肝素/壳聚糖微胶囊的制备及其抗凝血性能

采用层层自组装(LbL)技术制备了肝素/壳聚糖(HEP/CHI)5微胶囊,并研究了其抗凝血性能、胃肠道稳定性和毒副作用等。结果表明:该微胶囊具有球形结构;在pH 5.0、7.4中肝素能够缓慢可控地释放;在pH 5.0、7.4以及模拟胃液、肠液条件下具有稳定性;APTT法和全凝固实验验证了它在体外具有良好的抗凝血效果;并且对内皮细胞细胞毒性。因此,该微胶囊有望作为口服剂型,用于临床肝素给药。
Heparin/chitosan(HEP/CHI)5 microcapsules for anticoagulation were prepared by Layer-by-layer(LbL) technique. The stability of(HEP/CHI)5 microcapsules under pH 5.0 and 7.4,simulated gastric and intestinal juices conditions was studied respectively,APTT anticoagulant time and cytotoxicity of microcapsules against endothelial cells were estimated. Results indicated that(HEP/CHI)5 microcapsules were of spherical structure and stable in different simulated physiological milieus;they could behave favorable anticoagulant efficacy with no significant cytotoxicity. Thus,(HEP/CHI)5 microcapsules were promising for clinical heparin administration as a novel oral dosage form