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Hydrophilic Fluorescent Nanoprodrug of Paclitaxel for Glioblastoma Chemotherapy
[Image: see text] Highly water-soluble, nontoxic organic nanoparticles on which paclitaxel (PTX), a hydrophobic anticancer drug, has been covalently bound via an ester linkage (4.5% of total weight) have been prepared for the treatment of glioblastoma. These soft fluorescent organic nanoparticles (F...
Autores principales: | , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2019
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Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6844107/ https://www.ncbi.nlm.nih.gov/pubmed/31720536 http://dx.doi.org/10.1021/acsomega.9b02588 |
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author | Daniel, Jonathan Montaleytang, Maeva Nagarajan, Sounderya Picard, Sébastien Clermont, Guillaume Lazar, Adina N. Dumas, Noé Correard, Florian Braguer, Diane Blanchard-Desce, Mireille Estève, Marie-Anne Vaultier, Michel |
author_facet | Daniel, Jonathan Montaleytang, Maeva Nagarajan, Sounderya Picard, Sébastien Clermont, Guillaume Lazar, Adina N. Dumas, Noé Correard, Florian Braguer, Diane Blanchard-Desce, Mireille Estève, Marie-Anne Vaultier, Michel |
author_sort | Daniel, Jonathan |
collection | PubMed |
description | [Image: see text] Highly water-soluble, nontoxic organic nanoparticles on which paclitaxel (PTX), a hydrophobic anticancer drug, has been covalently bound via an ester linkage (4.5% of total weight) have been prepared for the treatment of glioblastoma. These soft fluorescent organic nanoparticles (FONPs), obtained from citric acid and diethylenetriamine by microwave-assisted condensation, show suitable size (Ø = 17–30 nm), remarkable solubility in water, softness as well as strong blue fluorescence in an aqueous environment that are fully retained in cell culture medium. Moreover, these FONPs were demonstrated to show in vitro safety and preferential internalization in glioblastoma cells through caveolin/lipid raft-mediated endocytosis. The PTX-conjugated FONPs retain excellent solubility in water and remain stable in water (no leaching), while they showed anticancer activity against glioblastoma cells in two-dimensional and three-dimensional culture. PTX-specific effects on microtubules reveal that PTX is intracellularly released from the nanocarriers in its active form, in relation with an intracellular-promoted lysis of the ester linkage. As such, these hydrophilic prodrug formulations hold major promise as biocompatible nanotools for drug delivery. |
format | Online Article Text |
id | pubmed-6844107 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2019 |
publisher | American Chemical Society |
record_format | MEDLINE/PubMed |
spelling | pubmed-68441072019-11-12 Hydrophilic Fluorescent Nanoprodrug of Paclitaxel for Glioblastoma Chemotherapy Daniel, Jonathan Montaleytang, Maeva Nagarajan, Sounderya Picard, Sébastien Clermont, Guillaume Lazar, Adina N. Dumas, Noé Correard, Florian Braguer, Diane Blanchard-Desce, Mireille Estève, Marie-Anne Vaultier, Michel ACS Omega [Image: see text] Highly water-soluble, nontoxic organic nanoparticles on which paclitaxel (PTX), a hydrophobic anticancer drug, has been covalently bound via an ester linkage (4.5% of total weight) have been prepared for the treatment of glioblastoma. These soft fluorescent organic nanoparticles (FONPs), obtained from citric acid and diethylenetriamine by microwave-assisted condensation, show suitable size (Ø = 17–30 nm), remarkable solubility in water, softness as well as strong blue fluorescence in an aqueous environment that are fully retained in cell culture medium. Moreover, these FONPs were demonstrated to show in vitro safety and preferential internalization in glioblastoma cells through caveolin/lipid raft-mediated endocytosis. The PTX-conjugated FONPs retain excellent solubility in water and remain stable in water (no leaching), while they showed anticancer activity against glioblastoma cells in two-dimensional and three-dimensional culture. PTX-specific effects on microtubules reveal that PTX is intracellularly released from the nanocarriers in its active form, in relation with an intracellular-promoted lysis of the ester linkage. As such, these hydrophilic prodrug formulations hold major promise as biocompatible nanotools for drug delivery. American Chemical Society 2019-10-24 /pmc/articles/PMC6844107/ /pubmed/31720536 http://dx.doi.org/10.1021/acsomega.9b02588 Text en Copyright © 2019 American Chemical Society This is an open access article published under an ACS AuthorChoice License (http://pubs.acs.org/page/policy/authorchoice_termsofuse.html) , which permits copying and redistribution of the article or any adaptations for non-commercial purposes. |
spellingShingle | Daniel, Jonathan Montaleytang, Maeva Nagarajan, Sounderya Picard, Sébastien Clermont, Guillaume Lazar, Adina N. Dumas, Noé Correard, Florian Braguer, Diane Blanchard-Desce, Mireille Estève, Marie-Anne Vaultier, Michel Hydrophilic Fluorescent Nanoprodrug of Paclitaxel for Glioblastoma Chemotherapy |
title | Hydrophilic Fluorescent Nanoprodrug of Paclitaxel
for Glioblastoma Chemotherapy |
title_full | Hydrophilic Fluorescent Nanoprodrug of Paclitaxel
for Glioblastoma Chemotherapy |
title_fullStr | Hydrophilic Fluorescent Nanoprodrug of Paclitaxel
for Glioblastoma Chemotherapy |
title_full_unstemmed | Hydrophilic Fluorescent Nanoprodrug of Paclitaxel
for Glioblastoma Chemotherapy |
title_short | Hydrophilic Fluorescent Nanoprodrug of Paclitaxel
for Glioblastoma Chemotherapy |
title_sort | hydrophilic fluorescent nanoprodrug of paclitaxel
for glioblastoma chemotherapy |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6844107/ https://www.ncbi.nlm.nih.gov/pubmed/31720536 http://dx.doi.org/10.1021/acsomega.9b02588 |
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