Abstract
Tetrahydrocurcumin (THC) has been well known for its superior antioxidant properties. Therefore, it is speculated that it might be effective to relieve oxidative stress-induced diseases, such as skin hyperpigmentation. In this work, an in vitro B16F10 melanoma cell model was used to study the impact of THC on the melanogenic process under stressed conditions. It was demonstrated that THC could effectively inhibit the α-MSH (melanocyte-stimulating hormone) induced melanin production in B16F10 melanoma cells and the expressions of three key enzymes involved with the biosynthetic process of melanin, tyrosinase (TYR), tyrosinase-related protein 1 (TRP-1), and tyrosinase-related protein 2 (TRP-2), were all significantly reduced. In addition, an in vitro human keratinocyte cell model was used to investigate the potential protective role of THC on H2O2-induced cytotoxicity. It was found that THC could prevent H2O2-induced oxidative stress based on the results of both the cell viability study and the intracellular ROS (reactive oxygen species) study assessed by the flow cytometry. Last, THC was formulated into a lecithin based nanoemulsion, and an in vitro Franz diffusion cell study using Strat-M® membrane concluded that the nanoemulsion could significantly enhance the membrane permeation compared to the unformatted THC suspension. This research demonstrated the anti-melanogenic benefits of THC on the melanoma and keratinocyte cell models and the topical delivery efficacy could be significantly enhanced using a lecithin based nanoemulsion.
Highlights
The skin is the largest organ in the human body, and its main functions are to regulate the moisture content and the temperature within the body, provide protection from external microorganisms, ultraviolet (UV) radiation, chemicals, etc. [1,2]
When the skin is exposed to external stress such as UV radiation, reactive oxidative species (ROS) are generated and accumulate extensively in the skin, which is usually detrimental to the cells [8]
The result from this study demonstrated the application of lecithin-based nanoemulsions for topical drug delivery enhancement
Summary
The skin is the largest organ in the human body, and its main functions are to regulate the moisture content and the temperature within the body, provide protection from external microorganisms, ultraviolet (UV) radiation, chemicals, etc. [1,2]. Pharmaceutics 2021, 13, 1185 activity, and cause unpleasant skin hyperpigmentation that can even lead to the initiation and progression of melanoma, a deadly skin cancer. UV radiation could stimulate the synthesis of certain biochemical factors such as alpha-melanocyte-stimulating hormone (α-MSH), endothelin-1 (ET-1), stem cell factor (SCF), etc. These could be secreted from keratinocytes and delivered to the neighboring melanocytes [13,14]. When melanocytes receive the excessive biochemical factors from keratinocytes, they upregulate the enzymes responsible for melanin synthesis and cause the overproduction of melanin, leading to skin hyperpigmentation
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