RU2846442C1 - Complex based on natural antioxidants - Google Patents

Abstract

FIELD: cosmetology.

SUBSTANCE: invention refers to cosmetology, chemical-pharmaceutical industry, namely to an antioxidant complex for skin care. An antioxidant complex for skin care characterized by the fact that it contains: broccoli extract (Brassica Oleracea Italica Extract), extract of Aloe Barbadensis leaves, bioflavonoids, propanediol, menthol, tetrasodium salt of ethylenediaminetetraacetic acid (EDTA) and purified water, with following ratio of components, wt. %: propanediol 3.0-10.0, bioflavonoids 0.02-0.05, broccoli extract 0.02-0.2, extract of Aloe Barbadensis leaves 0.1-0.5, tetrasodium salt of EDTA 0.05-0.15, menthol 0.25-0.35, purified water – balance.

EFFECT: complex described above is an effective antioxidant, is active and stable for the whole shelf life.

2 cl, 5 ex

Description

The invention relates to the field of cosmetology, the chemical and pharmaceutical industry and concerns antioxidant agents for the production of cosmetic and dermatological products, including for skin protection and care.

Antioxidant compounds are of great interest both for the pharmaceutical industry and in the field of cosmetology.

Internal factors such as inflammation and external factors such as exposure to certain medications, ionizing radiation, and environmental waste can increase the production of reactive oxygen species (ROS) and other free radicals (F.S. Pala, K. Tabakcioglu, Advances in Molecular Biology, 2007 (1), p.63-69). When it exceeds the body's antioxidant capacity, so-called oxidative stress occurs.

Additionally, with age, ROS production increases and antioxidant production decreases, leading to progressive imbalance. The deterioration caused by oxidative stress affects the skin environment in a variety of ways, including decreased collagen and elastin production and accelerated skin aging.

Oxidative stress accelerates reactions that damage skin cells and cause wrinkles, photoaging, elastosis, dryness and pigmentation of the skin.

Using cosmetics containing active antioxidants helps neutralize the formation of free radicals, thereby slowing down the visible signs of aging.

Some plant extracts may be a source of natural antioxidant compounds.

Recently, interest in plant antioxidants for cosmetic use has increased particularly, and many scientific studies point to their benefits (S.H. Chermahini et al., J. Med. Plant Res., 2011 (5), 3074-3077).

Cosmetic formulations typically contain various combinations of extracts from many plants, such as green tea, rosemary, grape seed, grape basil, bilberry, tomato, acerola seed, pine bark, and milk thistle. The extracts of these plants contain natural antioxidants, i.e., polyphenols, flavonoids, flavonols, stilbenes, and terpenes (including carotenoids and essential oils). Some commercial products contain pure natural compounds such as quercetin, kojic acid, and resveratrol (Korac RR, Khambholja KM., Pharmacogn Rev. 2011 Jul;5(10): 164-73).

Plant-based antioxidant extracts typically contain a mixture of natural compounds that may have improved effects and lower toxicity.

The selection of the right active plant extracts or compounds isolated from them, confirmation of their activity, as well as their stability in cosmetic products are important factors for the development of an effective product.

Unfortunately, most antioxidants are unstable and can cause many problems in the development of cosmetic products. Due to their instability, maintaining constant antioxidant activity in formulations throughout the stated shelf life is often problematic. For this reason, it is necessary to determine the antioxidant concentration during storage and control its chemical stability to ensure that the consumer receives a product with the stated activity.

Therefore, there is a need to develop new antioxidant agents in the form of combination products that are free from the above-mentioned disadvantages.

Various researchers have attempted to create complex antioxidant agents.

Thus, international patent application WO 9920242 A1, published 1999.04.29, discloses compositions for preparing external cosmetics, having antioxidant and antiradical action, as well as their beneficial effect on cell regeneration. A composition is described, containing at least one heteropolysaccharide and a compound selected from the group consisting of carotenoids and glucosinolates and/or sulforaphane and mixtures thereof. It can be in the form of an external cosmetic preparation containing a corresponding cosmetic filler suitable for local application, in particular, in the form of a lotion, ointment, body cream, etc.

Patent RU 2821503 C1, publ. 06/25/2024, concerns a composition for the manufacture of cosmetics, which contains a mixture of vegetable fatty and essential oils, while the vegetable fatty oils are: olive oil, coconut oil, hemp oil, flax seed oil, broccoli oil, and the vegetable essential oils are: bergamot, chamomile, lavender, lemon, orange, patchouli, vanilla, basil, sage, frankincense, ginger, grapefruit, jasmine, peppermint, rosemary, sandalwood, the composition also contains CBD oil, isopropyl palmitate, glyceryl stearate, cetearyl alcohol, glycerin, octyldodecanol, dimethicone, xanthan gum, sodium stearoyl glutamate, butylhydroxytoluene, phenoxyethanol, ethylhexylglycerin, fatty acids omega-3, Rhodiola rosea extract, licorice root extract, L-theanine, calcium, glycine, magnesium, vitamins B1, B2, B3, B5, B6, B12 and water. The composition exhibits an antioxidant effect. However, it has a complex and expensive composition.

