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Antibiotic accumulation in human polymorphonuclear leucocytes and lymphocytes.
Scandinavian Journal of Infectious Diseases. Supplementum
|January 1, 1985
Summary
Human immune cells accumulate certain antibiotics like doxycycline and erythromycin, but not beta-lactams or gentamicin. This cellular uptake and retention varies, impacting drug distribution in the body.
Area of Science:
- Pharmacology
- Cell Biology
- Infectious Diseases
Background:
- Understanding how antibiotics interact with human immune cells is crucial for optimizing antimicrobial therapy.
- Polymorphonuclear leukocytes and lymphocytes play key roles in host defense against infections.
Purpose of the Study:
- To investigate the cellular accumulation and retention of various radiolabeled antibiotics in human immune cells.
- To compare the uptake and release characteristics of different antibiotic classes.
Main Methods:
- Human polymorphonuclear leukocytes and lymphocytes were incubated with 10 different radiolabeled antibiotics (10 µg/ml) for 2 hours.
- Cellular and extracellular drug concentrations were determined using centrifugation.
- Drug release from cells into antibiotic-free medium was assessed.
Main Results:
- Beta-lactam antibiotics and gentamicin showed low cellular-to-extracellular concentration ratios (<1.0).
- Doxycycline, erythromycin, fusidic acid, and rifampicin exhibited significant cellular accumulation (ratios 13, 4.3, 7-10, and 2.5, respectively).
- Erythromycin, fusidic acid, and rifampicin were rapidly released, while doxycycline showed partial irreversible binding.
Conclusions:
- Certain antibiotics, notably doxycycline, accumulate within human immune cells.
- The differential cellular uptake and retention of antibiotics may influence their efficacy and pharmacokinetic profiles.
- Further research is needed to elucidate the clinical implications of antibiotic-cell interactions.