Determination of intracellular concentrations of free and two types of liposome-encapsulated enrofloxacin in anatolian shepherd dog monocytes.
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.
Baş
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Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Selçuk, Konya, Turkey. alevent@selcuk.edu.tr
Simşek
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A
Corlu
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Yazar
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Elmas
M
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Değim
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ZG
D000818:Animals; D000890:Anti-Infective Agents / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D002214:Capsules; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid; D004285:Dogs / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D004337:Drug Carriers; D000077422:Enrofloxacin; D024841:Fluoroquinolones; D008081:Liposomes; D008297:Male; D009000:Monocytes / Q000378:metabolism*; D010713:Phosphatidylcholines; D015363:Quinolones / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000494:pharmacology; D012016:Reference Values; D013211:Staphylococcus aureus / Q000187:drug effects
D000890:Anti-Infective Agents; D002214:Capsules; D004337:Drug Carriers; D024841:Fluoroquinolones; D008081:Liposomes; D010713:Phosphatidylcholines; D015363:Quinolones; D000077422:Enrofloxacin