The closest analogue (prototype) may be US patent 9889171 B2, published 2018.02.13, which describes a composition for topical application on the skin of mammals, containing one or more Brassica plant extracts - a source of the strong antioxidant sulforaphane. Additionally, the composition, for example, in the form of an antioxidant cream, may include turmeric extract, tea extract, Japanese wasabia extract, milk thistle extract, Piper nigrum extract. However, to ensure stability, a significant amount of emulsifiers and surfactants are introduced into the composition.

The objective of the present invention is to create a new effective antioxidant complex that maintains its activity and stability throughout its shelf life.

The problem is solved by the proposed composition of the antioxidant complex for skin care, containing broccoli extract (Brassica Oleracea Italica Extract), aloe barbadensis leaf extract (Aloe Barbadensis Leaf Extract), bioflavonoids, propanediol, menthol, tetrasodium salt of ethylenediaminetetraacetic acid (EDTA) and purified water in the following ratio of components, wt. %:

Propanediol 3.0-10.0 Bioflavonoids 0.02-0.05 Broccoli extract 0.02-0.2 Aloe Barbadensis Leaf Extract 0.1-0.5 Tetrasodium EDTA 0.05-0.15 Menthol 0.25-0.35 Water Rest

To maintain the health and comfort of the skin, it is necessary to enhance its protective functions, maintain the natural level of moisture, nutrition of skin cells, smooth out wrinkles, prevent oxidative stress, and, if necessary, provide a calming, anti-inflammatory and anti-edematous effect.

The developed complex allows to provide all these necessary effects due to the selected optimal recipe.

Bioflavonoids, also known as Vitamin P (A. Garg et al., Chemistry and pharmacology of the citrus bioflavonoid hesperidin, 2001, 15(8), p.655) are a component that combines a number of biologically active substances, such as hesperidin, rutin, quercetin and other polyphenols. Bioflavonoids are found in apples, apricots, berries (bilberries, blueberries, cherries, cranberries, black currants, raspberries, strawberries, red grapes), citrus fruits (grapefruits, oranges, lemons, tangerines), onions, spinach, etc.

Preferably (but not necessarily), citrus bioflavonoids are used according to the invention. They are known for their effectiveness, especially as strong antiradical agents, also exhibiting anti-inflammatory properties (Gupta A et al., Analysis of Citrus Bioflavonoid Content and Dipeptidyl Peptidase-4 Inhibitory Potential of Commercially Available Supplements. Molecules. 2022 Jul 25;27(15):4741).

Aloe Barbadensis Leaf Extract (CAS:94349-62-9) is well known for its immune system strengthening and antibacterial properties. Aloe contains phenols, vitamins C and E, which have antioxidant properties. The extract also provides a healing, moisturizing and restorative effect on skin cells. The introduction of the extract potentiates the action of other active components.

Broccoli extract (Brassica Oleracea Italica Extract) has pronounced antioxidant, anti-inflammatory and anticarcinogenic activity (Hwang JH, Lim SB. Antioxidant and anticancer activities of broccoli by-products from different cultivars and maturity stages at harvest. Prev Nutr Food Sci. 2015 Mar;20(1):8-14).

Menthol has a cooling effect and contributes to the comfortable sensation of the product. At the same time, its introduction also stabilizes the complex.

Propanediol is a natural component obtained in the process of fermenting corn sugar, it is an emollient that also exhibits a moisture-retaining and moisturizing effect. In the declared complex, it acts as a co-solvent. Together with menthol, it allows you to create an excellent texture, both for the complex itself and for possible cosmetic and dermatological creams and gels based on it.

In a particular case, an additional antioxidant, dimethylaminoethanol tartrate (DMAE), can be introduced in an amount of up to 0.5% may, which, in addition to its antiradical effect, strengthens cell membranes and removes the aging pigment lipofuscin from cells.

The composition can be prepared as follows. Tetrasodium EDTA is dissolved in purified water. Bioflavonoids, Broccoli extract, Aloe barbadensis leaf extract are added to the resulting solution and mixed. The resulting solution is introduced in parts into the previously obtained mixture of menthol and propanediol, as well as dimethylaminoethanol tartrate (if included), while mixing with a high-speed mixer.

