Preparation of liposomal nanoparticles incorporating terbinafine in vitro drug release studies

J Nanosci Nanotechnol. 2014 Jun;14(6):4529-33. doi: 10.1166/jnn.2014.9026.

Abstract

Terbinafine hydrochloride (TBH) (E)-N-(6,6-dimethyl-2-hepten-4-inyl)-N-methyl-1-naphthaline-methanamine(-hydrochloride) is an effective antifungal agent already existing on the market in the form of topical formulations. The present study deals with the preparation and physicochemical characterization (size, polydispersity, zeta-potential) of 1,2-Diacyl-sn-glycero-3-phosphocholine (EggPC) incorporating TBH in two different dispersion media (tris-buffered saline (TBS) of pH 7.4 or in phosphate buffer solution (PS) of pH 5.5) in order to investigate how pH of dispersion media affects the incorporation efficiency of TBH into liposomes. There were further prepared three Carbopol 934 hydrogels of different concentrations (0.5, 1 and 2%) and their viscosity was measured and evaluated. Moreover, the in vitro drug release from three liposomal gels was studied, in order to investigate the ability of liposomes to act as carriers for TBH in a gel. All formulations were found to retain their original physicochemical properties at least for three weeks. These early studies on the release kinetics from liposomal gel show that Korsmeyer-Peppas model could be the best fitted model concerning the TBH release profile and could be supported biophysically from extended Derjaguin-Landau-Verwey-Overbeek (DLVO) theory.

MeSH terms

  • Antifungal Agents / administration & dosage
  • Antifungal Agents / chemistry
  • Computer Simulation
  • Diffusion
  • Drug Stability
  • Kinetics
  • Liposomes / chemical synthesis*
  • Models, Chemical*
  • Nanocapsules / chemistry*
  • Nanocapsules / ultrastructure*
  • Naphthalenes / administration & dosage
  • Naphthalenes / chemistry*
  • Particle Size
  • Terbinafine

Substances

  • Antifungal Agents
  • Liposomes
  • Nanocapsules
  • Naphthalenes
  • Terbinafine