Avocado unsaponifiable substances for treating conditions caused by malassezia yeast

By using avocado unsaponifiable matter, especially avocado unsaponifiable matter containing a high content of furan lipids, the problem of side effects of treating diseases caused by Malassezia yeast in the prior art is solved, and effective anti-inflammatory and yeast growth inhibition effects are achieved, which is suitable for children and infants.

CN120603601APending Publication Date: 2025-09-05LAB EXPANSCIENCE SA
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Patent Information

Application Number
CN202380092083.9
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2022-12-21
Filing Date
2023-12-21
Publication Date
2025-09-05

AI Technical Summary

Technical Problem

Existing treatment options for diseases caused by Malassezia yeast, such as seborrheic dermatitis, have side effects. For example, long-term use of corticosteroids and antifungal drugs can lead to skin atrophy and capillary dilation, and the regulation of sebum secretion is insufficient to inhibit yeast growth.

Method used

Avocado unsaponifiable matter, particularly furan lipids containing at least 50% by weight, is used to inhibit the growth of Malassezia yeast through topical application and act as an anti-inflammatory and soothing agent. The preparation method includes heat treatment, saponification, precipitation, liquid/liquid extraction and purification steps.

Benefits of technology

Avocado unsaponifiables effectively inhibit the growth of Malassezia yeast, reduce the symptoms of diseases caused by it, such as seborrheic dermatitis, avoid the side effects of traditional treatments, and are suitable for children and infants.

✦ Generated by Eureka AI based on patent content.

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Abstract

The present invention relates to avocado unsaponifiables or compositions containing avocado unsaponifiables for use in the prevention and / or treatment of conditions and diseases caused by malassezia yeast, the avocado unsaponifiables containing at least 50% by weight of furan lipids relative to the total mass of the avocado unsaponifiables. The invention also relates to the cosmetic use of an avocado unsaponifiable substance or a composition containing an avocado unsaponifiable substance for the prevention and / or treatment of dandruff, the avocado unsaponifiable substance containing at least 50% by weight of furan lipids relative to the total mass of the avocado unsaponifiable substance. In addition, the invention also relates to a method for preparing the avocado unsaponifiable matter.
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Description

Technical Field

[0001] The present invention relates to avocado unsaponifiable matter or a composition comprising it for use in preventing and / or treating conditions and diseases caused by yeasts of the genus Malassezia. The present invention also relates to the cosmetic use of avocado unsaponifiable matter or a composition comprising it for preventing and / or treating dandruff. Furthermore, the present invention relates to a method for preparing avocado unsaponifiable matter. Background Art

[0002] The human microbiome contains a wide variety of microorganisms, such as bacteria, viruses and fungi. The Malassezia yeast is part of the Basidiomycetes and is part of the human commensal flora, especially in the scalp. The yeast releases hydrolytic enzymes (such as lipase and phospholipase C) that enable the lipids of this yeast host to produce fatty acids. In patients with seborrheic dermatitis, Malassezia yeast invades the stratum corneum, and the free fatty acids produced by the release of lipase are the origin of the inflammatory process. Inflammation leads to excessive proliferation of the stratum corneum and incomplete differentiation of keratinocytes, which alters the function of the stratum corneum, in particular its barrier function, resulting in easier entry of Malassezia yeast. Malassezia yeast is involved in many skin diseases, such as seborrheic dermatitis, Malassezia folliculitis, dandruff, pityriasis capitis or pityriasis versicolor.

[0003] Seborrheic dermatitis is a fairly common, benign, chronic, erythematous, scaly inflammatory skin disease that develops in flare-ups and most commonly affects the scalp and face, particularly the nasolabial folds and eyebrows. One typical form affects infants and presents as a yellow crust on the scalp (cradle cap) or face.

[0004] Cradle cap is a form of infantile seborrheic dermatitis (ISD) characterized by erythematous patches with oily scales on the scalp, with peak incidence during the third month of life. The factors that cause cradle cap are diverse. Excessive sebum production may be one of these factors, but it is not necessarily the cause: it causes dead keratinocytes to adhere to the skin surface and prevent physiological desquamation. Invasion of the stratum corneum by the Malassezia yeast, as mentioned above, is another factor.

