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将β-环糊精、环氧氯丙烷和氯化胆碱经一步缩聚反应制得阳离子环糊精聚合物(CPβCD),采用反相悬浮法制备壳聚糖微球(CS),再以环氧氯丙烷为交联剂制备具有CPβCD和CS双重特性的壳聚糖固载阳离子环糊精聚合物微球(CS/CPβCD),用核磁共振(1H-NMR),红外光谱(FT-IR),扫描电镜(SEM)和X射线衍射(XRD)对产物进行表征,以酮洛芬为模型药物,研究了CS/CPβCD微球的载药性能。结果表明,CS/CPβCD微球对酮洛芬的最大载药量为849.4 mg/g,吸附规律符合Freundlich等温方程,载药CS/CPβCD微球具有缓释性能,并且在模拟肠液中的缓释效果优于模拟胃液,为CS/CPβCD作为药物缓释载体提供了依据。

Cationicβ-cyclodextrin polymer(CPβCD) was synthesized by a one-step condensation ofβ-cyclodextrin,epoxychoropropane,and choline chloride.The as-prepared CPβCD was then cross-linked with chitosan microspheres prepared via an inverse phase suspension method using epichlorohydrin as the cross-linking agent to obtain chitosan bearing cationicβ-cyclodextrin polymer(CS/CPβCD).The structures of the products were characterized by1Hnucle- ar magnetic resonance spectrum(1H-NMR),Fourier transform infrared spectrum(FT-IR),X-ray diffraction(XRD) and scanning electron microscope(SEM).Drug performance was studied using ketoprofen as a model drug.The ex- perimental results indicated that the maximum drug-loading capacity of CS/CPβCD to ketoprofen was 849.4 mg/g,the adsorption equilibrium was fitted to Freundlich equation.The release of ketoprofen from CS/CPβCD microspheres was pH-sensitive.Fast release occurred in simulated gastric fiuid(pH1.2),while the release was slow in simulated intestinal fluid(pH 7.4).The research provides the basis of drug-loading performances of CS/CPβCD.

参考文献

[1] 曹佐英,张启修,魏琦峰.微波辐射下交联壳聚糖树脂固载化β-环糊精[J].高分子材料科学与工程,2003(03):204-207.
[2] 黄岚,辛剑宇,张楠,李建树.阳离子β-环糊精聚合物复合胰岛素的海藻酸钠/壳聚糖载药微球[J].中国组织工程研究与临床康复,2009(08):1481-1485.
[3] 胡智文,郑世睿,万军民,高磊,温会涛,陈文兴.纤维素纤维接枝β-环糊精预聚体的制备及包结性能[J].高分子材料科学与工程,2008(01):39-43.
[4] M. Prabaharan;R. Jayakumar .Chitosan-graft-β-cyclodextrin scaffolds with controlled drug release capability for tissue engineering applications[J].International Journal of Biological Macromolecules: Structure, Function and Interactions,2009(4):320-325.
[5] Prabaharan M;Mano JF .Hydroxypropyl chitosan bearing beta-cyclodextrin cavities: Synthesis and slow release of its inclusion complex with a model hydrophobic drug[J].Macromolecular bioscience,2005(10):965-973.
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