Evaluation of the Transepidermal Penetration of a Carnosine Complex in Gel Formulation by 3D Skin Models

Dissette, Valeria; Bignozzi, Carlo Alberto; Valacchi, Giuseppe; Pecorelli, Alessandra; Manfredini, Stefano; Vertuani, Silvia

doi:10.3390/cosmetics5040067

Cited by 6 publications

(6 citation statements)

References 18 publications

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“…15 Carnosine Hydrophilic dipeptide is a component of several tissues with pH buffering and excellent antioxidant properties due to metal ion chelation and scavenging reactive oxygen species (ROS) and peroxyl radicals. 16 Enzymatic Ubiquinone (coenzyme Q10)…”

Section: Oleuropeinmentioning

confidence: 99%

Antioxidants with proven efficacy and elastin‐conserving vitamin C—A new approach to free radical defense

Widgerow,

Ziegler,

Garruto

et al. 2023

J of Cosmetic Dermatology

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BackgroundThis paper describes the background research and validation related to the formulation of a novel antioxidant product. Two defined outcomes were sought. Firstly, a combined efficacy of antioxidant ingredients in quenching free oxygen radicals. Secondly, the investigation into whether a vitamin C derivative sodium salt was elastin conserving in contrast to current vitamin C/l‐ascorbic acid variations that have been reported to negatively affect elastin constitution and regeneration.Materials and MethodsA leading l‐ascorbic acid antioxidant available on the market was compared with the experimental new product in two studies. In the first experiment, the products were compared to assess their antioxidant properties. The evaluated products TOPICAL ANTIOXIDANT 1 and TOPICAL ANTIOXIDANT 2 were applied to human skin cultures (25–30 mg/cm2) for a total of 72 h of treatment and exposed to oxidative stress. The generation of free radicals was semi‐quantitatively assessed by measuring the fluorescence intensity of the deacetylation and oxidation of the probe dichlorofluorescein diacetate (DCFH‐DA). In the second experiment, an ex vivo skin model (derived from patients undergoing facelift procedures) was used to assess elastin preservation. Three skin explants were topically subjected to the two formulations daily for 7 days. The skin was then prepared and fixed for immunofluorescent assessment after staining with CD44 and tropoelastin antibodies. Images were then analyzed using ImageJ.ResultsA full description of the different components selected for the new formulation is presented. In the first study, the experimental formulation performed with absolute equivalence to the comparator in its radical quenching capacity; both showed extremely effective antioxidant function. In the second study, the comparator negatively affected the existing elastin with areas of breakdown and diminished staining. In contrast, the new formulation showed good conservation of healthy elastin in all sections demonstrating elastin preservation.ConclusionA new antioxidant formulation was carefully designed with multiple actives that show an equivalent antioxidant capacity to a leading product on the market. More importantly, the vitamin C component shows direct elastin conservation and improvement as opposed to the comparator, which had negative effects on elastin preservation. This is in keeping with little‐known literature reports on vitamin C and its negative effects on elastin and validates the use of a sodium salt derivative, which appears to have protective effects on elastin. These findings support the overall regenerative extracellular matrix changes seen with TriHex® technology in other products.

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Section: Oleuropeinmentioning

confidence: 99%

Antioxidants with proven efficacy and elastin‐conserving vitamin C—A new approach to free radical defense

Widgerow,

Ziegler,

Garruto

et al. 2023

J of Cosmetic Dermatology

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“…The enhanced skin permeability of carnosine complex was attributed to its better ability to interact with the electronic charges of the nitrogen atoms present on the long chain glycosaminoglycan as well as on the membrane proteins. The authors introduced the metal chelation as a good approach to increase the skin permeability of carnosine [31].…”

Section: Metal Complexationmentioning

confidence: 99%

“…Enhancement ratio = 36 [41] Note: All permeation studies except [31] have been performed using diffusion cells.…”

Section: Microneedles Human Cadaver Skinmentioning

confidence: 99%

“…Carnosine is an antioxidant dipeptide that has anti‐glycation activity and consequently the potential to be used as an anti‐wrinkle peptide. Carnosine (MW: 226.23 Da, clog P: −2.17) and its metabolite N‐acetylcarnosine (MW: 268.27 Da, clog P: −2.56) are also able to decrease UVB erythema in human skin [31]. Contrary to carnosine, N‐acetylcarnosine has been shown that it is not a substrate for carnosinase.…”

Section: Chemical Permeation Enhancersmentioning

confidence: 99%

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Skin permeability, a dismissed necessity for anti‐wrinkle peptide performance

