MC2394A1 - Composition intended to stop the fall and / or to promote - Google Patents

Description

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The present invention relates to a composition intended for application to the hair, eyelashes and nails, to promote growth, stop hair loss, in particular of hair, and, according to the individuals who use this composition, to promote the regrowth of said 5 hairs (hair, eyelashes and nails).

The composition essentially comprises a lipid product based on a mixture of fatty acid triglycerides. This composition is intended for extravascular application, the application of which is facilitated and the efficacy improved. 10 Japanese document number 1,425,610, which is an extension of French patent application FR-A-1,442,280, proposes a process for obtaining a substance with beneficial activity on hair growth, which consists of taking from the body of a freshly slaughtered mane-bearing animal the subcutaneous fatty tissue 15 from the implantation of said mane, and extracting from said tissue said substance, in the form of a semi-fluid fat at normal room temperature, which is soluble, at least when heated and for the most part, in 95% ethyl alcohol and which is devoid of cellular and protein matter.

20 This technique made it possible to obtain an interesting substance, without knowing precisely which molecules or compositions were actually active and, therefore, without any possibility of optimizing its physical and chemical properties.

Although effective, this composition has two drawbacks. These two drawbacks are as follows.

On the one hand, this oily substance must be applied directly to the hair, scalp or i-

nails. While this practice is fairly well accepted in some countries, consumers in some Western countries are more reserved. The present invention makes it possible to have active substances, similar to those described in Japanese document number 1,425,610, which is an extension of French patent application FR-A-1,442,280, which are encapsulated, giving them a non-greasy consistency.

35 On the other hand, the application of this composition to the hair and scalp complicates the in vivo fate of the active ingredient by systematically introducing an entry step into the organism characterized by the concept of

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Bioavailability, that is, the measurement of the intensity and speed of drug availability. This bioavailability depends on the physicochemical properties of the administered molecules, but also on the route of administration used and the pharmaceutical form used for administration.

The present invention eliminates these two drawbacks; its purpose is to facilitate this entry step and to improve the effectiveness of the lipid product by adding other active ingredients.

10 To this end, the present invention relates to a composition intended to stop the loss and/or promote the regrowth of hair, which is formed of a lipid product, itself consisting of a mixture of triglycerides of fatty acids having twelve to twenty carbon atoms, the fatty acids being able to be saturated or unsaturated; the composition is intended for extravascular application, characterized by the fact that the lipid product is enclosed in liposomes for better penetration of cells and a progressive and delayed action, and that the composition also comprises nanoparticle matrix vectors containing a mixture of silanol and acetyl-methionine for a progressive and targeted action.

It may contain a mixture of:

- 3-aminopropanesulfonic acid, also known as homotaurine,

- a bacterial filtrate based on peptones, and

25 - an extract of a water-soluble sulfated polysaccharide complex.

It may also contain D-panthenol.

It may also contain microemulsions of vitamins i

A and/or E.

30 On the one hand, vitamin A is esterified into palmitate, and on the other hand, vitamin E is esterified into acetate.

The total mass of the composition comprises:

- 3 to 5% of liposomes containing the lipid product,

- 2 to 4% of silanol and d1-acetylmethionine enclosed in 35 nanoparticle matrix vectors,

- 3 to 5% of the homotaurine mixture - bacterial filtrate - sulfated polysaccharides,

- 0.3 to 1% D-panthenol,

- 2 to 4% vitamin A microemulsion, and/or

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- 2 to 4% vitamin E microemulsion,

the complement being made up of excipient(s).

More specifically, the total mass of the composition comprises:

- 4% liposomes containing the lipid product,

5-3% of silanol and acetylmethionine enclosed in nanoparticle matrix vectors,

- 4% of the homotaurine mixture - bacterial filtrate - sulfated polysaccharides,

- 0.6% D-panthenol,

10-3% vitamin A microemulsion, and/or

- 3% vitamin E microemulsion,

the supplement consists of 1 alcohol-free excipient(s).

The fatty acids of the triglycerides, constituting the lipid product, are unsaturated in a proportion of 60 to 70% and saturated in a proportion of 30 to 40%.

