Cosmetic preparation for reducing fungal acne

Abstract

The present invention relates to cosmetic and / or dermatological preparations containing propylene glycol.

Description

[0001] Beiersdorf Aktiengesellschaft Hamburg

[0002] Cosmetic preparation for reducing fungal acne

[0003] The present invention relates to cosmetic and / or dermatological preparations containing propane-1,2-diol (INCI: Propylene Glycol).

[0004] A person's outward appearance can be influenced and enhanced through the use of cosmetic products. Regular use of cleaning, cosmetic, and care products ensures that people feel attractive, beautiful, and comfortable in their surroundings, and radiate this outwards.

[0005] The condition and therefore the appearance of the skin can be influenced by various factors. Besides aging, sun exposure, and other external factors, skin diseases can also significantly shape the skin's appearance. For example, the skin may be prone to blemishes. This manifests as the appearance of blackheads, pimples, pustules, or acne. All these forms primarily occur due to an overproduction of sebum (seborrhea). Sebum is a mixture of fatty acids, waxes, cholesterol, and lipids and serves as a protective secretion for the skin. In blemished skin, especially in cases of acne, the overproduced sebum serves as a breeding ground for various microorganisms, particularly bacteria and yeasts. These break down the sebum, and the resulting byproducts clog the skin's pores, leading to inflammation.In many cases, these heal only slowly and leave scar tissue, which permanently damages the appearance of the skin.

[0006] Acne (more precisely, acne vulgaris) primarily refers to the blockage of sebaceous glands by various bacterial pathogens, such as Cutibacterium acnes (C. acnes), which causes inflammation and scarring of the skin tissue. Acne occurs most frequently on the face, chest, back, or other areas where the density of sebaceous glands is higher. Factors contributing to acne can include hormonal changes, genetic predisposition, stress, cosmetics, environmental influences, medications, or certain foods. The treatment and prevention of acne can vary and depend on the severity, symptoms, and the causes and / or pathogens of the specific condition. Nevertheless, effective active ingredients are needed for the treatment of acne, which reduce microorganisms on the skin during the course of therapy.

[0007] A skin condition that resembles acne is Malassezia folliculitis. This condition is caused by the overproduction of yeast fungi of the genus / Wa / assez / a and manifests as red pimples, itching, and acne-like eczema. Like acne itself, Malassezia folliculitis occurs in areas of skin rich in sebum, such as the face or back. Due to the similar symptoms, this condition is also colloquially known as "fungal acne."

[0008] Consequently, the object of the present invention was to provide a preparation or a treatment method against Malassezia folliculitis.

[0009] Since Malassezia folliculitis is a fungal skin disease that nevertheless exhibits similar symptoms to bacterial acne, misdiagnosis and consequently incorrect treatment are common, which should be avoided by the patient. Furthermore, it is possible for patients to suffer from both bacterial acne and Malassezia folliculitis. In these cases, it would be advantageous to have treatments that are equally effective against both skin diseases.

[0010] Therefore, a further objective of the present invention was to provide a treatment option which ideally is effective against both bacterial acne and Malassezia folliculitis.

[0011] Malassezia yeasts are generally a component of the skin microbiome. In some individuals, however, they can act as pathogens and thus trigger Malassezia folliculitis. The following species of Malassezia yeast are found on the skin: M. caprae, M. cuniculi, M. dermatis, M. equine, M. furfur, M. globosa, M. japonica, M. nana, M. obtuse, M. pachydermatis, M. restricta, M. slooffiae, and M. sympodialis. The clinical picture of Malassezia folliculitis is most often caused by M. furfur.

[0012] For the treatment of Malassezia folliculitis, the first step is to keep the affected skin clean and dry. However, antifungal medications are increasingly used in therapy. In particular, the active ingredients ketoconazole or ciclopirox are used topically to reduce the yeast fungi. In more severe cases, oral therapy may also be used, employing the active ingredients itraconazole or fluconazole.

[0013] Ketoconazole, in particular, is a frequently used drug in the treatment of Malassezia folliculitis. However, increasing studies show that its effectiveness against fungal acne is limited.

[0014] Furthermore, it is known to those skilled in the art that active ingredients such as benzoyl peroxide, salicylic acid, and / or zinc derivatives are used in the topical treatment of Malassezia folliculitis. However, the use of these active ingredients has often proven insufficiently effective in the treatment of fungal acne.

