Biocompatibility and levofloxacin delivery of mesoporous materials

Eur J Pharm Biopharm. 2013 May;84(1):115-24. doi: 10.1016/j.ejpb.2012.11.029. Epub 2012 Dec 27.

Abstract

A comparative study of mesoporous matrices designed for both drug-loading methods, impregnation (IP) and surfactant-assisted drug loading (also denoted as one-pot, OP), has been carried out evaluating their physicochemical characteristics, cell response, drug delivery profiles, and antibacterial activity. Surfactant-free (calcined) and surfactant-templated (non-calcined) mesoporous silica have been used as IP and OP starting matrices, respectively. Both non-calcined and calcined matrices do not exert any cytotoxic effect on osteoblasts. However, non-calcined matrices induce on fibroblasts a significant proliferation delay with morphological alterations and dose-dependent increases in fibroblast size, internal complexity, and intracellular calcium content but without cell lysis and apoptosis. Residual ethanol and the surface silanol groups in these non-calcined matrices are involved in the observed fibroblast changes. Finally, both IP and OP matrices have been loaded with levofloxacin to compare them as drug delivery systems. Both IP and OP matrices exhibit similar in vitro levofloxacin release profiles, showing an initial fast delivery followed by a sustained release during long time periods. These profiles and the antimicrobial activity results suggest the use of these IP and OP matrices as local drug delivery systems in the osteomyelitis and other bone infection treatments.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Biocompatible Materials / administration & dosage*
  • Biocompatible Materials / chemistry*
  • Biocompatible Materials / pharmacokinetics
  • Cells, Cultured
  • Drug Delivery Systems / methods*
  • Fibroblasts / drug effects
  • Fibroblasts / metabolism
  • Humans
  • Levofloxacin / administration & dosage*
  • Levofloxacin / chemistry*
  • Levofloxacin / pharmacokinetics
  • Materials Testing / methods
  • Mice
  • Osteoblasts / drug effects
  • Osteoblasts / metabolism
  • Porosity

Substances

  • Biocompatible Materials
  • Levofloxacin