ES2354103A1 - Capillary composition activator of the sirtuinas and use of the sirtuinas. (Machine-translation by Google Translate, not legally binding) - Google Patents

Abstract

Activating capillary composition of sirtuins including a resveratrol component (5 - [(e) -2- (4-hydroxyphenyl) -ethenyl] benzene-1,3-diol) and/or oligomers thereof from extract of vitis vinifera vine, milk protein cytokines, lactose, inositol, acetyl cysteine and acetyl methionine, achillea millefolium extract, cinchona succirubra extract, tussilago farfara extract, laminaria algae extract, alaria esculenta extract and pantenyl ethyl ether/panthenol, besides other additional agents, in the form of lotion or shampoo, to prolong the anagen or hair growth phase over time by activating the sirtuins. (Machine-translation by Google Translate, not legally binding)

Description

Activating hair composition of sirtuins and use of it.

The present invention relates to a capillary composition activating the sirtuins and use Of the same. More particularly, the present invention relates to a hair composition that is capable of activating SIRT1, "NAD-dependent sirtuin-1 deacetylase", a protein encoded by the "SIRT1" gene, which regulates the activity of various transcription factors and sensitive enzymes to the availability of nutrients, as well as their use.

The hair composition of the invention makes it possible to prolong the anagen or hair growth phase over time thanks to a mixture of active ingredients that includes, among others, a resveratrol component (5 - [(E) -2- (4-hydroxyphenyl) ) ethenyl] benzene-1,3-diol) and / or oligomers thereof, from Vitis vinifera extract.

one

Numerous compositions containing resveratrol are known in the state of the art. For example, WO2006 / 087759, "Pharmaceutical composition comprising curcumin and resveratrol and uses thereof in medical field", claims a pharmaceutical composition comprising resveratrol and / or root of Polygonum cuspidatum and curcumin and / or root of Curcuma longa , as active ingredients in association with one or more pharmaceutically acceptable adjuvants and / or excipients. This composition is used for the treatment of cancer, skin diseases, to treat or prevent aging and for the treatment and prophylaxis of diseases of the pyloric system based on the anti-inflammatory and antineoplastic action of resveratrol and curcumin as an antioxidant mixture .

Similarly, ES 2 209 187 T3, "Compounds to base of resveratrol derivatives, "describes compounds of Resveratrol stable against air and light and the use of themselves as solar photoprotectors, as dietary products or as venotonic and vasculoprotective medications based on their antioxidant and anti-inflammatory properties.

Also in recent years they have appeared in the market very numerous dietary and cosmetic products that include resveratrol among its active ingredients, in particular for its anti-inflammatory, anti-aging or mimetic action of the caloric restriction

However, none of the documents or commercial products belonging to the state of the art describe a capillary composition activating the sirtuins that allows the anagen or hair growth phase to be prolonged in time thanks to a mixture of active ingredients that includes, among others, a component of resveratrol (5 - [(E) -2- (4-hydroxyphenyl) ethenyl] benzene-1,3-diol) and / or oligomers thereof, derived from Vitis vinifera extract.

Thus, the object of the present invention is a hair activating composition of the sirtuins that allows the anagen or hair growth phase to be prolonged over time thanks to a mixture of active ingredients that includes, among others, a resveratrol component (5- [(E) -2- (4-hydroxyphenyl) -etenyl] benzene-1,3-diol) and / or oligomers thereof, from Vitis vinifera extract. The activating composition of the sirtuins of the present invention includes other components, such as milk cytokines, inositol, acetyl cysteine and acetyl methionine, trichogenic auxin, laminaria algae extract, Alaria esculenta extract and panthenol, in addition to suitable solvents, antioxidants and additives For its formulation.

The hair has a cyclic growth called hair cycle, each follicle having its own cycle regardless of those around you. Basically, the phases of the hair cycle are:

Anagen phase: during which the hair is stuck to the papilla, it is born and grows. It extends for an average of three years. The shape of the follicle in this phase is similar to that of a onion, wider at the base than on the stem. The hair grows without cease because the follicle matrix cells divide by mitosis constantly.

Catagen phase: It is a transition phase. Be extends about 3 weeks, during which the growth is stops and separates from the papilla, ceasing the activity of the matrix cells, including melanocytes. The bulb takes a cylindrical appearance.

