Estudo de segurança e eficácia in vitro do ácido p-Cumárico e sua incorporação em emulsão cosmética óleo em água (O/A)
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Data
2019-04-01
Autores
Ramos, Wagner Soares
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Editor
Universidade Estadual Paulista (Unesp)
Resumo
O ácido p-cumárico (APC) é um composto fenólico não flavonóide que apresenta segurança e eficácia bem descritas na ciência dos alimentos devido suas propriedades antioxidante, antitumoral, anti-inflamatória, antimicrobiana e por apresentar baixa toxicidade oral. Essas propriedades são pouco exploradas em produtos para cuidados com a pele. O objetivo do presente estudo foi avaliar de forma in vitro a segurança e a eficácia do APC e incorporá-lo em emulsão cosmética óleo em água (O/A). Nossos estudos in vitro e alternativos ao uso de animais foram conduzidos para verificar a citotoxicidade do APC em células de queratinócitos (HaCat) e fibroblastos humanos (HDFa), o potencial de irritação ocular (HET-CAM) e a atividade antimicrobiana em diferentes cepas. Emulsões contendo APC foram submetidas ao estudo de estabilidade e de liberação, retenção e permeação cutâneas. Resultados: o IC50 do APC em células HaCat e HDFa foi 693,57 e 2.814,75 μg/mL, respectivamente. Além disso 100 μg de APC foram levemente tóxicos em membrana corioalantóica de ovo embrionado. As concentrações bactericidas mínimas em cepas de E. coli, S. aureus, P. aeruginosa e S. epidermidis, foram 3.000 μg/mL, 1.875 μg/mL, 3.750 μg/mL e 3.750 μg/mL, respectivamente. Emulsões contendo diferentes concentrações de APC foram estáveis durante o período de estabilidade acelerada. Após 12 horas 91,08 ± 0,03% do APC foi liberado da formulação e após 24 horas, 0,52 ± 0,18% e 0,94 ± 0,37% ficaram retidos no estrato córneo e na epiderme/derme, respectivamente. Nossos resultados indicam que as concentrações de APC estudadas podem ser eficazes e seguras para uso em cosméticos, incluindo aqueles para uso na região dos olhos, ainda que estudos complementares sejam necessários.
p-Coumaric acid (PCA) is a non flavonoid phenolic compound whose safety and efficacy widely described in food science papers due to antioxidant, antitumor, anti inflammatory properties, and low oral toxicity. These characteristics are poorly or no described when PCA is added to skin care products. The aim of the present study was to evaluate the safety and efficacy of PCA through in vitro assays, and then add it in oil in water cosmetic emulsion (O/W). Our in vitro trials, without animal use were conducted to predict PCA´s cytotoxicity in HaCat and HDFa cells, ophthalmic irritation potential, and antibacterial activity against differents strains. Emulsions with PCA has been tested to predict shelf life, dermal absorption, and dermal retention. Results: PCA´s IC50 in HaCat and HDFa cells was 693.57 and 2,814.75 μg.mL-1, respectively. In addition 100 μg of APC were slightly toxic in chorioallantoic membrane assay. The minimum bactericidal concentrations against E. coli, S. aureus, P. aeruginosa and S. epidermidis strains were 3,000 μg.mL-1, 1,875 μg.mL-1, 3,750 μg.mL-1, and 3,750 μg.mL-1 , respectively. Emulsions containing 0.04%, 0.06%, 0.08% and 0.10% of PCA were stable during self life testing for ninety days. After 12 hours 91.08 ± 0.03% of PCA was released of the emultion, and after 24 hours 0.52 ± 0.18% and 0.94 ± 0.37%, were present in stratum corneum and epidermis/dermis, respectively. Our findings indicate that PCA concentrations would be effective and safe to use in cosmetic products, even eye cosmetics, although complementary assays are necessary.
p-Coumaric acid (PCA) is a non flavonoid phenolic compound whose safety and efficacy widely described in food science papers due to antioxidant, antitumor, anti inflammatory properties, and low oral toxicity. These characteristics are poorly or no described when PCA is added to skin care products. The aim of the present study was to evaluate the safety and efficacy of PCA through in vitro assays, and then add it in oil in water cosmetic emulsion (O/W). Our in vitro trials, without animal use were conducted to predict PCA´s cytotoxicity in HaCat and HDFa cells, ophthalmic irritation potential, and antibacterial activity against differents strains. Emulsions with PCA has been tested to predict shelf life, dermal absorption, and dermal retention. Results: PCA´s IC50 in HaCat and HDFa cells was 693.57 and 2,814.75 μg.mL-1, respectively. In addition 100 μg of APC were slightly toxic in chorioallantoic membrane assay. The minimum bactericidal concentrations against E. coli, S. aureus, P. aeruginosa and S. epidermidis strains were 3,000 μg.mL-1, 1,875 μg.mL-1, 3,750 μg.mL-1, and 3,750 μg.mL-1 , respectively. Emulsions containing 0.04%, 0.06%, 0.08% and 0.10% of PCA were stable during self life testing for ninety days. After 12 hours 91.08 ± 0.03% of PCA was released of the emultion, and after 24 hours 0.52 ± 0.18% and 0.94 ± 0.37%, were present in stratum corneum and epidermis/dermis, respectively. Our findings indicate that PCA concentrations would be effective and safe to use in cosmetic products, even eye cosmetics, although complementary assays are necessary.
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Palavras-chave
Ácido p-cumárico, Atividade antimicrobiana, Citotoxicidade, Estudo de estabilidade, p-Coumaric acid, Antibacterial activity, Cytotoxicity, Shelf life testing