The possibility of implementing the invention can be illustrated by the examples presented below.

Example 1. Composition of the antioxidant complex

Propanediol 3.0 Citrus bioflavonoids 0.03 Broccoli extract 0.02 Aloe Barbadensis Leaf Extract 0.5 Tetrasodium EDTA 0.05 Menthol 0.3 Water Rest

Example 2. Composition of the antioxidant complex

Propanediol 10.0 Citrus bioflavonoids 0.02 Broccoli extract 0,1 Aloe Barbadensis Leaf Extract 0,1 Tetrasodium EDTA 0,1 Menthol 0.3 Water Rest

Example 3. Composition of the antioxidant complex

Propanediol 5.0 Bioflavonoids 0.02 Broccoli extract 0.05 Aloe Barbadensis Leaf Extract 0.3 Tetrasodium EDTA 0,1 Menthol 0.25 Dimethylaminoethanol tartrate 0.3 Water Rest

Example 4. Antioxidant activity

Antioxidant activity was studied using a photoaging model using squalene as a marker. Squalene is a skin lipid and is the most sensitive molecule to singlet oxygen and its peroxidation (Oxidization of squalene, a human skin lipid: a new and reliable marker of environmental pollution studies. Int J Cosmet Sci. 2015 Aug;37(4):357-65). The lipid is a factor associated with early inflammatory events in human skin that can lead to the development of acne and/or other harmful effects on the skin, such as pore clogging, hyperpigmentation, aging and skin malignancies.

The method for determining the antioxidant efficiency is based on measuring the rate of reduction of malondialdehyde (MDA) formation during squalene oxidation under the influence of UV radiation by comparing the measured amount of MDA in the tested samples (squalene plus complex) with the measured amount of MDA in the control samples (without the antioxidant complex). Each sample - plate (n=10) was exposed to UV at a dose of 10 J/ ^cm2 , onto which 300 μl of the complex according to Examples 1 or 2 were applied, mixed with a 10% solution of squalene (200 μl) in butanol. The amount of formed MDA was determined by fluorometric analysis using thiobarbituric acid. The antioxidant activity is judged by the % difference in the formed MDA. The complex according to Example 1 reduces UV-induced oxidation of squalene by an average of 56% compared to the control sample, the complex according to Example 2 - by an average of 52%. That is, the claimed antioxidant is very effective.

To study the stability of activity retention, the complex was hermetically sealed and stored for a period of 12 weeks at 40°C, which corresponds to 2 years of storage under standard conditions. Then, repeated studies were carried out. The reduction in UV-induced oxidation of squalene was 38% ±4 compared to the control sample, indicating the preservation of high antioxidant activity.

Example 5. Soothing and moisturizing effect on the skin

To evaluate the above effects, the classical TEWL (transepidermal water loss) test was used with a 1% sodium dodecyl sulfate solution in deionized water. Applications on strips of the test substance according to example 1 and a sodium dodecyl sulfate solution that causes erythema were applied to the skin area of the forearm of volunteers (n=14). Then, at different intervals, the level of erythema was measured. Already after 4 hours, a decrease in erythema by 21±4% was noted when using test samples, after 24 hours, erythema was not observed in 12 volunteers, in 1 - a mild degree, in 1 - moderate, which was not observed after 48 hours.

TEWL was measured using a Tewameter® MPA 5 on the day of application and after one week of use. The TEWL level in the control increased by 2%±4, in the test samples it decreased by 20±12%.

Also, in tests on volunteers, they were asked to subjectively evaluate the sensation of texture when applying the product, and all subjects noted a feeling of comfort and a slight rejuvenating effect.

The proposed composition can be used in the practice of cosmetologists and dermatologists as an independent remedy, as well as a basis for various cosmetic skin protection and care products, such as masks, creams or gels for hands or feet, foams or lotions for skin care, sunscreens, etc.

Claims (3)

1. An antioxidant complex for skin care, characterized by the fact that it contains broccoli extract (Brassica Oleracea Italica Extract), aloe barbadensis leaf extract (Aloe Barbadensis Leaf Extract), bioflavonoids, propanediol, menthol, tetrasodium salt of ethylenediaminetetraacetic acid (EDTA) and purified water in the following ratio of components, wt. %: propanediol 3.0-10.0 bioflavonoids 0.02-0.05 broccoli extract 0.02-0.2 Aloe Barbadensis Leaf Extract 0.1-0.5 Tetrasodium EDTA 0.05-0.15 menthol 0.25-0.35 purified water rest 2. The complex according to item 1, characterized in that it additionally includes up to 0.5% dimethylaminoethanol tartrate.