WO2005007126A1

WO2005007126A1 - Preparation for topical use having an elasticising and shaping effect on skin tissues

Info

Publication number: WO2005007126A1
Application number: PCT/IB2004/002240
Authority: WO
Inventors: Daniela Montanari; Manuela Guglielmo
Original assignee: Gecomwert Anstalt
Priority date: 2003-07-21
Filing date: 2004-07-05
Publication date: 2005-01-27
Also published as: CH693818A5

Abstract

A preparation for topical use for improving and/or increasing the tone of the skin, whose composition comprises: a) a biopolymer obtained from almond protein, b) one or more peptides isolated from an extract of malt, c) one or more polypeptides extracted from the marine alga Sea Lettuce is described.

Description

Preparation for topical use having an elasticlsing and shaping effect on skin tissues.

The invention relates to the field of cosmetic preparations of any form and consistency such as oils, aqueous solutions, water-alcohol solutions, gels, lipogels, ointments, emulsions, pastes, sticks, etc., which are used for topical use, on the face and/or the body, in order to act as a lifting cosmetic, that is to tighten the lines on the face and the body with an elasticising and shaping effect on the skin tissues, acting against the causes which give rise to its loss of elasticity.

Unlike wrinkles which form visible marks on the skin, as lines etched into the surface of the face, loss of elasticity and tone of the skin instead gives rise to lowering and deformation of the lines, the yielding and relaxation of skin tissues, with the epidermis sagging and slack.

In order to respond to the need to overcome the sagging of facial and body lines this invention has been developed by the applicant as the fruit of research into innovative solutions to obtain an effective shaping preparation.

The causes which give rise to loss of elasticity in the skin are more than one in number - mainly age and the resulting physiological slowing of cell activity. With the passage of the years the level of turnover decreases, the replacement of old fibres becomes slower, collagen fibres are fragmented, elastic fibres are disorganised, the skin tissues become more substantial and a progressive diminution in skin tone and elasticity is observed.

Another cause is the force of gravity. When the collagen and elastic web is no longer capable of counterbalancing the force of gravity obvious folds form on the face, and body as well, where the skin sags under the force of gravity.

Finally environmental agents such as the sun or drastic diets give rise to a loss of tone and accentuate expression lines. In particular prolonged exposure to sunlight causes acceleration of the normal process of skin ageing. The damage caused by solar rays occurs mainly at the level of the dermis, where it is the cause of solar elastosis with degeneration of the elastic fibres.

Relaxation of the skin begins to become apparent at around the age of 30. At 40 the line marking the oval of the face softens and becomes wrinkled because of the descent of the cheeks. After 50, following a reduction in the thickness, elasticity and tone of the skin, the cheeks become limp and the skin hangs with vertical folds. At 60 years lines are definitely sagging. The cosmetic preparation representing the invention in question is characterised by properties which make it able to act at various levels with a final combined effect of cosmetic shaping efficiency on the skin tissues. This preparation has been formulated to "stretch" not only the skin of the face but also that of the body; . in fact other parts of the body such as for example the bust, the stomach and the buttocks may suffer from sagging skin.

The beauty of the bust depends on the elasticity and turgor of the skin covering it and which, according to the experts, constitutes a natural brassiere. After the age of 30 the inevitable process of ageing begins with consequent physiological relaxation of the skin tissues, also accelerated by external causes such as a sudden change in weight, excessive exposure to the sun, pregnancy and breast feeding.

Women' s stomachs may undergo many changes due to excess weight, unbalanced diets, pregnancy, etc. The skin tissues relax, the profile becomes deformed and drooping. The skin of the buttocks covers but also supports the muscular mass of this part of the body. Their tone and firmness also depends on the turgor of the skin. The preparation to which the invention relates is, as mentioned, designed to act on the skin tissues with an elasticising and shaping effect as a "lifting cosmetic". In order to be able to offer a fully acting "lifting cosmetic" the inventors have identified an association between three active ingredients which are designed to act on the three levels of the skin, with an effective combined synergistic shaping effect. Our skin comprises three zones which are fundamental for the health and nutrition of the skin: epidermis, the dermal-epidermal junction, and the dermis. These zones undergo changes which become increasingly marked over time .

