高等学校化学学报

高等学校化学学报

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香草醛交联壳聚糖载药微球的性能及其成球机理分析

李峻峰1,2, 张利1, 李钧甫2, 邹琴1, 杨维虎1, 李玉宝1   

    1. 四川大学分析测试中心, 纳米生物材料研究中心, 成都 610064;
    2. 成都理工大学材料科学技术研究所, 成都 610059
  • 收稿日期:2008-04-23 修回日期:1900-01-01 出版日期:2008-09-10 发布日期:2008-09-10
  • 通讯作者: 李玉宝

Properties of Drug-loaded Chitosan Microspheres Crosslinked by Vanillin and Analysis of Microsphere-forming Mechanism

LI Jun-Feng1,2, ZHANG Li1, LI Jun-Fu2, ZOU Qin1, YANG Wei-Hu1, LI Yu-Bao1*   

    1. Research Center for Nano Biomaterials, Analytical & Testing Center, Sichuan University, Chengdu 610064, China;
    2. Institute of Materials Science & Technology, Chengdu University of Technology, Chengdu 610059, China
  • Received:2008-04-23 Revised:1900-01-01 Online:2008-09-10 Published:2008-09-10
  • Contact: LI Yu-Bao

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被引次数

39

摘要： 以壳聚糖溶液为水相、液体石蜡为油相形成油包水型乳液, 以香草醛为交联剂, 采用乳化交联法制得壳聚糖微球. 结合IR光谱和XRD测试, 分析了壳聚糖交联固化成球的机理: 壳聚糖和香草醛之间所发生的Schiff碱反应和氢键的形成以及缩醛化反应, 以此为基础共同形成交联结构从而使壳聚糖交联固化成球. 探讨了交联后壳聚糖微球结晶度降低的原因: 壳聚糖固化时分子链未充分进行有序的结晶排列, 交联后的壳聚糖结构较复杂, 从而破坏了原壳聚糖分子的规整性. 选用盐酸小檗碱为模型药物, 制备了香草醛交联的壳聚糖载药微球, SEM结果显示, 载药微球表面致密且球形度好, 微球粒径在5-15 μm之间. 此外, 采用分光光度计对载药微球的载药率、药物包封率和药物体外释放性质进行了测试和分析, 结果表明载药微球缓释效果明显.

关键词: 壳聚糖微球, 交联, 香草醛, 载药, 机理

Abstract: The chitosan microspheres were prepared by emulsion cross-linking method, and vanillin was used as a cross-linking agent in the water-in-oil (W/O) emulsion composed of chitosan aqueous solution and liquid paraffin. According to the results of IR and XRD, two main mechanisms lead to the formation of cross-linked chitosan microspheres: one was the Schiff base reaction and hydrogen bond formation, the other was the acetalization. It was also discussed that the reduction of cross-linked chitosan’s crystallinity was resulted from the lack of enough rearrangement of chitosan molecular linkages and the decline of regularity of crosslinked chitosan molecular with complex structure. Using berberine hydrochloride as the model drug, the drug-loaded chitosan microspheres were observed by SEM, and the results indicate that these microspheres showed dense surface and excellent sphere-forming ability, and the sizes of microspheres are in the range of 5—15 μm. In addition, the drug loading ratio and efficiency as well as drug releasing curves were also investigated in vitro, and the results show that chitosan microspheres displayed an excellent drug-controlled release.

Key words: Chitosan microsphere, Cross-linking, Vanillin, Drug-loaded, Mechanism

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