Telogen Phase: It is the rest and fall phase of hair, lasts about 3 months. The hair root takes on an aspect of match and remains inserted in the follicle.

Thus, when the hair finishes growing in the phase anagen, the reproduction of undifferentiated base cells of the follicle also stops, the root becomes progressively more narrow and the cells that are on top of the papilla suffer a cornification process. Finally, the root separates from the hair papilla and it falls out. Before it comes off, it starts the formation of a new hair at the base of the follicle.

The capillary composition of the invention including resveratrol and other active components is capable of stimulating the action of sirtuins, proteins intimately related to cell survival, which act by regulating the activity of other genes related to cellular defenses, neuronal activity, repair of damage, energy production and programmed cell death. The activation of the sirtuins rebalances the excessively accelerated hair cycle, thus preserving the capillary capital. Resveratrol causes mitochondria to increase their breathing, consuming a greater amount of oxygen, which produces NAD and eliminates NADH, which in turn is an inhibitor of these sirtuins. Recent studies have shown that resveratrol induces a significant change in metabolism by increasing the efficiency of bioenergetic extraction through an increase in the amount of mitochondria, the organelles responsible in the organisms for most of the synthesis of ATP (Placido Navas and Guillermo López-Lluch, Andalusian Center for Development Biology, Universidad Pablo de Olavide-CSIC,
Seville).

The capillary activating composition of the sirtuins of the present invention includes as active components, among others, a resveratrol component (5 - [(E) -2- (4-hydroxyphenyl) -ethenyl] benzene-1,3-diol) and / u oligomers thereof, from Vitis vinifera extract, milk cytokines, inositol, acetyl cysteine and acetyl methionine, trichogenic auxin, laminaria algae extract, Alaria esculenta extract and panthenol, in addition to solvents, antioxidants and suitable additives for its formulation .

In a preferred embodiment, the hair composition activating the sirtuins of the present invention includes the following active components in the percentages (by weight) indicated:

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2

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In one embodiment of the invention, the proportion of Vitis vinifera Vine Extract present in the composition is equivalent to approximately 0.002-0.02% of a mixture of resveratrol and its oligomers (Resveratrox®), providing a percentage of trans -resveratrol of approximately 0.0002 - 0.002%.

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The joint action of resveratrol and the rest of the active components mentioned above allow to prolong the anagen phase of the hair cycle as explained in more detail In the examples.

On the other hand, the cytokines present in the lactose-lactose proteins act as messengers and promoters of the anagen phase avoiding the appearance of factors of cell destruction, and together with inositol, allows cells respond to messages from the environment, especially with reference to environmental agents that cause oxidative stress and imbalances in cellular respiration Both components thus facilitate performance of resveratrol included in the composition of the invention. Similarly, cysteine and methionine in its form acetylated, sulfur amino acids keratin components, They stimulate growth and improve the hair shaft.

Extracts of Aquilea millefolium , Tussilago farfara and Cinchona cuccirubra , for example contained in a mixture of natural such as Tricogena Auxin , supplements the action of the aforementioned components, improving hair quality, activating hair cell respiration and balancing processes of oxidation-reduction in them.

The capillary composition of the invention is complemented with active ingredients derived from laminar seaweed extracts with 5-alpha-reductase inhibitory capacity and, therefore, improving the anti-inflammatory and anti-fat action of the composition of the invention; as well as with Alaria esculenta extract high in amino acids, in particular alanine, which fills the hair giving it body, softness, facilitates combing and prevents frizz. This extract of Alaria esculenta together with the panthenol and the panthenyl ethyl ether included in the composition of the invention also allow it to have a conditioning and hydration conditioning effect, thus improving the stem.
capillary.

Optionally, the hair composition of the invention may contain other active ingredients, such as Rosmarinus officinalis or Humulus lupus .

In a preferred embodiment of the composition of the invention, this is complemented with ingredients With antioxidant capacity. Among the antioxidant ingredients are They may cite, for example, ascorbic acid, ascorbyl palmitate, tocopherol, sodium ascorbate, beta-carotenes, flavonoids, BHT or BHA. More particularly ascorbic acid, ascorbyl palmitate and tocopherol in proportions by weight following, with respect to 100 g of the hair composition:

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4

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The capillary composition of the invention can be obtain by the usual processes known to the expert in the matter for its formulation in the form of, for example, lotion hair or shampoo For this, the composition of the invention includes various additional ingredients such as solvents, preservatives, sequestering agents, solubilizers, agents pH adjustment, perfumes, surfactants, conditioners, chelating agents, opacifiers, antioxidants, etc.

