Biopharmaceutical characterization of topical liposome formulations bearing 5-fluorouracil

Autor: Marija Glavas-Dodov, Emilija Fredro-Kumbaradzi, Sema Calis, Katerina Goracinova, Kristina Mladenovska, Maja Simonoska, Atila A. Hincal
Jazyk: angličtina
Rok vydání: 2003
Předmět:
Zdroj: Makedonsko Farmacevtski Bilten, Vol 48, Iss (1, 2), Pp 21-24 (2003)
Druh dokumentu: article
ISSN: 1409-8695
1857-8969
Popis: Liposome dispersions and liposome gel formulations for topical administration were evaluated as modified release delivery systems for 5-fluorouracil. Drug substance has been entrapped in the internal aqueous compartment of liposomes during the preparation. The concentration of 5-fluorouracil in the hydration medium was varied and the effect on the liposome characteristics was considered. Liposome gel formulations were prepared by incorporation of liophylized liposomes into a structured vehicle of chitosan. The decrease of the amount of aqueous phase bearing total drug quantity (drug/aqueous phase ratio from 1:100, 1:60, 1:40) led to an increase of the percentage of liposome-entrapped drug, and decreased percentage of drug release, while particle size analysis showed no changes in vesicle size. Liposome gel formulations showed initially a higher drug release rate in comparision with liposome dispersions, which could be related to the release of “free” 5-fluorouracil, leaked from liposomes due to the process of liophylization. This was followed by slower release (after 1.5 hour) as a result of the influence of the viscosity of the gel matrix.
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