WO2007003658A1

WO2007003658A1 - Composition in the form of a lipogel for cosmetic, cleansing and pharmaceutical use

Info

Publication number: WO2007003658A1
Application number: PCT/EP2006/063941
Authority: WO
Inventors: Palmiro Comini; Stefano Ravasio
Original assignee: Maycos Italiana Di Comini Miro & C. S.A.S.
Priority date: 2005-07-06
Filing date: 2006-07-06
Publication date: 2007-01-11
Also published as: EP1917075A1; ITMI20051273A1

Abstract

The present invention relates to a composition in the form a lipogel containing at least one lipophilic substance chosen from vegetable oils, synthetic triglycerides and liposoluble vitamins, at least one lipoprotein, at least one lipo-amino acid, and between 10% and 50% by weight of water.

Description

COMPOSITION IN THE FORM OF A LIPOGEL FOR COSMETIC, CLEANSING AND PHARMACEUTICAL USE

FIELD OF THE INVENTION The present invention relates to a hydrolipid composition containing at least one lipophilic substance chosen from vegetable oils, synthetic triglycerides and liposoluble vitamins, at least one lipoprotein and at least one lipo-amino acid. STATE OF THE ART Products for topical use, such as cleansing and body care products, are increasingly causing the consumer to exhibit allergies, itching, irritation, redness, skin dryness and general skin incompatibility.

Consequently, during the last few years research in the field of compositions for topical use, whether cosmetic or pharmaceutical, has focused on obtaining products with high toxicological and tolerability profiles based for example on substances of vegetable origin such as proteins, lipoproteins, amino acids, lipo- amino acid and lipids in general.

Amino acid and protein derivatives, for example, have demonstrated their value in reducing the deproteinizing effect of classical anionic surfactants present in cleansing preparations. However, the problem of excessive skin delipidization caused by synthetic surfactants still remains to be solved.

To this end, the use of native vegetable oils is ideal since these substances are similar to the natural lipid system of the skin. Their usage is rendered problematic, however, by their being strongly lipophilic and difficult to incorporate into traditional formulations for topical use. Furthermore, these substances have a strong ability to knock down foam so are therefore not suitable for use in cleansing formulations.

To overcome these drawbacks a number of concerns have made these oils (wheat, shea, soya, olive etc.) hydrophilic by oxyethylenation of the molecule. It is evident that these hydrophilic oils have lost all their natural molecular structure and are hence true non-ionic surfactants that can themselves cause skin irritation. SUMMARY OF THE INVENTION The present inventors have now surprisingly found that lipophilic substances such as vegetable oils, synthetic triglycerides and liposoluble vitamins can be rendered hydrophilic by their interaction under suitable conditions with lipoproteins and lipo- amino acids, giving rise to a lipogel having a high content of said lipophilic substances and able to produce, by diluting with water, highly stable dispersions which are non-viscous at high dilutions.

It has also been observed that, despite the high content of lipophilic substances, the aforesaid lipogel and its dilutions are able to spontaneously produce foam, thus resolving the foam knock down problem that is typical of vegetable oils when used with surfactants in cleansing products. Therefore, the present invention provides a composition in the form of a lipogel that contains at least one lipophilic substance chosen from vegetable oils, synthetic triglycerides and liposoluble vitamins, at least one lipoprotein and at least one lipo-amino acid. Further aspects of the present invention are processes for the preparation of said composition and products for cosmetic and/or cleansing or pharmaceutical use containing the aforesaid composition. DETAILED DESCRIPTION OF THE INVENTION

The present invention relates to a composition in the form of a lipogel containing at least one lipophilic substance chosen from vegetable oils, synthetic triglycerides and liposoluble vitamins, at least one lipoprotein, at least one lipo-amino acid and water in a quantity between 10% and 50% by weight, preferably between 10% and 20% by weight

The aforesaid composition preferably presents a weight ratio of total quantity of lipoprotein(s) and lipo-amino acid(s) to lipophilic substance(s) of between 1 :40 and 3:10, even more preferably between 3:40 and 1.6:10.

