Serotonergic-based therapies to decrease the impact of moderate to severe psoriasis: translation of fundamental research into industry

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The Use of Topical Emulsions containing Serotonergic Drugs to Modulate Skin Inflammation

Publication . Fonseca, Marta Pereira Torres Lopes da; Marto, Joana; Ribeiro, Helena

Psoriasis is a chronic, immune, and inflammatory skin disease characterized by the appearance of localized or generalized erythematous plaques on the skin. Currently there are several treatments, however, the use of topical treatments is often a challenge due to several factors such as the low rate of penetration of the drug into the skin, the necessary complementation with other treatments and the low adherence by patients. In this sense, this dissertation focused on the development of a topical treatment, namely the development of an oil-in-water (O/W) emulsion with physical-chemical and sensory characteristics appealing to the consumer and capable of performing the desired therapeutic function through the incorporation of antidepressant drugs of the selective serotonin reuptake inhibitor (ISRS) type. Thus, after pre-formulation studies, O/W emulsions prepared by a cold emulsification process were developed, optimized, and characterized. Different solvents were studied as well as the influence of different preservatives in the final properties of the O/W emulsions. The developed emulsions were characterized and selected through rheological tests, droplet size distribution tests and microscopy analysis. After the development of the emulsion (placebo), in vitro and in vivo tests were performed for the selection of the drug to be incorporated. Antidepressants drugs, such as, fluvoxamine maleate, escitalopram oxalate and sertraline hydrochloride were studied, and fluvoxamine maleate was selected because it presents more promising results in the improvement of psoriatic symptoms. The incorporation of fluvoxamine maleate led physical instability of the selected emulsion. Thus, it was necessary to change the composition of the emulsion until reaching physical stability, incorporating the HPMC polymer and replacing the agent thickening with Sepineo™ P 600. The physicochemical characterization of the final emulsion with or without fluvoxamine maleate, as well as the rheological behaviour and the microstructure analysis were part of the study. Both formulations present suitable topical physicochemical properties. In vivo biological efficacy (hydration, TEWL and moisture evaluation) and sensorial analysis were performed on placebo final emulsion. The application of placebo for 28 days improved the hydration and the skin barrier, and the results of sensorial analysis confirmed a good consumer acceptability. In conclusion, it was possible to develop an O/W emulsion containing an antidepressant drug, with the desired and appealing characteristics for possible consumers and with promising biological and therapeutic efficacy.

2021-02-01Dissertação de mestrado

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Entidade financiadora

Fundação para a Ciência e a Tecnologia

Programa de financiamento

3599-PPCDT

Número da atribuição

PTDC/MEC-DER/30198/2017