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Title: Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery
Author: Suñer Carbó, J. (Joaquim)
Calpena Campmany, Ana Cristina
Halbaut, Lyda
Clares Naveros, Beatriz
Rodríguez Lagunas, María José
Barbolini, Elena
Zamarbide Losada, Joanna
Boix Montañés, Antonio de Pádua
Keywords: Emulsions (Farmàcia)
Agents tensioactius
Emulsions (Pharmacy)
Surface active agents
Issue Date: 2-Feb-2019
Publisher: MDPI
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.
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It is part of: Pharmaceutics, 2019, vol. 11, num. 2, p. 66
Related resource:
ISSN: 1999-4923
Appears in Collections:Articles publicats en revistes (Bioquímica i Fisiologia)
Articles publicats en revistes (Farmàcia, Tecnologia Farmacèutica i Fisicoquímica)

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