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壳聚糖-g-聚甲基丙烯酸凝胶粒的制备及其药物释放行为

Preparation and Drug Release Behavior of Chitosan Grafted Poly(methacrylic acid) Gel Bead

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【作者】 陈世兰柳明珠吕少瑜金淑萍陈勇

【Author】 CHEN Shilana,b*,LIU Mingzhub,LU Shaoyub,JIN Shupingb,CHEN Yongb(aCollege of Chemistry and Chemical Engineering,Chongqing University of Science & Technology,Chongqing 401331,China; bCollege of Chemistry and Chemical Engineering,Lanzhou University,Lanzhou 730000,China)

【机构】 重庆科技学院化学化工学院兰州大学化学化工学院

【摘要】 以壳聚糖和甲基丙烯酸为原料,硝酸铈铵为引发剂,合成了不同接枝率的壳聚糖-g-聚甲基丙烯酸(CS-g-PMAA),用FTIR、1H NMR和元素分析表征了产物的结构,以柠檬酸三钠和戊二醛为交联剂制备了具有核壳结构的CS-g-PMAA载药体系。用UV/Vis检测了CS-g-PMAA粒子对模型药物的释放行为。结果表明,CS-g-PMAA接枝率为12.21%时药物释放速率最慢,其在pH=1.8介质中药物累积释放量(11 h)为44.18%,而壳聚糖粒子的累积释放量高达65.24%,即接枝改性壳聚糖粒子对药物的缓慢控制释放性能较好;CS-g-PMAA粒子的释药行为还依赖于介质的pH值和盐浓度,在低pH值和低盐浓度下,药物释放速率较快;酶环境下由于载体材料的降解使药物释放速率加快。分析了不同条件下CS-g-PMAA载药粒子中药物的释放机理。

【Abstract】 Chitosan grafted poly(methacrylic acid)(CS-g-PMAA) was synthesized using methacrylic acid and chitosan as precursors and cerium ammonium nitrate as initiator.Products with different grafting degree were characterized by means of FTIR,1H NMR and elemental analysis.Drug-loaded beads made from the as-prepared copolymers were fabricated by combining ionic-crosslink with chemical-crosslink using trisodium citrate and glutaraldehyde as crosslinking agent,respectively.The beads have a core-shell structure as revealed from scanning electron microscopy.The release behaviors of model drug incorporated in the beads were monitored using UV/Vis spectrophotometer and found to be dependent on pH and NaCl content.The results show that the drug release rate is slowest for CS-g-PMAA beads with grafting fraction(Gg) of 12.21%.The total drug release fraction for the CS-g-PMAA beads is 44.18% at pH=1.8 and is less than that of CS beads,which is 65.24%.Therefore,the grafting of CS could improve the drug release behavior.In addition,CS-g-PMAA beads have higher enzymatic stability than that of CS beads.

【基金】 重庆市教委科学技术研究项目(KJ111412);重庆市自然科学基金项目(CSTS,2008BB358)资助
  • 【文献出处】 应用化学 ,Chinese Journal of Applied Chemistry , 编辑部邮箱 ,2013年03期
  • 【分类号】TQ460.1
  • 【被引频次】5
  • 【下载频次】464
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