In accordance with a particularly preferred embodiment the lipophilic substance is chosen from natural oils of vegetable origin. Particularly preferred vegetable oils include those chosen from the group consisting of coconut oil, rice oil, sweet almond oil, maize oil, sunflower oil, rapeseed oil, avocado oil, macadamia oil, borage oil, jojoba oil and peanut oil.

As an alternative either to the aforesaid oil or in combination thereof, the composition of the invention can contain liposoluble vitamins such as vitamin A acetate, vitamin A palmitate, vitamin F and vitamin E acetate. The lipogel of the invention also contains at least one or more lipoproteins obtained by acylation of proteins, preferably hydrolysed proteins of vegetable origin. Said proteins of vegetable origin are preferably obtained from wheat, soya, rice, barley, pea, maize, lupin, potato or almond. The acylation of these proteins is preferably conducted with one or more fatty acids chosen from C₈-C₃₂ alkyl fatty acids and fatty acids contained in the aforesaid vegetable oils and synthetic triglycerides.

The lipo-amino acid(s) contained in the composition in lipogel form of the invention, are obtained by acylation of amino acids preferably with one or more fatty acids chosen from C₈-C32 alkyl fatty acids and fatty acids contained in the aforesaid vegetable oils and synthetic triglycerides.

For example, the lipo-amino acids of the invention can be obtained from amino acids such as sodium glutamate, glutamic acid, alanine, valine, leucine, isoleucine, proline, phenylalanine, tryptophan, methionine, glycine, serine, threonine, cysteine, tyrosine, asparagine, glutamine, aspartic acid, lysine, arginine, histidine by reaction with the vegetable fatty acids of coconut, palm, soya and with octanoic, decanoic, lauric, myristic, palmitic, stearic, linoleic, linolenic, behenic, erucic acids, etc.

Furthermore, the lipoproteins and lipo-amino acids used for preparing the composition of the invention can have the same qualitative fatty acid composition and can therefore be obtained by the simultaneous acylation of a mixture of amino acid(s) and protein(s) with fatty acids.

In accordance with a further embodiment of the present invention, the lipogel composition of the invention can also comprise, in addition to the aforementioned components, phospholipids, ceramides, sterols, sugars and trace elements, preferably so as to represent the qualitative composition of the natural hydrolipid acid mantle of the skin. These substances can be added either during the lipogel preparation phase or at its end, resulting in a composition having emollient and elasticising properties. The lipogel of the present invention is prepared by a process comprising the following steps: a) preparing a mixture comprising at least one lipophilic substance chosen from vegetable oils, synthetic triglycerides and liposoluble vitamins, at least one lipoprotein, at least one lipo-amino acid and water in a quantity between 10% and 50% by weight, preferably between 10% and 20% by weight; and b) homogenising the mixture from step a) until a lipogel is obtained. The mixture from step a) preferably contains the aforesaid components in a quantity such that the weight ratio of the total quantity of lipoprotein(s) and lipo- amino acid(s) to the quantity of lipophilic substance(s) is between 1 :40 and 3:10, preferably between 3:40 and 1.6:10.

Preferably, the aforesaid process is conducted at a temperature between 50 and

7O⁰C.

The agitation speed at which the homogenisation is conducted depends on a series of variables such as the type of homogenizer used and the composition and temperature of the mixture. In particular, the higher the temperature the less mechanical energy is required and therefore less agitation speed will be necessary for lipogel formation.

Usually, however, the homogenisation is conducted at a minimum agitation speed of 500 revolutions per minute. To begin with, homogenisation results in the formation of lipogel agglomerates of the substances. By persisting for a few more minutes with vortex agitation a compact lipogel structure results.

The lipogel of the invention can be diluted with water in a quantity sufficient to render it easily processable, obtaining stable dispersions from translucent to milky depending on degree of dilution. At high dilution these dispersions lose viscosity. Therefore, a further aspect of the present invention are aqueous dispersions of said lipogel composition, obtained by diluting said composition in water. The lipogel compositions or the aqueous dispersions of the invention can be used as such, or, alternatively, in combination with dermatologically acceptable excipients in traditional formulations for topical use.

The preparations obtained are more hydrating, more emollient and feel more pleasant on the skin than the corresponding preparations not containing the lipogel or the dispersions of the invention. Indeed, the cosmetic performance of the composition of the invention is unique and exceptional in terms of cosmetic feel, skin hydration and skin emollience.

