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Harvesting Murine Alveolar Macrophages and Evaluating Cellular Activation Induced by Polyanhydride Nanoparticles
Published on: June 8, 2012
In vitro uptake of SCH 27899 (evernimicin) by rat alveolar macrophages
S Zbaida1, J Brieland, P Krieter
1Department of Drug Metabolism and Pharmacokinetics, Schering-Plough Research Institute, Kenilworth, New Jersey 07033-1300, USA. shmuel.zbaida@spcorp.com
Abstract:
The in vitro uptake of [(14)C]evernimicin ([(14)C]SCH 27899) by primary cultures of rat alveolar macrophages and hepatocytes was determined. Both cell populations exhibited linear rates of uptake. However, the initial rate of drug uptake by alveolar macrophages was about threefold higher than that by hepatocytes. These findings demonstrate that [(14)C]evernimicin is taken up by rat alveolar macrophages, supporting the likelihood that the drug is able to reach sites of infection.
Insights
[(14)C]evernimicin uptake was studied in rat cells. Alveolar macrophages showed higher drug absorption than hepatocytes, suggesting the antibiotic can reach infection sites.
Area of Science:
- Pharmacology
- Cell Biology
- Drug Metabolism
Background:
- Evernimicin is an antibiotic with potential therapeutic applications.
- Understanding drug uptake is crucial for determining efficacy and distribution.
- Alveolar macrophages and hepatocytes are key cell types involved in drug disposition.
Purpose of the Study:
- To investigate the in vitro uptake of [(14)C]evernimicin by primary cultures of rat alveolar macrophages and hepatocytes.
- To compare the rates of [(14)C]evernimicin uptake between these two cell types.
Main Methods:
- Primary cultures of rat alveolar macrophages and hepatocytes were established.
- The in vitro uptake of radiolabeled [(14)C]evernimicin ([(14)C]SCH 27899) was measured in both cell populations.
- Uptake rates were analyzed to determine linearity and compare initial rates.
Main Results:
- Both alveolar macrophages and hepatocytes exhibited linear rates of [(14)C]evernimicin uptake over time.
- The initial rate of [(14)C]evernimicin uptake by alveolar macrophages was approximately threefold higher compared to hepatocytes.
- These findings indicate significant cellular absorption of the drug by macrophages.
Conclusions:
- [(14)C]evernimicin is effectively taken up by rat alveolar macrophages in vitro.
- The higher uptake rate in macrophages supports the potential for evernimicin to reach infection sites, particularly those involving macrophage-rich tissues.
- This cellular uptake characteristic is a positive indicator for the in vivo efficacy of evernimicin.
