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 st...

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Veröffentlicht in:Nanomedicine 2014, Vol.10 (1), p.197-205
Hauptverfasser: 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
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container_end_page 205
container_issue 1
container_start_page 197
container_title Nanomedicine
container_volume 10
creator 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
description 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.
doi_str_mv 10.1016/j.nano.2013.06.016
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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. 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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
title Controlled release of 5-fluorouracil from microporous zeolites
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