@misc{10481/54886,
year = {2019},
month = {2},
url = {http://hdl.handle.net/10481/54886},
abstract = {Efficient topical delivery of imidazolic antifungals faces the challenge of overcoming
its limited water solubility and its required long-lasting duration of treatments. In this paper,
a hydrophilic multiple emulsion (ME) of Bifonazole (BFZ) is shown to maximize its skin retention,
minimize its skin permeation, and maintain an acceptable level of being harmless in vivo.
The formulations were pharmaceutically characterized and application properties were assessed
based on viscosity measurements. Non-Newtonian pseudoplastic shear thinning with apparent
thixotropy was observed, facilitating the formulation retention over the skin. The in vitro release
profile with vertical diffusion cells showed a predominant square-root release kinetic suggesting
an infinite dose depletion from the formulation. Ex vivo human skin permeation and penetration
was additionally evaluated. Respective skin permeation was lower than values obtained with
a commercial O/W formulation. The combination of amphoteric and non-ionic surfactants increased
the bifonazole epidermal accumulation by a factor of twenty. This fact makes the possibility
of increasing its current 24 h administration frequency more likely. Eventual alterations of skin
integrity caused by the formulations were examined with epidermal histological analysis and in vivo
preclinical measurements of skin elasticity and water retrograde permeation. Histological analysis
demonstrated that the multiple emulsions were harmless. Additionally, modifications of in vivo skin
integrity descriptors were considered as negligible.},
organization = {There are no specific funding sources or universitary fellowship for this experimental work.
Article processing charges were partially supported by University of Barcelona.},
publisher = {MDPI},
keywords = {Multiple emulsion},
keywords = {Bifonazole},
keywords = {Pseudoplastic},
keywords = {Drug release},
keywords = {Skin penetration},
keywords = {Skin permeation},
keywords = {Skin integrity},
keywords = {TEWL},
keywords = {Epidermal histology},
title = {Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery},
doi = {10.3390/pharmaceutics11020066},
author = {Suñer-Carbó, Joaquim and Calpena-Campmany, Ana and Halbaut-Bellowa, Lyda and Clares Naveros, Beatriz and Rodriguez-Lagunas, María José and Barbolini, Elena and Zamarbide-Losada, Joanna and Boix-Montañés, Antonio},
}