Antimicrobial activity of fusidic acid inclusion complexes

Int J Infect Dis. 2020 Dec:101:65-73. doi: 10.1016/j.ijid.2020.09.1465. Epub 2020 Oct 1.

Abstract

Objectives: To synthesize and characterize the inclusion complexes of fusidic acid with β - cyclodextrin, followed by the evaluation of their antimicrobial activity against pure strain (Staphylococcus aureus ATCC 25,923) and isolated Staphylococcus from clinical cases.

Methods: The desired compounds were synthesized using molar ratio of fusidic acid: β-cyclodextrin of 1:1. Synthesized compounds were analyzed by Fourier Transform Infrared Spectroscopy (FTIR), X-Ray Diffraction (XRD), Scanning Electron Microscopy (SEM), and Thermal Analysis, and the results confirmed the formation of inclusion compounds by fusidic acid with β-cyclodextrin.

Results: Physical-chemical characterization confirmed the preparation of desired inclusion compounds, and the antimicrobial test confirmed that all compounds obtained have antimicrobial activity. Antimicrobial activity of freeze-drying complex againstS. aureus is similar with pure fusidic acid activity, being better than the cefoxitin one. Similar behavior was observed against methicillin-resistant S. aureus and S. epidermidis.

Conclusions: In the present work, three different inclusion complexes of fusidic acid were prepared using three different preparation methods. All inclusion complexes obtained presented good antimicrobial activity against differentS. aureus strains. Antimicrobial activity of these new prepared compounds was observed to be better than that of cefoxitin.

Keywords: Antimicrobial activity; Compounds characterization; Cyclodextrin; Fusidic acid.

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Freeze Drying
  • Fusidic Acid / chemistry
  • Fusidic Acid / pharmacology*
  • Humans
  • Methicillin-Resistant Staphylococcus aureus / drug effects
  • Microscopy, Electron, Scanning
  • Spectroscopy, Fourier Transform Infrared
  • Staphylococcus aureus / drug effects*
  • X-Ray Diffraction
  • beta-Cyclodextrins / chemistry
  • beta-Cyclodextrins / pharmacology

Substances

  • Anti-Bacterial Agents
  • beta-Cyclodextrins
  • Fusidic Acid