Ascorbic acid encapsulated into negatively charged liposomes exhibits increased skin permeation, retention and enhances collagen synthesis by fibroblasts

Abstract

Ascorbic acid (AA) is widely used in cosmetic formulations due to its antioxidant property and ability to increase collagen synthesis. Here, we encapsulated AA in vesicles with different lipid compositions. Negative liposome charge favored AA skin retention, with accumulation of 37 ± 12 and 74 ± 23 μg/cm2 in the epidermis and dermis, respectively, after 6 hours. Drug flux was influenced by the formulation composition, and both the presence of cholesterol and the liposomes surface charge were able to increase the amount of AA crossing the skin. The formulation was stable for at least 30 days and promoted a 7-fold increase in flux compared to free AA. Additionally, liposomes were able to interact better with keratinocytes and fibroblasts membranes. In vitro efficacy studies demonstrated that associating AA to these liposomes resulted in increased effectiveness of type I collagen synthesis by fibroblasts and regeneration of UVA-induced damage in keratinocytes. Our results demonstrate the applicability of AA-negatively charged liposomes in promoting AA cutaneous permeation and increasing the retention and flux of this molecule in the skin. This formulation also increased AA stability and effectiveness, opening new perspectives for its application in view of reducing certain skin ageing outcomes.

A Novel Role of Ascorbic Acid in Anti-Inflammatory Pathway and ROS Generation in HEMA Treated Dental Pulp Stem Cells

“…Our data evidenced in hDPSCs treated with 2 mM HEMA a decreased of cell viability starting from 24 up to 72 h, while the co-presence of AS was able to restored the proliferation rate in treated cells, this effect supports the strategic role of this antioxidant molecule in healing/regeneration process [64,65]. In fact, it has been demonstrated that AS promoted wound healing through matrix deposition, neo-vascularization and finally via secretion of inflammatory mediators [66].…”

Antioxidants as an Epidermal Stem Cell Activator

“…Searching for optimized formulation or delivery system is also important to enhance the permeation of the ingredients into skin. For example, ascorbic acid has limited application in the cosmetic field due to the unstable structure and low skin penetration [ 139 ]. The chemical modification of the hydroxyl group at the C-2 position of ascorbic acid produced stable derivatives such as 2-O-α-D glucopyranosyl-L-ascorbic acid (ascorbic acid 2-glucoside) [ 140 , 141 ].…”

Paper-Based Electrochemical Devices for the Pharmaceutical Field: State of the Art and Perspectives

“…Ascorbic acid has many functions in the maintenance of various biological activities, including beneficial effects on skin, activity as cofactor in collagen biosynthesis, and antioxidant capacity. In particular, the molecules of ascorbic acid neutralize the free radicals present in the intra and extracellular matrices, avoiding damage to lipid membrane, DNA, and proteins that would be caused by oxidative stress (Maione-Silva et al, 2019). In medicine, its topical application guarantees anti-inflammatory and depigmenting effects (Farris, 2005;Stamford, 2012), while in the pharmaceutical sector ascorbic acid is mainly detected in pharmaceutical products for the quality assessment of, e.g., dietary supplements.…”