title: Controlled release of 5-fluorouracil from microporous zeolites.
abstract: Zeolite particles with different pore diameter and particle size were loaded with the model anticancer drug 5-fluorouracil. The loaded zeolites were characterized by means of SEM, XRD, DSC, XPS, N2 physisorption and FT-IR. Higher loading of 5-FU was observed for NaX-FAU than BEA. Release studies were carried out in HCl 0.1N. Release of 5-FU from NaX-FAU showed exponential-type behaviour with the drug fully released within 10 min. In the case of BEA, the kinetics of 5-FU shows a multi-step profile with prolonged release over time. Molecular dynamics simulations showed that diffusion of the drug molecule through the BEA framework is lower than for NaX-FAU due to increased van der Waals interaction between the drug and the framework. The effect of zeolitic particles on the viability of Caco-2 monolayers showed that the NaX-FAU particles cause a reduction of cell viability in a more pronounced way compared with the BEA particles.
  
  
  BACKGROUND
  This article describes zeolite-based nanoparticles in generating time-controlled release of 5-FU from zeolite preparations for anti-cancer therapy.
authors.affiliation: Aristotle University of Thessaloniki, School of Pharmacy, Department of Pharmacology, Thessaloniki, Greece.
authors.forename: Marios
authors.initials: M
authors.lastname: Spanakis
authors.affiliation: Department of Materials Science, University of Patras, Rio, Patras, Greece; Foundation for Research and Technology, Hellas-Institute of Chemical Engineering Sciences-FORTH/ICE-HT, Patras, Greece.
authors.forename: Nikolaos
authors.initials: N
authors.lastname: Bouropoulos
authors.affiliation: Aristotle University of Thessaloniki, School of Pharmacy, Department of Pharmaceutical Technology, Thessaloniki, Greece.
authors.forename: Dimitrios
authors.initials: D
authors.lastname: Theodoropoulos
authors.affiliation: Foundation for Research and Technology, Hellas-Institute of Chemical Engineering Sciences-FORTH/ICE-HT, Patras, Greece.
authors.forename: Lamprini
authors.initials: L
authors.lastname: Sygellou
authors.affiliation: School of Pharmacy and Biomedical Sciences, University of Portsmouth, Portsmouth, UK.
authors.forename: Sinead
authors.initials: S
authors.lastname: Ewart
authors.affiliation: Foundation for Research and Technology, Hellas-Institute of Chemical Engineering Sciences-FORTH/ICE-HT, Patras, Greece.
authors.forename: Anastasia Maria
authors.initials: AM
authors.lastname: Moschovi
authors.affiliation: Foundation for Research and Technology, Hellas-Institute of Chemical Engineering Sciences-FORTH/ICE-HT, Patras, Greece.
authors.forename: Angeliki
authors.initials: A
authors.lastname: Siokou
authors.affiliation: Aristotle University of Thessaloniki, School of Pharmacy, Department of Pharmacology, Thessaloniki, Greece.
authors.forename: Ioannis
authors.initials: I
authors.lastname: Niopas
authors.affiliation: Aristotle University of Thessaloniki, School of Pharmacy, Department of Pharmaceutical Technology, Thessaloniki, Greece.
authors.forename: Kyriakos
authors.initials: K
authors.lastname: Kachrimanis
authors.affiliation: University of Delaware, Catalysis Center for Energy Innovation & Department of Chemical and Biomolecular Engineering, Newark, DE, USA.
authors.forename: Vladimiros
authors.initials: V
authors.lastname: Nikolakis
authors.affiliation: School of Pharmacy and Biomedical Sciences, University of Portsmouth, Portsmouth, UK.
authors.forename: Paul A
authors.initials: PA
authors.lastname: Cox
authors.affiliation: Aristotle University of Thessaloniki, School of Pharmacy, Department of Pharmacology, Thessaloniki, Greece.
authors.forename: Ioannis S
authors.initials: IS
authors.lastname: Vizirianakis
authors.affiliation: Aristotle University of Thessaloniki, School of Pharmacy, Department of Pharmaceutical Technology, Thessaloniki, Greece. Electronic address: dfatouro@pharm.auth.gr.
authors.forename: Dimitrios G
authors.initials: DG
authors.lastname: Fatouros
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000737:chemistry; D018938:Caco-2 Cells; D002470:Cell Survival / Q000187:drug effects; D004058:Diffusion; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D005472:Fluorouracil / Q000008:administration & dosage* / Q000737:chemistry; D006801:Humans; D007700:Kinetics; D056004:Molecular Dynamics Simulation; D053758:Nanoparticles / Q000008:administration & dosage* / Q000737:chemistry; D009369:Neoplasms / Q000188:drug therapy*; D017550:Spectroscopy, Fourier Transform Infrared; D017641:Zeolites / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D004337:Drug Carriers; D017641:Zeolites; D005472:Fluorouracil
keywords: Controlled release; Cytocompatibility; Molecular modeling; Zeolites