Open AccessBiopharmaceutical characterization of topical liposome formulations bearing 5-fluorouracil
Author(s) -
Marija Glavaš Dodov,
Emilija Fredro-Kumbaradzi,
Sema Çalış,
Katerina Goračinova,
Kristina Mladenovska,
Maja Simonoska,
A. A. Hıncal
Publication year - 2003
Publication title -
makedonsko farmacevtski bilten/makedonski farmacevtski bilten
Language(s) - English
Resource type - Journals
eISSN - 1857-8969
pISSN - 1409-8695
DOI - 10.33320/maced.pharm.bull.2002.48.004
Subject(s) - liposome , chromatography , chemistry , drug delivery , particle size , drug , aqueous two phase system , dosage form , drug carrier , aqueous solution , vesicle , pharmacology , biochemistry , membrane , organic chemistry , medicine
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.