Therefore, a further aspect of the present invention are formulations for topical use comprising the lipogel composition or the aqueous dispersions of the invention, optionally in combination with dermatologically acceptable excipients. The aforesaid formulations can be for cosmetic and/or cleansing and/or pharmaceutical use and can, for example, be in the form of a cream, milk, emulsion, gel, bath foam etc.

The formulations for pharmaceutical use obviously comprise, in addition to the lipogel or the dispersion of the invention, a pharmaceutical active principle and, optionally, dermatologically acceptable excipients.

In short, the formulations of the invention satisfy all the requirements of the field of preparations for topical use, in that the liposoluble vitamins, vegetable oils, synthetic triglycerides, lipoproteins and amino acids are skin compatible substances and safe from the toxicological viewpoint. The possibility of diluting the lipogel composition of the invention in water to obtain stable non-viscous dispersions also makes it suitable for use as such or in combination with suitable excipients in nebulizers as sprays, for example sun spray. Therefore the present invention also relates to a spray formulation containing the aqueous dispersions of the invention.

Finally, the composition in lipogel form of the present invention, or dilutions thereof in water, can act as an emulsifier for further additions of lipid substances in formulations for topical use, hence avoiding the use of synthetic emulsifiers which are less tolerated by the skin and leading to a more stable system. Therefore the present invention also relates to the use of the composition of the invention or its aqueous dispersions as emulsifiers in formulations for topical use, preferably cosmetic and/or cleansing and/or pharmaceutical formulations. The present invention will be illustrated in more detail by the examples to follow. EXAMPLE 1 Preparation of lipogel composition containing rice oil Composition:

Preparation method:

800 g of rice oil are weighed into a 1500 ml beaker and heated to 65°C-70°C. 40 g of a 30% potassium cocoyl hydrolysed wheat protein solution, 40 g of a 30% sodium cocoyl glycine solution and 40 g of a 30% sodium cocoyl glutamate solution are added. While maintaining the temperature at 6O⁰C, the mixture is vortex-agitated possibly at 1200 revolutions/minute with a turbine effect until a semisolid, glossy, easily soluble or easily water dispersible lipogel is obtained. The lipogel obtained presents the following characteristics:

EXAMPLE 2 a) Preparation of lipoqel composition containing rice oil

Composition:

Preparation method:

500 g of rice oil are weighed into a 1500 ml beaker and heated to 60°C. 40 g of a

30% potassium cocoyl hydrolysed wheat protein solution, 40 g of a 30% sodium cocoyl glycine solution and 40 g of a 30% sodium cocoyl glutamate solution are added. While maintaining the temperature at 60⁰C, the mixture is vortex-agitated until a glossy, firm and semisolid lipogel is obtained. At this point 380 g of distilled water are added first at 50⁰C then at ambient temperature; the mixture is homogenized until a very fine homogeneous solution is obtained which is cooled to ambient temperature.

The lipogel obtained presents the following characteristics:

Stability to thermal shock: 3 times at CONFORMS -18°C and at 40⁰C for 8 hours

b) Preparation of body milk

The composition of example 2a was used for preparing a body milk having the following composition:

Preparation method:

Feed in the water, the composition of example 2a then add the previously formed gel in small amounts together with the wheat and maize fibre mixture.

Mix well until completely homogenized and finally add the food grade fragrance and preservative.

EXAMPLE 3 a) Preparation of lipogel composition containing sweet almond oil

Composition:

200 g of sweet almond oil are weighed into a 1500 ml beaker and heated to 60°C.

40 g of a 30% potassium cocoyl hydrolysed soya protein solution, 40 g of a 30% sodium cocoyl aspartate solution and 40 g of a 30% sodium cocoyl proline solution are added.

At a temperature of 50°-60°C, vortex-agitation is applied until a glossy, semisolid lipogel is obtained to which 680 g of distilled water are added first at 50°C then at ambient temperature; the mixture is homogenized until a very fine homogeneous solution is obtained which is cooled to ambient temperature.

