Vitamin C–squalene bioconjugate promotes epidermal thickening and collagen production in human skin

Abstract

Vitamin C (Vit C) benefits to human skin physiology notably by stimulating the biosynthesis of collagen. The main cutaneous collagens are types I and III, which are less synthesized with aging. Vit C is one of the main promotors of collagen formation but it poorly bypasses the epidermis stratum corneum barrier. To address this challenge, we developed a lipophilic version of Vit C for improving skin diffusion and delivery. Vit C was covalently conjugated to squalene (SQ), a natural lipid of the skin, forming a novel Vit C–SQ derivative suitable for cream formulation. Its biological activity was investigated on human whole skin explants in an ex vivo model, through histology and protein and gene expression analyses. Results were compared to Vit C coupled to the reference lipophilic compound palmitic acid, (Vit C–Palmitate). It was observed that Vit C–SQ significantly increased epidermal thickness and preferentially favored collagen III production in human skin after application for 10 days. It also promoted glycosaminoglycans production in a higher extent comparatively to Vit C–Palmitate and free Vit C. Microdissection of the explants to separate dermis and epidermis allowed to measure higher transcriptional effects either in epidermis or in dermis. Among the formulations studied, the strongest effects were observed with Vit C–SQ.

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“…In this study, squalene was the most effective promoter in improving the permeability of APR through human abdominal skin. The squalenic acid chain confers high hydrophobicity for skin penetration of hydrophobic drugs, such as APR [ 47 ]. Squalene reduces the oxidative damage of free radicals in the skin; in addition, this promoter is present in a percent of around 13% in sebum which is produced by the sebaceous glands that correspond to small glands present in the skin that secrete sebum in hair follicles to lubricate skin and hair in animals [ 48 ].…”

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“…Vitamina C, também conhecida como ácido ascórbico, encontrada em diversos alimentos e vendida como suplemento, é um potente antioxidante e auxilia na produção de colágeno Atuante na reparação do tecido e na produção enzimática de certos neurotransmissores. É eficaz no combate às manchas, inibidora do melasma, rugas e linhas de expressão (Gref, 2020). Alzheimer (Mohd, 2020).…”

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