Among the agents the surfactants are may cite, for example, anionic surfactants such as Sodium Lauryl Sulfate, Sodium Laureth Sulfate, Disodium Laureth Sulfate; amphoteric surfactants such as Disodium Cocoamphodiacetate, Cocamidopropyl Betaine; non surfactants ionics such as Cocamide DEA, Cocamide MEA, PEG-4 Rapeseedamide Among the conditioning polymers may be mentioned, for example, Polyquaternium-7, Polyquaternium-22, PEG-15 Cocopolyamine Examples of sequestering agents are Disodium EDTA, EDTA, DTPA. Among the preservatives can be mentioned, for example, methylparaben, iodopropinyl butylcarbamate, DMDM hydantoin, methylchloroisothiazolinone, methylisothiazolinone. Among the agents of pH adjustment can be cited, for example, lactic acid, acid Citrus, NaOH, AMP. Examples of opacifying agents are styrene / VP copolymers, styrene / acrylate copolymers. How Examples of viscosity regulating agents are mentioned sodium chloride, magnesium chloride. Examples of solubilizers are PEG-40 - castor oil, PEG-60 Hydrogenated castor oil, laureth-9.

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In a preferred embodiment of the composition capillary of the invention in the form of lotion, this includes the following additional ingredients:

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5

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In an embodiment of the composition of the invention in the form of shampoo, this includes the following additional ingredients:

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Examples Evaluation of the effects of hair composition in shampoo and lotion in vivo

An in vivo study was carried out with 25 healthy human volunteers who were given the hair composition of the invention in the form of shampoo and single dose ampoules for routine use during 180
days.

Healthy volunteers were chosen for it with An Anagen / Telogen ratio <4 (Men: degrees Hamilton II-IV; women: grades Ludwig I-II) and who would not have undergone a previous hair treatment during the 3 months prior to study, without scalp pathologies and that were not undergoing prior treatment with medications that could cause alopecia or were habitual consumers of Nutricosmetics The purpose of the study was to evaluate the relationship between the anagen and telogen phase of the hair of the volunteers, as well as the general appearance of the hair, the detailed appearance of the leather scalp, the number of hair detached during styling ("Combing" test) and the number of hair shed during washing ("Washing" test).

Protocol

Before starting the study, the volunteers who will not wash their hair in the 48 hours prior to First initial check or comb in the 24 hours prior to this visit T0). During the first control visit, they were made general photographs of the scalp, photomicrographs of the scalp, initial tricograms, styling and washing tests of the hair of each volunteer. Volunteers were asked to wash the hair with the shampoo containing the composition of the invention on alternate days and that a single dose vial should be applied containing the composition of the invention in the scalp a diary. The volunteers did not use any other product of scalp treatment during the period of study completion

Tests performed 1. General hair photography

In the T0 and T180 control visits are made several photographs of the top of the head in order to check if the treatment under study improves the appearance General hair at a glance.

2. Observation and photography by micro camera

The microcamera (TrichoScan®) is a device of Professional diagnosis for skin examination. Its function is to allow expanded direct vision of an area of the leather scalp, for the observation of existing hair and state they are in By comparison of the images at T0 and T180 can be seen if there is an increase in the number of hair like this as the thickness of them. The images obtained at the beginning and at end of the study allow to assess the effectiveness of the treatment (Figure 1).

