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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...
Autores principales: | , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2021
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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. |
format | Online Article Text |
id | pubmed-8303372 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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