Preparation and in vitro/in vivo characterization of enteric-coated nanoparticles loaded with the antihypertensive peptide VLPVPR

Haiyan Sun, Dong Liu, Yan Li, Xuwei Tang, Yanli Cong Shenzhen Key Laboratory of Fermentation, Purification and Analysis, Shenzhen Polytechnic, Guangdong, People's Republic of China Abstract: Our previous study revealed that the peptide Val-Leu-Pro-Val-Pro-Arg (VLPVPR), which was prepared u...

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Autores principales: Sun HY, Liu D, Li Y, Tang XW, Cong YL
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Publicado: Dove Medical Press 2014
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spelling oai:doaj.org-article:84ae992a7a684d72a8692f31e4c9965e2021-12-02T05:08:58ZPreparation and in vitro/in vivo characterization of enteric-coated nanoparticles loaded with the antihypertensive peptide VLPVPR1178-2013https://doaj.org/article/84ae992a7a684d72a8692f31e4c9965e2014-04-01T00:00:00Zhttp://www.dovepress.com/preparation-and-in-vitroin-vivo-characterization-of-enteric-coated-nan-a16332https://doaj.org/toc/1178-2013 Haiyan Sun, Dong Liu, Yan Li, Xuwei Tang, Yanli Cong Shenzhen Key Laboratory of Fermentation, Purification and Analysis, Shenzhen Polytechnic, Guangdong, People's Republic of China Abstract: Our previous study revealed that the peptide Val-Leu-Pro-Val-Pro-Arg (VLPVPR), which was prepared using deoxyribonucleic acid recombinant technology, effectively decreased the blood pressure of spontaneous hypertensive rats; however, the effect only lasts 6 hours, likely due to its low absorption in the gastrointestinal tract. To overcome this problem, the purpose of this study was to characterize (methoxy-polyethylene glycol)-b-poly(D,L-lactide-co-glycolide)-b-poly(L-lysine) nanoparticles as in vitro and in vivo carriers for the effective delivery of VLPVPR. In our study, the VLPVPR nanoparticles were prepared using a double emulsion method, coated with Eudragit S100, and freeze-dried to produce enteric-coated nanoparticles. The optimized parameters from the double emulsion method was obtained from orthogonal experiments, including drug loading (DL) and encapsulated ratio (ER) at 6.12% and 86.94%, respectively, and the average particle size was below 100 nm. The release experiment demonstrated that the nanoparticles were sensitive to pH: almost completely released at pH 7.4 after 8 hours, but demonstrated much less release at pH 4.5 or pH 1.0 in the same amount of time. Therefore, the nanoparticles are suitable for enteric release. In vivo compared with the untreated group, the medium and high doses of orally administered VLPVPR nanoparticles reduced blood pressure for more than 30 hours, demonstrating that these nanoparticles have long-lasting and significant antihypertensive effects in spontaneously hypertensive rats. Keywords: mPEG-PLGA-PLL, in vivo studies, Val-Leu-Pro-Val-Pro-Arg peptide, enteric-coated, nanoparticle, antihypertensive peptideSun HYLiu DLi YTang XWCong YLDove Medical PressarticleMedicine (General)R5-920ENInternational Journal of Nanomedicine, Vol 2014, Iss Issue 1, Pp 1709-1716 (2014)
institution DOAJ
collection DOAJ
language EN
topic Medicine (General)
R5-920
spellingShingle Medicine (General)
R5-920
Sun HY
Liu D
Li Y
Tang XW
Cong YL
Preparation and in vitro/in vivo characterization of enteric-coated nanoparticles loaded with the antihypertensive peptide VLPVPR
description Haiyan Sun, Dong Liu, Yan Li, Xuwei Tang, Yanli Cong Shenzhen Key Laboratory of Fermentation, Purification and Analysis, Shenzhen Polytechnic, Guangdong, People's Republic of China Abstract: Our previous study revealed that the peptide Val-Leu-Pro-Val-Pro-Arg (VLPVPR), which was prepared using deoxyribonucleic acid recombinant technology, effectively decreased the blood pressure of spontaneous hypertensive rats; however, the effect only lasts 6 hours, likely due to its low absorption in the gastrointestinal tract. To overcome this problem, the purpose of this study was to characterize (methoxy-polyethylene glycol)-b-poly(D,L-lactide-co-glycolide)-b-poly(L-lysine) nanoparticles as in vitro and in vivo carriers for the effective delivery of VLPVPR. In our study, the VLPVPR nanoparticles were prepared using a double emulsion method, coated with Eudragit S100, and freeze-dried to produce enteric-coated nanoparticles. The optimized parameters from the double emulsion method was obtained from orthogonal experiments, including drug loading (DL) and encapsulated ratio (ER) at 6.12% and 86.94%, respectively, and the average particle size was below 100 nm. The release experiment demonstrated that the nanoparticles were sensitive to pH: almost completely released at pH 7.4 after 8 hours, but demonstrated much less release at pH 4.5 or pH 1.0 in the same amount of time. Therefore, the nanoparticles are suitable for enteric release. In vivo compared with the untreated group, the medium and high doses of orally administered VLPVPR nanoparticles reduced blood pressure for more than 30 hours, demonstrating that these nanoparticles have long-lasting and significant antihypertensive effects in spontaneously hypertensive rats. Keywords: mPEG-PLGA-PLL, in vivo studies, Val-Leu-Pro-Val-Pro-Arg peptide, enteric-coated, nanoparticle, antihypertensive peptide
format article
author Sun HY
Liu D
Li Y
Tang XW
Cong YL
author_facet Sun HY
Liu D
Li Y
Tang XW
Cong YL
author_sort Sun HY
title Preparation and in vitro/in vivo characterization of enteric-coated nanoparticles loaded with the antihypertensive peptide VLPVPR
title_short Preparation and in vitro/in vivo characterization of enteric-coated nanoparticles loaded with the antihypertensive peptide VLPVPR
title_full Preparation and in vitro/in vivo characterization of enteric-coated nanoparticles loaded with the antihypertensive peptide VLPVPR
title_fullStr Preparation and in vitro/in vivo characterization of enteric-coated nanoparticles loaded with the antihypertensive peptide VLPVPR
title_full_unstemmed Preparation and in vitro/in vivo characterization of enteric-coated nanoparticles loaded with the antihypertensive peptide VLPVPR
title_sort preparation and in vitro/in vivo characterization of enteric-coated nanoparticles loaded with the antihypertensive peptide vlpvpr
publisher Dove Medical Press
publishDate 2014
url https://doaj.org/article/84ae992a7a684d72a8692f31e4c9965e
work_keys_str_mv AT sunhy preparationandinvitroinvivocharacterizationofentericcoatednanoparticlesloadedwiththeantihypertensivepeptidevlpvpr
AT liud preparationandinvitroinvivocharacterizationofentericcoatednanoparticlesloadedwiththeantihypertensivepeptidevlpvpr
AT liy preparationandinvitroinvivocharacterizationofentericcoatednanoparticlesloadedwiththeantihypertensivepeptidevlpvpr
AT tangxw preparationandinvitroinvivocharacterizationofentericcoatednanoparticlesloadedwiththeantihypertensivepeptidevlpvpr
AT congyl preparationandinvitroinvivocharacterizationofentericcoatednanoparticlesloadedwiththeantihypertensivepeptidevlpvpr
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