Abstract
Carnosine has several physiological roles, from intracellular pH buffering to antioxidant activities, which all depend on bioavailability. This study was conducted in a human skin 3D model and focuses on the effects of the topical delivery of carnosine, from a dermo-cosmetic gel, through the stratum corneum in the presence of a magnesium ion as a complexing agent. To evaluate possible enhancement for small peptide delivery to the skin from simple cosmetic formulations, we discovered that complexation was able to improve the delivery of carnosine into human skin 3D models by application in gel formulation. The concentrations of carnosine released in the underlying media and those that remained in the reconstructed human epidermis (RHE) tissues after 24 and 48 h exposure were measured. Moreover, the influence of magnesium ions was also evaluated comparing the same formulation with and without the salt. The results obtained in this study support hypothesis that magnesium can influence the delivery of small peptides and that the gel formulation based on the carnosine-magnesium complex allows for superior delivery of carnosine in the lower skin layer at a concentration up to 60% more than carnosine alone.
Highlights
The efficacy of any cosmetic product containing an active ingredient is determined by two factors: The intrinsic activity of the molecule and the delivery of this molecule to its site of action
To evaluate whether the new gel formulation containing the carnosine complex was able to improve the delivery of dipeptides into human skin by topical application, the concentrations of carnosine released in the underlying media and those that remained in the reconstructed human epidermis (RHE) tissues after 24 and 48 h exposure were measured
At the first-time point, 24 h after the topical application, higher L-carnosine levels were detected in the medium from the RHE treated with the carnosine complex compared to those measured in the media of control tissues (p = 0.028; Table 2 and Figure 1)
Summary
The efficacy of any cosmetic product containing an active ingredient is determined by two factors: The intrinsic activity of the molecule and the delivery of this molecule to its site of action. The intrinsic activity of an active ingredient, or its capability to express efficacy, dictates its functional profile but does not guarantee the efficacy of the final formulation containing the ingredient. The active ingredient must be delivered to the site of action at the right concentrations and the right time. This criterion applies to all types of active ingredients with any functionality and is of particular importance in dermo-cosmetic science [1]. To reach effective concentrations in the cutaneous tissues deeper layers, the uppermost barrier, the stratum corneum (SC), must be overcome
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