Synthesis and characterization of a pH-sensitive conjugate of isoniazid with Fe3O4@SiO2 magnetic nanoparticles

Bioorg Med Chem Lett. 2013 Aug 15;23(16):4692-5. doi: 10.1016/j.bmcl.2013.05.103. Epub 2013 Jun 11.

Abstract

The Letter describes the preparation and characterization of a conjugate of isoniazid (INH) with magnetic nanoparticles Fe3O4@SiO2 115±60 nm in size. The INH molecules were attached to the surface of nanoparticles by a covalent pH-sensitive amidine bond. The conjugate was characterized by X-ray diffraction, SEM, dynamic light scattering, IR spectroscopy and microanalysis. The conjugate released isoniazid under in vitro conditions (pH=4; 37 °C; t1/2≈115 s). In addition, the cytotoxicity of the Fe3O4@SiO2-INH conjugate was evaluated in SK-BR-3 cells using the xCELLigence system.

Keywords: Isoniazid; Magnetic nanoparticle; Prodrug; Tuberculostatic agent; pH-sensitivity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / toxicity
  • Cell Proliferation / drug effects
  • Cells, Cultured
  • Ferric Compounds / chemistry*
  • Hydrogen-Ion Concentration
  • Isoniazid / chemical synthesis*
  • Isoniazid / chemistry
  • Isoniazid / toxicity*
  • Magnetics*
  • Microscopy, Electron, Scanning
  • Nanoparticles / chemistry*
  • Silicon Dioxide / chemistry*
  • X-Ray Diffraction

Substances

  • Anti-Bacterial Agents
  • Ferric Compounds
  • ferric oxide
  • Silicon Dioxide
  • Isoniazid