3. Tricogram

It consists of tensile extraction of a determined number of scalp hair in order to know at what stage of the hair growth cycle they are like this as the initial and final appearance of hair bulbs. The tricogram It is a "snapshot" of the state of the roots or hair bulbs and, therefore, of the scalp at a certain time (Figure 2). Depending on the results, lets know if the hair is renew normally or if there is any alteration of the cycles capillaries In this study, we try to find out if the treatment with the composition described in the present invention is capable of improve the initial tricogram of the scalp and if it produces a improvement in the physiology of the bulbs and hair sheaths. For This is done at the beginning (T0) and at the end of the study (T180). How precondition, each volunteer will not have washed or treated the hair with no cosmetic product at least 48 hours prior to realization of the tricogram, to keep the hair that are near the end of the telogen phase and avoid reduction artificial percentage of telogenic hairs observed in the tricogram The parieto-occipital zone is selected left to make hair taking. Tweezers are placed pean in the part closest to the skin of the scalp and it tracts in the direction of hair growth. The process of traction is repeated as many times as necessary until you get the number of hair needed for the tricogram - between 15 and 25 approx. Immediately after epilation, hair bulbs will mounted on glass slides with the roots parallel to each other others, are fixed with Canada Balm as a transparent medium for microscopy and a coverslip is placed, being ready for microscopic study. This way it is calculated:

A0

number of hair in anagen phase at T0 (before treatment)

T0

number of hair in telogen phase at T0 (before treatment)

% A0

percentage of hair in anagen phase a T0

% T0

percentage of hair in telogen phase a T0

A0 / T0

relationship between hair in anagen phase and in phase telogenous to T0

A180

number of hair in anagen phase a T180

T180

number of hair in telogen phase a T180

% A180

percentage of hair in anagen phase a T180

% T180

percentage of hair in telogen phase a T180

A180 / T180

relationship between hair in anagen phase and in phase telogen to T180

and the results are evaluated taking as reference the tricogram values considered as "normal" in the bibliography consulted. As an example, the efficacy study of the Prodhyhair concentré® asset, of Laboratoires Prod'Hyg, accepts as "normal" a value of anagen / telogen ratio greater than or equal to 4. Consequently, in This study will be considered that the anagen / telogen ratio is normal if A / T \ geq 4.

4. Hair and wash tests

The number of hairs determined is determined detached during hair styling in conditions standardized (test "combing"). It is intended that, after treatment with the composition described in the present invention, the number of hair detached during styling is less than initial. For this, the tests are carried out at the beginning (T0), in the middle (T90) and at the end of the study (T180). As a precondition, the volunteers come to control without having washed their hair at least in the previous 48 hours and without having combed the hair in the 24 hours above, in order to keep the hair that are near the end of the telogen phase and avoid reduction Artificial percentage of hairs in telogen phase. After combing 30 Sometimes the scalp of each volunteer, the hair detached - in the comb and on the comb - are collected for post count. The bibliography shows that in the scalp human shed every day between 30 and 100 hair on average (in function of the amount of hair). Consequently, values higher than the previous ones should be considered anomalous and, for Thus, indicative of a hair loss process. Likewise way, the number of hairs detached during washing hair (test "washing") in conditions Standardized It is intended that, after treatment with the composition described in the present invention, the number of hairs detached during styling is less than the initial. For it each volunteer's scalp and hair is washed detached, both from the wash water and its handling, collect for later count.

Results 5. Observation with microcamera

The photographs obtained from the recordings with microcamera at 70 magnification of the scalp provide valuable information on the regeneration of hair. The comparison of the microphotographs of the same area of the scalp at the beginning (T0) and at the end (T180) of the study allows know if there has been hair regeneration, greater quantity and / or thickness. Figure 1 shows three images of micro cameras that they represent the best results obtained, which coincide with the Tricogram results. In the three selected volunteers, observe more hair at the end of the treatment, it is say, there is higher capillary density. They also show more hair thick and more pigmented.

6. Tricogram

The results of the tricogram at the end of study (T180) shown in figure 2 show that 100% of the volunteers have experienced an increase in the number of hairs in growth phase (anagen phase) after 6 months of application of the composition of the invention; also 12 of the 25 volunteers exceeds 15% increase in anagen phase or growth, one of them exceeding the 25% increase.

7. Hair and wash test

The results of these essays. After 90 days of treatment, 68% of volunteers experience a reduction of hair detached by hairstyle compared to T0. After 180 days of treatment 92% of volunteers experience a reduction in the number of hairs detached by hairstyle. Likewise, in the wash test, after 90 days of treatment 84% of volunteers experience a reduction in the number of hair detached from the moment initial and, after 180 days, 92% experience a reduction in number of hair detached by washing.

