorption capacity can get up to 105 mg/g,displaying the high efficiency of drug-loading.The in vitro release behavior of the drug-carrying microspheres is highly pH-dependent.In the medium of pH=1,the drug is not released,while in the medium of pH=7.4,the burst release phenomenon will be produced,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-氟尿嘧啶 pH依赖性 结肠定位释放 

分 类 号：R94[医药卫生—药剂学]