Abstract:

O-quarternary ammonium chitosan bearing carboxymethyl-b-cyclodextrin（QCSCD）was 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 FTIR，EA and SEM. Using ketoprofen（KP）as a model drug，the release behavior of QCSCD in mimic gastric and intestinal solutions was investigated in comparison with that of chitosan bearing cyclodextrin（CSCD）. Experimental results indicated that QCSCD showed a higher drug-loading capacity with the maximum ketoprofen adsorption of 3.97 mg/mg. Compared with CSCD，QCSCD 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.

摘要：

对壳聚糖进行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FTIR、EA和SEM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QCSCD的pH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。