title: Delivery of epidrugs.
abstract: Inhibitors of epigenetic targets have entered clinical trials with some success, in particular for combined therapies. Like many other chemotherapeutics these new classes of molecules have dose-limiting toxicities and highly active metabolism in vivo resulting in lower efficacy than expected. This review presents drug delivery strategies proposed to prolong epigenetic inhibitor effects while reducing toxicities and metabolic clearance. Inspired from the work done in cancer-targeted strategies, prodrugs and nanoparticle-based drug delivery systems are discussed in a comprehensive way, detailing the chemical and physiological principles of the selected releasing method and, when available, how epigenetic chemistry can be exploited.
authors.affiliation: Institut de Chimie des Milieux et Matériaux de Poitiers, CNRS, UMR 7582, 4 rue Michel Brunet, B28, F-86000 Poitiers, France.
authors.forename: Fatima
authors.initials: F
authors.lastname: el Bahhaj
authors.affiliation: Department of Pharmaceutical Gene Modulation, Groningen Research Institute of Pharmacy, University of Groningen, Anthonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
authors.forename: Frank J
authors.initials: FJ
authors.lastname: Dekker
authors.affiliation: Institute of Chemistry, UMR CNRS 7272, Parc Valrose, Nice 06108 Cedex 2, France.
authors.forename: Nadine
authors.initials: N
authors.lastname: Martinet
authors.affiliation: Institut de Chimie des Milieux et Matériaux de Poitiers, CNRS, UMR 7582, 4 rue Michel Brunet, B28, F-86000 Poitiers, France. Electronic address: philippe.bertrand@univ-poitiers.fr.
authors.forename: Philippe
authors.initials: P
authors.lastname: Bertrand
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D016503:Drug Delivery Systems; D015195:Drug Design; D044127:Epigenesis, Genetic; D006801:Humans; D053758:Nanoparticles; D009369:Neoplasms / Q000188:drug therapy / Q000235:genetics; D011355:Prodrugs
chemical_list: D000970:Antineoplastic Agents; D011355:Prodrugs