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Int. J. Mol. Sci. 2016, 17(12), 1977; doi:10.3390/ijms17121977

Enhanced and Extended Anti-Hypertensive Effect of VP5 Nanoparticles

1
School of Applied Chemistry and Biological Technology, Shenzhen Polytechnic, Shenzhen 518055, China
2
College of Pharmacy, Southwest University for Nationalities, Chengdu 610041, China
3
State Key Laboratory of Biotherapy and Cancer Center, West China Hospital, and Collaborative Innovation Center for Biotherapy, Sichuan University, Chengdu 610041, China
4
Department of Medical Oncology, Dana-Farber Cancer Institute and Harvard Medical School, Boston, MA 02115, USA
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Qinghua Qin
Received: 29 September 2016 / Revised: 11 November 2016 / Accepted: 18 November 2016 / Published: 25 November 2016
(This article belongs to the Section Biomaterial Sciences)
View Full-Text   |   Download PDF [2284 KB, uploaded 25 November 2016]   |  

Abstract

Hypertension has become a significant global public health concern and is also one of the most common risk factors of cardiovascular disease. Recent studies have shown the promising result of peptides inhibiting angiotensin converting enzyme (ACE) in lowering the blood pressure in both animal models and humans. However, the oral bioavailability and continuous antihypertensive effectiveness require further optimization. Novel nanoparticle-based drug delivery systems are helpful to overcome these barriers. Therefore, a poly-(lactic-co-glycolic) acid nanoparticle (PLGANPs) oral delivery system, of the antihypertensive small peptides Val-Leu-Pro-Val-Pro (VLPVP, VP5) model, was developed in this study and its antihypertensive effect was investigated in spontaneously hypertensive rats (SHRs) for the first time. The obtained VP5 nanoparticles (VP5-NPs) showed a small particle size of 223.7 ± 2.3 nm and high entrapment efficiency (EE%) of 87.37% ± 0.92%. Transmission electronic microscopy (TEM) analysis showed that the nanoparticles were spherical and homogeneous. The optimal preparation of VP5-NPs exhibited sustained release of VP5 in vitro and a 96 h long-term antihypertensive effect with enhanced efficacy in vivo. This study illustrated that PLGANPs might be an optimal formulation for oral delivery of antihypertensive small peptides and VP5-NPs might be worthy of further development and use as a potential therapeutic strategy for hypertension in the future. View Full-Text
Keywords: PLGA nanoparticles; antihypertensive peptide; oral administration; sustained release; continuously antihypertensive effect PLGA nanoparticles; antihypertensive peptide; oral administration; sustained release; continuously antihypertensive effect
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Yu, T.; Zhao, S.; Li, Z.; Wang, Y.; Xu, B.; Fang, D.; Wang, F.; Zhang, Z.; He, L.; Song, X.; Yang, J. Enhanced and Extended Anti-Hypertensive Effect of VP5 Nanoparticles. Int. J. Mol. Sci. 2016, 17, 1977.

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