[0015] Another disadvantage is that while known active ingredients and combinations of active ingredients reduce Malassezia yeasts when applied topically to human skin, the occurrence of side effects often prevents visible improvements in the skin's appearance. Therefore, there remains a need for active ingredients and / or combinations of active ingredients that enable effective treatment of Malassezia folliculitis but are gentler on the skin, thus causing less or no irritation.

[0016] In the topical treatment of Malassezia folliculitis, the active ingredients are often administered in cleansing preparations (rinse-off) or in the form of creams. The frequently high oil content of such formulations can, in turn, lead to oily skin, which then promotes the growth of bacteria and yeasts. For this reason, a further objective of the invention was to provide an aqueous preparation for the treatment of Malassezia folliculitis that can nevertheless be applied as a leave-on product to human skin.

[0017] Surprisingly for the expert, a cosmetic and / or dermatological preparation has now been made available which, when used conventionally, leads to the death of Cutibacterium acnes (C. acnes) and / or Malassezia furfur (M. furfur).

[0018] The present invention relates to a cosmetic and / or dermatological preparation comprising propane-1,2-diol (INCI: Propylene Glycol).

[0019] A further object of the invention is the cosmetic use of a preparation according to the invention for reducing Cutibacterium acnes and / or Malassezia furfur on human skin. A further object of the invention is the preparation according to the invention for use in the treatment of acne and / or Malassezia folliculitis on human skin.

[0020] Another object of the invention is the preparation according to the invention for use in the treatment of acne and / or Malassezia folliculitis on the face and / or back.

[0021] The publication “Antimycotic activity of propane-1,2-diol” (by J. Faergemann and T. Fredriksson, Sabouraudia, Vol. 18, 1980, 163-166) is known to those skilled in the art. However, the disclosed results could not provide any indication of the present invention.

[0022] This document describes the use of propylene glycol and its antifungal effect; however, it discloses the use of large quantities (9 wt%) of propylene glycol. Increased exposure to propylene glycol at high concentrations can lead to skin irritation and allergic reactions in the form of skin redness. Furthermore, high propylene glycol concentrations accelerate the penetration of other ingredients into the skin. Therefore, a further objective of the invention was to provide an effective preparation and / or treatment method without increasing the penetration of other ingredients into the skin.

[0023] It has also proven advantageous that the preparation according to the invention is effective in the treatment of both bacterial acne and Malassezia folliculitis. The preparation according to the invention exhibits a synergistic effect in reducing Cutibacterium acnes and Malassezia furfur. Thus, the invention represents a combination product for the treatment of acne and fungal acne. Furthermore, the aqueous preparation is a gentle application that can be used as a leave-on product and can therefore remain on the skin throughout the treatment period.

[0024] Where CFU (column forming unit) values ​​are given in this disclosure for determining the therapeutic effect of the preparation according to the invention against C. acnes and / or M. furfur, these refer to a measurement using a suspension test. The suspension test was carried out as follows. Stock cultures of the pathogens to be investigated in glycerol, which were prepared according to European Standard 12353, are stored in a refrigerator at 5°C. First, a first passage is prepared from the stock culture. For this purpose, the respective culture is streaked onto a suitable agar plate using a disposable inoculating loop (see table Culture Conditions). This culture is then incubated under the appropriate conditions. Now, a second passage is prepared from this first passage by picking up some colonies with a sterile inoculating loop and then streaking them onto another new agar plate.This second passage is then incubated for 5 days at the appropriate temperature and can then be used for the respective suspension test.

[0025] To prepare the culture suspensions, a few colonies from the described second passage are collected using a sterile inoculating loop, added to 10 mL of medium (see table: Culture conditions) in a baffle flask containing 5g of glass beads (0 = 4 mm), and shaken for 3 minutes. A cell count of 1 x 10⁻⁶ per mL is then determined for the culture suspensions. A 7 to 1x10 A 8. For this purpose, an optical density (OD) is determined with an Eppendorf photometer at 600 nm by diluting the suspension and an OD = 0.2 is set for the suspension.

