Controlled release of 5-fluorouracil from microporous zeolites

• Published in: Nanomedicine Vol. 10; no. 1; pp. 197 - 205
• Main Authors: Spanakis, Marios, PhD, Bouropoulos, Nikolaos, PhD, Theodoropoulos, Dimitrios, MSc, Sygellou, Lamprini, PhD, Ewart, Sinead, MSc, Moschovi, Anastasia Maria, PhD, Siokou, Angeliki, PhD, Niopas, Ioannis, PhD, Kachrimanis, Kyriakos, PhD, Nikolakis, Vladimiros, PhD, Cox, Paul A., PhD, Vizirianakis, Ioannis S., PhD, Fatouros, Dimitrios G., PhD
• Format: Journal Article
• Language: English
• Published: United States Elsevier Inc 2014
• Subjects: Antineoplastic Agents - administration & dosage; Antineoplastic Agents - chemistry; Caco-2 Cells; Cell Survival - drug effects; Controlled release; Cytocompatibility; Diffusion; Drug Carriers - administration & dosage; Drug Carriers - chemistry; Fluorouracil - administration & dosage; Fluorouracil - chemistry; Humans; Internal Medicine; Kinetics; Molecular Dynamics Simulation; Molecular modeling; Nanoparticles - administration & dosage; Nanoparticles - chemistry; Neoplasms - drug therapy; Spectroscopy, Fourier Transform Infrared; Zeolites; Zeolites - administration & dosage; Zeolites - chemistry; Cytocompatibility; Zeolites; Molecular modeling; Controlled release
• ISSN: 1549-9634; 1549-9642
• DOI: 10.1016/j.nano.2013.06.016

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 0.1 N. 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. From the Clinical Editor This article describes zeolite-based nanoparticles in generating time-controlled release of 5-FU from zeolite preparations for anti-cancer therapy.