Abstract
Purpose: To prepare and characterize a water-in-oil nanoemulsion of 5-fluorouracil (5FU) for enhanced skin penetration. Methods: Nanoemulsions of 5FU were prepared using Capyrol (propylene glycol monocaprylate). Transcutol (highly purified diethylene glycol monoethyl ether) and polyethylene glycol (PEG) 400 as oil, surfactant and co-surfactant, respectively. The optimized formulations were subjected to heating - cooling cycling, centrifugation and freeze - thaw cycling to assess their stability. Particle size distribution and zeta potential of the nanoemulsions were evaluated. Furthermore, in vitro and in vivo skin permeation studies were carried out on the formulations in a rat model. Skin irritation studies were also performed on rats to assess the irritation potential of the formulations. The 1 % w/v of Carbopol 934 gel loaded with 1 % 5FU was used as control (FU gel). Results: The results showed that the mean droplet size of the nanoemulsions was ~100 nm with a zeta potential of ± 15. Significant increase in permeability was also observed for the nanoemulsion formulations compared with control. The steady-state flux (Jss), enhancement ratio and permeability coefficient (Kp) for optimized nanoemulsion formulation were significantly (p < 0.05) higher than those of the conventional gel (control). Both in vitro and in vivo skin retention results indicate higher drug release from the nanoemulsion (292.45 μg/cm 2 ) than for control (121.42 μg/cm 2 ). Mean irritation index for the nanoemulsion was significantly lower than for control. Conclusion: The results suggest that a water-in-oil nanoemulsion is safe and can potentially be used to promote skin penetration of 5FU following topical application on the skin for the treatment of some skin diseases. Keywords: Nanoemulsion, Controlled release, 5-Fluorouracil, Skin penetration, Skin irritation
Highlights
5-Fluorouracil (5FU) is an antineoplastic agent used for the treatment of skin diseases such as psoriasis, cutaneous premalignant, malignant lesions and basal-cell carcinoma [1]
The present study describes the potential of nanoemulsion systems for topical delivery of 5FU that achieve the goal of increased skin permeation without the use of additional permeation enhancers
From each phase diagram constructed, different points were selected from nanoemulsion region for incorporation surfactant, co-surfactant and oil. 1 % (w/w) of FU was dissolved in aqueous phase of all selected nanoemulsion formulation
Summary
5-Fluorouracil (5FU) is an antineoplastic agent used for the treatment of skin diseases such as psoriasis, cutaneous premalignant, malignant lesions and basal-cell carcinoma [1]. One of the most promising formulation for enhancement of skin permeation of drugs is nanoemulsion [4]. An improved 5FU nanoemulsion formulation with a high degree of permeation could be useful in the treatment various skin diseases. The present study describes the potential of nanoemulsion systems for topical delivery of 5FU that achieve the goal of increased skin permeation without the use of additional permeation enhancers. From each phase diagram constructed, different points were selected from nanoemulsion region for incorporation surfactant, co-surfactant and oil. Prepared nanoemulsion FU2, placebo formulation (control), 5 % SLS and plain carbopol gel containing 1 % 5FU (plain gel) were applied to the dorsal surface (3 cm2) of each group of mice after removal of its hair by clipping. Differences were considered statistically significant at p < 0.05
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