Topical compositions

Abstract

The present invention relates to topical compositions comprising erythrulose and hydroxyacetophenone as well as the use thereof for the prevention and/or treatment of ailments associated with Malassezia yeast, Propionibacterium acnes as well as the protection against molds such as in particular Aspergillus brasiliensis.

Claims

1. A topical composition comprising erythrulose and from 0.01 wt. % to 2 wt. %, based total weight of the composition, of hydroxyacetophenone.

2. The topical composition according to claim 1, wherein the erythrulose is present in an amount from 0.005 to 5 wt. %, based on the total weight of the composition.

3. The topical composition according to claim 1, wherein the hydroxyacetophenone is p-hydroxyacetophenone.

4. The topical composition according to claim 1, wherein the composition is a cosmetic or pharmaceutical composition.

5. The topical composition according to claim 4, wherein the composition is a shampoo preparation, a hair conditioner, an oil-in-water (O/W) emulsion, a water-in-oil (W/O) emulsion or a gel.

6. The topical composition according to claim 1, wherein the composition further comprises water and at least one agent selected from the group consisting of surfactants, emulsifiers, thickeners and oils.

7. The topical composition according to claim 1, wherein the hydroxyacetophenone is present in an amount from 0.1 wt. % to 1 wt. %, based on the total weight of the composition.

8. The topical composition according to claim 1, wherein the hydroxyacetophenone is present in an amount from 0.1 wt. % to 0.6 wt. %, based on the total weight of the composition.

9. The topical composition according to claim 1, wherein the erythrulose is present in an amount from 0.01 to 3 wt. %, based on the total weight of the composition.

10. The topical composition according to claim 1, wherein the erythrulose is selected is present in an amount from 0.025 to 2 wt. %, based on the total weight of the composition.

11. A method of treating skin and/or scalp which comprises contacting the skin and/or scalp with the topical composition according to claim 1.

12. The method according to claim 11, wherein the method is for the treatment, prevention and/or prophylaxis of itching skin and/or for maintaining a healthy skin homeostasis and/or for maintaining skin microbiome balance.

13. A method for the treatment of itching skin and/or for maintaining a healthy skin homeostasis and/or for maintaining skin microbiome balance, wherein the method comprises topically applying to skin an effective amount of the topical composition according to claim 1.

14. The method according to claim 13, wherein the method is for the treatment, prevention and/or prophylaxis of Malassezia yeast.

15. The method according to claim 14, wherein the Malassezia yeast comprises Malassezia furfur.

16. The method according to claim 15, wherein the diseases and/or disorders are selected from the group consisting of pityriasis versicolor, dandruff formation, seborrheic dermatitis, atopic dermatitis and psoriasis.

17. A method for the prevention and/or prophylaxis of acne, wherein the method comprises topically applying to skin an amount of the topical composition according to claim 1 sufficient to provide prevention and/or prophylaxis of acne.

Description

EXAMPLE 1: ANTIMICROBIAL EFFICACY

(1) Actives: Erythrulose from DSM Nutritional products SymSave® H from Symrise (p-Hydroxyacetophenone)

(2) The antimicrobial efficacy is assessed in analogy to the regulatory challenge test method (NF EN ISO11930). Thus, solutions of the respective active(s) in physiological serum with 0.85 wt.-% NaCl in the concentrations as outlined in the tables below were prepared under sterile conditions. The solutions of the active(s) were then deposed in 96-deep well plates (1.6 ml/well). The wells were contaminated with Malassezia furfur, Propionibacterium acnes, respectively Aspergillus brasiliensis to obtain the initial contamination as outlined in table 1, 2 and 3. After contamination, each well was thoroughly mixed to ensure a homogeneous distribution of the microbes. Then each plate was incubated at 22° C. for 24 h. The counting of the (remaining) population was carried out 24 h after contamination. The results are outlined in the tables below.

