Oral nanoparticles containing naringenin suppress atherosclerotic progression by targeting delivery to plaque macrophages  

作　　者：Mengran Guo Zhongshan He Zhaohui Jin Lingjing Huang Jingmei Yuan Shugang Qin Xinchun Wang Lili Cao Xiangrong Song 

机构地区：[1]Department of Critical Care Medicine,Department of Anesthesiology and Translational Neuroscience Center,Department of Clinical Pharmacy,Frontiers Science Center for Disease-related Molecular Network,State Key Laboratory of Biotherapy and Cancer Center,West China Hospital,Sichuan University,Chengdu 610000,China [2]First Affiliated Hospital of the Medical College,Shihezi University,Shihezi 832008,China [3]College of Medicine,Chengdu University,Chengdu 610000,China

出　　处：《Nano Research》2023年第1期925-937,共13页纳米研究（英文版）

基　　金：This study was supported by the Youth Fund of National Natural Science Foundation of China(No.82104081);Sichuan Province Science and Technology Support Program(No.2020JDRC0052);the 1.3.5 Project for Disciplines of excellence,West China Hospital,Sichuan University(No.ZYGD18020/ZYJC18006);Science and Technology Project of Xinjiang Production and Construction Corps(No.2022AB020).

摘　　要：Atherosclerosis is the main cause of ischemic stroke and myocardial infarction diseases.Nanoparticles have shown unique benefits for atherosclerosis treatment by targeting the lesional macrophages of plaques.However,most of the nanocarriers are administered intravenously,which is inconvenient and may cause complications.Herein,we developed an oral lipid-polymer based nanoparticles(FA-LNPs)decorated with folic acid,which can not only effectively overcome intestinal mucosal-epithelial barrier by increasing the transmembrane transport through intestinal epithelial and the accumulation in Peyer’s patches but also actively target to the aortic plaque sites and accumulate in lesional macrophages.Subsequently,naringenin(Nrg),one of the antiinflammation drugs,was designed to be the oral nanomedicine(FA-LNPs/Nrg)for the first time via the encapsulation of FALNPs.FA-LNPs/Nrg presented highly anti-atherosclerotic efficacy.After the atherosclerotic ApoE−/−mice were treated by FALNPs/Nrg via oral administration for three months,the aortic lesion area,plaque area,and necrotic core area of the aortic root were significantly decreased.Meanwhile,the lipid-related blood parameters recovered to normal levels.Our study provides a promising approach to atherosclerosis treatment based on the novel oral targeting delivery system.

关 键 词：ATHEROSCLEROSIS MACROPHAGES Peyer’s patches oral delivery folic acid NARINGENIN 

分 类 号：R541.4[医药卫生—心血管疾病]