The inventors have therefore formulated the preparation according to the invention for age bands from 30 to 60 years with increasing doses of the 3 main tensioning and toning ingredients, each of which is specific for one of the 3 zones. It is in fact possible to speak of a surface action, or action on the epidermis, a median action, or action on the dermal-epidermal junction, and a deep action, or action on the dermis. The epidermis is a tissue comprising cells with rapid turnover which starts with the mitotic activity of the germinating cells in the basal layer.

The structure - and the function - of the dermal- epidermal junction between the epidermis and the dermis, which does not have any cells, and which is of a glycoprotein nature, and performs the fundamental task of stabilising adhesion between the two tissues, regulating exchanges between them, but also supporting the overlying epidermis, is of particular importance. The dermal-epidermal junction acts as a physical and elastic support for the epidermis; during the ^■ ageing process it becomes progressively thinner and this causes relaxation of the skin. - -

The uppermost part of this junction comprises a lamina, known as the basal lamina, which adheres to the membranes of the germinating cells in the epidermis and comprises a non-collagen glycoprotein known as "laminin". The latter is a large molecule consisting of 5 subunits in a cruciform arrangement. The dermis comprises the matrix supporting the skin. It is substantially formed of cells (the fibroblasts) surrounded by fibres (organised in networks of collagen and elastic fibres) and a fundamentally amorphous substance produced by these cells (the extracellular matrix) .

Collagen fibres are high strength fibres; in fact their ultimate tensile strength is close to that of steel. The elongation (deformation) of the fibre is small (2%) ; collagen does not therefore have elastic properties .

The elastic fibres run separately, branching and anastomosing, forming a network. They can be easily extended, returning to their original length when the tensile force ceases, but they are much less strong than collagen fibres; chemically they are formed of elastin. The main active ingredients in the preparation according to the invention have therefore been selected to act on each of these in one of the three zones just described.

The methods of action of the main active ingredients are described below. An almond protein biopolymer exercises a surface action on the epidermis, molecules extracted from malt act on the median zone and an active ingredient of maritime origin instead has a deep action on the dermis. The synergistic action of the 3 main active ingredients on the three levels of the skin provides a treatment which is capable of combating the sagging of facial and body lines .

In order to act on the surface of the epidermis the inventors have used a biopolymer obtained from almond protein. It comprises a three-dimensional network of high molecular weight proteins (over 500,000 Daltons) which are adsorbed onto the surface of the skin forming a continuous elastic film having an immediate lifting effect. This network is obtained through the formation of cross-linking - with the help of a polymerising agent - between monomers having dimensions, a structure and solubility which are perfectly defined, selected and controlled through the enzyme hydrolysis of almond proteins. The main production stages in obtaining this active ingredient are the following:

- solubilisation of ground almonds

- controlled enzyme hydrolysis

- separation of the soluble and insoluble phases by filtration

- polymerisation of the soluble phase

- ultrafiltration

- sterilising filtration

A description of the aminogram of the biopolymer is provided below: lysine 7.45%, arginine 7.95%, histidine 2.92%, aspartic acid 15.90%, glutamic acid 15.43%, tyrosine 3.55%, phenylalanine 5.18%, proline 5.07%, glycine 3.98%, threonine 3.48%, serine 5.36%, alanine 4.65%, isoleucine 5.12%, leucine 5.98%.