The fatty acids of triglycerides, which constitute the lipid product, are made up of carbon chains:

- eighteen carbon atoms in 45 to 65% of cases,

- with sixteen carbon atoms in 28 to 40% of cases,

20 - with fourteen carbon atoms in 4 to 5% of cases, and

- to twelve, fifteen, seventeen, nineteen and/or twenty carbon atoms in the remaining cases.

Nanoparticle matrix vectors consist of an inorganic silica matrix, forming a polar and porous network, which acts with polarized areas on the surface of target cells.

The present invention relates to a composition intended to stop the loss and/or promote the regrowth of hair appendages such as hair, which is essentially formed of a lipid product and nanoparticulate matrix vectors.

triglycerides of fatty acids having twelve to twenty carbon atoms. However, it may also contain, possibly, other types of glycerides, such as monoglycerides, in small quantities.

Fatty acids can be unsaturated or non-saturated.

In fact, the fatty acids that make up triglycerides are unsaturated in a proportion of 60 to 70%, and of course, are saturated in a proportion of 30 to 40%.

This lipid product consists of a mixture of

They are also composed of carbon chains with eighteen carbon atoms in 45 to 65% of cases, sixteen carbon atoms in 28 to 40% of cases, fourteen carbon atoms in 4 to 5% of cases, and finally, twelve, fifteen, seventeen, nineteen, and/or twenty carbon atoms in the remaining cases, corresponding to very small proportions. It is always possible to find acids with a different number of carbon atoms in residual quantities.

In a preferential mode of constitution of fatty acids 10 forming triglycerides, fatty acids with eighteen carbon atoms are unsaturated by two or three double bonds, while fatty acids with sixteen carbon atoms are unsaturated by one double bond.

These fatty acids come mainly from the oil of 15 horsehair buns.

This horsehair oil is characterized by the presence of five main fatty acids which mostly contain either sixteen or eighteen carbon atoms.

Acids with an odd number of carbon atoms, namely 20, 15, 17 and 19, are very few in number, as are branched fatty acids of iso or ante-iso form.

This composition is intended for extravascular application, for example by superficial application to the hair and scalp.

25 Moreover, it finds preferential application in the context of androgenetic seborrheic alopecia, but also in acute diffuse alopecia of reactive origin.

In fact, the lipid product is enclosed in liposomes i'

which have the role of improving its penetration into cells and delaying its stimulatory action.

The main advantage of using liposomes lies in their nature and size.

Thus, the liposome is a microscopic lipid vesicle that possesses a dual potential.

35 On the one hand, it is a reservoir of an active ingredient, thus isolating and protecting it from an aggressive biological environment. This active ingredient is, of course, the lipid product which will subsequently be called the natural hair activator, or NPA (registered trademark).

On the other hand, it carries the active ingredient and allows it to reach biological sites that were previously difficult to access, due to the physico-chemical properties of the administered molecule.

In pharmacokinetic terms, liposomes could therefore 5 act on the in vivo fate of the active ingredients they contain and carry, first by improving bioavailability for a given route of administration, and second by significantly modifying tissue distribution, allowing for better targeting to biological sites of activity. 10 The incorporation of the natural hair growth activator into

The interior of the liposome helps to mask its physicochemical properties and to isolate it from chemical and/or enzymatic degradation.

We will not revisit the preparation methods for the 15 liposomes, which are already well-established in the prior art. However, in practical terms, liposomes obtained by dispersing natural, water-insoluble polar lipids can be used.

For example, soy phospholipids are essentially 20% composed of phosphoglyceride and can be used in this case.

Furthermore, liposomes can be selected based on whether they are unilamellar or multilamellar, depending on the desired latency period for the natural activator of the 25 hair follicles trapped within the liposome. The thicker the liposome wall, the more the active ingredient will be delayed in its action.

Nevertheless, it is useful to have an action that is more

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Faster, more immediate. To achieve this, 30% of the natural activator of hair follicles is used in conjunction with nanoparticle matrix vectors containing methiosilane. Thus, cosmetology, like pharmacology, must meet increasing demands, particularly regarding the specificity of active ingredients. Part of the research effort has been directed towards the synthesis of more specific active molecules.

Solutions have also been provided by innovations, particularly in pharmaceutical formulation, and notably by so-called "controlled-release" systems. Their ability to modify the release of active ingredients allows, on the one hand, for a longer shelf life.

