Encapsulated Activated Grape Seed Extract: A Novel Formulation with Anti-Aging, Skin-Brightening, and Hydration Properties

Abstract

Protein phosphatase 2A (PP2A) is a master regulatory protein that plays a critical role in oxidative stress signaling. A novel, proprietary grape seed extract called Activated Grape Seed Extract (AGSE), enriched for PP2A-activating flavonoids, was recently developed and demonstrated to have antioxidant and anti-inflammatory activities. AGSE is a purple-colored powder, with limited solubility restricting its use in a broad range of formulations. Our aim was to develop a formulation that reduced the color and increased the solubility of AGSE, allowing its skin-health-enhancing properties to be utilized in a wider array of products, and to test it clinically. Encapsulation was performed utilizing a liposome and hydroxypropyl-β-cyclodextrin, (HPCD)-based approach to produce Encapsulated AGSE (E-AGSE). Human dermal fibroblasts and epidermal keratinocytes were used to determine expression levels of aging and dermal–epidermal junction (DEJ) markers. EpiDerm™ was UVB-irradiated to measure the effects against cytokine release, DNA damage, apoptosis, and skin barrier. Human melanocytes were used to determine melanin production and mushroom tyrosinase was used for inhibitory activity. A 4-week, 31-subject sensitive-skin clinical was performed with 2% E-AGSE Essence to assess its activity on human skin. We demonstrated that E-AGSE inhibits PP2A demethylation, increases key anti-aging (collagen I, III, elastin) and DEJ markers, protects against UVB-induced DNA damage, reduces inflammation, and promotes filaggrin in vitro. Moreover, E-AGSE reduces melanin production via tyrosinase inhibition. Clinical assessment of E-AGSE showed that it reduces the appearance of wrinkles, brightens the skin, and boosts hydration. E-AGSE is a novel grape seed extract formulation enriched for PP2A-activating flavonoids that is clinically effective in sensitive skin, providing several benefits.