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© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.

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.

Details

Title
Biopharmaceutical Development of a Bifonazole Multiple Emulsion for Enhanced Epidermal Delivery
Author
Suñer-Carbó, Joaquim 1 ; Calpena-Campmany, Ana 1   VIAFID ORCID Logo  ; Halbaut-Bellowa, Lyda 1 ; Clares-Naveros, Beatriz 2   VIAFID ORCID Logo  ; Rodriguez-Lagunas, María José 3   VIAFID ORCID Logo  ; Barbolini, Elena 4 ; Zamarbide-Losada, Joanna 4 ; Boix-Montañés, Antonio 1   VIAFID ORCID Logo 

 Department of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Av. Joan XXIII s/n, 08028 Barcelona, Spain; Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, Diagonal 645, 08028 Barcelona, Spain 
 Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, Diagonal 645, 08028 Barcelona, Spain; Department of Pharmacy and Pharmaceutical Technology, Faculty of Pharmacy, University of Granada, Campus de la Cartuja, s/n. 18071 Granada, Spain 
 Department of Biochemistry and Physiology, Faculty of Pharmacy and Food Sciences, University of Barcelona, Av. Joan XXIII s/n, 08028 Barcelona, Spain 
 Department of Pharmacy and Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, Av. Joan XXIII s/n, 08028 Barcelona, Spain 
First page
66
Publication year
2019
Publication date
2019
Publisher
MDPI AG
e-ISSN
19994923
Source type
Scholarly Journal
Language of publication
English
ProQuest document ID
2550227168
Copyright
© 2019 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.