KR20210070508A - Polyphenolic grape extract and cosmetic product comprising said extract - Google Patents

Abstract

The present invention relates to a polyphenolic grape extract comprising the following descriptions: total polyphenol index (TPI) 100 to 1,000; gallic acid/L with a polyphenol content of 2,000 to 25,000 mg expressed as the equivalent of gallic acid; and pH of 2 to 4. The present invention further relates to a cosmetic composition comprising the extract and uses thereof to manufacture a cosmetic product.

Description

Polyphenol-based grape extract and cosmetics containing the extract {POLYPHENOLIC GRAPE EXTRACT AND COSMETIC PRODUCT COMPRISING SAID EXTRACT}

The present invention is included in the field of pharmaceuticals and cosmetics, and in particular relates to a concentrated cosmetic formulation containing, as a basic ingredient, a polyphenol-rich red grape extract having high antioxidant activity.

The skin has innate antioxidant defense mechanisms (enzymatic and non-enzymatic) to face environmental aggression. However, when there are too many stimuli, these endogenous defense mechanisms are insufficient to prevent the combined adverse effects, leading to skin problems including aging of the skin.

Studies conducted in the field of etiology of light-induced aging have demonstrated that light-induced aging is caused at least in part by reactive oxygen species (ROS), better known as free radicals. These reactive oxygen species occur not only when the skin is exposed to attacks such as ultraviolet rays, but also during the course of natural aging [Hadshiew, IM et al., "Photoprotective mechanisms of human skin. Regulation by oligonucleotides", Hautarzt, 2002, 53(3), 167-173]

The first step in achieving healthy skin that is protected against these attacks is the use of long-lasting cosmetics, which, in addition to a good diet, ensure desirable protection.

In this sense, one of the objects of the present invention is to provide products that enable a cosmetic response to oxidative stress, in addition to alleviating the direct and collateral damage caused to the body.

This cosmetic response is based on the use of active ingredients from a wide variety of sources (Sevin, A et al., "Effect of polyphenols on skin damage caused by UV A radiation; an experimental study in rats", Journal of the European Academy of Dermatology and Venereology, 2007, 21(5), 650-656]

Of all the cosmetic reactions produced by medical and dermo-pharmaceutical research, grape polyphenols, especially red grape polyphenols, are the ones that trap free radicals, delay cell and skin aging and promote collagen, elastin and hyaluronic acid in the skin They are considered to be the most attractive ingredients because of the potential they offer in terms of great benefits to the body, such as the urge to create. Phenolic compounds are present in the majority of plant species frequently consumed by humans, and they are characterized by including various secondary metabolites having a benzene ring with at least one hydroxyl group as a common feature. In addition, these compounds have high antioxidant capacity [Wang, H et al., "Total antioxidant capacity of fruits", J Agric Food Chem, 1996, 44, 701-705] In particular, polyphenolic grape compounds are particularly active in skin cells, especially epidermal cells and Present in both seeds, they are characterized in that they contain, in most cases, phenols in the form of oligomers and polymers, which, due to their chemical structure as electron donors, have significant antioxidant activity that is much higher than that of vitamin C or vitamin E. [Kinsella et al., "Possible mechanisms for the protective role of antioxidants in wine and plant foods", Food Technology, 1993, 85-89] In addition to the above effects, dermatitis, varicose ulcers, and vascular retinal diseases, preventable stages, early stages, Arrest in the developmental and advanced stages of carcinogenesis, act in cellular aging causing degenerative diseases such as Parkinson's or Alzheimer's, and delay skin aging, improve elasticity, increase cellular vitality, and reduce oxidative stress There is a lot of clinical evidence proving the anti-inflammatory properties of polyphenols as to how they work in reducing the effects and providing protection against external skin attack.

In recent years, the use of wine gourd in the elaboraion of cosmetics is increasing remarkably. Accordingly, various patents claim compositions in which the basic ingredients of grape extract and other cosmetic excipients are evoked. However, unlike the present invention, the raw materials of these methods are not based solely on lees. This means, for example, that patent ES 223468

This is why, in addition to the use of wine gourd, the use of grape seeds and/or skins is described. Patent ES 2228284 also describes a composition characterized in that it also contains black grape stems. Patent ES 2274842 also describes the use of grape seeds, grape leaves and grape skin extracts. In particular, this last patent aims at the mixing of the active ingredients of different grape extracts for the mixing of the active ingredients (ie catechin, quercetin, and resveratrol) on an individual basis.