[0005] In the prior art, treatment strategies for seborrheic dermatitis (including cradle cap) aim to regulate sebum production, calm skin inflammation, and reduce the growth of Malassezia yeast. Such treatments include the use of anti-inflammatory drugs (e.g., corticosteroids for skin use) and antifungal drugs (e.g., ketoconazole, lithium gluconate, or ciclopirox). Treatment may also involve emollients (e.g., mineral or olive oils or petrolatum), and exfoliants (e.g., salicylic acid).

[0006] In general, the treatment of choice for conditions and diseases caused by Malassezia yeasts, particularly pityriasis versicolor and seborrheic dermatitis, is antifungal and anti-inflammatory therapy. Actions targeting sebum secretion are generally insufficient to treat conditions and diseases caused by Malassezia yeasts.

[0007] Furthermore, normal sebum secretion does not prevent the initiation of the abnormal growth cycle of Malassezia yeast. Therefore, treatments that act solely on sebum secretion, for example by inhibiting 5-alpha reductase activity, are not a treatment option for these conditions. Furthermore, sebum secretion is not controlled solely by the 5-alpha reductase pathway; it can be activated by other pathways or for other reasons, such as physical or psychological stress.

[0008] Long-term use of corticosteroids may cause side effects such as skin atrophy, striae, telangiectasia, folliculitis, hypopigmentation, and habituation, while long-term use of antifungals may cause side effects such as contact dermatitis. In addition, other treatments have limitations; for example, lithium gluconate is only suitable for treating adults with normal immune function.

[0009] Therefore, there is a real need for a composition for preventing and / or treating diseases caused by Malassezia yeasts, which composition can be applied topically, does not have the side effects of the above-mentioned corticosteroids and antifungal drugs, and can be used in children, infants and newborns.

[0010] In the context of the present invention, the applicant surprisingly found that avocado unsaponifiables are able to inhibit the growth of Malassezia yeasts.

[0011] In its international patent application WO2004 / 012496, the applicant describes a method for obtaining unsaponifiable avocados rich in furanic lipids. Generally speaking, unsaponifiable avocados are used to treat certain connective tissue diseases (e.g., osteoarthritis), joint conditions (e.g., rheumatism), or periodontal diseases (e.g., gingivitis or periodontitis) (see, for example, international patent application WO2013 / 098293).

[0012] Thus, the applicants have found that avocado unsaponifiables can be used to prevent and / or treat conditions and diseases caused by Malassezia yeasts, in particular for preventing and / or treating seborrheic dermatitis, in particular infantile seborrheic dermatitis (e.g. cradle cap, pityriasis capitis, Malassezia folliculitis, pityriasis versicolor and dandruff).

[0013] In fact, avocado unsaponifiables can inhibit the growth of Malassezia yeast and act as an anti-inflammatory, soothing, and / or antipruritic agent. Summary of the Invention

[0014] According to a first aspect, the present invention relates to an avocado unsaponifiable matter for use in preventing and / or treating pathologies and diseases caused by Malassezia yeasts, said avocado unsaponifiable matter containing at least 50% by weight, preferably at least 60% by weight, of furanic lipids relative to the total mass of the avocado unsaponifiable matter.

[0015] According to a second aspect, the present invention relates to a composition comprising avocado unsaponifiable matter containing at least 50% by weight, preferably at least 60% by weight, of furanic lipids relative to the total mass of avocado unsaponifiable matter, for use in preventing and / or treating pathologies and diseases caused by yeasts of the genus Malassezia.

[0016] According to a third aspect, the present invention relates to the cosmetic use of avocado unsaponifiable matter containing at least 50% by weight, preferably at least 60% by weight, of furanic lipids relative to the total mass of avocado unsaponifiable matter for preventing and / or treating dandruff.

[0017] According to a fourth aspect, the present invention relates to the cosmetic use of a composition comprising avocado unsaponifiable matter containing at least 50% by weight, preferably at least 60% by weight, of furanic lipids relative to the total mass of avocado unsaponifiable matter, for preventing and / or treating dandruff.

