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Antitumor Activity of Rosmarinic Acid-Loaded Silk Fibroin Nanoparticles on HeLa and MCF-7 Cells

Rosmarinic acid (RA), one of the most important polyphenol-based antioxidants, has drawn increasing attention because of its remarkable bioactive properties, including anti-inflammatory, anticancer and antibacterial activities. The aim of this study was to synthesize and characterize RA-loaded silk...

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Autores principales: Fuster, Marta G., Carissimi, Guzmán, Montalbán, Mercedes G., Víllora, Gloria
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8467615/
https://www.ncbi.nlm.nih.gov/pubmed/34578069
http://dx.doi.org/10.3390/polym13183169
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author Fuster, Marta G.
Carissimi, Guzmán
Montalbán, Mercedes G.
Víllora, Gloria
author_facet Fuster, Marta G.
Carissimi, Guzmán
Montalbán, Mercedes G.
Víllora, Gloria
author_sort Fuster, Marta G.
collection PubMed
description Rosmarinic acid (RA), one of the most important polyphenol-based antioxidants, has drawn increasing attention because of its remarkable bioactive properties, including anti-inflammatory, anticancer and antibacterial activities. The aim of this study was to synthesize and characterize RA-loaded silk fibroin nanoparticles (RA-SFNs) in terms of their physical–chemical features and composition, and to investigate their antitumor activity against human cervical carcinoma and breast cancer cell lines (HeLa and MCF-7). Compared with the free form, RA bioavailability was enhanced when the drug was adsorbed onto the surface of the silk fibroin nanoparticles (SFNs). The resulting particle diameter was 255 nm, with a polydispersity index of 0.187, and the Z-potential was −17 mV. The drug loading content of the RA-SFNs was 9.4 wt.%. Evaluation of the in vitro drug release of RA from RA-SFNs pointed to a rapid release in physiological conditions (50% of the total drug content was released in 0.5 h). Unloaded SFNs exhibited good biocompatibility, with no significant cytotoxicity observed during the first 48 h against HeLa and MCF-7 cancer cells. In contrast, cell death increased in a concentration-dependent manner after treatment with RA-SFNs, reaching an IC(50) value of 1.568 and 1.377 mg/mL on HeLa and MCF-7, respectively. For both cell lines, the IC(50) of free RA was higher. The cellular uptake of the nanoparticles studied was increased when RA was loaded on them. The cell cycle and apoptosis studies revealed that RA-SFNs inhibit cell proliferation and induce apoptosis on HeLa and MCF-7 cell lines. It is concluded, therefore, that the RA delivery platform based on SFNs improves the antitumor potential of RA in the case of the above cancers.
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spelling pubmed-84676152021-09-27 Antitumor Activity of Rosmarinic Acid-Loaded Silk Fibroin Nanoparticles on HeLa and MCF-7 Cells Fuster, Marta G. Carissimi, Guzmán Montalbán, Mercedes G. Víllora, Gloria Polymers (Basel) Article Rosmarinic acid (RA), one of the most important polyphenol-based antioxidants, has drawn increasing attention because of its remarkable bioactive properties, including anti-inflammatory, anticancer and antibacterial activities. The aim of this study was to synthesize and characterize RA-loaded silk fibroin nanoparticles (RA-SFNs) in terms of their physical–chemical features and composition, and to investigate their antitumor activity against human cervical carcinoma and breast cancer cell lines (HeLa and MCF-7). Compared with the free form, RA bioavailability was enhanced when the drug was adsorbed onto the surface of the silk fibroin nanoparticles (SFNs). The resulting particle diameter was 255 nm, with a polydispersity index of 0.187, and the Z-potential was −17 mV. The drug loading content of the RA-SFNs was 9.4 wt.%. Evaluation of the in vitro drug release of RA from RA-SFNs pointed to a rapid release in physiological conditions (50% of the total drug content was released in 0.5 h). Unloaded SFNs exhibited good biocompatibility, with no significant cytotoxicity observed during the first 48 h against HeLa and MCF-7 cancer cells. In contrast, cell death increased in a concentration-dependent manner after treatment with RA-SFNs, reaching an IC(50) value of 1.568 and 1.377 mg/mL on HeLa and MCF-7, respectively. For both cell lines, the IC(50) of free RA was higher. The cellular uptake of the nanoparticles studied was increased when RA was loaded on them. The cell cycle and apoptosis studies revealed that RA-SFNs inhibit cell proliferation and induce apoptosis on HeLa and MCF-7 cell lines. It is concluded, therefore, that the RA delivery platform based on SFNs improves the antitumor potential of RA in the case of the above cancers. MDPI 2021-09-18 /pmc/articles/PMC8467615/ /pubmed/34578069 http://dx.doi.org/10.3390/polym13183169 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
Fuster, Marta G.
Carissimi, Guzmán
Montalbán, Mercedes G.
Víllora, Gloria
Antitumor Activity of Rosmarinic Acid-Loaded Silk Fibroin Nanoparticles on HeLa and MCF-7 Cells
title Antitumor Activity of Rosmarinic Acid-Loaded Silk Fibroin Nanoparticles on HeLa and MCF-7 Cells
title_full Antitumor Activity of Rosmarinic Acid-Loaded Silk Fibroin Nanoparticles on HeLa and MCF-7 Cells
title_fullStr Antitumor Activity of Rosmarinic Acid-Loaded Silk Fibroin Nanoparticles on HeLa and MCF-7 Cells
title_full_unstemmed Antitumor Activity of Rosmarinic Acid-Loaded Silk Fibroin Nanoparticles on HeLa and MCF-7 Cells
title_short Antitumor Activity of Rosmarinic Acid-Loaded Silk Fibroin Nanoparticles on HeLa and MCF-7 Cells
title_sort antitumor activity of rosmarinic acid-loaded silk fibroin nanoparticles on hela and mcf-7 cells
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8467615/
https://www.ncbi.nlm.nih.gov/pubmed/34578069
http://dx.doi.org/10.3390/polym13183169
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