ITMI20100840A1 - TOPICAL PHYTOTHERAPY COMPOSITIONS - Google Patents

Description

â € œTOPICAL PHYTOTHERAPY COMPOSITIONSâ €

Field of invention

The present invention relates to topical compositions comprising essential oil of tea tree, wheat germ oil, fat-soluble extract or helichrysum oil, and possibly also Argania Spinosa oil, with anti-inflammatory, cosmetic, moisturizing, emollient, reparative, restructuring, antibacterial, antifungal and antiviral.

State of the art

The organism reacts to tissue lesions due to biological (microorganisms, viruses), chemical, physical-mechanical (trauma, radiation) or pathologies (for example dermatitis) through the inflammatory process and the chemical mediators of inflammation (histamine, leukotrienes) , prostaglandins, thromboxanes, interleukins, etc.); the defense of the organism involves various phenomena, especially at the vascular level, which render the harmful factors ineffective and allow the repair of the damage suffered by the tissues.

Tea tree essential oil has been used for a long time in the topical therapy of bacterial, fungal and viral infections; the phytocomplex is generally used as it contains various active ingredients which, with their synergistic action, contribute to bacteriostatic, antifungal and antiviral activity.

Wheat germ oil, rich in tocopherol, is known for its antioxidant and emollient properties, which are important in the re-epithelialization phase.

Helichrysum has been used for many years as an anti-inflammatory and anti-infective.

Argan (Argania Spinosa) in oil has antioxidant and restructuring properties.

Description of the invention

It has now been found that the association of tea tree essential oil, wheat germ oil, fat-soluble extract or helichrysum oil, and possibly also Argania Spinosa oil, exerts an anti-inflammatory, cosmetic, moisturizing, emollient, repairing, restructuring, antibacterial, antifungal and antiviral extremely powerful, and a strong intra- and extracellular antioxidant action.

Therefore the present invention relates to compositions comprising: a) essential oil of tea tree (Melaleuca alternifolia),

b) wheat germ oil (Triticum vulgare), e

c) fat-soluble extract or helichrysum oil (i.e. Helichrysum italicum or Helichrysum arenarium or Helichrysum stoechas),

and also possibly d) Argania Spinosa oil (Argan oil).

According to an aspect of the invention, these compositions can be used to treat dermatological diseases of inflammatory, bacterial, fungal or viral origin, to favor the protective activities and the cell regeneration process at the cutaneous level.

The mechanism of action of the compositions of the invention must be considered as a system that acts on several levels on the inflammatory process. A first action occurs in the first phase of inflammation, counteracting the production of free radicals, thus slowing down the inflammatory process; the second level is represented by the direct action on microorganisms, with the alteration of the membrane; a third level is the action during the reparative phase, stimulating the production of collagen and elastin. It should be emphasized that, in consideration of the results obtained with the compositions of the invention, superior to the simple sum of the actions exercised by the individual active components, it can be hypothesized, without however being linked to this hypothesis, that the three active components of the compositions of the ™ invention act through a reciprocal synergy mechanism. It has therefore been found that the particular association of tea tree oil, wheat germ oil, fat-soluble extract or helichrysum oil and possibly Argania Spinosa oil of the invention is able to enhance the anti-inflammatory, antibacterial and antifungal properties of the tea tree. itself and at the same time to promote protective activities and the process of cellular regeneration and tissue restructuring.

Wheat germ oil, thanks to its emollient, moisturizing and antioxidant action, acts in synergy with the phytocomplex of Melaleuca alternifolia essential oil, fat-soluble extract or helichrysum oil and Argan oil Spinosa in turn enhance and enhance the action of Melaleuca alternifolia as they play an active part in the inflammatory process and on the trophism of the skin.

According to a preferred aspect of the present invention, essential oil of Melaluca alternifolia at 2%, Triticum vulgare oil from 2% to 5%, fat-soluble extract or helichrysum oil at 5% and possibly Argania Spinosa (fruit) oil will be used as active components. at 3%.

