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Type: Journal article
Title: Histone deacetylase inhibitors delivery using nanoparticles with intrinsic passive tumor targeting properties for tumor therapy
Author: Bahhaj, F.E.
Denis, I.
Pichavant, L.
Delatouche, R.
Collette, F.
Linot, C.
Pouliquen, D.
Grégoire, M.
Héroguez, V.
Blanquart, C.
Bertrand, P.
Citation: Theranostics, 2016; 6(6):795-807
Publisher: Ivyspring International
Issue Date: 2016
ISSN: 1838-7640
Statement of
Fatima el Bahhaj, Iza Denis, Loic Pichavant, Régis Delatouche, Floraine Collette, Camille Linot, Daniel Pouliquen, Marc Grégoire, Valérie Héroguez, Christophe Blanquart, Philippe Bertrand
Abstract: Fast clearance, metabolism and systemic toxicity are major limits for the clinical use of anti-cancer drugs. Histone deacetylase inhibitors (HDACi) present these defects despite displaying promising anti-tumor properties on tumor cells in vitro and in in vivo model of cancers. Specific delivery of anti-cancer drugs into the tumor should improve their clinical benefit by limiting systemic toxicity and by increasing the anti-tumor effect. In this work, we describe a simple and flexible polymeric nanoparticle platform highly targeting the tumor in vivo and triggering impressive tumor weight reduction when functionalized with HDACi. Our nanoparticles were produced by Ring-Opening Metathesis Polymerization of azido-polyethylene oxide-norbornene macromonomers and functionalized using click chemistry. Using an orthotopic model of peritoneal invasive cancer, a highly selective accumulation of the particles in the tumor was obtained. A combination of epigenetic drugs involving a pH-responsive histone deacetylase inhibitor (HDACi) polymer conjugated to these particles gave 80% reduction of tumor weight without toxicity whereas the free HDACi has no effect. Our work demonstrates that the use of a nanovector with theranostic properties leads to an optimized delivery of potent HDACi in tumor and then, to an improvement of their anti-tumor properties in vivo.
Keywords: Polymeric nanoparticle; epigenetic; HDAC; cancer; theranostics; peritoneal; mesothelioma
Rights: © Ivyspring International Publisher. Reproduction is permitted for personal, noncommercial use, provided that the article is in whole, unmodified, and properly cited. See for terms and conditions. This is an open access article distributed under the terms of the Creative Commons Attribution (CC BY-NC) License. See for full terms and conditions.
RMID: 0030066012
DOI: 10.7150/thno.13725
Appears in Collections:Medicine publications

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