Citation: Zhao Shengnan, Li Jinhua, Wang Fazhan, Yu Ting, Zhou Yang, He Lili, Zhang Yi, Yang Jian. Semi-elastic core-shell nanoparticles enhanced the oral bioavailability of peptide drugs[J]. Chinese Chemical Letters, ;2020, 31(5): 1147-1152. doi: 10.1016/j.cclet.2019.07.009 shu

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

Zhao Shengnan ^a,c,1 ,
Li Jinhua ^a,b,1 ,
Wang Fazhan ^a,b,1 ,
Yu Ting ^a,b ,
Zhou Yang ^a ,
He Lili ^c,*, ,
Zhang Yi ^b,*, ,
Yang Jian ^a,*,

a.
School of Applied Chemistry and Biological Technology, Shenzhen Polytechnic, Shenzhen 518055, China
b.
Department of Pancreatic Surgery, West China Hospital, Sichuan University, Chengdu 610041, China
c.
College of Pharmacy, Southwest Minzu University, Chengdu 610041, China

Received Date: 17 April 2019
Revised Date: 6 June 2019
Accepted Date: 3 July 2019
Available Online: 3 July 2019

Figures(4)

The rigidity of nanoparticles was newly reported to influence their oral delivery. Semi-elastic nanoparticles can enhance the penetration in mucus and uptake by epithelial cells. However, it is still challenging and unclear that the semi-elastic core-shell nanoparticles can enhance the oral bioavailability of peptide drugs. This 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 drug. The antihypertensive peptide Val-Leu-Pro-Val-Pro (VP5) loaded LNPs (VP5-LNPs) were prepared by a modified thin-film ultrasonic dispersion method. Uptake experiment was performed in Caco-2 and HT-29 cells and monitored by high content screening (HCS) and flow cytometric (FCM). Pharmacokinetics of VP5-LNPs was carried out in Sprague-Dawley (SD) rats and analyzed by DAS 2.0. The 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 structure. VP5-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 oral bioavailability. The 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.
- Semi-elastic nanoparticles,
- Oral bioavailability,
- Lipid nanoparticles,
- Antihypertensive peptide,
- Pharmacokinetics
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沈阳化工大学材料科学与工程学院沈阳 110142