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Article in English | MEDLINE | ID: mdl-12241030

ABSTRACT

In this study, it was evaluated the accumulation of free and two types of liposome-encapsulated enrofloxacin (LEE) at the doses of 0.25, 0.5 and 1 microg/ml, which were clinically relevant concentrations into monocytes of healthy Anatolian shepherd dogs. Enrofloxacin was encapsulated with two different types of liposome in multilamellar large vesicles (MLV). Type A MLV composed of 15 mg egg phosphatidylcholine and 35 mg cholesterol, Type B MLV composed of phosphatidylcholine (PC), cholesterol and enrofloxacin, in a molar ratio of 1 : 1 : 1. The mean sizes of Type A and Type B liposome were found to be 7.65 and 4.27 microm, respectively. However, the mean encapsulation rate determined of Type A (13 +/- 2%) was found lower than Type B liposome (44 +/- 3%). The amounts of intracellular enrofloxacin concentrations were determined by high performance liquid chromatography. Type B LEE accumulated significantly higher level into monocytes when compared to free drug or Type A liposome. This study showed that Type B LEE markedly concentrated within monocytes and may improve the antibacterial efficacy of the antibiotic.


Subject(s)
Anti-Infective Agents/pharmacokinetics , Dogs/metabolism , Fluoroquinolones , Monocytes/metabolism , Quinolones/pharmacokinetics , Animals , Anti-Infective Agents/administration & dosage , Anti-Infective Agents/pharmacology , Capsules , Chemistry, Pharmaceutical , Chromatography, High Pressure Liquid , Dose-Response Relationship, Drug , Drug Carriers , Enrofloxacin , Liposomes , Male , Phosphatidylcholines , Quinolones/administration & dosage , Quinolones/pharmacology , Reference Values , Staphylococcus aureus/drug effects
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