(3) TABLE-US-00001 TABLE 1 Results obtained with Malassezia furfur Time Malassezia furfur # Test solution [h] colony count [cfu/ml] Δ* 1a 0.5 wt.-% Erythrulose° 0 3300 1b 24 3300  ±0% 2a 0.5 wt.-% 0 3300 2b p-Hydroxyacetophenone 24 550  −83% 3a 0.5 wt.-% Erythrulose° 0 3300 3b 0.5 wt.-% 24 0 −100% p-Hydroxyacetophenone.sup.+ *Δ = ({microorganism count t = 0 h} − {microorganism count t = 24}/{microorganism count t = 0}) * 100 °corresponds to 0.4 wt.-% of active

(4) As can be seen in the table above erythrulose at a concentration of 0.5% does not exert any anti-fungal effect against Malassezia furfur, which would result in a reduction thereof. However, erythrulose is able to boost the efficacy of p-hydroxyacetophenone against Malassezia furfur, when combined therewith.

(5) TABLE-US-00002 TABLE 2 Results obtained with Propionibacterium acnes Time P. acnes colony Δ* Test solution [h] counts [cfu/ml] [%] 0.5 wt.-% Erythrulose° 0 500000 0.5 wt.-% 24 3 −100% p-Hydroxyacetophenone.sup.+ °corresponds to 0.4 wt.-% of active.*Δ = ({microorganism count t = 0 h} − {microorganism count t = 24}/{microorganism count t = 0}) * 100

(6) As can be retrieved from table 2, the combination of erythrulose and p-hydroxyacetophenone is highly active against P. acnes.

(7) TABLE-US-00003 TABLE 2 Results obtained with Aspergillus brasiliensis Aspergillus Time brasiliensis Log step Test solution [h] colony count [cfu/ml] reduction 0.5 wt.-% Erythrulose° 0 10000 24 100 2 0.4 wt.-% 0 10000 p-Hydroxyacetophenone 24 100 2 0.25 wt.-% Erythrulose* 0 10000 0.2 wt.-% 24 0 4 p-Hydroxyacetophenone °corresponds to 0.4 wt.-% of active *corresponds to 0.2 wt.-% of active

(8) (The term “Log reduction” is a well-known mathematical term used to show the relative number of cells, germs, microbes, etc., reduced in or on something, e.g. a 2 log reduction means the number of microbes is 100 times smaller and a 3 log reduction means the number of microbes is 1000 times smaller).

(9) As can be seen in table 3 the combination of erythrulose and hydroxyacetophenone shows a synergistic effect against Aspergillus brasiliensis.

EXAMPLE 2: O/W FOUNDATION

(10) TABLE-US-00004 Ingredients INCI wt. % Deionised Water Aqua Ad 100 Glycerin Glycerin 2.00 Triethanolamine Triethanolamine 0.80 Paratexin Methylparaben EP 0.20 Keltrol Xanthan Gum 0.30 Erythrulose Erythrulose 0.5 Titanium dioxide C.I. 77891 4.57 SunCROMA yellow C.I. 77492 0.30 iron oxide SunCROMA red C.I. 77491 0.13 iron oxide SunCROMA black C.I. 77499 0.20 iron oxide DC 556 Phenyl Trimethicone 3.60 Stearic Acid Stearic Acid 1.4 Cetyl Alcohol Cetyl Alcohol 3.0 Paratexin P Propylparaben EP 0.1 p-Hydroxyacetophenone Hydroxyacetophenone 0.5

EXAMPLE 3: ALCOHOL FREE FACIAL TONIC

(11) TABLE-US-00005 Ingredients INCI wt. % Polysorbate 20 Polysorbate 20 2.00 Alpaflor Calendula AO Calendula Officinalis Extract, 0.80 Glycerin, Water Alpaflor Buddleja AO Buddleja Davidii Extract, Glycerin, 0.80 Water Ariasilk Phospholipd Sodium Coco PG-Dimonium 0.50 CDM Chloride Phosphate Fragrance Parfum 0.10 Deionised Water Aqua Ad 100 Citric Acid Citric Acid 0.01 Erythrulose Erythrulose 0.75 Paratexin FRP Ethylparaben, Butylparaben, 0.10 Propylparaben, Isobutylparaben p-Hydroxyacetophenone Hydroxyacetophenone 0.7 

