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Interactions between quinolone antibiotics and phospholipid membrane for prediction of alveolar macrophage uptake in

Jin Sun1, Yoshiharu Deguchi, Ji-Min Chen

  • 1Department of Pharmaceutics, Shenyang Pharmaceutical University, Shen yang 110016, China. sunjin66@21cn.com

Acta Pharmacologica Sinica
|April 30, 2002
PubMed
Abstract

Insights

Investigating drug uptake by alveolar macrophages (AMs), this study found that liposome/buffer systems and immobilized artificial membrane (IAM) chromatography better predict drug accumulation than the n-octanol/buffer system.

Area of Science:

  • Pharmacokinetics and Drug Metabolism
  • Cellular Biology
  • Biophysical Chemistry

Background:

  • Alveolar macrophages (AMs) play a crucial role in lung immunity and drug disposition.
  • Understanding drug interactions with cellular membranes is vital for predicting pharmacokinetic behavior.
  • Quinolones, a class of antibiotics, exhibit varying membrane permeability influenced by their physicochemical properties.

Purpose of the Study:

  • To evaluate different membrane-mimicking systems for predicting alveolar macrophage (AM) drug uptake.
  • To compare the effectiveness of immobilized artificial membrane (IAM) chromatography, liposome/buffer systems, and n-octanol/buffer systems in assessing drug-membrane interactions.
  • To determine the primary mechanism of drug transport across the AM membrane.

Main Methods:

  • Isolated AMs were cultured and incubated with quinolone drugs.
  • Drug uptake was quantified by measuring drug and protein concentrations post-incubation.
  • Lipophilicity was assessed using IAM chromatography (lg k(IAM)), a liposome/buffer system (lg D(L/B,7.4)), and an n-octanol/buffer system (lg D(O/B,7.4)).

Main Results:

  • IAM chromatography and the liposome/buffer system showed highly correlated lipophilicity measurements (r² = 0.93).
  • Both lg k(IAM) and lg D(L/B,7.4) significantly correlated with AM drug accumulation (r² = 0.89 and 0.92, respectively), outperforming lg D(O/B,7.4) (r² = 0.67).
  • Correlations for influx rate into AMs were comparable across the three systems for amphoteric quinolones and quinidine.

Conclusions:

  • Liposome/buffer and IAM chromatography provide comparable and distinct lipophilicity measurements compared to the n-octanol/buffer system.
  • AM drug accumulation is better predicted by lg k(IAM) or lg D(L/B,7.4), indicating their utility in pharmacokinetic modeling.
  • Passive diffusion is the predominant mechanism for drug transport across the AM membrane.

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