JP-2026514250-A - Composition comprising niacinamide and resveratrol salicylate

Abstract

[Solution] A topical skincare composition comprising niacinamide and one or more salicylic acid resveratrols. The composition increases energy levels in epidermal keratinocytes while mitigating oxidative damage associated with increased ATP production due to the application of niacinamide. It also increases the expression of AQP-3, CLDN-1, and CLDN-4, resulting in improved skin barrier function and increased moisture retention. Preferred compositions are in the form of a cream, lotion, serum, or gel, and can be implemented as a mixture or emulsion. [Selection Diagram] Figure 1

Inventors

• スタファ，クロジャン
• ゴイアーツ，アール シー．
• ドング，ケリー
• モリス，ケルシー
• マッカーシー，ジェームズ
• マンモーネ，トーマス
• ペルノデット，ナディーン

Assignees

• イーエルシー マネージメント エルエルシー

Dates

Publication Date

20260507

Application Date

20240430

Priority Date

20230502

Claims (6)

1. A topical composition comprising niacinamide and one or more types of resveratrol salicylate.
2. The aforementioned one or more types of resveratrol salicylate 3-Salicylate-5,4'-Dihydroxystilbene 5-Salicylate-3,4'-Dihydroxystilbene 4'-Salicylate-3,5-Dihydroxystilbene 3,5-disalithylate-4'-hydroxystilbene, 3,4'-disalithylate-5-hydroxystilbene, A topical composition according to claim 1, selected from the group consisting of 4',5-disalithylate-3-hydroxystilbene and 3,5,4'-trisalithylatestilbene.
3. The topical composition according to claim 1, wherein the concentration of niacinamide is in the range of about 0.0001% to about 5% of the total weight of the composition, and the concentration of resveratrol salicylate is in the range of about 0.001% to about 5% of the total weight of the composition.
4. The topical composition according to claim 3, further comprising 0.1% to 2% trehalose and 0.1% to 2% betaine.
5. The topical composition according to claim 3, further comprising an aqueous base acceptable as a cosmetic, and optionally an oil phase.
6. The topical composition according to claim 5, wherein the composition is in the form of a water-in-oil or oil-in-water emulsion.

Description

This invention relates to topical compositions, more specifically, to topical skincare compositions that enhance energy levels and regulate water content in skin cells while mitigating the effects of oxidation. Adenosine monophosphate-activated protein kinase (AMPK) is considered a major metabolic regulator that affects numerous metabolic pathways. AMPK is an enzyme complex that detects the intracellular AMP/ATP ratio. An increase in this ratio (indicating energy depletion) activates the AMPK metabolic switch, leading to several mechanisms to increase cellular energy levels, including fat burning, ketosis, and increased glucose uptake by cells. If energy deficiency is maintained for a sufficiently long period, AMPK triggers a process that leads to mitochondrial biosynthesis (the creation of new mitochondria). Known activators of AMPK include niacinamide and resveratrol. Niacinamide (also known as nicotinamide) is one of the three forms of vitamin B3. It is water-soluble and has the following general formula: Niacinamide is used both orally and topically. Topical application of niacinamide is known to treat acne, psoriasis, rosacea, and other inflammatory skin conditions. Niacinamide has been suggested to exhibit anti-inflammatory, anti-aging, anti-cancer, and skin-moisturizing properties. See, for example, Chen, A. C. N., & Damian, D. L. (2014). Nicotinamide and the skin. Australian Journal of Dermatology, 55(3), 169-175. doi:/10.1111/ajd. 12163. Niacinamide is a precursor to nicotinamide adenine dinucleotide (NAD). Within cells, niacinamide is converted to nicotinamide adenine dinucleotide, which acts as an electron transporter and is an essential component for cellular energy production (ATP) via electron transport and oxidative phosphorylation. Increased availability of precursor niacinamide is thought to promote ATP production and enhance energy-dependent cellular processes such as DNA repair. Simultaneously, as cells produce more energy, levels of potentially harmful byproducts, particularly reactive oxygen species, also increase. Resveratrol, also known as 3,4',5-trihydroxystilbene, has the general formula: It is a polyhydroxysubstituted compound having [a specific characteristic]. Resveratrol possesses potent antioxidant, anti-inflammatory, and life-extending properties. It helps stimulate collagen production while protecting the skin from the damaging effects of free radicals. Due to its perceived rejuvenating properties, resveratrol is incorporated into various cosmetic formulations, such as skin creams. However, one problem with resveratrol is its general instability in cosmetic formulations. This problem has been addressed by derivatizing resveratrol by reacting one or more hydroxyl groups with substituents that confer stability when resveratrol is incorporated into cosmetics. In particular, esterifying resveratrol with inorganic acids, organic carboxylic acids, or reacting hydroxyl groups to form alkoxy substituents or glycosides is known to provide resveratrol derivatives that are stable in cosmetic emulsions and enable the formulation of cosmetics with the aesthetic and stability required for commercially successful products. See, for example, U.S. Patents 8,084,496 and 9,220,669, which describe salicylic acid esters of resveratrol. Objective of the Invention The main objective of the present invention is to provide a topical composition that increases energy levels in skin cells by increasing the rate of ATP production, while also providing protection from oxidized species generated in the process. Another object of the present invention is to increase the levels of AQP-3, CLDN-1, and CLDN-4 in epidermal keratinocytes, thereby improving the skin's barrier function and increasing moisture retention. A further object of the present invention is to provide a skincare composition comprising niacinamide, at least one resveratrol salicylate, an aqueous phase, and optionally an oil phase. The present invention relates to a topical skincare composition comprising niacinamide and one or more types of resveratrol salicylate. Preferred compositions are in the form of a cream, lotion, emulsion, gel, serum, and/or powder. Figure 1 shows the oxygen consumption rate by NHDF treated with niacinamide.Figure 2 shows the oxygen consumption rate by NHDF treated with niacinamide and salicylic acid resveratrol.Figure 3 shows the changes in peroxide species levels in NHDF, comparing niacinamide, resveratrol salicylate, and a combination of niacinamide and resveratrol salicylate.Figure 4 shows the oxygen consumption rate over 90 minutes using NHDF treated with niacinamide.Figure 5 shows the oxygen consumption rate over 90 minutes using NHDF treated with niacinamide and salicylate resveratrol.Figure 6 shows the measured NAD+/NADH levels in NHDF cells from 28-year-old and 68-year-old individuals treated with various concentrations of salicylic acid resveratrol, niacinamide, and combinations of niacinamide and salicyli