Controlled release of 5-fluorouracil from microporous zeolites

Nanomedicine. 2014 Jan;10(1):197-205. doi: 10.1016/j.nano.2013.06.016. Epub 2013 Aug 3.

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.

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.

Keywords: Controlled release; Cytocompatibility; Molecular modeling; Zeolites.

MeSH terms

  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Agents / chemistry
  • Caco-2 Cells
  • Cell Survival / drug effects
  • Diffusion
  • Drug Carriers / administration & dosage
  • Drug Carriers / chemistry
  • Fluorouracil / administration & dosage*
  • Fluorouracil / chemistry
  • Humans
  • Kinetics
  • Molecular Dynamics Simulation
  • Nanoparticles / administration & dosage*
  • Nanoparticles / chemistry
  • Neoplasms / drug therapy*
  • Spectroscopy, Fourier Transform Infrared
  • Zeolites / administration & dosage*
  • Zeolites / chemistry

Substances

  • Antineoplastic Agents
  • Drug Carriers
  • Zeolites
  • Fluorouracil