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Intracellular and extracellular penetration of azithromycin into inflammatory and noninflammatory blister fluid

C D Freeman1, C H Nightingale, D P Nicolau

  • 1Department of Pharmacy, Hartford Hospital, Connecticut 06115.

Antimicrobial Agents and Chemotherapy
|October 1, 1994
PubMed

Insights

Azithromycin effectively penetrates blister fluid in volunteers after a 5-day course. Significant differences were observed in drug concentrations within inflammatory and non-inflammatory blister cells.

Area of Science:

  • Pharmacology
  • Infectious Diseases
  • Clinical Research

Background:

  • Azithromycin is a widely used antibiotic.
  • Understanding drug penetration into specific tissues is crucial for optimizing treatment efficacy.
  • Blister fluid models offer a unique in vivo system to study drug distribution.

Purpose of the Study:

  • To quantify azithromycin penetration into blister fluid.
  • To compare azithromycin concentrations in different biological compartments.
  • To investigate azithromycin's presence in leukocytes within blister chambers.

Main Methods:

  • Six healthy volunteers received a 5-day regimen of azithromycin (1.5 g total).
  • Azithromycin concentrations were measured in blister fluid, serum, and paper disks.
  • The mass of azithromycin within inflammatory and non-inflammatory blister chamber leukocytes was determined.

Main Results:

  • Significant differences in azithromycin concentrations were found between paper disks and serum.
  • Significant differences in azithromycin mass were observed in inflammatory versus non-inflammatory blister chamber leukocytes (P < 0.05).

Conclusions:

  • Azithromycin demonstrates penetration into blister fluid.
  • The drug's distribution varies significantly between inflammatory and non-inflammatory cellular components within blisters.
  • These findings contribute to understanding azithromycin's pharmacokinetics in inflammatory conditions.

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