Targeted nanocarriers for mitogen-activated protein kinase inhibitor delivery to treat coronary artery spasm

Micro & nano letters

article

Ke Li¹  Lin Wang³  Cangbao Xu¹  Yaping Zhang¹  Fan Cheng⁴  Lingqiao Shao⁴  Min Jia¹  Xueping Li²  Wenhua Zhan⁵ 

[1] Shaanxi Key Laboratory of Ischemic Cardiovascular Disease, Shaanxi Key Laboratory of Brain Disorders, Institute of Basic and Translational Medicine, Xi'an Medical University;Shaanxi Provincial Research Center for the Project of Prevention and Treatment of Respiratory Diseases, College of Clinical Medicine, Xi'an Medical University;Prenatal Diagnosis Center, Northwest Women and Childrens Hospital;Department of Basic Medical Science, Xi'an Medical University;Department of Radiotherapy, General Hospital of Ningxia Medical University;Key Laboratory of Biomedical Information Engineering of Education Ministry, School of Life Science and Technology, Xi'an Jiaotong University

关键词: drugs;    molecular biophysics;    cellular biophysics;    nanoparticles;    enzymes;    biomedical materials;    nanomedicine;    diseases;    drug delivery systems;    blood vessels;    electrokinetic effects;    effective targeted delivery;    arterial tissue culture model;    endothelin type B receptor;    CAS;    targeted nanocarriers;    mitogen-activated protein kinase inhibitor delivery;    coronary artery spasm;    serious ischaemic cardiac disease;    vascular smooth muscle cells;    endothelin receptor B type;    U0126 nanoparticles;    drug loading;   

DOI  :  10.1049/mnl.2019.0495

学科分类：计算机科学（综合）

来源: Wiley

【 摘 要 】

Coronary artery spasm (CAS) causes serious ischaemic cardiac disease. The hyper-reactivity of vascular smooth muscle cells, which ascribe the up-regulation of endothelin receptor B type, is a key abnormality responsible for the pathological constriction of arteries in CAS. In this study, the nanocarriers were prepared and optimised for the delivery of U0126, which is an inhibitor of the mitogen-activated protein kinase, to treat pathological constriction of arteries. First, cationic amphipathic starch and hyaluronic acid were used in the encapsulation of U0126 to form U0126 nanoparticles (NPs). The shape of the U0126 NPs was spherical with a typical core–shell structure. The size was 94.1 ± 10.2 nm and the zeta potential was −20.3 ± 5.1 mV. Maximal encapsulation efficiencies and drug loading of U0126 in the NPs were 96.2 ± 3.1 and 8.2 ± 2.5%, respectively. U0126 NPs showed very great stability and could perform an effective targeted delivery. An arterial tissue culture model was used in the investigation of anti-constriction. In comparison with treatment with the free drug, the U0126 NPs significantly decreased the effective dosage, enhanced the effect of anti-constriction, and down-regulated the endothelin type B receptor in the culture model. These results suggest that U0126 NPs have a significant potential for the treatment of CAS.

【 授权许可】

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