Publication: Folic Acid-Modified Ibrutinib-Loaded Silk Fibroin Nanoparticles for Cancer Cell Therapy with Over-Expressed Folate Receptor
Authors
Fuster, M. G. ; Montalbán, M. G. ; Moulefera, I. ; Víllora Cano, Gloria ; Kaplan, D. L.
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Facultad de Química
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Publisher
MDPI
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DOI
https://doi.org/10.3390/pharmaceutics15041186
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info:eu-repo/semantics/article
Description
© 2023 by the authors____ This document is the published version of a published work that appeared in final form in Pharmaceutics____
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/pharmaceutics15041186
Abstract
The anticancer drug ibrutinib (IB), also known as PCI-32765, is a compound that irreversibly
inhibits Bruton’s tyrosine kinase (BTK) and was initially developed as a treatment option for B-cell
lineage neoplasms. Its action is not limited to B-cells, as it is expressed in all hematopoietic lineages
and plays a crucial role in the tumor microenvironment. However, clinical trials with the drug
have resulted in conflicting outcomes against solid tumors. In this study, folic acid-conjugated
silk nanoparticles were used for the targeted delivery of IB to the cancer cell lines HeLa, BT-474,
and SKBR3 by exploiting the overexpression of folate receptors on their surfaces. The results were
compared with those of control healthy cells (EA.hy926). Cellular uptake studies confirmed total
internalization of the nanoparticles functionalized by this procedure in the cancer cells after 24 h,
compared to nanoparticles not functionalized with folic acid, suggesting that cellular uptake was
mediated by folate receptors overexpressed in the cancer cells. The results indicate that the developed
nanocarrier can be used for drug targeting applications by enhancing IB uptake in cancer cells with
folate receptor overexpression.
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Silk fibroin , Folate receptor , Brutinib , Nanoparticles , Cancer , HeLa , BT-474 , SKBR3 , EA.hy926
Citation
Pharmaceutics. 2023 Apr 7 15(4):1186.
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