F. Scaglione et al., A NEW MODEL EXAMINING INTRACELLULAR AND EXTRACELLULAR ACTIVITY OF AMOXICILLIN, AZITHROMYCIN, AND CLARITHROMYCIN IN INFECTED-CELLS, Chemotherapy, 39(6), 1993, pp. 416-423
An in vitro infection model was created using a suspension of macropha
ges, polymorphonuclear leukocytes, lymphocytes, fibroblasts, and human
serum to which pathogen and antibiotic were added. Separate intracell
ular and extracellular antibiotic concentrations and activity against
Staphylococcus aureus and Legionella pneumophila were assessed for thr
ee antimicrobial agents: amoxicillin, azithromycin and clarithromycin.
Amoxicillin was found almost exclusively in extracellular fluid, wher
e it was active; intracellularly, it was ineffective. Azithromycin, in
contrast, was primarily concentrated and active intracellularly, with
little activity in extracellular fluid. Clarithromycin was present in
both compartments and possessed significant activity both intracellul
arly and extracellularly.