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中北大学化学工程系,太原,030051
纸质出版日期:2012-9-20,
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门吉英, 高保娇, 陈志萍. 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[J]. 高分子学报, 2012,(9):943-951.
Ji-ying Men, Bao-jiao Gao, Zhi-ping Chen. PREPARATION OF GRAFTED MICROSPHERES CPVA-g-PSSS AND STUDIES ON THEIR CHARACTER OF DRUG CARRYING AND COLON-SPECIFIC DRUG DELIVERY FOR 5-FLUOROURACIL[J]. Acta Polymerica Sinica, 2012,(9):943-951.
门吉英, 高保娇, 陈志萍. 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[J]. 高分子学报, 2012,(9):943-951. DOI: 10.3724/SP.J.1105.2012.12003.
Ji-ying Men, Bao-jiao Gao, Zhi-ping Chen. PREPARATION OF GRAFTED MICROSPHERES CPVA-g-PSSS AND STUDIES ON THEIR CHARACTER OF DRUG CARRYING AND COLON-SPECIFIC DRUG DELIVERY FOR 5-FLUOROURACIL[J]. Acta Polymerica Sinica, 2012,(9):943-951. DOI: 10.3724/SP.J.1105.2012.12003.
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.
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
Sodium 4-styrene sulfonateCrosslinked polyvinyl alcohol microspheresGraft polymerization5-FluorouracilpH-dependenceColon-specific drug delivery
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