摘要
肝素(hep)作为一种抗凝剂,在临床医学上广泛应用。本文以肝素为亲水段、去氧胆酸(DOCA)为疏水段合成了一种肝素类两亲性的聚合物(hep-DOCA,HD),并通过水相自组装方法,制备纳米胶束(HD-IDM),装载具有抗血栓作用的吲哚美辛(IDM),协同实现材料的抗凝血功能。通过动态光散射、Zeta电势和透射电子显微镜(TEM)等技术手段表征了纳米胶束结构和性能。当纳米胶束载药量为0.0913mg/mL时,载药纳米胶束浓度为0.4g/L,此时细胞存活率为92.81%,溶血率为0.83%,表明载药胶束具有良好的生物相容性。肝素钠,hep-DOCA和HD-IDM的全血凝血指数分别为86.48%、77.47%和89.53%,全血凝血时间分别为927、837和965s,血栓凝块实验中产生的血栓质量分别为0.11、0.20和0.07g,证明载药纳米胶束具有优良的抗凝血效果。
Heparin has been used as anti-thrombotic agents clinically.In this work,the copolymer based on hydrophilic heparin and hydrophobic deoxycholic acid(hep-DOCA,HD)was synthesized.Indometacin(IDM)-loaded HD micelles were prepared through aqueous self-assembly to enhance the anti-thrombotic capability of micelles synergistically and characterized by dynamic light scattering,Zeta potential and transmission electron microscopry(TEM).When the drug content of the nanomicelles was 0.0913 g/L,the concentration of the drug-loaded nanomicelle was 0.4 g/L,and the cell survival rate and hemolysis rate were 92.81%and 0.83%,indicating that the drug-loaded nanomicelles had good biocompatibility.The whole blood coagulation indexes of heparin sodium,hep-DOCA and HD-IDM were 86.48%,77.47%and 89.53%,respectively.The whole blood coagulation time was 927,837 and 965 s,respectively.The thrombus mass produced in the thrombus clotting experiment was 0.11,0.20 and 0.07 g,respectively,which confirmed that the drug-loaded nanomicelles had excellent anticoagulant effect.
作者
王焱明
李伟佳
钱升旭
赵巍
杨鹤
辛志荣
WANG Yanming;LI Weijia;QIAN Shengxu;ZHAO Wei;YANG He;XIN Zhirong(Chemistry and Chemical Engineering,Yantai University,Yantai,Shandong 264005,China)
出处
《应用化学》
CAS
CSCD
北大核心
2019年第6期641-648,共8页
Chinese Journal of Applied Chemistry
基金
山东省自然科技基金(ZR2019MEM008)资助项目~~
关键词
肝素
去氧胆酸
纳米胶束
吲哚美辛
抗凝血
heparin
deoxycholic acid
micelles
indomethacin
anticoagulant