Mortazavi

Moghimi

2022

Intern J of Cosmetic Sci

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Background:The skin offers various benefits and potential for peptide delivery if its barrier performance can be reduced temporarily and reversibly. As peptides possess high molecular weight, hydrophilic nature (in most cases), and ionizable groups in the structure, their skin delivery is highly challenging. Apart from this, they are susceptible to the proteolytic enzymes in the skin. Anti-wrinkle peptides, like other peptides, suffer from insufficient skin permeability, while most of them must penetrate deep in the skin to present their efficacy. Although the cellular studies indicate the effectiveness of such peptides, without the ability to permeate the skin sufficiently, this efficacy is useless. Poor skin permeability of anti-wrinkle peptides has led to ongoing research for finding feasible and noninvasive enhancement methods that would be desirable for consumers of cosmetic products. Method:In this paper, the possibility of skin permeation of anti-wrinkle peptides as well as the chemical, physical, and encapsulation approaches that have been employed to date to increase permeability of these difficult molecules are thoroughly reviewed.Results: Most anti-wrinkle peptides are not appropriate candidates for skin permeation and the use of enhancement methods is essential to increase their permeability. To do so, only some permeability enhancement approaches have been applied so far, including chemical modification with hydrophobic moieties or cell penetrating peptides, metal complexation, chemical permeation enhancers, iontophoresis, microneedles, and encapsulation in nanocarriers. The results of studies published on the skin permeability of anti-wrinkle peptides carnosine, GHK, PKEK, GEKG, GQPR, and KTTKS indicate that the skin permeability of these peptides can be successfully increased. Conclusion:Although the skin permeability of most anti-wrinkle peptides is not high enough and most anti-wrinkle peptides might not reach their targets in the skin at right concentrations, their permeability can be increased to therapeutic concentrations using various enhancement approaches. K E Y W O R D Santi-wrinkle peptides, cosmetic peptides, permeability enhancement approaches, skin delivery of peptides, skin permeability | 233 MORTAZAVI and MOGHIMI Résumé Contexte: La peau offre divers avantages et a la faculté de recevoir des peptides si l'on parvient à réduire temporairement et de manière réversible sa capacité à fonctionner comme une barrière. Comme les peptides ont un poids moléculaire élevé, une nature hydrophile (dans la plupart des cas) et possèdent des groupes ionisables dans leur structure, il est très difficile d'en faire bénéficier la peau. En outre, ils sont sensibles aux enzymes protéolytiques de la peau. Les peptides antirides, comme d'autres peptides, souffrent d'une capacité insuffisante de perméation de la peau ; or, la plupart d'entre eux doivent y pénétrer profondément pour avoir une efficacité.Bien que les études cellulaires indiquent l'efficacité de ces peptides, s'ils sont incapables de pénétrer s...

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“…The delivery of carnosine through the stratum corneum in the presence of magnesium ions results in skin-soothing and antioxidant properties allowing protection against oxidative stress. [3]. Moreover, carnosine prevents the fibroblast senescence process caused by HNE (4-hydroxy-2-nonenal) or acrolein adducts with elastin isoforms [4,5].…”

Section: Introductionmentioning

confidence: 99%

Oxidative Stress Modulation by Carnosine in Scaffold Free Human Dermis Spheroids Model: A Proteomic Study

Aiello

Rescigno

Méloni

et al. 2022

IJMS

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Carnosine is an endogenous β-alanyl-L-histidine dipeptide endowed with antioxidant and carbonyl scavenger properties, which is able to significantly prevent the visible signs of aging and photoaging. To investigate the mechanism of action of carnosine on human skin proteome, a 3D scaffold-free spheroid model of primary dermal fibroblasts from a 50-year-old donor was adopted in combination with quantitative proteomics for the first time. The label free proteomics approach based on high-resolution mass spectrometry, integrated with network analyses, provided a highly sensitive and selective method to describe the human dermis spheroid model during long-term culture and upon carnosine treatment. Overall, 2171 quantified proteins allowed the in-depth characterization of the 3D dermis phenotype during growth and differentiation, at 14 versus 7 days of culture. A total of 485 proteins were differentially regulated by carnosine at 7 days, an intermediate time of culture. Of the several modulated pathways, most are involved in mitochondrial functionality, such as oxidative phosphorylation, TCA cycle, extracellular matrix reorganization and apoptosis. In long-term culture, functional modules related to oxidative stress were upregulated, inducing the aging process of dermis spheroids, while carnosine treatment prevented this by the downregulation of the same functional modules. The application of quantitative proteomics, coupled to advanced and relevant in vitro scaffold free spheroids, represents a new concrete application for personalized therapies and a novel care approach.

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Evaluation of the Transepidermal Penetration of a Carnosine Complex in Gel Formulation by 3D Skin Models

Cited by 6 publications

References 18 publications

Antioxidants with proven efficacy and elastin‐conserving vitamin C—A new approach to free radical defense

Antioxidants with proven efficacy and elastin‐conserving vitamin C—A new approach to free radical defense

Skin permeability, a dismissed necessity for anti‐wrinkle peptide performance

Oxidative Stress Modulation by Carnosine in Scaffold Free Human Dermis Spheroids Model: A Proteomic Study

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