[0018] According to a fifth aspect, the present invention relates to a method for preparing avocado unsaponifiable matter, comprising at least the following steps:

[0019] i. a heat treatment step of the avocado oil concentrate, advantageously carried out at a temperature ranging from 60°C to 90°C, preferably 80°C,

[0020] ii. a step of saponifying the avocado oil concentrate in the presence of an ethanolic or aqueous alkali solution of the sodium hydroxide or potassium hydroxide type to obtain an avocado unsaponifiable,

[0021] iii. an optional step of precipitating the soap obtained in step ii.,

[0022] iv. at least one step of extraction of the product obtained in step ii. or iii., wherein the avocado unsaponifiable matter is purified by liquid / liquid or solid / liquid extraction using at least 50% by volume of a solvent chosen from ethyl acetate, propyl acetate and butyl acetate relative to the total volume of the extraction solvent, and

[0023] v. Optional additional purification steps of distillation and / or deodorization.

[0024] definition

[0025] For the purposes of the present invention, the term "Malassezia yeast" refers to yeasts of any species and varieties belonging to the genus Malassezia (also known as the genus Pityrosporum). Examples of yeast species that may be mentioned, but are not limited to, are Malassezia furfur, in particular strain CIP 1634.86, Malassezia globosa, Malassezia restricta, Malassezia sympodialis, Malassezia obtuse, Malassezia slooffiae, Malassezia pachydermatis and Malassezia folliculitis.

[0026] For the purposes of the present invention, "dandruff" refers to the unsightly clumps of dead cells present on the scalp.

[0027] For the purposes of this invention, "pityriasis versicolor" refers to a skin infection caused by Malassezia furfur that appears as multiple scaly plaques that are white to brown to pink.

[0028] For the purposes of the present invention, "minimum inhibitory concentration (MIC)" refers to the minimum concentration of a compound that inhibits the growth of a given microorganism.

[0029] "Avocado oil concentrate" or "avocado concentrate" refers to avocado oil concentrated in its unsaponifiable fraction, advantageously by molecular distillation or cold crystallization.

[0030] For the purposes of this invention, "Malsezai folliculitis" is an inflammatory skin disease that typically presents as an itchy follicular papulopustular rash distributed over the upper body of young adults; this disease of fungal etiology is similar to acne vulgaris and is also known as pityrosporum folliculitis.

[0031] In general, the unsaponifiable matter is that portion of the fatty matter which remains insoluble in water after prolonged exposure to alkaline alkali and can be extracted with organic solvents. Five major groups of substances are present in the unsaponifiable matter of most vegetable oils: saturated or unsaturated hydrocarbons, aliphatic or terpene alcohols, sterols (or "phytosterols"), tocopherols and tocotrienols, carotenoids, and xanthophylls.

[0032] According to the present invention, avocado furan lipids are lipids consisting of a linear C 11 -C 19 (Preferred C 13 -C 17) Furans having a monosubstituted hydrocarbon chain which is saturated or contains one or more olefinically or acetylenically unsaturated chains.

[0033] The avocado unsaponifiable matter of the present invention comprises at least one fraction rich in furanic lipids (fraction H) and one fraction rich in polyhydroxy fatty alcohols (fraction I). Fraction H appears first on the gas chromatography of avocado oil unsaponifiable matter.

[0034] Part H is:

[0035] - In thin layer chromatography, it migrates at a frontier position with an Rf of 0.9.

[0036] - is eluted first in silica gel high pressure liquid chromatography,

[0037] -Mainly appears in gas chromatography.

[0038] The term "rich in" means that the content of the above-mentioned different components is higher than the average content of the corresponding components in all vegetable oils well known to those skilled in the art. DETAILED DESCRIPTION

[0039] A first object of the present invention relates to an avocado unsaponifiable matter for use in the prevention and / or treatment of pathologies and diseases caused by Malassezia yeasts, said avocado unsaponifiable matter containing at least 50% by weight, preferably at least 60% by weight, of furanic lipids relative to the total mass of the avocado unsaponifiable matter.