The viscoelastic film which forms on the skin represents a comfortable soft support which reinforces the lifting effects on the underlying zone. The immediate tensioning effect of the active ingredient has been evaluated using a Cutometer, an instrument which links the increase in skin elasticity with the increase in a number of numerical parameters. The measurements were made on the skin of 12 volunteers before application of a placebo and the tensioning polymer, and 2 hours afterwards. An increase of 12.1% in the parameters correlated with skin elasticity was found on skin to which the active ingredient had been applied, while the placebo caused an increase of 7.1%. Particular peptides extracted from malt which have been biotechnologically modified are responsible for the median action of the preparation. The amino acid composition of this active ingredient is provided below: hydroxyproline 0.6%, asparagine 10.48%, threonine 3.02%, serine 4.55%, glutamine 20.11%, proline 8.92%, glycine 9.56%, alanine 7.50%, valine 6.57%, methionine 1.39%, isoleucine 4.12%, leucine 7.71%, tyrosine 1.81%, phenylalanine 4.05%, histidine 2.06%, hydroxylysine 0.26%, lysine 3.34%, arginine 3.94%. The biopeptides generated by bacterial conversion acquire specific biological activities which render them capable of acting as cell messengers for the cells synthesising laminin, stimulating them to produce these glycoproteins . The increase in the presence of laminin, which decreases with age, helps to increase the strength and tone of the epidermis. In order to evaluate the activity of this active ingredient in vitro tests were performed on reconstructed mature skin; it was found that the presence of the active ingredient in the culture medium caused a 61% increase in the production of laminin in comparison with placebo after 14 days incubation. Display techniques using florescence microscopy have demonstrated that the active ingredient penetrates the skin. This active ingredient is therefore capable of compensating for the reduced synthesis of laminin, one of the key molecules involved in bonding between the dermis and epidermis. Strengthening this adhesion ensures a solid base and firmness for the skin.

The structures which support the skin are as already described to be found in the dermis. In order to provide support for the skin tissues the inventors have considered it necessary to act at this depth with an active ingredient of maritime origin having a composition very similar to elastin. The source of this active ingredient is the marine alga Sea Lettuce from which polypeptides (present in the structure of the alga in a quantity of approximately 77%) , whose composition is very similar to elastin, have been extracted.

This green alga (Ulva lactuca) appears to be extremely fragile, but its fronds are very strong specifically because of the presence of a network of elastic fibres similar to that in humans. Because of this network it has sufficient elasticity not to be affected by hydrostatic pressure and resist the fury of the sea. The main stages in production for obtaining the active ingredient are as follows:

- washing

- grinding

- microgrinding

- specific extraction - concentration

- atomisation

This active ingredient is multifunctional; it is in fact capable of encouraging the cellular regeneration of fibroblasts, increasing the utilisation of cell energy, stimulating protein synthesis, encouraging the new synthesis of collagen recompacting the extracellular matrix of the dermis and combating the degradation of elastin with an anti-elastase effect. Through the action of the sun and specific enzymes known as elastases the elastic fibres degenerate, become disorganised and form scattered masses giving rise to a loss of elasticity in the skin. The active ingredient extracted from the alga Sea Lettuce has anti-elastase activity, that is it inhibits the enzyme activity of elastases as a result of the changes which it induces in the conformation of the enzyme, thus protecting the elasticity of the supporting fibres. It is therefore clear that it has a fully regenerative activity on the supporting structures, which is reflected in visibly more supported skin tissues.

The inventors envisage that these three active ingredients will be used in products for both the face and the skin, in increasing doses depending upon the age range being treated. In formulations for the body the inventors suggest that a specific plant extract should also be included for each zone treated.

Some plant extracts which have advantageous effects on particular zones of the body will be provided by way of example .

The preparation for the bust may be enriched by extract of Equisetum, because of its elasticising properties and the improvement of the nutrition of the skin in that zone.

Echinacea extract may be useful for use on the skin of the stomach because of its toning action on relaxed skin tissues.

The formulation for the buttocks may be enriched with Centella extract which is useful for tissue nutrition and also because it helps to optimise skin elasticity.

The subject matter of this invention is therefore a preparation for topical use as described in appended claim 1.

Some preferred embodiments whose composition, as will be seen, has been modified in a "targeted" way in order to selectively obtain an increase and improvement in the tone of the skin covering particular parts of the body will now be described in greater detail.

