Pharmacokinetic properties and tissue concentrations of enrofloxacin and ciprofloxacin were compared after intramuscular (i.m.) administrations of free and liposome-encapsulated enrofloxacin at the dose of 5 mg/kg body weight (bw). Twelve healthy adult New Zealand white rabbits were used in the experiment. Blood samples were obtained at 10, 20, 40, 60 and 90 min and 2, 4, 6, 8 and 12 h and tissue samples were collected 24 h after injection. Concentrations of drugs in serum were determined by high-performance liquid chromatography. Pharmacokinetics were best described by a two-compartment open model. Results indicated that absorption rate was slow, peak concentration was higher (P < 0.05), and the time to peak concentration (tmax congruent with 1.5 h) was significantly longer (P < 0.05) for liposome-encapsulated enrofloxacin (LEE) when compared with free enrofloxacin. Values of elimination half-life (t1/2beta = 12.9 h) and mean residence time (MRT = 17.6 h) of liposome-encapsulated enrofloxacin were longer (P < 0.05) and total clearance (Cl = 0.43 l/h/kg) was lower than those of free form. Moreover, the distribution volume at steady-state (Vd(ss) = 14.4 l/kg) of enrofloxacin administered encapsulated into liposomes was significantly higher (P < 0.05) than that of free enrofloxacin (FE). The tissue levels of enrofloxacin and ciprofloxacin after LEE injection were not different (P > 0.05) from FE. In conclusion, the result of present study suggest that LEE may be a beneficial and valuable formulation in the treatment of infectious diseases caused by sensitive pathogens in animals, providing sustained drug release from injection side and prolonged therapeutic serum concentrations after i.m. administration.
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Dtsch Tierarztl Wochenschr
June 2005
Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Selçuk, Konya, Turkey.
The aim of this study was to evaluate the intracellular activity of two types of liposome-encapsulated enrofloxacin (LE) compared with free enrofloxacin and non-treated control against Staphylococcus aureus, phagocytosed by monocytes in healthy Anatolian Shepherd dogs. Enrofloxacin was encapsulated with two different types of liposome in multilamellar large vesicles (MLV). Type A MLV were composed of 15 mg phosphatidylcholine and 35 mg cholesterol, Type B MLV were composed of phosphatidylcholine, cholesterol and enrofloxacin in a molar ratio of 1:1:1.
View Article and Find Full Text PDFMethods Enzymol
August 2005
Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Granada, Granada, Spain.
Encapsulation of certain antibiotics in liposomes can enhance their effect against microorganisms invading cultured cells and in animal models. We describe the incorporation of amikacin, streptomycin, ciprofloxacin, sparfloxacin, and clarithromycin in a variety of liposomes. We delineate the methods used for the evaluation of their efficacy against Mycobacterium avium-intracellulare complex (MAC) infections in macrophages and in the beige mouse model of MAC disease.
View Article and Find Full Text PDFJ Vet Med B Infect Dis Vet Public Health
December 2002
Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Selcuk, Konya, Turkey.
Pharmacokinetic properties and tissue concentrations of enrofloxacin and ciprofloxacin were compared after intramuscular (i.m.) administrations of free and liposome-encapsulated enrofloxacin at the dose of 5 mg/kg body weight (bw).
View Article and Find Full Text PDFJ Vet Med B Infect Dis Vet Public Health
August 2002
Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine, University of Selçuk, Konya, Turkey.
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.
View Article and Find Full Text PDFAm J Vet Res
November 1995
Department of Peptides, CID, CSIC, Barcelona, Spain.
Enrofloxacin was encapsulated in multilamellar liposomes composed of phosphatidylcholine and cholesterol (molar ratio, 1:1), and its potential use as sustained release formulation was evaluated. The encapsulated drug was administered IM to rabbits (n = 6). Results indicated that absorption rate was slow, compared with previous studies; additionally, peak concentration was lower (0.
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