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Delivery of Proapoptotic Agents in Glioma Cell Lines by TSPO Ligand–Dextran Nanogels
Translocator protein 18-kDa (TSPO) is a versatile mitochondrial target for molecular imaging and therapy. Moreover, selective TSPO ligands have been widely investigated for diagnostic purposes and explored to target drug delivery systems directed to cancer cells overexpressing TSPO. Indeed, poly(d,l...
Autores principales: | , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5979576/ https://www.ncbi.nlm.nih.gov/pubmed/29641449 http://dx.doi.org/10.3390/ijms19041155 |
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author | Lopalco, Antonio Cutrignelli, Annalisa Denora, Nunzio Perrone, Mara Iacobazzi, Rosa Maria Fanizza, Elisabetta Lopedota, Angela Depalo, Nicoletta de Candia, Modesto Franco, Massimo Laquintana, Valentino |
author_facet | Lopalco, Antonio Cutrignelli, Annalisa Denora, Nunzio Perrone, Mara Iacobazzi, Rosa Maria Fanizza, Elisabetta Lopedota, Angela Depalo, Nicoletta de Candia, Modesto Franco, Massimo Laquintana, Valentino |
author_sort | Lopalco, Antonio |
collection | PubMed |
description | Translocator protein 18-kDa (TSPO) is a versatile mitochondrial target for molecular imaging and therapy. Moreover, selective TSPO ligands have been widely investigated for diagnostic purposes and explored to target drug delivery systems directed to cancer cells overexpressing TSPO. Indeed, poly(d,l-lactic-co-glycolic acid (PLGA) polymers and nanocarriers decorated with TSPO ligands are capable of transporting TSPO ligands inside cancer cells, inducing survival inhibition in cancer cells and producing mitochondrial morphology modification. The aim of this work was to prepare nanogels (NGs) made with TSPO ligand dextran conjugates (TSPO-Dex) that are useful as potential delivery systems of two TSPO ligands as apoptotic agents. Synthesis and complete characterization of TSPO–dextran conjugates, an average molecular weights analysis, TSPO ligand release profiles, thermal behaviour and swelling studies were achieved. NG preparation, characterization and in vitro biological studies were also performed. The release of TSPO ligands released from dextran conjugates at 37 °C occurred in human serum at a faster rate than that detected in phosphate buffer. Cytotoxicity studies demonstrated that NGs produced from TSPO ligand–dextran conjugates induce survival inhibition in rat C6 glioma cell lines. Cellular uptake was also proven by fluorescence microscopy. |
format | Online Article Text |
id | pubmed-5979576 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-59795762018-06-10 Delivery of Proapoptotic Agents in Glioma Cell Lines by TSPO Ligand–Dextran Nanogels Lopalco, Antonio Cutrignelli, Annalisa Denora, Nunzio Perrone, Mara Iacobazzi, Rosa Maria Fanizza, Elisabetta Lopedota, Angela Depalo, Nicoletta de Candia, Modesto Franco, Massimo Laquintana, Valentino Int J Mol Sci Article Translocator protein 18-kDa (TSPO) is a versatile mitochondrial target for molecular imaging and therapy. Moreover, selective TSPO ligands have been widely investigated for diagnostic purposes and explored to target drug delivery systems directed to cancer cells overexpressing TSPO. Indeed, poly(d,l-lactic-co-glycolic acid (PLGA) polymers and nanocarriers decorated with TSPO ligands are capable of transporting TSPO ligands inside cancer cells, inducing survival inhibition in cancer cells and producing mitochondrial morphology modification. The aim of this work was to prepare nanogels (NGs) made with TSPO ligand dextran conjugates (TSPO-Dex) that are useful as potential delivery systems of two TSPO ligands as apoptotic agents. Synthesis and complete characterization of TSPO–dextran conjugates, an average molecular weights analysis, TSPO ligand release profiles, thermal behaviour and swelling studies were achieved. NG preparation, characterization and in vitro biological studies were also performed. The release of TSPO ligands released from dextran conjugates at 37 °C occurred in human serum at a faster rate than that detected in phosphate buffer. Cytotoxicity studies demonstrated that NGs produced from TSPO ligand–dextran conjugates induce survival inhibition in rat C6 glioma cell lines. Cellular uptake was also proven by fluorescence microscopy. MDPI 2018-04-11 /pmc/articles/PMC5979576/ /pubmed/29641449 http://dx.doi.org/10.3390/ijms19041155 Text en © 2018 by the authors. 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 (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Lopalco, Antonio Cutrignelli, Annalisa Denora, Nunzio Perrone, Mara Iacobazzi, Rosa Maria Fanizza, Elisabetta Lopedota, Angela Depalo, Nicoletta de Candia, Modesto Franco, Massimo Laquintana, Valentino Delivery of Proapoptotic Agents in Glioma Cell Lines by TSPO Ligand–Dextran Nanogels |
title | Delivery of Proapoptotic Agents in Glioma Cell Lines by TSPO Ligand–Dextran Nanogels |
title_full | Delivery of Proapoptotic Agents in Glioma Cell Lines by TSPO Ligand–Dextran Nanogels |
title_fullStr | Delivery of Proapoptotic Agents in Glioma Cell Lines by TSPO Ligand–Dextran Nanogels |
title_full_unstemmed | Delivery of Proapoptotic Agents in Glioma Cell Lines by TSPO Ligand–Dextran Nanogels |
title_short | Delivery of Proapoptotic Agents in Glioma Cell Lines by TSPO Ligand–Dextran Nanogels |
title_sort | delivery of proapoptotic agents in glioma cell lines by tspo ligand–dextran nanogels |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5979576/ https://www.ncbi.nlm.nih.gov/pubmed/29641449 http://dx.doi.org/10.3390/ijms19041155 |
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