[0040] A second object of the present invention relates to a composition comprising avocado unsaponifiable matter containing at least 50% by weight, preferably at least 60% by weight, of furanic lipids relative to the total mass of the avocado unsaponifiable matter, for use in preventing and / or treating pathologies and diseases caused by Malassezia yeasts.

[0041] According to a preferred embodiment of the present invention, the conditions and diseases caused by Malassezia yeasts are selected from seborrheic dermatitis, in particular infantile seborrheic dermatitis (e.g. cradle cap, pityriasis capitis, Malassezia folliculitis and pityriasis versicolor). Preferably, the conditions and diseases caused by Malassezia yeasts are selected from seborrheic dermatitis, in particular infantile seborrheic dermatitis (e.g. cradle cap).

[0042] Conditions and diseases caused by Malassezia yeasts may be selected from seborrheic dermatitis, in particular infantile seborrheic dermatitis (eg cradle cap, pityriasis capitis, Malassezia folliculitis, pityriasis versicolor and dandruff).

[0043] In another preferred embodiment, the avocado unsaponifiable matter contains at least 5% by weight, preferably at least 7% by weight, of polyhydroxylated fatty alcohols relative to the total mass of the avocado unsaponifiable matter.

[0044] Advantageously, the avocado unsaponifiable matter of the invention contains at least 0.8% by weight, preferably at least 1% by weight, of sterols relative to the total mass of the avocado unsaponifiable matter.

[0045] The preferred route of administration of the avocado unsaponifiables or compositions of the present invention is topical.

[0046] Advantageously, the composition comprising avocado unsaponifiable matter contains at least 0.25% by weight, preferably 0.50% by weight, of avocado unsaponifiable matter relative to the total mass of the composition.

[0047] According to a preferred embodiment, avocado unsaponifiable matter can be obtained by a method comprising at least the following steps:

[0048] i. a heat treatment step of the avocado oil concentrate, advantageously carried out at a temperature ranging from 60°C to 90°C, preferably 80°C,

[0049] ii. a step of saponifying the avocado oil concentrate in the presence of an ethanolic or aqueous alkali solution of the sodium hydroxide or potassium hydroxide type to obtain an avocado unsaponifiable,

[0050] iii. an optional step of precipitating the soap obtained in step ii.,

[0051] iv. at least one step of extraction of the product obtained in step ii. or iii., wherein the avocado unsaponifiable matter is purified by liquid / liquid or solid / liquid extraction using at least 50% by volume of a solvent chosen from ethyl acetate, propyl acetate and butyl acetate, relative to the total volume of the extraction solvent, preferably ethyl acetate, and

[0052] v. Optional additional purification steps of distillation and / or deodorization.

[0053] A third object of the present invention relates to the cosmetic use of avocado unsaponifiable matter containing at least 50% by weight, preferably at least 60% by weight, of furanic lipids relative to the total mass of the avocado unsaponifiable matter for preventing, reducing and / or treating dandruff.

[0054] A fourth object of the present invention relates to the cosmetic use of a composition comprising avocado unsaponifiable matter containing at least 50% by weight, preferably at least 60% by weight, of furanic lipids relative to the total mass of avocado unsaponifiable matter, for preventing, reducing and / or treating dandruff.

[0055] A particular embodiment of the present invention relates to avocado unsaponifiable matter or a composition comprising avocado unsaponifiable matter, the unsaponifiable matter containing at least 50% by weight, preferably at least 60% by weight, of furanic lipids relative to the total mass of the unsaponifiable matter, for use in preventing, reducing and / or treating dandruff. Dandruff is preferably treated on a healthy body and a healthy scalp.

[0056] In another preferred embodiment, the avocado unsaponifiable matter contains at least 5% by weight, preferably at least 7% by weight, of polyhydroxylated fatty alcohols relative to the total mass of the avocado unsaponifiable matter.

[0057] Advantageously, the avocado unsaponifiable matter of the invention contains at least 0.8% by weight, preferably at least 1% by weight, of sterols relative to the total mass of the avocado unsaponifiable matter.

[0058] The preferred route of administration of the avocado unsaponifiables or compositions of the present invention is topical.

[0059] Advantageously, the composition comprising avocado unsaponifiable matter contains at least 0.25% by weight, preferably 0.50% by weight, of avocado unsaponifiable matter relative to the total mass of the composition.

