Sustained release of liposome-encapsulated enrofloxacin after intramuscular administration in rabbits

Ana Cabanes From the Department of Peptides, CID, CSIC Jordi Girona 18-26, 08034 Barcelona (Cabanes, Reig, Garcia Antón), and Unitat de Farmacologia i Toxicologia, Facultat de Veterinària, Universitat Autònoma de Barcelona, 08193 Bellaterra (Arboix), Spain.

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Francesca Reig From the Department of Peptides, CID, CSIC Jordi Girona 18-26, 08034 Barcelona (Cabanes, Reig, Garcia Antón), and Unitat de Farmacologia i Toxicologia, Facultat de Veterinària, Universitat Autònoma de Barcelona, 08193 Bellaterra (Arboix), Spain.

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José M. Garcia Antón From the Department of Peptides, CID, CSIC Jordi Girona 18-26, 08034 Barcelona (Cabanes, Reig, Garcia Antón), and Unitat de Farmacologia i Toxicologia, Facultat de Veterinària, Universitat Autònoma de Barcelona, 08193 Bellaterra (Arboix), Spain.

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Margarida Arboix From the Department of Peptides, CID, CSIC Jordi Girona 18-26, 08034 Barcelona (Cabanes, Reig, Garcia Antón), and Unitat de Farmacologia i Toxicologia, Facultat de Veterinària, Universitat Autònoma de Barcelona, 08193 Bellaterra (Arboix), Spain.

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SUMMARY

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 (0.5 ± 0.1 µg/ml), and the time to peak concentration was considerably longer for liposome-encapsulated enrofloxacin (1.5 ± 1.08 hours) than for unencapsulated drug. Apparent elimination half-life of drug in the body was significantly (P < 0.05) increased (4.05 ± 1.08 hours) when it was administered encapsulated in liposomes. Large-size liposomes containing enrofloxacin administered im to rabbits gave sustained drug release from the injection site, providing therapeutic and prolonged plasma concentrations of drug in the body.

SUMMARY

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 (0.5 ± 0.1 µg/ml), and the time to peak concentration was considerably longer for liposome-encapsulated enrofloxacin (1.5 ± 1.08 hours) than for unencapsulated drug. Apparent elimination half-life of drug in the body was significantly (P < 0.05) increased (4.05 ± 1.08 hours) when it was administered encapsulated in liposomes. Large-size liposomes containing enrofloxacin administered im to rabbits gave sustained drug release from the injection site, providing therapeutic and prolonged plasma concentrations of drug in the body.

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