According to a particularly preferred aspect, such components may be present in the compositions of the invention within the following preferred percentage ranges, where these percentages are intended on the total composition:

a) essential oil of Melaluca alternifolia: from 1.5% to 2.5%,

b) Triticum vulgare oil: from 1.5% to 5%,

c) fat-soluble extract of helichrysum: from 1.5% to 6%,

or helichrysum oil: from 4.5% to 6%,

d) Argania Spinosa fruit oil: from 3% to 6%.

The compositions of the invention have proved effective in the treatment of various dermatological diseases, thanks to their anti-inflammatory, cosmetic, moisturizing, emollient, restoring and restructuring action on the skin and can be used in all those situations in which bacterial / fungal infections are present. / viral and in which it is necessary to restore the physiological balance at the level of the skin barrier.

The essential oil of Melaleuca alternifolia, which can be obtained by steam distillation of fresh leaves, contains a high concentration of terpinene-4-ol (> 36%), considered the main active component, and a low concentration of 1.8 cineole (<4.5%), which at high concentrations can be irritating. The oil, in stabilized form and meeting the standards indicated in various Pharmacopoeias (for example British Pharmaceutical Codex 1949 p. 597-578; Martindale; The Extra Pharmacopoeia 28 ° ed, 1982 p. 678), whose composition is reported in J. Agric., Food Chem. 1989, 37, 1330, is active against various bacteria and fungi, is used in topical applications in the treatment of various dermatological infections; at a concentration of 2% its use is considered safe, with a low risk of irritation for the skin; the adverse events observed are occasional, the essential oil of tea tree is irritating only in high doses or if it is not stored correctly; in this case, allergic reactions due to oxidation products develop. The essential oil of Melaleuca alternifolia has proven effective in particular against Candida, in the treatment of seborrheic dermatitis, acne, in the presence of psoriasis or herpes.

The components of the essential oil of tea tree (Melaleuca alternifolia) act mainly by causing alterations in the membrane of microorganisms, causing the lysis and denaturation of proteins; An antioxidant action was also observed, which is important in fighting free radicals, which increase during inflammation, and an action in favoring re-epithelialization; moreover, the use of the phytocomplex in its entirety is useful for making the most of the synergistic action between the components and has the advantage of not altering the saprophytic bacterial flora present on the skin and necessary to maintain physiological balance.

The main component of wheat germ oil (Triticum vulgare) is vitamin E (essentially present as alpha-tocopherol), known for its antioxidant properties and above all for maintaining efficient redox reactions that inactivate free radicals; free radicals are highly reactive chemical compounds, which can damage molecules of biological importance and compromise the functionality of various organs and tissues, involved in the physiopathology of many pathologies in man.

Topical formulations based on vitamin E find wide application in dermatology, especially in the treatment of cutaneous xerosis, associated or not with itching. Furthermore, several studies have shown that vitamin E is the main antioxidant substance at the level of lipid structures; on the skin, its antioxidant action is carried out at the level of cell membranes, protecting them from the aggression of free radicals and counteracting the oxidation of polyunsaturated fatty acids, both at the level of the lipid structures and of the extracellular matrix. Wheat germ oil moisturizes and regenerates the skin, for example by increasing the synthesis of elastin and collagen.

The medicinal properties of helichrysum have been known for a long time: it contains flavonoids, nerol, caffeic acid, proanthocyanidins, tannins and among its properties the anti-inflammatory, anti-allergic and anti-edematous properties stand out. It is used in topical preparations for the treatment of various skin diseases, such as psoriasis and eczema, has a preventive action on erythema and some dermatitis and a decongestant and photoprotective action: it is able to modify pictures different clinicians but having a similar pathogenetic state; the mechanism of action involves various substances: the sterol and triterpene compounds present can be considered pre-hormones, transformable by the organism, in case of deficiency states, into adrenal cortical hormones; a series of inhibitory derivatives which act on the inflammatory cascade have recently been discovered; other substances, such as proanthocyanidins, have an antioxidant action.

In conclusion, the compositions of the invention have shown the absence of side or allergenic effects, efficacy in the treatment of various dermatological diseases, and a good tolerability, and can also be useful in combating relapses, as they do not induce alterations of the saprophytic flora present. on the skin or phenomena of resistance.

