Voriconazole is cytotoxic at locally delivered concentrations: a pilot study

Clin Orthop Relat Res. 2013 Oct;471(10):3165-70. doi: 10.1007/s11999-013-2860-7.

Abstract

Background: Fungal infections are rare but major problems when they involve orthopaedic implants. Preferred treatment in North America is two-staged: resection and then delayed reconstruction, with local delivery of an antifungal between stages. The effect of voriconazole, a hydrophobic antifungal, on local tissues and wound healing is unclear.

Questions/purposes: We asked: (1) Is voriconazole cytotoxic to fibroblasts or osteoblasts at target concentrations for local delivery? And (2) if cytotoxic, can fibroblasts or osteoblasts resume proliferation after voriconazole is removed?

Methods: We exposed 5000 fibroblasts or osteoblasts/well to voriconazole concentrations of 0, 1, 5, 10, 25, 100, 500, 1000, 5000, 10,000, and 20,000 μg/mL (n=4 wells/concentration) in 24-well plates. At 3 and 7 days, cell growth was assessed with alamarBlue® and light microscopy. After Day 7, exposure to voriconazole was stopped and incubation continued for 4 days in medium with no voriconazole. On Day 11, cell growth (recovery) was assessed with alamarBlue® and light microscopy.

Results: Increasing voriconazole concentration to more than 100 μg/mL decreased osteoblast and fibroblast growth. Cell growth recovered after 7 days' exposure to 1000 μg/mL or less.

Conclusions: Voriconazole is cytotoxic to osteoblasts and fibroblasts, but cell growth recovers over 4 days after exposure to 1000 μg/mL or less.

Clinical relevance: Cytotoxicity seen from voriconazole to mouse osteoblasts and fibroblasts occurs at concentrations achievable clinically from local delivery. It may be prudent to limit the dose of voriconazole in antibiotic-loaded bone cement.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antifungal Agents / administration & dosage*
  • Antifungal Agents / therapeutic use
  • Cell Line
  • Cell Proliferation / drug effects*
  • Cell Survival / drug effects*
  • Fibroblasts / drug effects*
  • Mice
  • Mycoses / drug therapy
  • Osteoblasts / drug effects*
  • Pilot Projects
  • Pyrimidines / administration & dosage*
  • Pyrimidines / therapeutic use
  • Triazoles / administration & dosage*
  • Triazoles / therapeutic use
  • Voriconazole

Substances

  • Antifungal Agents
  • Pyrimidines
  • Triazoles
  • Voriconazole