化工进展

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O-季铵化改性壳聚糖固载环糊精的制备及其载药性能

毛扬帆,李明春,辛梅华,谢钦钦   

  1. 华侨大学材料科学与工程学院,福建省高校功能材料重点实验室,福建 厦门361021
  • 出版日期:2010-09-05 发布日期:2010-09-05

Synthesis of O-quarternary ammonium chitosan bearing cyclodextrin

MAO Yangfan,LI Mingchun,XIN Meihua,XIE Qinqin   

  1. College of Material Science and Engineering,Huaqiao University,The Key Laboratory for Functional Materials
  • Online:2010-09-05 Published:2010-09-05

摘要:

壳聚糖进行O-季铵化改性,并与羧甲基-β-环糊精在均相条件下进行缩合反应,制得O-季铵化壳聚糖固载环糊精(QCSCD),用FTIREASEM对产物进行表征。以酮洛芬为模型药物,研究其载药及药物释放行为。结果表明,季铵盐基团的引入提高了QCSCD的载药量,为3.97mg/mg,并且改变了QCSCDpH响应性能。与壳聚糖固载环糊精相反,QCSCD在模拟胃液中的释放速率很快,而在模拟肠液中具有缓释性能。

Abstract:

O-quarternary ammonium chitosan bearing carboxymethyl-b-cyclodextrinQCSCDwas synthesized by grafting carboxymethyl-b-cyclodextrin onto O-quarternary ammonium chitosan in the presence of EDC and NHS. The structure of QCSCD was characterized by FTIREA and SEM. Using ketoprofenKPas a model drugthe release behavior of QCSCD in mimic gastric and intestinal solutions was investigated in comparison with that of chitosan bearing cyclodextrinCSCD. Experimental results indicated that QCSCD showed a higher drug-loading capacity with the maximum ketoprofen adsorption of 3.97 mg/mg. Compared with CSCDQCSCD behaved an opposite pH responsibility and represented more stable release of the entrapped ketoprofen in mimic intestinal solution. These results suggested that QCSCD could be used as a potential biodegradable delivery system for controlled release of hydrophobic drugs with pH-responsive capability.

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