Tropical Journal of Pharmaceutical Research
Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, Nigeria
Vol. 15, No. 11, 2016, pp. 2311-2319
Bioline Code: pr16305
Full paper language: English
Document type: Research Article
Document available free of charge
Tropical Journal of Pharmaceutical Research, Vol. 15, No. 11, 2016, pp. 2311-2319
© Copyright 2016 - Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, 300001 Nigeria.
Topical nano-delivery of 5-fluorouracil: Preparation and characterization of water-in-oil nanoemulsion|
Siddalingam, Rajinikanth & Chidambaram, Kumarappan
Purpose: To prepare and characterize a water-in-oil nanoemulsion of 5-fluorouracil (5FU) for enhanced
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/cm2) than for control (121.42 μg/cm2). 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
Nanoemulsion; Controlled release; 5-Fluorouracil; Skin penetration; Skin irritation
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