<b>Encapsulation of 5-fluorouracil in liposomes for topical administration</b> - DOI: 10.4025/actascitechnol.v25i1.2240

Abstract

This work aims to compare different methodologies for the preparation of dipalmitoylphosphatidylcholine/cholesterol (DPPC/Chol) liposomes entrapping the anticancer agent 5-fluorouracil (5-FU), a drug usually employed in melanoma therapy, designed for topical administration. The lipid vesicles were produced by dry lipid film hydration followed by extrusion, by ethanol injection and by reverse phase evaporation, while 5-FU was passively or actively incorporated into the liposomes. The results demonstrated that vesicle loading and stability can be controlled by the experimental procedure used to entrap the drug. Different initial drug to lipid molar ratios strongly affect encapsulation efficiency. The reverse-phase evaporation method resulted in the largest 5-FU encapsulation efficiency, around 6%. The preparation of these vesicles did not result in detectable drug degradation. During 4 weeks, no aggregation of liposomes was observed, however, extensive drug leakage from the vesicles was noticed.