【作者】 张颖锴； 王光磊； 刘晓丽； 谢操； 魏刚； 倪京满； 陆伟跃；

【Author】 Yinkai Zhang1,2,Guanglei Wang1,Xiaoli Liu1,Cao Xie1,Gang Wei1,Jingman Ni2,Weiyue Lu1 (1School of Pharmacy,Fudan University,Shanghai 201203;2 School of Pharmacy,Lanzhou University,Gansu Lanzhou 730000)

【机构】 复旦大学药学院； 兰州大学药学院；

【摘要】 目的探讨人源性α-防御素HNP1用于修饰生物黏附给药系统的可行性。方法采用表面等离子共振(SPR)技术评价HNP1在不同pH和浓度条件下与黏蛋白之间的相互作用,小动物活体成像考察荧光探针标记的HNP1在离体兔眼角膜表面的消除,并与植物来源的麦胚凝集素(WGA)进行比较,凝血实验评价HNP1的生物安全性。结果 HNP1能够在较宽的pH范围内与黏蛋白相互作用,二者的结合强度在碱性条件下减弱,并且呈现浓度依赖性。HNP1能够滞留于离体兔眼角膜表面,其延缓荧光探针消除的效果与WGA相当,而且不引起红细胞凝集。结论 HNP1是一种新型的生物黏附材料,在黏膜给药方面具有良好的应用前景。更多还原

【Abstract】 Aim The purpose of this work is to explore the feasibility of developing human α-defensins HNP1 mediated bioadhesive drug delivery system. Method The interactions between HNP1 and mucin under various pH conditions and concentrations were evaluated by surface plasmon resonance (SPR) technology. The elimination of fluorescent probe-labeled HNP1 from isolated rabbit corneal was investigated using Kodak In-Vivo Imaging Systems, and was compared with that of plant lectin - wheat germ agglutinin (WGA). Erythrocytic aggregation was used to assess the biological safety of HNP1. Results:HNP1 interacted with mucin in a wide pH range. Their binding decreased under basic conditions, and increased in a concentration-dependent manner. The eliminative behaviors of HNP1 from isolated cornea were similar with that of WGA, both of them prolonged the resident time of fluorescent probe. Furthermore, HNP1 did not result in Erythrocytic aggregation. Conclusion:HNP1 is a novel bioadhesive material with good biological safety, and is promising in developing mucous drug delivery system.更多还原