In a preferred embodiment the preparation according to the invention has a composition comprising:

- between 0.001 and 4% of the said almond protein biopolymer, - between 0.001 and 4% of the said peptides isolated from a malt extract, between 0.001 and 4% of the said polypeptides extracted from the marine alga Sea Lettuce. The preparation so obtained makes it possible to achieve an improvement in the elasticity of the skin of the face, as has been demonstrated by the previously mentioned tests, combating sagging of the lines, but may also be equally effective regardless of the part of the body to which it is applied. In a second embodiment of the preparation according to the invention Equisetum extract is added to the base preparation previously described in an amount of between 0.05 and 5% of the total weight of the composite preparation so obtained. A numerical example is provided below for greater clarity. If 100 grams of the base preparation mentioned above containing 0.001 to 4 g of almond biopolymer, 0.001 to 4 g of peptides extracted from the alga Sea Lettuce and from 0.001 to 4 g of peptides isolated form a malt extract are obtained and 0.05 to 5.3 g of Equisetum extract are added to it then 100.05 - 105.3 g of a composite preparation especially favouring elasticisation of the skin is obtained and, as mentioned, is particularly suitable for application to the skin of the bust.

If in a similar way to that first illustrated Echinacea extract is added to the base preparation in an amount from 0.05 to 5% of the total weight of the composite preparation so obtained, a composition is obtained which, as expected, proved to be particularly suitable for obtaining the best effects when applied to the skin of the stomach.

If finally, still proceeding as stated above, Centella extract is added to the base preparation in an amount between 0.05 and 5% of the total weight of the composite preparation so obtained, a composition which is particularly suitable for achieving the best results when applied to the skin of the buttocks is obtained. Of course other composite preparations of the type described above containing other extracts of plant origin which are suitable for parts of the body other than those considered hitherto may also be prepared. It is however pointed out that, although the composite preparations described above obtain the best results of the "targeted" type on the skin covering particular parts of the body, application of the preparation to the face as described in claim 1 nevertheless achieves more than satisfactory effects on the elasticity and tone of the skin tissues in this area.

Claims

Clai'ms

1. Preparation for topical use suitable for improving and/or increasing the elasticity of the skin and for application in increasing doses according to age, comprising three active ingredients targeted to act on the skin at three levels, having a combined effective shaping effect, characterised in that its composition comprises: a) a biopolymer obtained from almond protein for surface action on the epidermis; b) one or more peptides isolated from a malt extract for median action at the dermal-epidermal junction, c) one or more polypeptides extracted from the marine alga Sea Lettuce for deep action in the dermis.

2. Preparation according to claim 1, in which: d) the said biopolymer obtained from almond protein is present in a concentration between 0.001 and 4% by weight, e) the said one or more peptides isolated from an extract of malt are present in an amount between 0.001 and 4% by weight, f) the said one or more polypeptides extracted from the alga Sea Lettuce are present in an amount between 0.001 and 4% by weight.

3. Preparation according to any one of the preceding claims, in which Equisetum extract is added in an amount between 0.05 and 5% of the total weight of the preparation.

4. Preparation according to one of claims 1 or 2, in which Echinacea extract is added in an amount between 0.05 and 5% of the total weight of the preparation.

5. Preparation according to either of claims 1 or 2, in which Centella extract is added in an amount between 0.05 and 5% of the total weight of the preparation.

6. Preparation according to one of the preceding claims, in which the said biopolymer obtained from almond protein has the following aminogram: lysine 7.45%, arginine 7.95%, histidine 2.92%, aspartic acid 15.90%, glutamic acid 15.43%, tyrosine 3.55%, phenylalanine 5.18%, proline 5.07%, glycine 3.98%, threonine 3.48%, serine 5.36%, alanine 4.65%, isoleucine 5.12%, leucine 5.98%.

7. Preparation according to one of claims 1 to 5, in which the said peptides isolated from a malt extract have the following amino acid composition: hydroxyproline 0.6%, asparagine 10.48%, threonine 3.02%, serine 4.55%, glutamine 20.11%, proline 8.92%, glycine 9.56%, alanine 7.50%, valine 6.57%, methionine 1.39%, isoleucine 4.12%, leucine 7.71%, tyrosine 1.81%, phenylalanine 4.05%, histidine 2.06%, hydroxylysine 0.26%, lysine 3.34%, arginine 3.94%.