[0060] According to a preferred embodiment, avocado unsaponifiable matter can be obtained by a method comprising at least the following steps:

[0061] i. a heat treatment step of the avocado oil concentrate, advantageously carried out at a temperature ranging from 60°C to 90°C, preferably 80°C,

[0062] ii. a step of saponifying the avocado oil concentrate in the presence of an ethanolic or aqueous alkali solution of the sodium hydroxide or potassium hydroxide type to obtain an avocado unsaponifiable,

[0063] iii. an optional step of precipitating the soap obtained in step ii.,

[0064] iv. at least one step of extraction of the product obtained in step ii. or iii., wherein the avocado unsaponifiable matter is purified by liquid / liquid or solid / liquid extraction using at least 50% by volume of a solvent chosen from ethyl acetate, propyl acetate and butyl acetate, relative to the total volume of the extraction solvent, preferably ethyl acetate, and

[0065] v. Optional additional purification steps of distillation and / or deodorization.

[0066] The solvent system (extraction solvent) of step iv is preferably ethyl acetate.

[0067] The compositions allowing the implementation of the invention comprise a pharmaceutically or dermatologically or cosmetically acceptable carrier, i.e. a carrier compatible with the skin, in any dosage form customary for topical application, in particular in the form of aqueous, hydroalcoholic or oily solutions, oil-in-water or water-in-oil or multiple emulsions, hydrogels or oleogels, liquid anhydrous products, dispersions of oil in an aqueous phase using spheres which may be polymer nanoparticles (e.g. nanospheres and nanocapsules) or, better still, ionic and / or non-ionic lipid vesicles, transdermal devices or any other form of topical application.

[0068] The composition may have varying degrees of fluidity and have the appearance of a white or colored cream, ointment, lotion, wash, serum, paste, mousse, gel, shampoo, or conditioner.

[0069] Advantageously, the pharmaceutically, dermatologically or cosmetically acceptable medium is a cream.

[0070] The composition of the present invention may also contain adjuvants commonly used in the fields of pharmacy, dermatology or cosmetology, such as hydrophilic or lipophilic gelling agents, hydrophilic or lipophilic active agents, thickeners, preservatives, antioxidants, solvents, fragrances, chelating agents, odor absorbers, chemical or mineral filters, mineral pigments, surfactants, polymers, silicone oils and dyes. The amount of these various adjuvants is the amount conventionally used in the field under consideration, for example 0.01% to 20% of the total weight of the composition. Depending on their properties, these adjuvants can be introduced into the fat phase, the aqueous phase, the lipid vesicles and / or the nanoparticles.

[0071] As oils that can be used in the compositions for implementing the invention, mention may be made of mineral oils, oils of vegetable origin (apricot oil, sunflower oil, plum oil), oils of animal origin, synthetic oils, silicone oils and fluorinated oils (perfluoropolyethers). Fatty alcohols (cetyl alcohol), fatty acids and waxes (beeswax) can also be used as fats.

[0072] As emulsifiers and co-emulsifiers that can be used in the present invention, for example, fatty acid polyethylene glycol esters (such as PEG-40 stearate, PEG-100 stearate), fatty acid polyol esters (such as glyceryl stearate and sorbitan tristearate) may be mentioned.

[0073] As hydrophilic gelling agents, mention may be made in particular of carboxyvinyl polymers (carbomers), acrylic acid copolymers (e.g. acrylate / alkyl acrylate copolymers), polyacrylamides, polysaccharides, natural gums and clays, and as lipophilic gelling agents, mention may be made of modified clays (e.g. bentonite, fatty acid metal salts, hydrophobic silica and polyethylene).

[0074] The mode of administration, dosage and optimal dosage form of the compounds and compositions according to the present invention can be determined according to the criteria usually considered when formulating a pharmaceutical, dermatological or cosmetic treatment suitable for a patient, such as the extent of the skin area to be treated, tolerance to treatment, and skin type.

[0075] Advantageously, the avocado unsaponifiable material according to the invention can be obtained according to the methods described in International Patent Application WO 2004 / 012496, Patent FR 2 678 632 and International Patent Application WO 2013 / 014344.

