应用化学

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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

陈世兰1,2*,柳明珠2,吕少瑜2,金淑萍2,陈勇2   

  1. (1.重庆科技学院化学化工学院 重庆 401331;2.兰州大学化学化工学院 兰州 730000)
  • 收稿日期:2012-05-10 修回日期:2012-06-28 出版日期:2013-03-10 发布日期:2013-03-10
  • 通讯作者: 陈世兰,副教授; Tel/Fax:023-65023757; E-mail:zhouchen1978@126.com; 研究方向:智能高分子材料
  • 基金资助:
    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

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

CHEN Shilan1,2*, LIU Mingzhu2, LU Shaoyu2, JIN Shuping2, CHEN Yong2   

  1. (1.College of Chemistry and Chemical Engineering,Chongqing University of Science & Technology,Chongqing 401331,China;
    2.College of Chemistry and Chemical Engineering,Lanzhou University,Lanzhou 730000,China)
  • Received:2012-05-10 Revised:2012-06-28 Published:2013-03-10 Online:2013-03-10

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。

关键词: 壳聚糖, 甲基丙烯酸, 接枝共聚, 药物释放, 核壳结构

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.

Key words: chitosan, methacrylic acid, graft copolymer, drug release, core-shell structure

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