Core-shell lipid-polymeric nanoparticles for enhanced oral bioavailability and antihypertensive efficacy of KY5 peptide

作     者：Jingmei Yuan Mengran Guo Shengnan Zhao Jinhua Li Xinchun Wang Jian Yang Zhaohui Jin Xiangrong Song Jingmei Yuan;Mengran Guo;Shengnan Zhao;Jinhua Li;Xinchun Wang;Jian Yang;Zhaohui Jin;Xiangrong Song

作者机构：Department of Critical Care MedicineDepartment of Clinical PharmacyFrontiers Science Center for Disease-related Molecular NetworkState Key Laboratory of Biotherapy and Cancer CenterWest China HospitalSichuan UniversityChengdu 610041China School of Applied Chemistry and Biological TechnologyShenzhen PolytechnicShenzhen 518055China First Affiliated Hospital of the Medical CollegeShihezi UniversityShihezi 832008China 

出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)

年 卷 期：2023年第34卷第4期

页      面：158-163页

核心收录：

学科分类：07[理学] 08[工学] 070205[理学-凝聚态物理] 100702[医学-药剂学] 1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 080501[工学-材料物理与化学] 0805[工学-材料科学与工程（可授工学、理学学位）] 080502[工学-材料学] 0703[理学-化学] 0702[理学-物理学] 100602[医学-中西医结合临床] 10[医学] 

基　　金：supported by the Youth Fund of National Natural Science Foundation of China (No. 82104081) the Science and Technology Project of Shenzhen (No. JCYJ20170413155047512) the 1.3.5 project for disciplines of excellence,West China Hospital,Sichuan University (No. ZYGD18020/ZYJC18006) the Sichuan Province Science and Technology Support Program (No. 2020JDRC0052) the Science and Technology Project of Xinjiang Production and Construction Corps (No. 2022AB020) 

主　　题：Hypertension Core-shell lipid-polymeric nanoparticles KY5 Antihypertensive peptides Oral delivery 

摘      要：Hypertension is the leading risk factor for death and disability, and hypertensive patients always need long-term oral antihypertensive drugs. Some bioactive peptides that extracted from animals or plants have shown excellent advantages on antihypertension. However, the oral delivery of these peptides is always failure on account of instability and poor absorption in the gastrointestinal tract. Herein, we developed a core-shell lipid-polymeric nanoparticle for oral delivery of a highly efficient antihypertensive peptide KY5(KY5-CSs). KY5-CSs had a particle size of 216.7 ± 2.5 nm, with a narrow PDI of 0.07 ± *** zeta potential was-4.1 ± 0.1 m V. It exhibited good stability in 4 ℃ and possessed a controlled release behavior in gastrointestinal tract. The cellular uptake study proved that the lipid shell imparted unique capability of permeation across the mucus layer and internalization by Caco-2/HT-29 cells. In addition, KY5-CSs enhanced in situ intestinal absorption in SD rats. The pharmacokinetic studies and antihypertensive efficacy showed a superior oral absorption and antihypertensive effect of KY5-CSs than KY5-NPs. In conclusion, the core-shell lipid-polymeric nanoparticles will provide attractive potential for oral delivery of antihypertensive peptides.