[0026] For the suspension test, 900 pL of the preparation to be tested are placed in a sterilized Eppendorf tube. (For the respective control test, 900 pL of diluent are used.) A duplicate determination is always performed in each test. For this purpose, 100 pL of the prepared culture suspensions are added. From this point onward, 1:10 dilutions of all samples are prepared with neutralization medium after 5 min, 10 min, 20 min, and 60 min (900 pL neutralization medium + 100 pL test sample). From this dilution, a 1:1000 dilution is then prepared (990 pL neutralization medium + 10 pL of the 1:10 dilution). The dilutions thus prepared are then plated onto agar plates (see table: Culture Conditions) using a spiral plater and incubated. After incubation (see table Culture Conditions), the plates are evaluated on the countermat to determine the column forming unit (CFU). Table: Culture Conditions

[0027] Cultivation in an anaerobic atmosphere using anaerobic pads.

[0028] Where weight percentages (wt%) are given below without reference to a specific composition or mixture, these percentages always refer to the total weight of the cosmetic and / or dermatological preparation. Where ratios of components / substances / groups of substances are disclosed below, these ratios refer to the weight ratios of the components / substances / groups of substances mentioned.

[0029] The terms “according to the invention”, “advantageous according to the invention”, “advantageous in the sense of the present invention”, etc., always refer, within the scope of the present disclosure, to both the preparation according to the invention and the use according to the invention.

[0030] Unless otherwise stated, all tests were conducted under standard conditions. "Standard conditions" means 20°C, 1013 hPa, and a relative humidity of 50%.

[0031] When the term skin is used, it preferably refers to human skin.

[0032] When the term “against Malassezia furfur” is used in this revelation, it means that Malassezia furfur will be killed and / or the spread of Malassezia furfur will be prevented and / or reduced.

[0033] The cosmetic and / or dermatological preparation according to the invention is characterized in that it contains 1,2-propanediol (INCI: Propylene Glycol). Furthermore, it is advantageous if the total proportion of propylene glycol is 0.1 to 5.0 wt.%, preferably 0.5 to 3.0 wt.%, and particularly preferably 1.0 to 1.5 wt.% based on the total weight of the preparation. The cosmetic and / or dermatological preparation according to the invention is advantageously characterized in that it contains gluconolactone (INCI: Gluconolactone). Gluconolactone is a lactone formed by intramolecular esterification of gluconic acid. In one embodiment, it is preferred if the gluconolactone is a glucono-1,5-lactone, wherein the intramolecular esterification to the lactone occurs between the C-5 hydroxyl group and the C-1 carboxyl group of the gluconic acid. Furthermore, it is advantageous if the total proportion of gluoconolactone is between 0.1 and 2.0 wt.-%, preferably from 0.1 to 1.8 wt.% and particularly preferably from 1.0 to 1.8 wt.% based on the total weight of the preparation.

[0034] Furthermore, it has proven advantageous within the meaning of the invention that the preparation contains, in addition to gluconolactone, an acid complex composed of gluconolactone and at least one other acid. Advantageous acids as components of the acid complex are lactic acid (INCI: Lactic Acid), glycolic acid (INCI: Glycolic Acid), citric acid (INCI: Citric Acid), ascorbic acid (INCI: Ascorbic Acid), malic acid (INCI: Malic Acid), and / or tartaric acid (INCI: Tartaric Acid). It is further advantageous if this acid complex constitutes a total proportion of 0.5 to 10 wt.%, preferably 1.0 to 5.0 wt.%, and particularly preferably 1.0 to 2.2 wt.% based on the total weight of the preparation.

[0035] It has proven advantageous for the preparation to contain lactic acid (INCI: Lactic Acid) and / or its salts. If lactic acid and / or its salts are included, it is advantageous if the proportion of these components is between 0.01 and 1.9 wt.%, preferably 0.01 and 0.5 wt.%, based on the total weight of the preparation.

[0036] Furthermore, it has proven advantageous if the preparation contains glycolic acid (INCI: Glycolic Acid). If glycolic acid is included, it is advantageous if the proportion is 0.01 to 0.2 wt.%, preferably 0.1 to 0.2 wt.%, based on the total weight of the preparation.

