Econazole nitrate-loaded MCM-41 for an antifungal topical powder formulation

J Pharm Sci. 2010 Nov;99(11):4738-45. doi: 10.1002/jps.22183.

Abstract

The aim of this article was to prepare a topical powder for the treatment of fungal infections, such as Candida intertrigo and tinea pedis. Thus, an econazole nitrate (ECO) formulation with improved drug dissolution and proper moisture adsorption was designed. ECO was melt with the mesoporous silicate MCM-41 (drug/MCM-41 1/3) and the resulting inclusion compound was characterized by X-ray powder diffraction (XRPD) and differential scanning calorimetry (DSC). The drug loading was confirmed by the decrease of specific surface area and pore volume between MCM-41 and the inclusion compound. Formulations containing the inclusion compound were prepared and submitted to in vitro dissolution test and in vitro antifungal activity. A remarkable dissolution rate improvement as well as a higher antifungal activity was observed for the inclusion compound if compared to a commercial product. Moisture sorption properties for MCM-41 and formulations were evaluated as well.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Topical
  • Antifungal Agents / administration & dosage*
  • Antifungal Agents / pharmacology*
  • Calorimetry, Differential Scanning
  • Candida albicans / drug effects*
  • Candidiasis / drug therapy
  • Drug Carriers / chemistry*
  • Drug Stability
  • Econazole / administration & dosage*
  • Econazole / pharmacology*
  • Humans
  • Humidity
  • Powder Diffraction
  • Silicon Dioxide / chemistry*
  • Solubility
  • X-Ray Diffraction

Substances

  • Antifungal Agents
  • Drug Carriers
  • MCM-41
  • Econazole
  • Silicon Dioxide