The lipogel composition obtained presents the following characteristics:

EXAMPLE 4

Preparation of lipogel composition containing liposoluble vitamins

Composition:

Preparation:

175 g of retinyl palmitate, 1 ,700,000 I. U., and 175 g of tocopheryl acetate are weighed into a 1500 ml beaker. The entirety is heated to 6O⁰C and 50 g of a 30% sodium lauryl hydrolysed rice protein solution, 50 g of a 30% sodium palmitoyl glutamate solution and 50 g of a 30% sodium lauryl glycine solution are added.

At a temperature of 40°-70°C, vortex-agitation is applied until a shiny, semitransparent lipogel is obtained to which 500 g of distilled water are added first at 50°C then at ambient temperature; the lipogel is then completely homogenized in water.

The lipogel obtained presents the following characteristics:

EXAMPLE 5

Preparation of after-sun fluid emulsion spray

Composition:

Preparation method:

Feed in the water, add the compositions of examples 3 and 4 and agitate until homogenized. Finish the product by adding fragrance, panthenol and preservative.

EXAMPLE 6

Preparation of face cream Composition:

Preparation method:

Feed in the composition of example 2 and the glyceryl stearate. Heat to 65°C, agitate until completely homogenized and add the jojoba and borage oils. Cool to

35⁰C and add the fragrance and preservative. Having attained ambient temperature, discharge the product.

Characteristics of the preparation obtained:

EXAMPLE 7

Preparation of anti-ageing face cream

Preparation method

Mix the glyceryl stearate, cetearyl alcohol, sodium palmitoyl hydrolysed wheat protein with the capric/caprylic acid palmitate, jojoba oil, borage oil and macadamia oil at 65°C.

Dissolve the panthenol in water heated to 60°C. Add the water to the waxes dissolved in oil with vortex-agitation, preferably using a turbine. Cool to a temperature of 35°C and add the composition of example 4.

Finish the product by adding the preservatives imidazolidinyl urea and methyl- propyl parabens.

Characteristics of the product obtained:

EXAMPLE 8

Preparation of anti-free radical body gel

Preparation method:

Dissolve the urea, imidazolidinyl urea and allantoin in cold water. When dissolved under vortex-agitation, add the Carbomer 940. After a few minutes, once the powder is dissolved, add the 2 glycolic extracts, sodium lactate, panthenol and the composition of example 4 in this order. After a few moments add the arginine: a milky gel will form.

Finish the product by adding fragrance and the preservative Kathon CG.

Characteristics of the product obtained:

EXAMPLE 9 Preparation of shower gel

Preparation method:

Feed in the water, dissolve the maltodextrin and add the other ingredients in the stated order. Adjust the pH with lactic acid to around pH 6.3. Finish the product by adding fragrance and preservative.

EXAMPLE 10 b) Preparation of dry skin cream

Composition:

Preparation method

Heat the glyceryl stearate, cetearyl alcohol, potassium palmitoyl hydrolysed wheat protein with the triglycerides of capric/caprylic acid and the ethylhexyl palmitate to 65°C. Dissolve the panthenol and hyaluronic acid in hot water. Under vortex- agitation with turbine slowly add the water to the waxes dissolved in oil. Cool to a temperature of 35⁰C and add the lipogel of examples 1 and 4. Finish the product by adding fragrance and preservative. The product obtained presents the following characteristics:

EXAMPLE 11 a) Preparation of lipogel composition containing coconut oil Composition:

Preparation method:

200 g of coconut oil are weighed into a 1500 ml beaker and heated to 65°C-70°C. 25 g of a 30% potassium cocoyl hydrolysed wheat protein solution, 13 g of a 30% sodium cocoyl glycine solution and 13 g of a 30% sodium cocoyl glutamate solution are added. While maintaining the temperature at 60°C, the mixture is vortex-agitated at 1200 revolutions/minute with turbine effect until a semisolid, glossy and easily soluble or easily water dispersible lipogel is obtained. Add the water first at 6O⁰C then at ambient temperature. The product obtained presents the following characteristics:

b) Preparation of hvpoallergenic bath foam for children Composition:

Preparation method:

Dissolve the wheat and starch fibres in the composition of example 11a), then add the lipo-amino acids.