"This not only achieves the desired effects but also reduces undesirable side effects. This helps prevent overdoses, as the delivery of the active ingredient is better distributed by improving its bioavailability.

5 All these qualities are essential for the cosmetician.

Nanoparticle matrix vectors, containing a mixture based on silanol and acetylmethionine, form the third generation of release systems which is based on a new advantage that complements sustained release. 10 This is targeting.

These new vectors are capable of binding to specific sites from which the active ingredient, methionine, is progressively released. This targeting is expressed, in fact, in terms of affinities.

15 In the case of the present invention, the nanoparticulate matrix vectors consist of an inorganic silica matrix forming a polar and porous network which acts with the polarized areas on the surface of the target cells.

Similarly, nanoparticle matrix vectors, 20 associated with silanol and acetylmethionine, allow for the targeting of the cells to be treated. Due to their much smaller size compared to liposomes and their targeted action, matrix vectors have a more precise and complementary effect on other cells.

25 In addition, the released methionine is directly and more rapidly assimilated by the target cells.

It is therefore easy to understand that the composition, according to the invention, will have a more complete action, whether in place of

and in duration. It essentially combines the natural activator of the 30 hair follicles trapped within liposomes for optimized action and better penetration into the cells to be treated.

The composition also includes a mixture made up of the combination of three components.

The first component consists of 3-aminopropane 35 sulfonic acid, with the formula:

NH2-CH2-CH2-CH2-SO3H.

This acid is more simply called homotaurine. It is derived from taurine.

Taurine is one of the most abundant free amino acids in mammalian tissues. This amino acid, not encoded by the genetic code, is also found in nerve axons. Among other properties, taurine exerts a protective and stabilizing influence on cell membranes, protecting their permeability and acting as an osmoregulator. It also protects against oxidants and free radicals.

Homotaurine is a synthetic molecule not found in animal tissues. It possesses certain properties that differ from taurine. Furthermore, homotaurine is an analog of gamma-aminobutyric acid (GABA), in which the sulfonic acid group -SO3H is replaced by a carboxylic acid group -CO0H.

Homotaurine is described as a molecule with a hypotensive effect, acting by blocking vasoconstriction and increasing blood flow. This property allows for better blood flow to the scalp.

Finally, homotaurine plays a role as a cellular transporter of certain metal ions, such as calcium, magnesium, and possibly other ions. The role of sodium, potassium, manganese, copper, and zinc ions is currently being extensively studied in certain metabolic disorders accompanied by skin and/or scalp symptoms.

The second component of this mixture consists of a bacterial filtrate obtained from a strain of microorganisms i

cultivated in a specific medium, which induces the secretion of 30 metabolites with stimulatory activity.

The base medium consists of selected peptones; the ingredients of the culture medium are chosen to direct metabolic pathways.

The bacterial filtrate is, in fact, obtained after decantation, 35 filtration and purification and is mainly rich in peptides.

The third and final component of this mixture is an extract of a sulfated polysaccharide complex that is soluble in water.

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Sulfumopolysaccharides play an essential role in the hygiene of the hair follicle, particularly in the regulation of sebaceous secretions.

More specifically, it is a complex of 5-sulfated polysaccharides that are soluble in water, which is present in connective tissue and synovial fluid.

The composition intended to stop hair loss and/or promote the growth of hair and nails may also contain D-panthenol, with the formula:

10 CH20H-C(CH3)2-CH0H-C0-NH-(CH2)2-CH2OH.

D-panthenol is an essential element for hair growth and a dual-action hair fortifier.

First, it has a stimulating effect on the hair bulb. When applied to the scalp, D-panthenol penetrates, is converted into pantothenic acid, and is preferentially deposited in the hair matrix. At this level, the multiplication of matrix cells consumes a large amount of oxygen and glucose. This energy metabolism is governed by the Krebs cycle, in which pantothenic acid plays a role.

Next, an action at the level of the hair fiber, with a volumizing effect, a repairing effect and a moisturizing effect.

The composition includes, depending on the case, microemulsions of vitamin A and/or vitamin E. It is, in fact, 25% vitamin A palmitate and vitamin E acetate in microemulsified form.

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Microemulsification enhances the properties of these vitamins.

