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Tuning the Transdermal Delivery of Hydroquinone upon Formulation with Novel Permeation Enhancers

1
Department of Pharmaceutics and Food Technology, School of Pharmacy, Complutense University of Madrid, Ramón y Cajal square, 28040 Madrid, Spain
2
University Institute of Industrial Pharmacy, Complutense University, 28040 Madrid, Spain
3
Department of Medicine and Medical Specialties, Alcalá University, 28040 Madrid, Spain
4
School of Pharmacy and Biomedical Sciences, University of Portsmouth, St. Michael’s Building, White Swan Road, Portsmouth PO1 2DT, UK
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2019, 11(4), 167; https://doi.org/10.3390/pharmaceutics11040167
Received: 7 March 2019 / Revised: 29 March 2019 / Accepted: 31 March 2019 / Published: 4 April 2019
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Abstract

Hydroquinone (HQ) is an anti-hyperpigmentation agent with poor physicochemical stability. HQ formulations are currently elaborated by compounding in local pharmacies. Variability in the characteristics of HQ topical formulations can lead to remarkable differences in terms of their stability, efficacy, and toxicity. Four different semisolid O/W formulations with 5% HQ were prepared using: (i) Beeler´s base plus antioxidants (F1), (ii) Beeler´s base and dimethyl isosorbide (DMI) as solubiliser (F2), (iii) olive oil and DMI (F3), and (iv) Nourivan®, a skin-moisturising and antioxidant base, along with DMI (F4). Amongst the four formulations, F3 showed the greatest physicochemical stability with less tendency to coalescence but with marked chromatic aberrations. An inverse correlation was established by multivariate analysis between the mean droplet size in volume and the steady-state flux, which explains why F3, with the smallest droplet size and the most hydrophobic excipients, exhibited the highest permeation across both types of membranes with enhancement ratios of 2.26 and 5.67-fold across Strat-M® and mouse skin, respectively, compared to F1. It is crucial to understand how the HQ is formulated, bearing in mind that the use of different excipients can tune the transdermal delivery of HQ significantly. View Full-Text
Keywords: hydroquinone; transdermal delivery; Franz cells; permeability enhancers; stability; multivariate analysis hydroquinone; transdermal delivery; Franz cells; permeability enhancers; stability; multivariate analysis
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Serrano, D.R.; Gordo, M.J.; Matji, A.; González, S.; Lalatsa, A.; Torrado, J.J. Tuning the Transdermal Delivery of Hydroquinone upon Formulation with Novel Permeation Enhancers. Pharmaceutics 2019, 11, 167.

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