Finish the cleansing product by adding antibacterial fragrance.

Characteristics of the final product:

c) Preparation of body milk for children Composition:

Preparation method:

Dissolve the wheat and starch fibres in the composition prepared in example 11a.

Adjust the pH to 6.

Finish the body milk by adding antibacterial fragrance.

The product obtained presents the following characteristics:

Stability to thermal shock: 3 times at - CONFORMS 18°C and at 40⁰C for 8 hours

Claims

1. Composition in the form of a lipogel containing at least one lipophilic substance chosen from vegetable oils, synthetic triglycerides and liposoluble vitamins, at least one lipoprotein, at least one lipo-amino acid and between 10% and 50% by weight of water.

2. Composition as claimed in claim 1 wherein the quantity of water is between 10% and 20%.

3. Composition as claimed in claims 1 or 2, wherein the weight ratio of the total quantity of lipoprotein(s) and lipo-amino acid(s) to the quantity of lipophilic substance(s) is between 1 :40 and 3:10.

4. Composition as claimed in claim 3 wherein said weight ratio is between 3:40 and 1.6:10.

5. Composition as claimed in claims 1 to 4 wherein said vegetable oils are chosen from the group consisting of coconut oil, rice oil, sweet almond oil, maize oil, sunflower oil, rapeseed oil, avocado oil, macadamia oil, borage oil, jojoba oil and peanut oil.

6. Composition as claimed in claims 1 to 4 wherein said liposoluble vitamins are chosen from the group consisting of vitamin A acetate, vitamin A palmitate, vitamin F and vitamin E acetate.

7. Composition as claimed in claims 1 to 6 wherein said lipoprotein is obtained by acylation of hydrolysed proteins of vegetable origin.

8. Composition as claimed in claim 7 wherein said proteins are obtained from wheat, soya, rice, barley, pea, maize, lupin, potato or almond.

9. Composition as claimed in claims 7 or 8 wherein said acylation is conducted with one or more fatty acids chosen from C₈-C32 alkyl fatty acids and fatty acids contained in said triglyceride based oils.

10. Composition as claimed in claims 1 to 9 wherein said lipo-amino acid is obtained by acylation of an amino acid with one or more fatty acids chosen from C₈-C₃₂ alkyl fatty acids and fatty acids contained in said triglyceride based oils.

11. Composition as claimed in claims 1 to 10 wherein said lipoprotein and said lipo-amino acid present the same qualitative fatty acid composition.

12. Composition as claimed in claims 1 to 11 also comprising phospholipids, ceramides, sterols, sugars and trace elements.

13. Process for preparing a composition in the form of a lipogel as claimed in claims 1 to 12 comprising the following steps: a) preparing a mixture comprising at least one lipophilic substance chosen from vegetable oils, synthetic triglycerides and liposoluble vitamins, at least one lipoprotein, at least one lipo-amino acid and water in a quantity between 10% and 50% by weight; b) homogenizing the mixture from step a) until a lipogel is obtained.

14. Process as claimed in claim 13 wherein in said mixture from step a) the weight ratio of the total quantity of lipoprotein(s) and lipo-amino acid(s) to lipophilic substance(s) is between 1 :40 and 3:10.

15. Process as claimed in claim 14 wherein said ratio is between 3:40 and 1.6:10.

16. Process as claimed in claims 13 to 15 wherein steps a) and b) are conducted at a temperature between 50° and 70°C.

17. Aqueous dispersions obtained by diluting a composition claimed in claims 1 to 13 in water.

18. Formulations for topical use comprising a composition claimed in claims 1 to

13 or an aqueous dispersion claimed in claim 17, optionally in combination with dermatologically acceptable excipients.

19. Formulations as claimed in claim 18 for cosmetic and/or cleansing and/or pharmaceutical use.

20. Formulations as claimed in claims 18 or 19 in the form of a cream, milk, emulsion, gel or bath foam.

21. Formulation as claimed in claims 16 to 18 in the form of a spray containing an aqueous dispersion claimed in claim 17.

22. Use of a composition as claimed in claims 1 to 12 or of an aqueous dispersion claimed in claim 17 as an emulsifier in formulations for topical use.