Antimycotic influence of beta-cyclodextrin complexes--in vitro measurements using laser nephelometry in microtiter plates

Int J Pharm. 2006 Mar 27;311(1-2):113-21. doi: 10.1016/j.ijpharm.2005.12.028. Epub 2006 Jan 25.

Abstract

To determine the in vitro susceptibility of fungal organisms to beta-cyclodextrin (CD) complexes with the antifungal agents econazole-nitrate (EC) and ciclopirox-olamine (CI), a fast, rapid and simple method using laser nephelometry in 96-microtiter plate is used. The antimycotic influence of the complexes against Candida albicans DSM 11225 and Candida krusei ATCC 6258 species was determined using this method. A rapid inhibition and even killing of both fungi was observed only above certain concentrations of complex ranged between 12.5 and 100 microg/ml for beta-CD-econazole complex (CD-EC), while for the complex with ciclopirox-olamine (CD-CI) the range was between 150 and 400 microg/ml. The stability constants of the CD complexes with the two antimycotic derivatives are given. In addition, the nephelometric method allows the determination of solubilities of active agents. Thus, the improvement of solubility of both antimycotic agents in PBS buffer solution was observed by complexation with CD.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Calorimetry, Differential Scanning
  • Candida albicans / drug effects
  • Candida albicans / growth & development
  • Candida albicans / metabolism
  • Chemistry, Pharmaceutical
  • Ciclopirox
  • Drug Stability
  • Econazole / chemistry
  • Econazole / pharmacology
  • Excipients / chemistry*
  • Fluorescent Dyes
  • Lasers*
  • Microbial Sensitivity Tests*
  • Microchemistry*
  • Nephelometry and Turbidimetry / methods*
  • Pyridones / chemistry
  • Pyridones / pharmacology
  • Solubility
  • beta-Cyclodextrins / chemistry*

Substances

  • Antifungal Agents
  • Excipients
  • Fluorescent Dyes
  • Pyridones
  • beta-Cyclodextrins
  • Ciclopirox
  • Econazole