Publication: Antitumor Activity of Rosmarinic Acid-Loaded Silk Fibroin Nanoparticles on HeLa and MCF-7 Cells
Authors
Fuster, M. G. ; Carissimi, G. ; Montalbán, M. G. ; Víllora Cano, Gloria
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Facultad de Química
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Publisher
MDPI
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DOI
https://doi.org/10.3390/polym13183169
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info:eu-repo/semantics/article
Description
© 2021 by the authors____ This document is the published version of a published work that appeared in final form in Polymers____
This document is made available under the CC-BY 4.0 license http://creativecommons.org/licenses/by/4.0 ____
To access the final edited and published work see:
https://doi.org/10.3390/polym13183169
Abstract
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
IC50 value of 1.568 and 1.377 mg/mL on HeLa and MCF-7, respectively. For both cell lines, the IC50
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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Citation
Polymers 2021, 13(18), 3169
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