The compositions of the present invention may also contain other active components, having a complementary action or in any case useful for the purposes of the invention, such as for example vitamin C, antioxidants against the oxidation of tea tree oil.

The compositions of the present invention can be formulated in a manner suitable for topical administration and will be prepared according to conventional methods well known in the pharmaceutical technique, such as those described in "Remington's Pharmaceutical Handbook", Mack Publishing Co., N.Y., USA, using excipients, diluents, bulking agents, anti-caking agents acceptable for their final use.

Examples of preferred formulations according to the present invention are gels, emulsions (oil in water (o / w) and water in oil (w / o)), creams, ointments, sprays, powders, lotions, foams, tissues, gauze.

Some specific examples of formulations of the invention are reported below.

Example 1 - Detergent Formulation

The cleansing formulation, useful for cleansing the skin or hair, for example, consists of (the percentages are in ml of the total volume of the formulation):

ƒ Melaleuca alternifolia (Melaleuca) oil 2%

ƒ Triticum vulgare (Wheat Germ) oil 5%

ƒ Helichrysum italicum (Helichrysum) extract 2%

Excipients:

ƒ Water

ƒ Magnesium Laurate Sulphate

ƒ PEG-40 hydrogenated castor oil

ƒ Polysorbate 80

ƒ Propylene glycol

ƒ Cocamidopropylbetaine

ƒ PEG-120 methylglucose dioleate

ƒ Sorbitol

ƒ Sodium lauroylsarcosinate

ƒ Disodium laurate sulfur succinate chloride

ƒ Sodium dehydroacetate

ƒ disodium EDTA

ƒ Sodium benzoate

ƒ Sodium salicylate

ƒ Citric acid

ƒ Limonene

Example 2 - Cream formulation

The formulation in the form of cream, can be used for example on the body, on the face, is made up of (the percentages are in ml of the total volume of the formulation):

ƒ Melaleuca alternifolia (Melaleuca) oil 2%

ƒ Triticum vulgare (Wheat Germ) oil 5%

ƒ Helichrysum italicum (Helichrysum) extract 5% Excipients:

ƒ Water

ƒ Cetyl alcohol

Di-C12-C13alkyl maleate

Propylene glycol

Cetearyl isononanoate

Decyl oleate

Potassium palmitoyl hydrolyzate of wheat proteins Glyceryl stearate

Cetearyl alcohol

Xanthan gum

Dimethicone

Disodium EDTA

Sorbic acid

Butyloctanoic acid

Sodium dehydroacetate

Unsaponifiable from Olive Oil (Olea Europea) Tocopheryl acetate

Limonene

Linaiolo

Claims (8)

CLAIMS 1. Topical compositions comprising: a) tea tree essential oil, b) wheat germ oil, e c) fat-soluble extract of helichrysum or helichrysum oil. 2. Compositions according to claim 1, further comprising d) Argania Spinosa fruit oil. 3. Compositions according to claim 1 or 2, wherein the components vary within the following percentage ranges on the total composition: a) tea tree essential oil: from 1.5% to 2.5%, b) wheat germ oil: from 1.5% to 5%, c) fat-soluble extract of helichrysum: from 1.5% to 6% o Helichrysum oil: from 4.5% to 6%. 4. Compositions according to any one of the preceding claims, further comprising d) Argania Spinosa fruit oil: from 3% to 6%. 5. Compositions according to any one of the preceding claims, comprising: a) tea tree essential oil: 2%, b) wheat germ oil: from 2% to 5%, e c) fat-soluble extract or helichrysum oil: 5%. 6. Compositions according to claim 5, further comprising d) Argania Spinosa fruit oil: 3%. 7. Compositions according to any one of the preceding claims, wherein said compositions are in the form of gels, o / w emulsions, w / o emulsions, creams, ointments, sprays, powders, lotions, foams, wipes, gauze. 8. Compositions comprising: a) tea tree essential oil, b) wheat germ oil, e c) fat-soluble extract or helichrysum oil, and optionally d) Argania Spinosa fruit oil, for topical use in the treatment of dermatological diseases of inflammatory, bacterial, fungal or viral origin, and to promote protective activities and the process of cell regeneration in the skin.