Development of Dextran-Coated Magnetic Nanoparticles Loaded with Protocatechuic Acid for Vascular Inflammation Therapy

Vascular inflammation plays a crucial role in the progression of various pathologies, including atherosclerosis (AS), and thus it has become an attractive therapeutic target. The protocatechuic acid (PCA), one of the main metabolites of complex polyphenols, is endowed with anti-inflammatory activity...

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Main Authors: Maria Anghelache, Mihaela Turtoi, Anca Roxana Petrovici, Adrian Fifere, Mariana Pinteala, Manuela Calin
Format: Article
Language:English
Published: MDPI AG 2021-09-01
Series:Pharmaceutics
Subjects:
Online Access:https://www.mdpi.com/1999-4923/13/9/1414
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author Maria Anghelache
Mihaela Turtoi
Anca Roxana Petrovici
Adrian Fifere
Mariana Pinteala
Manuela Calin
author_facet Maria Anghelache
Mihaela Turtoi
Anca Roxana Petrovici
Adrian Fifere
Mariana Pinteala
Manuela Calin
author_sort Maria Anghelache
collection DOAJ
description Vascular inflammation plays a crucial role in the progression of various pathologies, including atherosclerosis (AS), and thus it has become an attractive therapeutic target. The protocatechuic acid (PCA), one of the main metabolites of complex polyphenols, is endowed with anti-inflammatory activity, but its formulation into nanocarriers may increase its bioavailability. In this study, we developed and characterized dextran shell‒iron oxide core nanoparticles loaded with PCA (MNP-Dex/PCA) and assessed their cytotoxicity and anti-inflammatory potential on cells acting as key players in the onset and progression of AS, namely, endothelial cells (EC) and monocytes/macrophages. The results showed that MNP-Dex/PCA exert an anti-inflammatory activity at non-cytotoxic and therapeutically relevant concentrations of PCA (350 μM) as supported by the reduced levels of inflammatory molecules such as MCP-1, IL-1β, TNF-α, IL-6, and CCR2 in activated EC and M1-type macrophages and functional monocyte adhesion assay. The anti-inflammatory effect of MNP-Dex/PCA was associated with the reduction in the levels of ERK1/2 and p38-α mitogen-activated protein kinases (MAPKs) and NF-kB transcription factor. Our data support the further development of dextran shell-magnetic core nanoparticles as theranostic nanoparticles for guidance, imaging, and therapy of vascular inflammation using PCA or other anti-inflammatory compounds.
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spelling doaj.art-1e46063cce3f4fa3a8e2cbb7856dfe262023-11-22T14:47:21ZengMDPI AGPharmaceutics1999-49232021-09-01139141410.3390/pharmaceutics13091414Development of Dextran-Coated Magnetic Nanoparticles Loaded with Protocatechuic Acid for Vascular Inflammation TherapyMaria Anghelache0Mihaela Turtoi1Anca Roxana Petrovici2Adrian Fifere3Mariana Pinteala4Manuela Calin5“Medical and Pharmaceutical Bionanotechnologies” Laboratory, Institute of Cellular Biology and Pathology “Nicolae Simionescu” of the Romanian Academy, B.P. Hasdeu 8, 050568 Bucharest, Romania“Medical and Pharmaceutical Bionanotechnologies” Laboratory, Institute of Cellular Biology and Pathology “Nicolae Simionescu” of the Romanian Academy, B.P. Hasdeu 8, 050568 Bucharest, Romania“Centre of Advanced Research in Bionanoconjugates and Biopolymers” Department, “Petru Poni” Institute of Macromolecular Chemistry, 41A Grigore Ghica-Voda Alley, 700487 Iasi, Romania“Centre of Advanced Research in Bionanoconjugates and Biopolymers” Department, “Petru Poni” Institute of Macromolecular Chemistry, 41A Grigore Ghica-Voda Alley, 700487 Iasi, Romania“Centre of Advanced Research in Bionanoconjugates and Biopolymers” Department, “Petru Poni” Institute of Macromolecular Chemistry, 41A Grigore Ghica-Voda Alley, 700487 Iasi, Romania“Medical and Pharmaceutical Bionanotechnologies” Laboratory, Institute of Cellular Biology and Pathology “Nicolae Simionescu” of the Romanian Academy, B.P. Hasdeu 8, 050568 Bucharest, RomaniaVascular inflammation plays a crucial role in the progression of various pathologies, including atherosclerosis (AS), and thus it has become an attractive therapeutic target. The protocatechuic acid (PCA), one of the main metabolites of complex polyphenols, is endowed with anti-inflammatory activity, but its formulation into nanocarriers may increase its bioavailability. In this study, we developed and characterized dextran shell‒iron oxide core nanoparticles loaded with PCA (MNP-Dex/PCA) and assessed their cytotoxicity and anti-inflammatory potential on cells acting as key players in the onset and progression of AS, namely, endothelial cells (EC) and monocytes/macrophages. The results showed that MNP-Dex/PCA exert an anti-inflammatory activity at non-cytotoxic and therapeutically relevant concentrations of PCA (350 μM) as supported by the reduced levels of inflammatory molecules such as MCP-1, IL-1β, TNF-α, IL-6, and CCR2 in activated EC and M1-type macrophages and functional monocyte adhesion assay. The anti-inflammatory effect of MNP-Dex/PCA was associated with the reduction in the levels of ERK1/2 and p38-α mitogen-activated protein kinases (MAPKs) and NF-kB transcription factor. Our data support the further development of dextran shell-magnetic core nanoparticles as theranostic nanoparticles for guidance, imaging, and therapy of vascular inflammation using PCA or other anti-inflammatory compounds.https://www.mdpi.com/1999-4923/13/9/1414magnetic nanoparticlesdextranprotocatechuic acidanti-inflammatory activityendothelial cellsmacrophages
spellingShingle Maria Anghelache
Mihaela Turtoi
Anca Roxana Petrovici
Adrian Fifere
Mariana Pinteala
Manuela Calin
Development of Dextran-Coated Magnetic Nanoparticles Loaded with Protocatechuic Acid for Vascular Inflammation Therapy
Pharmaceutics
magnetic nanoparticles
dextran
protocatechuic acid
anti-inflammatory activity
endothelial cells
macrophages
title Development of Dextran-Coated Magnetic Nanoparticles Loaded with Protocatechuic Acid for Vascular Inflammation Therapy
title_full Development of Dextran-Coated Magnetic Nanoparticles Loaded with Protocatechuic Acid for Vascular Inflammation Therapy
title_fullStr Development of Dextran-Coated Magnetic Nanoparticles Loaded with Protocatechuic Acid for Vascular Inflammation Therapy
title_full_unstemmed Development of Dextran-Coated Magnetic Nanoparticles Loaded with Protocatechuic Acid for Vascular Inflammation Therapy
title_short Development of Dextran-Coated Magnetic Nanoparticles Loaded with Protocatechuic Acid for Vascular Inflammation Therapy
title_sort development of dextran coated magnetic nanoparticles loaded with protocatechuic acid for vascular inflammation therapy
topic magnetic nanoparticles
dextran
protocatechuic acid
anti-inflammatory activity
endothelial cells
macrophages
url https://www.mdpi.com/1999-4923/13/9/1414
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