Semi-elastic core-shell nanoparticles enhanced the oral bioavailability of peptide drugs

作     者：Shengnan Zhao Jinhua Li Fazhan Wang Ting Yu Yang Zhou Lili He Yi Zhang jian Yang Shengnan Zhao;Jinhua Li;Fazhan Wang;Ting Yu;Yang Zhou;Lili He;Yi Zhang;Jian Yang

作者机构：School of Applied Chemistry and Biological TechnologyShenzhen PolytechnicShenzhen 518055China Department of Pancreatic SurgeryWest China HospitalSichuan University.Chengdu 610041China College of PharmacySouthwest Minzu UniversityChengdu 610041China 

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

年 卷 期：2020年第31卷第5期

页      面：1147-1152页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 10[医学] 

基　　金：financially supported by the Science and Technology Project of Shenzhen(No.JCYJ20170413155047512) Scientific Research Foundation of the Science and Technology Department of Sichuan Province,China(No.2018JY0143) 

主　　题：Semi-elastic nanoparticles Oral bioavailability Lipid nanoparticles Antihypertensive peptide Pharmacokinetics 

摘      要：The rigidity of nanoparticles was newly reported to influence their oral ***-elastic nanoparticles can enhance the penetration in mucus and uptake by epithelial ***,it is still challenging and unclear that the semi-elastic core-shell nanoparticles can enhance the oral bioavailability of peptide *** study was for the first time to validate the semi-elastic coreshell poly(lactic-co-glycolic acid)(PLGA)-lipid nanoparticles(LNPs)as the carrier of the oral peptide *** antihypertensive peptide Val-Leu-Pro-Val-Pro(VP5)loaded LNPs(VP5-LNPs)were prepared by a modified thin-film ultrasonic dispersion *** experiment was performed in Caco-2 and HT-29 cells and monito red by high content screening(HCS)and flow cyto metric(FCM).Pharmacokinetics of VP5-LNPs was carried out in Sprague-Dawley(SD)rats and analyzed by DAS *** optimal VP5-LNPs had an average particle size of 247.3±3.8 nm,zeta potential of-6.57±0.45 mV and excellent entrapment efficiency(EE)of 89.88%±1.23%.Transmission electron microscope(TEM)and Differential scanning calorimeter(DSC)further confirmed the core-shell ***5-LNPs could increase the cellular uptake in vitro and have a 2.55-fold increase in AUC0-72 h,indicating a great promotion of the o ral *** semi-elastic LNPs remarkably improved the oral availability of peptide and could be a promising oral peptide delivery system for peptide drugs in the future.