On the other hand, the patent ES 2172475 aims at a composition based not only on extracts of vine leaves, but also on the basis of grape juice, wine or mixtures thereof. In addition, the cosmetic composition of the patent is characterized in that it contains at least one alpha hydroxyl acid, but also contains grape seed oil.

In addition, the specific situation of the above technical patent is, contrary to the purpose of the present invention, other polyphenols so as not to be present in the final product.

A process comprising isolating a specific compound from According to patent ES 2209187, resveratrol is

It exists in the form of esters, monomers and oligomers obtained from tree trunks.

Patent ES 2225548 aims at the use of ellagic acid in the form of salts, metal complexes, mono or polyester derivatives, mono or polyacylates and carbonates and carbamates derived from hydroxyl groups. The patent also describes the use of compositions for skin protection and topical application of keratin materials to prevent, mitigate and/or inhibit the adverse effects of toxic gases such as ozone, metals and organic waste compounds from combustion.

Meanwhile, patents US 20070148109 and US 20090247490 propose phosphorylation of polyphenols in order to protect them.

This is a way of avoiding their loss as the compounds are very sensitive to foreign substances. In addition, phosphorylation of polyphenols, including enzymes that phosphorylate the polyphenols and turn them into an active state, retards their distribution into keratinous tissues such as skin, hair and nails.

Other patents, such as the Spanish patent ES 2130594 suggest microencapsulation. In particular, the use of mixtures of different fruit juices or plant extracts, or mixtures of extracts from plant parts, is described in the laboratory of microencapsulation.

The method for obtaining the microencapsulation is based on polycondensation between one plant polyphenol and one crosslinking agent, mainly diacid halides, after their lyophilization and rehydration have been carried out.

In addition, fermentation of yeast-based polyphenol-based extracts has been proposed in patents such as US 20100021532 for the purpose of a composition for personal care.

Cosmetics obtained from prior patents are very diverse. Therefore, some of them have specific effects, such as the products described in ES223468 that show anti-cellulite activity, or the products described in ES 2228284 that act on tired legs. In addition, other products, such as those described in ES 2209187, exhibit sunscreen properties, which is why they are suitably used in sunscreen cosmetics.

It is an object of the present invention to propose a new cosmetic formulation comprising at least one polyphenolic extract.

It is also an object of the present invention to use such cosmetic formulations in the elaboration of functional luxury cosmetics, characterized in that they combine the benefits of other natural polyphenols present in their compositions.

In this method, the first object of the present invention is a polyphenolic grape (Vitis vinifera) extract, characterized in that it exhibits the following description: a total polyphenol index measured by a spectroscopic technique such as ultraviolet-visible spectrophotometry ( TPI) is 100-1000, preferably 350-700. Ultraviolet-visible spectrophotometry is an analytical technique based on absorption of radiation by molecules present in a sample being analyzed. Each molecule according to its electron configuration can absorb certain types of radiation depending on its wavelength. In particular, the polyphenol-based compound in solution absorbs radiation in the ultraviolet wavelength region (λ=280 nm);

The polyphenol content expressed as the equivalent of gallic acid (GEA) and measured according to the Folin Ciocalteu method is 2000-25,000 mg gallic acid/L, preferably 8000-17,000 mg gallic acid/L. The Pauline-Ciocalto method involves a spectrophotometric reading of the absorbance of a solution at a wavelength of 765 nm [Harman D, J Gerontol, 1956, 11, 298-300]; pH is 2-4. The acidic pH of the extract being used ensures good skin compatibility because of its slightly acidic skin.

Although red grapes are preferred, several types of grapes can be used as raw materials for the extract. Specifically and preferably these extracts are derived from the skins or hulls which envelope the pulp of the grapes after pressing.

