槲皮素包合物微球的制备及其体外释放研究

目的:制备槲皮素β-环糊精包合物-壳聚糖微球(QT-CD-CM),并考察其理化性质和药物体外释放性能。方法:采用有机溶剂挥发法制备槲皮素β-环糊精包合物,再用乳化分散-离子交联法、以三聚磷酸钠为交联剂制备壳聚糖微球,并考察其形态、粒径、包封率、载药量和体外释放情况。结果:制备的QT-CD-CM形态规则、均质、无粘连,平均粒径(3.327±0.124)μm,包封率为32.4%,载药量为12.3%,在5%乙醇-磷酸盐缓冲液介质中72h可以达到完全释药,释药过程符合一级动力学模型。结论:QT-CD-CM理化性质及体外释药性能良好,制备工艺简单,有望成为理想的槲皮素给药系统。

Study on the Preparation of Quercetin Inclusion Complex Microsphere and Its Drug Release in Vitro

OBJECTIVE：To prepare Quercetin-β-cyclodextrin inclusion complex-chitosan microspheres（QT-CD-CM）,and to investigate their physiochemical property and release characteristics in vitro.METHODS：The quercetin-β-cyclodextrin inclusion complexes were prepared by organic solvent evaporation methods,and then formed chitosan microspheres which were prepared using emulsion-linking technique with sodium tripolyphosphate as the cross-linker.The morphology,particle size,encapsulation efficiency,drug-loading amount and release kinetics of microspheres were investigated.RESULTS：Prepared QT-CD-CM were regular,discrete and uniform spheres with mean particle size of（3.327±0.124） μm,encapsulation efficiency of 32.4% and drug-loading amount of 12.3%.Prepared microspheres released completely in 5% ethanol-PBS in 72 h,which was in line with first-order kinetic model.CONCLUSION：QT-CD-CM are sound in physicochemical and release property and simple in preparation technology,and can be used as ideal drug delivery system for quercetin.