[0037] The cosmetic and / or dermatological preparation according to the invention may advantageously contain at least one preservative. Preservatives are defined as those preservative substances that are authorized for use in cosmetic products in Europe according to the German Cosmetics Regulation and Regulation (EC) No. 1223 / 2009 on cosmetic products. The at least one preservative may advantageously be selected from the group consisting of phenoxyethanol (INCI: Phenoxyethanol), sodium benzoate (INCI: Sodium Benzoate), piroctone olamine (INCI: Pirotone Olamine), and / or benzyl alcohol (INCI: Benzyl Alcohol). Advantageously, the proportion of the at least one preservative in the preparation according to the invention is 0.1 to 0.9 wt.%, preferably 0.4 to 0.9 wt.%, and particularly preferably 0.5 to 0.9 wt.%, based on the total weight of the preparation.

[0038] In a preferred embodiment, the cosmetic and / or dermatological preparation contains phenoxyethanol as a preservative. If phenoxyethanol is included, it is preferred that the total proportion of phenoxyethanol is 0.1 to 0.9 wt.%, preferably 0.4 to 0.9 wt.%, and particularly preferably 0.6 to 0.9 wt.% based on the total weight of the preparation.

[0039] Further preferred embodiments of the invention are characterized by the inclusion of glycerin. If glycerin is included, it is preferred that the total glycerin content is 0.1 to 10 wt.%, preferably 1.0 to 5.0 wt.%, and particularly preferably 1.0 to 3.0 wt.% based on the total weight of the preparation.

[0040] Furthermore, it is advantageous if the pH value of the cosmetic and / or dermatological preparation is between 3.5 and 4.6, preferably between 3.8 and 4.3. The pH value is preferably adjusted by the addition of lactic acid (INCI: Lactic Acid), sodium hydroxide (INCI: Sodium Hydroxide) and / or citric acid (INCI: Citric Acid).

[0041] Furthermore, it is advantageous if the cosmetic and / or dermatological preparations according to the present invention contain water as a cosmetic carrier, wherein water is present in a total proportion of 75 wt.% to 95 wt.%, preferably 75 wt.% to 85 wt.%, based on the total weight of the preparation.

[0042] Furthermore, it is advantageous if the cosmetic and / or dermatological preparation is a toner and / or a facial toner.

[0043] In a preferred embodiment, the preparation according to the invention is characterized by the fact that it is transparent under normal conditions.

[0044] Furthermore, it is advantageous within the meaning of the present invention if the preparation is free of salicylic acid. It is also advantageous if the preparation according to the invention does not contain any substances that release formaldehyde. Formaldehyde should be avoided in cosmetic products because it is suspected of causing cancer and allergies. One formaldehyde-releasing preservative is DMDM ​​hydantoin (glydant). It is therefore advantageous within the meaning of the present invention if the cosmetic and / or dermatological preparation is free of DMDM ​​hydantoin (glydant).

[0045] It can be advantageous if the cosmetic and / or dermatological preparation according to the invention contains cellulose gum (INGI: Cellulose Gum) for regulating viscosity. If cellulose gum is included, it is advantageous if the proportion of this component is 0.01 to 0.1 wt.%, preferably 0.01 to 0.05 wt.% based on the total weight of the preparation.

[0046] Furthermore, it is advantageous if the cosmetic and / or dermatological preparations according to the present invention contain ethanol, wherein ethanol is present in a total proportion of 4.0 wt.% to 20.0 wt.%, preferably 7.0 wt.% to 10.0 wt.%, based on the total weight of the preparation.

[0047] It can be advantageous if the cosmetic and / or dermatological preparation according to the invention contains at least one humectant. Humectants are defined as substances or mixtures of substances that give cosmetic preparations the property of reducing the loss of moisture from the stratum corneum (also called transepidermal water loss (TEWL)) and / or positively influencing the hydration of the stratum corneum after application or distribution on the skin surface. Advantageous humectants within the meaning of the present invention are, for example, 1,2-hexanediol, methylpropanediol, ethylhexylglycerin, butylene glycol, methylpropanediols, biosaccharide gum-1, glycine sorbitol, soya, ethylhexyloxyglycerin, pyrrolidone carboxylic acid, caprylyl glycol, decylene glycol, and urea.

[0048] If 1,2-hexanediol is included, it is advantageous if the proportion of this component is 0.1 to 1.0 wt.%, preferably 0.3 to 1.0 wt.% based on the total weight of the preparation.