In a particularly preferred embodiment of the present invention, the method used for obtaining the extract is that described in application ES 2319032. The method is based on the collection of residual liquor from wine distillation followed by solid-liquid extraction by countercurrent continuous diffusion. This method is characterized in that the polyphenol-based extract obtained contains not only polyphenols, but also other components and molecules produced from the vineyard, which is a mixture of simple polyphenols artificially produced in a factory or laboratory by characterizing the extract. different from

These polyphenolic compounds present in the extract can be identified based on high performance liquid chromatography (HPLC) analysis. In particular, in this method, the polyphenolic extract of the present invention may contain at least one polyphenolic compound selected from the group consisting of pigments, flavonols, flavan-3-ols and phenolic acids, and any combination thereof. can

In a specific embodiment of the present invention, the compound is included in the polyphenolic extract in the following amounts:

Pigment: 100 to 500 mg/L, preferably 300 to 400 mg/L;

Flavonols: 100-500 mg/L, preferably 200-300 mg/L;

Flavan-3-ol: 1000-1500 mg/L, preferably 1350-1450 mg/L;

Phenolic acid: 100-500 mg/L, preferably 200-300 mg/L.

Accordingly, another object of the present invention is a cosmetic composition comprising the polyphenol-based extract as described above. In addition, the cosmetic composition is characterized in that it contains at least 85% by weight of natural ingredients with respect to the total.

Preferred in the group consisting of rosehip oil, caviar extract, jojoba oil and wheat germ oil, and any combination thereof, in addition to the polyphenolic extracts described above, preferably included in a concentration of 2% to 10% by weight of the total cosmetic composition It is characterized in that it also comprises at least one vehicle comprising one or more cosmetically acceptable excipients selected from These ingredients are characterized in that they are ingredients of high-end cosmetics.

Another object of the present invention is, as described above, at least one vehicle comprising at least one cosmetically acceptable excipient preferably selected from the group consisting of rosehip oil, caviar extract, jojoba oil and wheat germ oil and at least one It is a method employed to obtain the cosmetic composition, characterized in that it comprises a mixture with a polyphenol-based extract of

The synergistic effect of the various components in the composition is mainly a result of high antioxidant power, and it has been demonstrated that the skin aging process can be prevented. In addition, several aesthetic benefits derived from the use of cosmetic compositions have been demonstrated as a result of their antioxidant power to delay skin aging, improve skin elasticity, and prevent wrinkles. It has also been demonstrated to increase cellular vitality and vascular resistance, strengthen the microcirculatory system, reduce the effects of oxidative stress, and protect the skin against environmental attack and smoke. It also inhibits free radicals that cause skin aging and premature oxidation.

Accordingly, another object of the present invention is the use of said composition in the elaboration of cosmetics. These cosmetics include anti-aging nourishing creams, preferably designed for aging or damaged skin, in order to create a more complete and moist skin appearance by preferably restoring the skin's protective barrier; preferably a moisturizing cream for the face, which not only provides sun protection, but also prevents skin dryness, keeps the skin moist all day and freshens the skin; Alternatively, an eye contour cream that acts on fine wrinkles and provides luster and relief of sagging under the eyes and dark circles due to the decongestant effect that stimulates the microcirculatory system can be preferably configured.

However, the cosmetics may be developed into other products such as facial toner, cleansing milk, body milk, serum, and the like, and thus is not limited thereto.

In another specific embodiment of the present invention, the cosmetic may consist of an oral cosmetic.

In addition to the advantages indicated above, these cosmetics derived from their cosmetic compositions are characterized as being environmentally friendly as they do not contain parabens, mineral oils or synthetic colorants.

It is preferred that the cosmetic product be stored in an inert and sealed container which provides greater stability and barrier to light and air.

1 is a diagram showing the inhibition of generation of reactive oxygen species caused by pretreatment with formulations tested at different concentrations after exposure to three doses of UVA irradiation. Values are expressed as a percentage of reactive oxygen species inhibition compared to untreated cells exposed to the same amount of UVA irradiation.
Figure 2 is a diagram showing the inhibition of the production of reactive oxygen species caused by pretreatment with the regimen tested at a concentration of 05 mg/ml compared to the inhibition caused by vitamin C.

