Abstract
Rosacea is the most common inflammatory skin disease. It is characterized by erythema, inflammatory papules and pustules, visible blood vessels, and telangiectasia. The current treatment has limitations and unsatisfactory results. Pioglitazone (PGZ) is an agonist of peroxisome proliferator-activated receptors (PPARs), a nuclear receptor that regulates important cellular functions, including inflammatory responses. The purpose of this study was to evaluate the permeation of PGZ with a selection of penetration enhancers and to analyze its effectiveness for treating rosacea. The high-performance liquid chromatography (HPLC) method was validated for the quantitative determination of PGZ. Ex vivo permeation experiments were realized in Franz diffusion cells using human skin, in which PGZ with different penetration enhancers were assayed. The results showed that the limonene was the most effective penetration enhancer that promotes the permeation of PGZ through the skin. The cytotoxicity studies and the Draize test detected cell viability and the absence of skin irritation, respectively. The determination of the skin color using a skin colorimetric probe and the results of histopathological studies confirmed the ability of PGZ-limonene to reduce erythema and vasodilation. This study suggests new pharmacological indications of PGZ and its possible application in the treatment of skin diseases, namely rosacea.
Highlights
Rosacea is a chronic inflammatory disease of the skin [1,2,3]
After having taken into consideration the role of peroxisome proliferator-activated receptors (PPARs)-γ as an important immunomodulator with anti-inflammatory properties, the aim of this study was to evaluate the efficacy of the PGZ solution with a selection of penetration enhancers to improve its permeability for treating rosacea using an in vivo model
Data are expressed as percentage of coefficient of variation (CV) and precision of method
Summary
The clinical features appear principally in the central region of the face and include the presence of facial erythema, inflammatory papules and pustules, telangiectasia, and edema [4,5,6] It predominantly affects women and fair-skinned people and can occur at any age but is more frequent in middle-aged individuals [7,8]. The estimated prevalence of rosacea among the population of Europe and United States has a wide range from less than 1% to more than 20%, likely due to differences in the methods used and the populations studied [9,10] It has been associated with several comorbidities such as depression and anxiety [11,12], dyslipidemia, hypertension, cardiovascular diseases, and metabolic diseases [13,14,15]. The characterization of inflammatory infiltrate in this disease has revealed the activation of T lymphocytes, T-helper 1 (Th1) and T-helper 17 (Th17) cells, as well as the presence of macrophages and mast cells, which mediate the inflammatory reactions and development of the disease [21,22]
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