Claims (20)

1. Sirtuine activating capillary composition characterized in that it includes a resveratrol component (5 - [(E) -2- (4-hydroxyphenyl) -etenyl] benzene-1,3-diol) and / or oligomers thereof derived from extract of Vitis vinifera vine , milk protein cytokines, lactose, inositol, acetyl cysteine and acetyl methionine, Achillea millefolium extract, Cinchona succirubra extract, Tussilago farfara extract, laminaria algae extract, Alaria esculenta extract and panthenyl ethyl ether / panthenol . 2. Capillary composition according to claim 1, characterized in that it includes 0.001-0.50% acetyl cysteine, 0.001-0.50% acetyl methionine, 0.006-0.50% inositol, 0.001-0.50 % of milk proteins, 0.001-0.50% lactose, 0.006-0.50% panthenyl ethyl ether, 0.01-0.50% Achillea millefolium extract, 0.01-0.50 % of Cinchona succirubra extract, 0.01-0.50% of Tussilago farfara extract, 0.006-0.50 % of Vitis vinifera vine extract, 0.05-1.00% of laminaria algae extract , 0.0075-0.05% of Alaria esculenta extract and 0.05-2.00% of panthenol, the percentages being expressed as% by weight. 3. Capillary composition according to claim 2, characterized in that the proportion of Vitis vinifera extract present in the composition of the invention is equivalent to approximately 0.002-0.02% of a mixture of resveratrol and its oligomers, providing a percentage of trans-resveratrol of approximately 0.0002 - 0.002%. 4. Capillary composition according to claim 1 or 2, characterized in that it also includes solvents, antioxidants, anionic, amphoteric or non-ionic surfactants, conditioning polymers, sequestering agents, preservatives, pH adjusting agents, opacifying agents, viscosity regulating agents , solubilizers and / or perfume. 5. Hair composition according to claim 4, characterized in that as antioxidants it contains ascorbic acid, ascorbyl palmitate and tocopherol. 6. Hair composition according to claim 5, characterized in that the antioxidants are present in the following proportions by weight: ascorbic acid 0.0010-0.01%, ascorbyl palmitate 0.004-0.01% and tocopherol 0.01-0, one%. 7. Capillary composition according to claim 4, characterized in that it includes 90-97% solvents, 0.10-1.00% preservatives, 0.05-0.30% sequestering agents, 0.10- 1.00% solubilizers, 0.01-0.10% pH adjusting agents and 0.10-1.00% perfume. 8. A hair composition according to claim 7, characterized in that the solvents consist of 70-85% water, 10-50% denat alcohol. and 0.50 - 5.0% glycols. 9. Capillary composition according to claim 7, characterized in that the sequestering agents are EDTA-disodium and because the solubilizers are PEG-40-castor oil. 10. Capillary composition according to claim 4, characterized in that the anionic surfactants are included in a weight ratio of 5-10%, the amphoteric surfactants in a weight ratio of 1-5% and the nonionic surfactants in a proportion by weight of 0.5-3%. 11. Capillary composition according to claim 4, characterized in that the conditioning polymers are included in a weight ratio of 0.1 to 2%. 12. Hair composition according to claim 4, characterized in that the sequestering agents are included in a weight ratio of 0.01 to 0.2%. 13. Capillary composition according to claim 4, characterized in that the preservatives are included in a weight ratio of 0.01 to 1.0%. 14. Capillary composition according to claim 4, characterized in that the pH adjusting agents are included in a weight ratio of 0.01 to 0.50%. 15. Capillary composition according to claim 4, characterized in that the opacifiers are included in a weight ratio of 0.1 to 1.0%. 16. Capillary composition according to claim 4, characterized in that the viscosity regulating agents are included in a weight ratio of 0.1 to 1.0%. 17. Hair composition according to claim 4, characterized in that it contains perfume in a weight ratio of 0.1 to 1.0%. 18. Hair composition according to claims 1 to 2 and 5 to 9 characterized in that it is formulated in the form of a hair lotion. 19. Hair composition according to claims 1 to 2 and 10 to 17 characterized in that it is formulated in the form of hair shampoo. 20. Use of the hair composition according to claims 18 and 19 in the form of lotion or hair shampoo to prolong the anagen or growth phase of the hair and thus prevent hair loss and preserve capital capillary.