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Intracellular penetration and activity of gemifloxacin in human polymorphonuclear leukocytes

I García1, A Pascual, S Ballesta

  • 1Department of Microbiology, School of Medicine, University of Seville, Seville 41009, Spain.

Antimicrobial Agents and Chemotherapy
|October 19, 2000
PubMed

Insights

Gemifloxacin effectively penetrates human immune cells (PMN), reaching high intracellular levels. This antibiotic demonstrates potent activity against Staphylococcus aureus within these cells at therapeutic concentrations.

Area of Science:

  • Pharmacology
  • Microbiology
  • Cell Biology

Background:

  • Understanding antibiotic penetration into immune cells is crucial for treating intracellular bacterial infections.
  • Polymorphonuclear leukocytes (PMN) play a key role in host defense against bacteria like Staphylococcus aureus.

Purpose of the Study:

  • To evaluate the intracellular penetration and activity of gemifloxacin in human PMN.
  • To determine the factors influencing gemifloxacin uptake by PMN.

Main Methods:

  • Measurement of intracellular and extracellular gemifloxacin concentrations in human PMN.
  • Assessment of gemifloxacin's effect on intracellular Staphylococcus aureus.
  • Investigation of uptake kinetics and influencing factors (temperature, cell viability, membrane stimuli).

Main Results:

  • Gemifloxacin achieved intracellular concentrations eight times higher than extracellular levels.
  • Uptake was rapid, reversible, and nonsaturable, influenced by temperature, cell viability, and membrane stimuli.
  • Gemifloxacin exhibited intracellular activity against Staphylococcus aureus at therapeutic concentrations.

Conclusions:

  • Gemifloxacin demonstrates significant intracellular penetration into human PMN.
  • The drug maintains intracellular activity against Staphylococcus aureus, suggesting potential efficacy in treating infections involving these cells.

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