Abstract
As is known, many antioxidants from plant extracts have been used as additives in skincare products to prevent skin damage following overexposure to environmental pollutants. 7,3′,4′-trihydroxyisoflavone (734THIF), an isoflavone compound, possesses various biological activities, including antioxidant, antityrosinase, photodamage protection, and anticancer effects. Unfortunately, 734THIF has poor water solubility, which limits its skin penetration and absorption, and subsequently influences its biological activity. The aim of the present study was to investigate the mechanisms for the improvement in water solubility and skin penetration of 2-hydroxypropyl-β-cyclodextrin (HPBCD) inclusion complex with 734THIF (5-7HP). We also determined its photostability, antipollutant activity in HaCaT keratinocytes, and moisturizing effect in human subjects. Our results showed that 734THIF was embedded into the lipophilic inner cavity of HPBCD and its water solubility and skin penetration were thereby improved through amorphous transformation, surface area enhancement, and hydrogen bonding formation between 734THIF and HPBCD. In addition, 5-7HP inhibited PM-induced ROS generation and then downregulated ROS-mediated COX-2 and MMP9 production and AQP-3 consumption by inhibiting the phosphorylation of MAPKs. Consequently, we suggest that 5-7HP is a safe and photostable topical ingredient to enhance the skin penetration of 734THIF and skin hydration, and therefore 5-7HP may be used as an antipollutant additive in skin care products.
Highlights
Air pollution has gradually increased recently and is an important issue that the World Health Organization (WHO) is concerned about
Higuchi and Connors showed that good inclusion complex formation is the major factor for the improvement of drug solubility [28]
Tsihoensecormespulletsx.indicated that 734THIF with 5 mM HPBCD is a good ratio for preparing 734THIF inclusion complex
Summary
Air pollution has gradually increased recently and is an important issue that the World Health Organization (WHO) is concerned about. Several articles have indicated that PMs cause human body damage including cardiovascular diseases [2], respiratory symptoms [3], and skin aging, which includes wrinkle formation and pigmentation [4,5]. The skin is the first line of defense against external substances such as PMs. When the skin is exposed to “exogenous-aging PM factors” for a long time, it is easy to induce reactive oxygen species (ROS) and inflammatory proteins (e.g., COX-2) and downregulate moisture proteins (e.g., filaggrin) [6] to cause skin aging and damage. Reduced levels of AQP-3 result in impairments in skin hydration, elasticity, glycerol content in skin and is found in psoriasis patients [8]; there is no report regarding whether exogenous aging PMs factors would cause AQP-3 expression to affect skin moisture.
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