Acta Pharm. 53 (2003) 241-250

5-Fluorouracil in topical liposome gels for anticancer treatment - Formulation and evaluation

MARIJA GLAVAS-DODOV,^1* EMILIJA FREDRO-KUMBARADZI,¹  KATERINA GORACINOVA,¹
SEMA CALIS,²  MAJA SIMONOSKA¹  and ATILA A. HINCAL²

mglavasdodov@yahoo.com

¹Department of Pharmaceutical Technology, Faculty of Pharmacy, University "Ss Cyril and Methodious", Skopje, Macedonia
²Department of Pharmaceutical Technology, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey

Liposome gels, bearing an antineoplastic agent 5-fluorouracil, intended for topical application have been prepared and drug release properties in vitro have been evaluated. Different formulations of liposomes were prepared by the film hydration method by varying the lipid phase composition (PL 90H/cholesterol mass ratio) and hydration conditions of dry lipid film (drug/aqueous phase mass ratio). Topical liposome gels were prepared by incorporation of lyophilized liposomes into a structured vehicle (1%, m/m, chitosan gel base). Also, hydrogels containing different concentrations of 5-fluorouracil were prepared and drug release properties were investigated. The rate of drug release from liposome gels was found to be dependent of the bilayer composition and of hydration conditions of dry lipid film. Also, liposomes embedded into a structured vehicle of chitosan showed significantly slower release than hydrogels. The drug release obeyed the Higuchi diffusion model, while liposomes act as reservoir systems for continuous delivery of encapsulated drug.

Keywords: liposomes, 5-fluorouracil, chitosan gel, drug release