[0076] For example, avocado unsaponifiables can be obtained from avocado concentrate processed using:

[0077] - saponification of avocado concentrate in the presence of an ethanolic base solution of the sodium hydroxide or potassium hydroxide type;

[0078] - Wash with water;

[0079] - purification by liquid / liquid extraction in the presence of a solvent such as dichloroethane (DCE) or methyl isobutyl ketone (MIBK) (the method described in patent FR2678632 for DCE and in patent application WO2013 / 014344 for MIBK);

[0080] -The solvent and residual impurities can be removed by distillation / deodorization to obtain the purified unsaponifiable fraction.

[0081] The avocados used as a base for the preparation of avocado oil may preferably undergo a preliminary dehydration or drying step, advantageously carried out at a temperature ranging from -50°C to 75°C. Methods for extracting avocado oil are known to those skilled in the art. Avocado oil can in particular be extracted by cold pressing or using solvents at low temperatures.

[0082] Avocado oil concentrate itself can be obtained by vacuum molecular distillation (usually at 10 -3 millibars and 10 -1 mbar) and is advantageously obtained at a distillation temperature between 150° C. and 350° C., generally between 180° C. and 260° C., or by cold crystallization. The concentrate obtained is then advantageously subjected to a heat treatment at a temperature between 40 and 150° C., for example between 80 and 130° C.

[0083] The present invention also relates to a non-therapeutic cosmetic hair care method for preventing and / or treating dandruff, comprising applying an avocado unsaponifiable matter or a composition comprising it as defined above, in particular the application comprising applying said unsaponifiable matter or a composition comprising it to the hair.

[0084] The present invention also relates to a method for preventing and / or treating conditions and diseases caused by Malassezia yeasts, comprising administering, in particular topically administering, to a subject in need thereof an effective amount of avocado unsaponifiable matter as defined above or a composition comprising avocado unsaponifiable matter. Conditions and diseases caused by Malassezia yeasts are as defined above.

[0085] The cosmetic uses and cosmetic care methods according to the invention are generally carried out on healthy skin or healthy parts of the body and are not therapeutic.

[0086] The present invention particularly relates to the treatment of conditions and diseases caused by yeasts of the genus Malassezia.

[0087] Another object of the present invention relates to a method for preparing avocado unsaponifiable matter, comprising at least the following steps:

[0088] i. a heat treatment step of the avocado oil concentrate, advantageously carried out at a temperature ranging from 60°C to 90°C, preferably 80°C,

[0089] ii. a step of saponifying the avocado oil concentrate in the presence of an ethanolic or aqueous alkali solution of the sodium hydroxide or potassium hydroxide type to obtain an avocado unsaponifiable,

[0090] iii. an optional step of precipitating the soap obtained in step ii.,

[0091] iv. at least one step of extraction of the product obtained in step ii. or iii., wherein the avocado unsaponifiable matter is purified by liquid / liquid or solid / liquid extraction using at least 50% by volume of a solvent chosen from ethyl acetate, propyl acetate and butyl acetate relative to the total volume of the extraction solvent, and

[0092] v. Optional additional purification steps of distillation and / or deodorization.

[0093] The solvent of step iv is preferably ethyl acetate.

[0094] Alternatively, the heat treatment of step i. may be carried out on the avocado oil and / or on the avocados used as a basis for the preparation of the oil before the concentration step.

[0095] The following examples are intended to illustrate the invention in a non-limiting manner.

[0096] Example

[0097] Example 1: Determination of the minimum inhibitory concentration of Malassezia furfur in liquid culture medium containing avocado unsaponifiables and other products

[0098] This example aims to study the effect of avocado unsaponifiables according to the invention on Malassezia furfur compared to another avocado product (avocado oil concentrate) and two other soy products (soybean oil concentrate and soy unsaponifiables).

[0099] Preparation method of soybean oil concentrate

[0100] Crude soybean oil or refined soybean oil was heated under high vacuum (10 -3 millibars and 10 -2 The molecular distillation treatment is carried out at a pressure between 100 and 200 mbar) and a distillation temperature between 200° C. and 300° C.

