Dataset Information

Human Skin Permeation Studies with PPAR? Agonist to Improve Its Permeability and Efficacy in Inflammatory Processes.

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.

SUBMITTER: Silva-Abreu M

PROVIDER: S-EPMC5751151 | biostudies-literature | 2017 Nov

REPOSITORIES: biostudies-literature

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Human Skin Permeation Studies with PPARγ Agonist to Improve Its Permeability and Efficacy in Inflammatory Processes.

Silva-Abreu Marcelle M Espinoza Lupe Carolina LC Rodríguez-Lagunas María José MJ Fábrega María-José MJ Fábrega María-José MJ Espina Marta M García María Luisa ML Calpena Ana Cristina AC

International journal of molecular sciences 20171128 12

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 o ...[more]

PMID: 29182532

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Project description:Dermal aging is characterized by states of oxidative stress, chronic inflammation, and abnormal proteolytic degradation due to the action of hydrogen peroxide, superoxide, 5-lipoxygenase, and elastase, respectively. Noteworthy elastase inhibition has previously been reported, and so this study aimed to investigate the ability of Myrsine africana and myrsinoside B to reduce the activity of hydrogen peroxide, superoxide, and 5-lipoxygenase as supplementary mechanisms of action by which M. africana may reduce the appearance of wrinkles. The use of maltose microneedles were also investigated as a means to enhance the delivery of myrsinoside B into the skin as this is a crucial aspect to investigate when characterizing the efficacy of an active ingredient. Myrsine africana has traditionally been used for skin allergies, boils, and to purify blood (as an astringent) and was selected for this study based on it use in skincare. The crude extract exhibited IC50's of 56.08 ± 2.88 and 132.74 ± 1.64 µg/ml against the hydrogen peroxide and superoxide radicals, while myrsinoside B exhibited IC50's of 52.19 ± 4.16 and 192.14 ± 3.52 µg/ml, respectively. The IC50 of the extract and compound against 5-lipoxygenase was 29.65 ± 2.92 and 29.33 ± 3.08 µg/ml, respectively. No toxicity was observed in vitro at the highest concentration tested. Microneedle treatment increased the permeation of the active through the skin after 24 h to 12.46 ± 5.14 µg/cm2 compared to the passive group (1.30± 0.85 µg/cm2). The amount of active retained in the epidermis and dermis was 8.97 ± 0.90 and 6.98 ± 0.73 µg/cm2 respectively, greater than the retention observed in the passive group (3.24 ± 1.41 and 3.27 ± 1.47 µg/cm2, respectively). M. africana and myrsinoside B showed promising antioxidant and anti-inflammatory activity thus supporting the potential of M. africana and myrsinoside B as anti-wrinkle agents. Further, treatment of dermatomed human skin with maltose microneedles facilitated topical delivery of myrsinoside B and provided an effective means for compound delivery to ensure maximum effect.

Dataset Information

Human Skin Permeation Studies with PPAR? Agonist to Improve Its Permeability and Efficacy in Inflammatory Processes.

Publications

Human Skin Permeation Studies with PPARγ Agonist to Improve Its Permeability and Efficacy in Inflammatory Processes.

Similar Datasets

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