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Controlled Release of 18-β-Glycyrrhetinic Acid from Core-Shell Nanoparticles: Effects on Cytotoxicity and Intracellular Concentration in HepG2 Cell Line

18β-glycyrrhetinic acid (GA) is a pentacyclic triterpene with promising hepatoprotective and anti-Hepatocellular carcinoma effects. GA low water solubility however reduces its biodistribution and bioavailability, limiting its applications in biomedicine. In this work we used core-shell NPs made of P...

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Autores principales: Nocca, Giuseppina, D’Avenio, Giuseppe, Amalfitano, Adriana, Chronopoulou, Laura, Mordente, Alvaro, Palocci, Cleofe, Grigioni, Mauro
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8303372/
https://www.ncbi.nlm.nih.gov/pubmed/34300811
http://dx.doi.org/10.3390/ma14143893
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author Nocca, Giuseppina
D’Avenio, Giuseppe
Amalfitano, Adriana
Chronopoulou, Laura
Mordente, Alvaro
Palocci, Cleofe
Grigioni, Mauro
author_facet Nocca, Giuseppina
D’Avenio, Giuseppe
Amalfitano, Adriana
Chronopoulou, Laura
Mordente, Alvaro
Palocci, Cleofe
Grigioni, Mauro
author_sort Nocca, Giuseppina
collection PubMed
description 18β-glycyrrhetinic acid (GA) is a pentacyclic triterpene with promising hepatoprotective and anti-Hepatocellular carcinoma effects. GA low water solubility however reduces its biodistribution and bioavailability, limiting its applications in biomedicine. In this work we used core-shell NPs made of PolyD-L-lactide-co-glycolide (PLGA) coated with chitosan (CS), prepared through an osmosis-based methodology, to efficiently entrap GA. NPs morphology was investigated with SEM and TEM and their GA payload was evaluated with a spectrophotometric method. GA-loaded NPs were administered to HepG2 cells and their efficiency in reducing cell viability was compared with that induced by the free drug in in vitro tests. Cell viability was evaluated by the MTT assay, as well as with Electric Cells-Substrate Impedance Sensing (ECIS), that provided a real-time continuous monitoring. It was possible to correlate the toxic effect of the different forms of GA with the bioavailability of the drug, evidencing the importance of real-time tests for studying the effects of bioactive substances on cell cultures.
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spelling pubmed-83033722021-07-25 Controlled Release of 18-β-Glycyrrhetinic Acid from Core-Shell Nanoparticles: Effects on Cytotoxicity and Intracellular Concentration in HepG2 Cell Line Nocca, Giuseppina D’Avenio, Giuseppe Amalfitano, Adriana Chronopoulou, Laura Mordente, Alvaro Palocci, Cleofe Grigioni, Mauro Materials (Basel) Article 18β-glycyrrhetinic acid (GA) is a pentacyclic triterpene with promising hepatoprotective and anti-Hepatocellular carcinoma effects. GA low water solubility however reduces its biodistribution and bioavailability, limiting its applications in biomedicine. In this work we used core-shell NPs made of PolyD-L-lactide-co-glycolide (PLGA) coated with chitosan (CS), prepared through an osmosis-based methodology, to efficiently entrap GA. NPs morphology was investigated with SEM and TEM and their GA payload was evaluated with a spectrophotometric method. GA-loaded NPs were administered to HepG2 cells and their efficiency in reducing cell viability was compared with that induced by the free drug in in vitro tests. Cell viability was evaluated by the MTT assay, as well as with Electric Cells-Substrate Impedance Sensing (ECIS), that provided a real-time continuous monitoring. It was possible to correlate the toxic effect of the different forms of GA with the bioavailability of the drug, evidencing the importance of real-time tests for studying the effects of bioactive substances on cell cultures. MDPI 2021-07-12 /pmc/articles/PMC8303372/ /pubmed/34300811 http://dx.doi.org/10.3390/ma14143893 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Nocca, Giuseppina
D’Avenio, Giuseppe
Amalfitano, Adriana
Chronopoulou, Laura
Mordente, Alvaro
Palocci, Cleofe
Grigioni, Mauro
Controlled Release of 18-β-Glycyrrhetinic Acid from Core-Shell Nanoparticles: Effects on Cytotoxicity and Intracellular Concentration in HepG2 Cell Line
title Controlled Release of 18-β-Glycyrrhetinic Acid from Core-Shell Nanoparticles: Effects on Cytotoxicity and Intracellular Concentration in HepG2 Cell Line
title_full Controlled Release of 18-β-Glycyrrhetinic Acid from Core-Shell Nanoparticles: Effects on Cytotoxicity and Intracellular Concentration in HepG2 Cell Line
title_fullStr Controlled Release of 18-β-Glycyrrhetinic Acid from Core-Shell Nanoparticles: Effects on Cytotoxicity and Intracellular Concentration in HepG2 Cell Line
title_full_unstemmed Controlled Release of 18-β-Glycyrrhetinic Acid from Core-Shell Nanoparticles: Effects on Cytotoxicity and Intracellular Concentration in HepG2 Cell Line
title_short Controlled Release of 18-β-Glycyrrhetinic Acid from Core-Shell Nanoparticles: Effects on Cytotoxicity and Intracellular Concentration in HepG2 Cell Line
title_sort controlled release of 18-β-glycyrrhetinic acid from core-shell nanoparticles: effects on cytotoxicity and intracellular concentration in hepg2 cell line
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8303372/
https://www.ncbi.nlm.nih.gov/pubmed/34300811
http://dx.doi.org/10.3390/ma14143893
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