[0101] The compounds shown in the following table were obtained.

[0102] Table 1

[0103]

[0104] Preparation method of soybean unsaponifiable matter

[0105] The soybean concentrate or soybean oil refining by-product obtained by the above method (see patent application WO2012 / 104319) is processed as follows:

[0106] - saponification of the soy concentrate in the presence of an alkali ethanol solution such as sodium hydroxide or potassium hydroxide to eliminate residual fatty acids;

[0107] - Wash with water;

[0108] - purification by liquid / liquid extraction in the presence of a solvent such as dichloroethane (DCE) or methyl isobutyl ketone (MIBK) (the method described in patent application WO 2012 / 104319 is used for MIBK);

[0109] - The solvent and residual impurities were removed by distillation / deodorization to obtain the purified unsaponifiable fraction shown in the table below.

[0110] Table 2

[0111]

[0112] Method for preparing avocado concentrate

[0113] Crude avocado oil obtained according to the method described in application WO 2004 / 012496 was heated under high vacuum (approximately 5.10 -3 The concentrate was treated by molecular distillation at 400 mbar (0.1 mmol / l) and a distillation temperature of about 250° C. The resulting concentrate was brought to a temperature of 80° C.

[0114] The compounds shown in the following table were obtained.

[0115] Table 3

[0116]

[0117]

[0118] Preparation method of avocado unsaponifiable matter

[0119] The first step involves saponifying the avocado concentrate obtained using the above-described method. To this end, the avocado oil concentrate, followed by water and 50% potassium hydroxide, are introduced sequentially into a reactor. The system is then refluxed with stirring, and sodium chloride is then added after cooling. A separation step is then carried out by filtration or decantation to recover the fraction containing the unsaponifiable matter. This precipitate is then extracted with ethyl acetate. The unsaponifiable matter is then recovered by evaporating the solvent. The product is then subjected to a deodorization step by injecting 100°C steam under vacuum conditions of 30 to 50 mbar.

[0120] Table 4

[0121]

[0122] plan

[0123] The minimum inhibitory concentration (MIC) of the different test products was determined using a method suitable for 96-well plate liquid culture. MIC measurement studies were performed according to the GLYcoDiag technology using the microbial strain Malassezia furfur as the organism (reference American Type Culture Collection (ATCC): 14521). Cultures were reconstituted according to the instructions of the collection that provided the reference strain. The following products were tested: soy concentrate, soy unsaponifiables, avocado unsaponifiables, and avocado concentrate.

[0124] Preparation of samples and test microorganisms

[0125] The various products listed above were pre-dissolved in olive oil at the following concentrations: final concentration in the culture medium (expressed as weight percentage): 1%, 0.5%, 0.25%, 0.1%, 0.05% and 0.01%.

[0126] Prepare analytical blanks and use them in the same manner as test samples:

[0127] - Blanks corresponding only to microbial environments;

[0128] - a blank consisting of olive oil, prepared at 5% (w / w) directly in the microbiological culture medium associated with each microbial strain;

[0129] - The control group consisted of The compositions were prepared at 5% (w / w) directly in the microbial culture medium associated with each microbial strain. Phenoxyethanol is a compound known to inhibit the growth of Malassezia furfur.

[0130] To determine the MIC of the test product, six serial dilutions were tested directly in a medium designed to promote the growth of M. furfur strains (96-well microplates). Each dilution point was then diluted at approximately 1.10 μg / well. 5 The rate of cfu / mL was contaminated by the test strain. Finally, the test samples were incubated at 32.5°C ± 2.5°C for 48 h, taking care to respect the respiratory type of the facultative aerobic and anaerobic strains.

[0131] result

[0132] At the end of the incubation period, the presence or absence of turbidity indicated the state of microbial growth. The last dilution corresponding to no growth of M. furfur was retained as the minimum inhibitory concentration (MIC).

[0133] The study was conducted with n = 3. The results are shown in the following table.

