摘要
合成RGD肽修饰的聚(2-乙基-2-噁唑啉)(PEOz)接枝壳聚糖聚离子胶束(RGD-PIC),包载抗凝药物重组水蛭素-2(rHV_(2)),对载药胶束进行药剂学性质、体外释药、抗血栓效果及体内药动学评价。结果表明,RGD-PIC载药胶束的平均粒径为(297.0±23.07)nm,Zeta电位为(-7.36±3.60)mV,包封率为96.66%±0.22%,载药量为6.59%±0.025%;体外释药试验结果表明,载药胶束具有明显的缓释效果;APTT试验结果表明,rHV_(2)-RGD-PIC能显著延长血浆凝固时间。RGD-PIC胶束在抗凝方面大大优于普通胶束,体内循环时间长,可用作rHV_(2)的血小板靶向递送和长循环的载体。
The recombinant hirudin-2(rHV_(2))loaded poly(2-ethyl-2-oxazoline)(PEOz)grafted chitosan polyion micelles(RGD-PIC)modified by RGD peptide was prepared and characterized,and the pharmacological properties,in vitro release,antithrombotic effect and in vivo pharmacokinetics of drug-loaded micelles were evaluated.The results showed that the average particle size of RGD-PIC drug-loaded micelles was(297.0±23.07)nm,the Zeta potential was(-7.36±3.60)mV,the encapsulation efficiency was 96.66%±0.22%,and the drug loading was 6.59%±0.025%.The in vitro drug release test results showed that the drug-loaded micelles had a significant slow-release effect.The APTT test results showed that rHV_(2)-RGD-PIC could significantly prolong the plasma clotting time.RGD-PIC micelles were much better than ordinary micelles in anticoagulation,and had a long circulation time in the body.They can be used as a carrier for targeted platelet delivery and long circulation of rHV_(2).
作者
赵阳光
任佩佩
杨壮壮
张士忠
皇甫涵祯
杨万成
王小宁
ZHAO Yangguang;REN Peipei;YANG Zhuangzhuang;ZHANG Shizhong;HUANGFU Zhenhan;YANG Wancheng;WANG Xiaoning(Pharmaceutical Institute,Xi'an Medical University,Shaanxi Xi'an 710021,China)
出处
《广州化工》
CAS
2024年第20期36-39,共4页
GuangZhou Chemical Industry
基金
2022陕西省大学生创新创业训练项目(S202211840077)
2021陕西省大学生创新创业训练项目(S202111840068)
西安医学院2022年科研能力提升计划项目(2022NLTS060)
2023陕西省教育厅青年创新团队项目(23JP156)。