(Example)

The following illustrates, but is not limited to, a series of examples of the present invention:

Example 1 - Cosmetic composition

The following cosmetic composition for topical administration, based on the obtained polyphenolic grape extract and exhibiting the characteristics as described above, was induced by a prior art method.

11 Antioxidant moisturizing cream with red grape polyphenols;

12 Antioxidant nourishing cream with red grape polyphenols;

13 Antioxidant Eye Contour Cream with Red Grape Polyphenols

Table 1 details the components and amounts corresponding to each of the above compositions.

Example 2 - Stability Test

In this second example, the present inventors confirmed the high skin compatibility of cosmetics by conducting a clinical study under an airtight patch for 48 hours after only one application on the skin of the back to an adult subject. Based on the results obtained under the applied experimental conditions, the skin compatibility of this study product was considered to be very good.

We also conducted a final clinical safety test of the cosmetic product in healthy adult subjects to confirm its high skin compatibility and potentially delayed lack of skin sensitivity. Taking into account the results obtained under the applied experimental conditions, a single skin application and repeated application of the present product under an occlusive patch to a healthy adult subject did not cause primary irritation or cumulative irritation, or sensitivity of the skin.

Example 3 - Efficacy Test

During the tests conducted, the inventors confirmed that, as shown in FIG. 1 , samples of all concentrations tested were effective in reducing the production of reactive oxygen species after being stressed by UVA radiation.

Thus, the tested formulation (nutrition cream) exhibits inhibitory activity against UVA radiation induced by the release of reactive oxygen species in human keratinocytes. As shown in FIG. 2 , the greatest effect (-579%) was confirmed at a concentration of 05 mg/ml.

Conclusion The present inventors have found that, while focusing on the fact that the cosmetic of the present invention has high skin compatibility and effectiveness for UVA radiation, UV protection, and does not irritate the eye area, the above examples demonstrate the optimal properties of the cosmetic of the present invention. has proven

Claims (13)

A polyphenol-based grape extract comprising the following technical details.
Total Polyphenol Index (TPI) 100-1000; Gallic acid/L with a polyphenol content of 2000 to 25,000 mg expressed as an equivalent of gallic acid; pH 2-4 The method of claim 1,
A polyphenol-based grape extract, characterized in that it is derived from the skin of red grapes. 3. The method according to claim 1 or 2,
Polyphenols present in the polyphenolic grape extract are selected from the group consisting of pigments, flavonols, flavan-3-ols and phenolic acids, and any combination thereof. 4. The method of claim 3,
The polyphenol-based grape extract, characterized in that it is identified in the following amount.
· Color 100-500 mg/L;
· Flavonols 100-500 mg/L;
· Flavan-3-ol 1000-1500 mg/L; and
・Phenolic acid 100-500 mg/L A cosmetic composition comprising the polyphenol-based grape extract according to any one of claims 1 to 4. 6. The method of claim 5,
A cosmetic composition comprising at least one vehicle further comprising one or more excipients in addition to the polyphenolic grape extract. 7. The method of claim 6,
wherein the excipient is selected from the group consisting of rosehip oil, caviar extract, jojoba oil and wheat germ oil, and any combination thereof. 6. A method for obtaining a cosmetic composition according to any one of claims 1 to 5, comprising at least one polyphenolic grape extract according to any one of claims 1 to 4 and at least one excipient. A method comprising a mixture of one vehicle. 9. The method of claim 8,
wherein the excipient is selected from the group consisting of rosehip oil, caviar extract, jojoba oil and wheat germ oil or any combination thereof. Use of a cosmetic composition according to any one of claims 5 to 7, characterized in that it is for the preparation of topical cosmetics. Use of the cosmetic composition according to claim 5 or 6, characterized in that it is for the manufacture of a cosmetic for oral use. A cosmetic comprising the cosmetic composition according to any one of claims 5 to 7. 13. The method of claim 12,
The cosmetic is a cosmetic, characterized in that selected from the group consisting of anti-aging nourishing cream, moisturizing cream and eye contour cream.

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