Synthesis and characterization of peptide conjugated human serum albumin nanoparticles for targeted cardiac uptake and drug delivery.

Congestive heart failure, a prominent cardiovascular disease results primarily from myocardial infarction or ischemia. Milrinone (MRN), a widely used clinical drug for heart failure, improves myocardial contractility and cardiac function through its inotropic and vasodilatory effects. However, lacki...

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Autores principales: Nikita Lomis, Susan Westfall, Dominique Shum-Tim, Satya Prakash
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Publicado: Public Library of Science (PLoS) 2021
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Acceso en línea:https://doaj.org/article/f53209f561d9469298410cd38fc20f70
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spelling oai:doaj.org-article:f53209f561d9469298410cd38fc20f702021-12-02T20:13:59ZSynthesis and characterization of peptide conjugated human serum albumin nanoparticles for targeted cardiac uptake and drug delivery.1932-620310.1371/journal.pone.0254305https://doaj.org/article/f53209f561d9469298410cd38fc20f702021-01-01T00:00:00Zhttps://doi.org/10.1371/journal.pone.0254305https://doaj.org/toc/1932-6203Congestive heart failure, a prominent cardiovascular disease results primarily from myocardial infarction or ischemia. Milrinone (MRN), a widely used clinical drug for heart failure, improves myocardial contractility and cardiac function through its inotropic and vasodilatory effects. However, lacking target specificity, it exhibits low bioavailability and lower body retention time. Therefore, in this study, angiotensin II (AT1) peptide conjugated human serum albumin nanoparticles (AT1-HSA-MRN-NPs) have been synthesized for targeted delivery of MRN to the myocardium, overexpressing AT1 receptors under heart failure. The NPs were surface functionalized through a covalent conjugation reaction between HSA and AT1. Nanoparticle size was 215.2±4.7 nm and zeta potential -28.8±2.7 mV and cumulative release of MRN was ~72% over 24 hrs. The intracellular uptake of nanoparticles and cell viability was studied in H9c2 cells treated with AT1-MRN-HSA-NPs vs the control non-targeted drug, MRN Lactate under normal, hypoxic and hypertrophic conditions. The uptake of AT1-HSA-MRN-NPs in H9c2 cells was significantly higher as compared to non-targeted nanoparticles, and the viability of H9c2 cells treated with AT1-MRN-HSA-NPs vs MRN Lactate was 73.4±1.4% vs 44.9±1.4%, respectively. Therefore, AT1-HSA-MRN-NPs are safe for in vivo use and exhibit superior targeting and drug delivery characteristics for treatment of heart failure.Nikita LomisSusan WestfallDominique Shum-TimSatya PrakashPublic Library of Science (PLoS)articleMedicineRScienceQENPLoS ONE, Vol 16, Iss 9, p e0254305 (2021)
institution DOAJ
collection DOAJ
language EN
topic Medicine
R
Science
Q
spellingShingle Medicine
R
Science
Q
Nikita Lomis
Susan Westfall
Dominique Shum-Tim
Satya Prakash
Synthesis and characterization of peptide conjugated human serum albumin nanoparticles for targeted cardiac uptake and drug delivery.
description Congestive heart failure, a prominent cardiovascular disease results primarily from myocardial infarction or ischemia. Milrinone (MRN), a widely used clinical drug for heart failure, improves myocardial contractility and cardiac function through its inotropic and vasodilatory effects. However, lacking target specificity, it exhibits low bioavailability and lower body retention time. Therefore, in this study, angiotensin II (AT1) peptide conjugated human serum albumin nanoparticles (AT1-HSA-MRN-NPs) have been synthesized for targeted delivery of MRN to the myocardium, overexpressing AT1 receptors under heart failure. The NPs were surface functionalized through a covalent conjugation reaction between HSA and AT1. Nanoparticle size was 215.2±4.7 nm and zeta potential -28.8±2.7 mV and cumulative release of MRN was ~72% over 24 hrs. The intracellular uptake of nanoparticles and cell viability was studied in H9c2 cells treated with AT1-MRN-HSA-NPs vs the control non-targeted drug, MRN Lactate under normal, hypoxic and hypertrophic conditions. The uptake of AT1-HSA-MRN-NPs in H9c2 cells was significantly higher as compared to non-targeted nanoparticles, and the viability of H9c2 cells treated with AT1-MRN-HSA-NPs vs MRN Lactate was 73.4±1.4% vs 44.9±1.4%, respectively. Therefore, AT1-HSA-MRN-NPs are safe for in vivo use and exhibit superior targeting and drug delivery characteristics for treatment of heart failure.
format article
author Nikita Lomis
Susan Westfall
Dominique Shum-Tim
Satya Prakash
author_facet Nikita Lomis
Susan Westfall
Dominique Shum-Tim
Satya Prakash
author_sort Nikita Lomis
title Synthesis and characterization of peptide conjugated human serum albumin nanoparticles for targeted cardiac uptake and drug delivery.
title_short Synthesis and characterization of peptide conjugated human serum albumin nanoparticles for targeted cardiac uptake and drug delivery.
title_full Synthesis and characterization of peptide conjugated human serum albumin nanoparticles for targeted cardiac uptake and drug delivery.
title_fullStr Synthesis and characterization of peptide conjugated human serum albumin nanoparticles for targeted cardiac uptake and drug delivery.
title_full_unstemmed Synthesis and characterization of peptide conjugated human serum albumin nanoparticles for targeted cardiac uptake and drug delivery.
title_sort synthesis and characterization of peptide conjugated human serum albumin nanoparticles for targeted cardiac uptake and drug delivery.
publisher Public Library of Science (PLoS)
publishDate 2021
url https://doaj.org/article/f53209f561d9469298410cd38fc20f70
work_keys_str_mv AT nikitalomis synthesisandcharacterizationofpeptideconjugatedhumanserumalbuminnanoparticlesfortargetedcardiacuptakeanddrugdelivery
AT susanwestfall synthesisandcharacterizationofpeptideconjugatedhumanserumalbuminnanoparticlesfortargetedcardiacuptakeanddrugdelivery
AT dominiqueshumtim synthesisandcharacterizationofpeptideconjugatedhumanserumalbuminnanoparticlesfortargetedcardiacuptakeanddrugdelivery
AT satyaprakash synthesisandcharacterizationofpeptideconjugatedhumanserumalbuminnanoparticlesfortargetedcardiacuptakeanddrugdelivery
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