[0134] Table 5

[0135]

[0136]

[0137] X: No inhibitory effect detected

[0138] Avocado unsaponifiables demonstrated an MIC of 0.25% against M. furfur strains; this MIC was lower than that obtained with the known antifungal agent phenoxyethanol. On the other hand, neither of the two concentrate samples tested, soy concentrate and avocado concentrate, showed inhibitory activity against M. furfur strains. Notably, soy unsaponifiables also showed no inhibitory activity against M. furfur, thus demonstrating the specificity of the activity of the avocado unsaponifiables according to the present invention.

Claims

1. An avocado unsaponifiable matter for use in preventing and / or treating pathologies and diseases caused by Malassezia yeasts, wherein the avocado unsaponifiable matter contains at least 50% by weight, preferably at least 60% by weight, of furanic lipids relative to the total mass of the avocado unsaponifiable matter.

2. A composition comprising avocado unsaponifiable matter containing at least 50% by weight, preferably at least 60% by weight, of furanic lipids relative to the total mass of the avocado unsaponifiable matter for use in preventing and / or treating pathologies and diseases caused by Malassezia yeasts.

3. The composition comprising avocado unsaponifiable matter for use according to claim 2, characterized in that The composition contains at least 0.25% by weight, preferably 0.50% by weight, of avocado unsaponifiable matter relative to the total mass of the composition.

4. The avocado unsaponifiable matter for use according to claim 1, or the composition comprising the avocado unsaponifiable matter for use according to claim 2 or 3, characterized in that Conditions and diseases caused by Malassezia yeasts are selected from seborrheic dermatitis, in particular infantile seborrheic dermatitis, such as cradle cap, pityriasis capitis, Malassezia folliculitis, pityriasis versicolor and dandruff.

5. Avocado unsaponifiable matter for use according to claim 1 or 4 or a composition comprising avocado unsaponifiable matter for use according to any one of claims 2 to 4, characterized in that The avocado unsaponifiable matter contains at least 5% by weight, preferably at least 7% by weight, of polyhydroxylated fatty alcohol relative to the total mass of the avocado unsaponifiable matter.

6. Avocado unsaponifiable matter for use according to any one of claims 1 and 4 to 5 or a composition comprising avocado unsaponifiable matter for use according to any one of claims 2 to 5, characterized in that Topical application of avocado unsaponifiables or a composition comprising avocado unsaponifiables.

7. Avocado unsaponifiable matter for use according to any one of claims 1 and 4 to 6 or a composition comprising avocado unsaponifiable matter for use according to any one of claims 2 to 6, characterized in that The avocado unsaponifiable matter is obtained by a method comprising at least the following steps: i. a heat treatment step of the avocado oil concentrate, advantageously carried out at a temperature ranging from 60°C to 90°C, preferably 80°C, ii. a step of saponifying the avocado oil concentrate in the presence of an ethanolic or aqueous alkali solution of the sodium hydroxide or potassium hydroxide type to obtain an avocado unsaponifiable, iii. an optional step of precipitating the soap obtained in step ii., iv. at least one step of extraction of the product obtained in step ii. or iii., wherein the avocado unsaponifiable matter is purified by liquid / liquid or solid / liquid extraction using at least 50% by volume of a solvent chosen from ethyl acetate, propyl acetate and butyl acetate relative to the total volume of the extraction solvent, and v. Optional additional purification steps of distillation and / or deodorization.

8. A method for preparing avocado unsaponifiable matter, comprising at least the following steps: i. a heat treatment step of the avocado oil concentrate, advantageously carried out at a temperature ranging from 60°C to 90°C, preferably 80°C, ii. a step of saponifying the avocado oil concentrate in the presence of an ethanolic or aqueous alkali solution of the sodium hydroxide or potassium hydroxide type to obtain an avocado unsaponifiable, iii. an optional step of precipitating the soap obtained in step ii., iv. at least one step of extraction of the product obtained in step ii. or iii., wherein the avocado unsaponifiable matter is purified by liquid / liquid or solid / liquid extraction using at least 50% by volume of a solvent chosen from ethyl acetate, propyl acetate and butyl acetate relative to the total volume of the extraction solvent, and v. Optional additional purification steps of distillation and / or deodorization.

9. The method for preparing avocado unsaponifiable matter according to claim 8, wherein the extraction solvent in step iv. is ethyl acetate.

Citation Information

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