[0049] Furthermore, the preparations according to the invention may comprise further additives and / or active ingredients, provided these are not incompatible with the preparations according to the invention. Advantageous additives and / or active ingredients are selected from the group consisting of color pigments, perfumes, licochalcone A, hyaluronic acid, and / or carnitine. Comparative experiments and examples

[0050] The following examples are intended to illustrate the present invention without limiting it. Unless otherwise stated, all quantities, proportions, and percentages are based on the weight and total quantity or total weight of the preparations.

[0051] The following formulations were prepared for the comparative tests. Formulations Cf. 1 to Cf. 2 are not according to the invention, while Ex. 1 to Ex. 2 are according to the invention.

[0052] The preparations listed above were manufactured and their properties were investigated in a comparative study using suspension tests against the pathogens C. acnes and M. furfur. The following table of test results also includes a column for an untreated control in the suspension tests.

[0053] Data is given in CFU (Colony forming unit)

[0054] The formulations according to the invention show a surprising reduction of C. acnes and / or M. furfur in the suspension test. Such a reduction of CFlIs could not be achieved with other formulations.

[0055] The following examples are intended to further illustrate the invention without limiting it:

Claims

Patent claims 1. Cosmetic and / or dermatological preparation comprising propane-1,2-diol (INCI: Propylene Glycol).

2. Cosmetic and / or dermatological preparation according to claim 1, characterized in that the total proportion of propylene glycol is 0.1 to 5.0 wt.%, preferably 0.5 to 3.0 wt.% and particularly preferably 1.0 to 1.5 wt.% based on the total weight of the cosmetic preparation.

3. Cosmetic and / or dermatological preparation according to one of the preceding claims, characterized in that the preparation contains gluconolactone (INCI: Glucon- nolactone).

4. Cosmetic and / or dermatological preparation according to one of the preceding claims, characterized in that the total proportion of gluconolactone is 0.1 to 2.0 wt.%, preferably 0.1 to 1.8 wt.% and particularly preferably of 1.0 to 1.8% by weight based on the total weight of the cosmetic preparation.

5. Cosmetic and / or dermatological preparation according to one of the preceding claims, characterized in that it contains lactic acid (INCI: Lactic Acid), wherein it is advantageous if the proportion of lactic acid is from 0.01 to 1.9 wt.%, preferably 0.01 to 0.5 wt.%, based on the total weight of the preparation.

6. Cosmetic and / or dermatological preparation according to one of the preceding claims, characterized in that it contains glycolic acid (INCI: Glycolic Acid), wherein it is advantageous if the proportion of glycolic acid is 0.01 to 0.2 wt.%, preferably 0.1 to 0.2 wt.%, based on the total weight of the preparation.

7. Cosmetic and / or dermatological preparation according to one of the preceding claims, characterized in that it contains phenoxyethanol, wherein it is advantageous if the proportion of phenoxyethanol is 0.1 to 0.9 wt.%, preferably 0.4 to 0.9 wt.% and particularly preferably 0.6 to 0.9 wt.%, based on the total weight of the preparation.

8. Cosmetic and / or dermatological preparation according to one of the preceding claims, characterized in that it contains glycerin, wherein it is advantageous if the proportion of glycerin is from 0.1 to 10 wt.%, preferably from 1.0 to 5.0 wt.% and in particular preferably from 1.0 to 3.0 wt.% based on the total weight of the preparation.

9. Cosmetic and / or dermatological preparation according to one of the preceding claims, characterized in that the pH value of the preparation is from 3.5 to 4.6, preferably from 3.8 to 4.

3.

10. Cosmetic and / or dermatological preparation according to one of the preceding claims, characterized in that the preparation comprises water as a cosmetic carrier, wherein the total proportion of water is advantageously from 75 wt.% to 95 wt.%, preferably 75 wt.% to 85 wt.% based on the total weight of the cosmetic preparation.

11. Cosmetic and / or dermatological preparation according to one of the preceding claims, characterized in that it is a toner and / or a facial toner.

12. Cosmetic and / or dermatological preparation according to one of the preceding claims, characterized in that it is a transparent solution.

13. Cosmetic and / or dermatological preparation according to one of the preceding claims, characterized in that it is free of salicylic acid.

14. Preparation according to any of the preceding claims for use in the treatment of acne and / or Malassezia folliculitis on human skin.

15. Cosmetic use of a preparation according to any of the preceding claims for reducing Malassezia furfur on human skin.

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