Skin delivery of 5-fluorouracil from ultradeformable and standard liposomes in-vitro

Abstract

The potential use of ultradeformable and standard liposomes as skin drug delivery systems was investigated in-vitro. An improved experimental design gave a good measure for skin deposition of drug. This avoided the contamination that can occur due to incomplete washing of the donor before direct determination of the amount of drug in the skin. The design used aqueous ethanolic receptor which is believed to diffuse into skin, disrupting deposited liposomes (if any) and thus releasing both bound and free drug. The receptor fluid was refined by testing different concentrations of ethanol. The applied dose was also optimized. Using the improved design and the optimum dose, an ultradeformable formulation was compared with four traditional liposomes for skin delivery of 5-fluorouracil (5-FU). The best receptor was 50% aqueous ethanol and the optimum dose was 20 microL. The ultradeformable formulation was superior to standard liposomes in the skin delivery of 5-FU. Of the traditional liposomes, the non-rigid preparation was the best. However, stabilization of the liposome membrane with cholesterol abolished the benefit of this non-rigid preparation. It was concluded that ultradeformable vesicles are promising agents for skin delivery of drugs.

Optimized permeation enhancer for topical delivery of 5-fluorouracil-loaded elastic liposome using Design Expert: part II

“…Enhanced drug deposition and reduced systemic availability for reduced systemic side effects of 5-FU were investigated earlier using conventional liposome and deformable liposome without permeation enhancer after topical application (El Maghraby et al, 2001). The authors reported improved permeation of 5-FU through the human SC using deformable liposome composed of PC and sodium cholate.…”

Preparation of Curcumin-Loaded Liposomes and Evaluation of Their Skin Permeation and Pharmacodynamics

“…The mini-column centrifugation method was used to assay entrapment efficiency [24]. Sephadex G50 was chosen, swollen in distilled water for at least 12 h and stored at 4 °C.…”

Potential of Diallyl Sulfide Bearing pH-Sensitive Liposomes in Chemoprevention Against DMBA-Induced Skin Papilloma

“…This clearly suggests that liposomization offers a new and effective option to increase the chemo-preventive and anticarcinogenic potential of DAS in cancer therapy. The increased efficacy of liposomized DAS could be attributed to the fact that liposomes act as a sustained release system allowing greater accumulation of drug molecules at the tumor site than that achieved by its free form (29,38,39,40).…”