As for vitamin A, its properties include protective action on the superficial stratum corneum of the epidermis, prevention of excessive desquamation and capillary fragility, combating hyperkeratinization, and finally, promoting tissue regeneration.

As for vitamin E, it has an action at level 35 of neutralizing activity on free radicals, increasing cutaneous microcirculation, anti-inflammatory activity and moisturizing function.

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The total mass of the composition is between 3 and 5% for liposomes containing the lipid product or natural activator of hair, 2 to 4% of silanol and acetyl-methionine enclosed in nanoparticle matrix vectors, 3 to 5% of the homotaurine - bacterial filtrate - sulfated polysaccharide mixture, 0.3 to 1% of D-panthenol, 2 to 4% of vitamin A microemulsion, and/or 2 to 4% of vitamin E microemulsion, the remainder being made up of alcohol-free excipient(s).

In practice, the total masses are chosen precisely from the average of the values that have just been given.

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Claims (10)

DEMANDS 1. Composition intended to stop hair loss and/or promote regrowth of hair and nails, which is formed of a lipid product, itself composed of a mixture of fatty acid triglycerides 5 having twelve to twenty carbon atoms, the fatty acids may or may not be saturated; the composition is intended for extravascular application, characterized by the fact that the lipid product is enclosed in liposomes for better cell penetration and a progressive 10 and delayed action, and that the composition also includes nanoparticulate matrix vectors containing a mixture of silanol and acetyl-methionine for a progressive and targeted action. 2. Composition according to claim 1, characterized by the 15. The fact that it contains a mixture: - 3-aminopropanesulfonic acid, with the formula: NH2-CH2-CH2-CH2-SO3H said homotaurine 20 - a bacterial filtrate based on peptones, and - an extract of a water-soluble sulfated polysaccharide complex. 3. Composition according to any one of claims 1 or 2, characterized by the fact 25 that it contains D-panthenol. 4. Composition according to any one of claims 1 r at 3, characterized by the fact that it contains microemulsions of vitamins A and/or E. 5. Composition according to claim 4, characterized by the 30. The fact that vitamin A is esterified into palmitate, and/or that vitamin E is esterified into acetate. 6. Composition according to any one of claims 1 to 5, characterized by the fact 35 that the total mass of the composition comprises: - 3 to 5% of liposomes containing the lipid product, - 2 to 4% of silanol and acetyl-methionine enclosed in 11 nanoparticle matrix vectors, - 3 to 5% of the homotaurine mixture - bacterial filtrate - sulfated polysaccharides, - 0.3 to 1% D-panthenol, 5 - 2 to 4% vitamin A microemulsion, and/or - 2 to 4% vitamin E microemulsion, the complement being made up of excipient(s). 7. Composition according to any one of claims 1 to 6, characterized in that the total mass of the composition comprises: - 4% liposomes containing the lipid product, - 3% of silanol and acetyl-methionine enclosed in nanoparticle matrix vectors, - 4% of the homotaurine mixture - bacterial filtrate - 15 sulfated polysaccharides, - 0.6% D-panthenol, - 3% vitamin A microemulsion, and/or - 3% vitamin E microemulsion, The supplement consists of alcohol-free excipient(s). 20 8. Composition according to claim 1, characterized in that the fatty acids of the triglycerides, constituting the lipid product, are unsaturated in a proportion of 60 to 70% and saturated in a proportion of 30 to 40%. 25 9. Composition according to any one of claims 1 or 8, characterized by the fact that the fatty acids of the triglycerides, constituting the lipid product, are made up of carbon chains: i - eighteen carbon atoms in 45 to 65% of cases, 30 - sixteen carbon atoms in 28 to 40% of cases, - with fourteen carbon atoms in 4 to 5% of cases, and - to twelve, fifteen, seventeen, nineteen and/or twenty carbon atoms in the remaining cases. 10. Composition according to any one of claims 1, 35, 6 or 7, characterized in that the nanoparticulate matrix vectors consist of an inorganic silica matrix, forming a polar and porous network, which interacts with polarized areas on the surface of target cells. tPai- Profcuragppr^ Raved words: null A Amâ,r(: '?f,Lhi lle?nne' Added words: null [' cîHirî" Public Limited Company Laboratories A^FPTA