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Delivery of Proapoptotic Agents in Glioma Cell Lines by TSPO Ligand–Dextran Nanogels

Department of Pharmacy–Drug Sciences, University of Bari “Aldo Moro”, Via Orabona, St. 4, 70125 Bari, Italy
Institute for Physical and Chemical Processes (IPCF)-CNR, SS Bari, Via Orabona, St. 4, 70125 Bari, Italy
Istituto tumori IRCCS “Giovanni Paolo II”, Flacco, St. 65, 70124 Bari, Italy
Department of Chemistry, University of Bari “Aldo Moro”, 70125 Bari, Italy
Author to whom correspondence should be addressed.
Int. J. Mol. Sci. 2018, 19(4), 1155;
Received: 2 March 2018 / Revised: 7 April 2018 / Accepted: 8 April 2018 / Published: 11 April 2018
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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. View Full-Text
Keywords: translocator protein; dextran; TSPO ligand; bioconjugate; nanogels translocator protein; dextran; TSPO ligand; bioconjugate; nanogels

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Lopalco, A.; Cutrignelli, A.; Denora, N.; Perrone, M.; Iacobazzi, R.M.; Fanizza, E.; Lopedota, A.; Depalo, N.; De Candia, M.; Franco, M.; Laquintana, V. Delivery of Proapoptotic Agents in Glioma Cell Lines by TSPO Ligand–Dextran Nanogels. Int. J. Mol. Sci. 2018, 19, 1155.

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