利用接枝微球CPVA-g-PMAA与酮洛芬分子间的氢键相互作用构建结肠定位释药体系

Constituting Colon-Specific Drug Delivery by Utilizing Hydrogen Bonding between Grafted Microspheres CPVA-g-PMAA and Ketoprofen

通过表面引发接枝聚合,在交联聚乙烯醇(CPVA)微球表面实施了甲基丙烯酸(MAA)的表面引发接枝聚合,制备了高接枝度的接枝微球CPVA-g-PMAA。利用接枝微球CPVA-g-PMAA与酮洛芬(KPF)主-客体之间的氢键相互作用构建结肠定位释药体系。分析了接枝微球CPVA-g-PMAA对KPF的吸附(载药)性能与吸附机理,深入研究了载药微球在不同pH介质中的释放行为。实验结果表明,在酸性介质中,受主-客体之间强氢键作用的驱动,接枝微球CPVA-g-PMAA对KPF分子表现出强吸附能力,吸附容量接近10mg/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,释药程度很低;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 surface-initiated graft polymerization of methacrylic acid（MAA） was performed in an aqueous solution,resulting in the grafted microspheres CPVA-g-PMAA.Utilizing hydrogen bonding between grafted microspheres CPVA-g-PMAA and ketoprofen（KPF）,colon-specific drug delivery was constituted.On this basis,the adsorption property of the grafted microspheres CPVA-g-PMAA for KPF,namely drug carrying ability,was mainly investigated and the adsorption mechanism was explored.In vitro release behavior of the drug-carried microspheres was also examined.Results show that in the acidic medium,the grafted microspheres CPVA-g-PSSS exhibit very strong adsorption ability for KPF by driving of hydrogen bond interaction.The adsorption capacity can get up to about 10 mg/g,displaying the higher efficiency of drug carrying.The in vitro release behavior of the drug carrying microspheres is highly pH-dependent.In the medium of pH=1,the release degree of the drug is small,while in the medium of pH=7.4,a burst release phenomenon will be produced,displaying an excellent colon-specific drug delivery behavior.