EXAMPLE 4: W/O CREAM

(12) TABLE-US-00006 Ingredients INCI wt. % Cremophor WO-7 PEG-7 Hydrogenated 2.50 Castor Oil Elfacos ST-9 PEG-45/Dodecyl Glycol 2.00 Copolymer Cirebelle 303 Synthetic Wax 5.00 Cirebelle 109L Synthetic Wax 7.20 Miglyol 818 Caprylic/Capric/Linoleic 5.00 Triglyceride Eutanol G Octyldodecanol 7.50 Cetiol OE Dicaprylyl Ether 9.20 Deionised Water Aqua Ad 100 Glycerin Glycerin 5.00 Propylene Glycol Propylene Glycol 2.00 Euxyl PE 9010 Phenoxyethanol and 0.80 Ethylhexylglycerin Erythrulose Erythrulose 0.3 p-Hydroxyacetophenone Hydroxyacetophenone 0.1

EXAMPLE 5: SOOTHING GEL

(13) TABLE-US-00007 Ingredients INCI wt. % Deionised Water Aqua Ad 100 Keltrol CG RD Xanthan Gum 0.50 Sodium Benzoate Sodium Benzoate 0.20 Potassium Sorbate Potassium Sorbate 0.25 Alpaflor Marrabium AO Glycerin, Aqua, Marrubium Vulgare, 3.00 Sodium Benzoate, Potassium Sorbate Erythrulose Erythrulose 0.45 p-Hydroxyacetophenone Hydroxyacetophenone 0.65

EXAMPLE 6: O/W LOTION

(14) TABLE-US-00008 Ingredients INCI wt. % Deionised Water Aqua Ad 100 Menthol Menthol 0.10 Keltrol CG SFT Xanthan Gum 1.25 Ceralution ES Ceteareth-25, Di Sodium Ethylene 2.00 Dicocamide PEG-15 Disulfate Isofol 20 Octyldodecanol 5.00 Paratexin EC5 Benzoic Acid Benzyl Alcohol, 1.00 Dehydroacetic Acid, Sorbic Acid Erythrulose Erythrulose 0.4 p-Hydroxyacetophenone Hydroxyacetophenone 0.3

EXAMPLE 7: FACIAL CLEANSING GEL

(15) TABLE-US-00009 Ingredients INCI wt. % Deionised Water Aqua Ad 100 Carbopol AQUA SF-1 Acrylates Copolymer 7.50 Polymer Texapon NSO-BZ Sodium Laureth Sulfate 41.00  Miranol Ultra C 32 Sodium Cocoamphoacetate 5.00 Hostapon CLG Sodium Lauroyl Glutamate 4.50 Jaguar C 162 Hydroxypropyl Guar 1.00 Hydroxypropyltrimonium Chloride Erythrulose Erythrulose 0.3  Euxyl K 300 Phenoxyethanol & Methylparaben & 0.80 Propylparaben & Ethylparaben & Butylparaben & Isobutylparaben Alpaflor Malvia AO Glycerin, Aqua, Malva Sylvestris 2.00 (Mallow) Flower Extract, Potassium Sorbate, Sodium Benzoate Parfum Limette Fragrance q.s. FD&C Yellow 5 CI 19140 0.50 Frescolat Plus Menthyl Lactate, Menthol 0.20 Dehyton AB-30 Coco Betaine 2.00 Rewoderm LI S 80 PEG-200 Hydrogenated Glyceryl 1.00 Palmate & PEG-7 Glyceryl Cocoate Citric Acid Citric Acid q.s. p-Hydroxyacetophenone Hydroxyacetophenone 0.5 

EXAMPLE 8: LEAVE-ON HAIR AND SCALP CONDITIONER

(16) TABLE-US-00010 Ingredients INCI wt. % Deionised Water Aqua Ad 100 Ethanol DEB 96 Alcohol denat. 30.00 PVP/VA Copolymer PVP/VA Copolymer 2.50 Euxyl K-300 Phenoxyethanol, Methylparaben, 0.80 Butylparaben, Ethylparaben, Propylparaben, Isobutylparaben Protachem HCO-40 PEG-40 Hydrogenated Castor Oil 0.50 Fragrance ADAM Parfum 0.10 Triethanolamine 99% Triethanolamine 0.01 FD & C Yellow No 5 CI 19140, Aqua 0.10 (0.5% Solution) FD & C Blue No 1 CI 42090, Aqua 0.10 (0.5% Solution) Erythrulose Erythrulose 0.1 p-Hydroxyacetophenone Hydroxyacetophenone 0.3

EXAMPLE 9: SHAMPOO

(17) TABLE-US-00011 INCI Nomenclature wt. % Aqua (water) Ad 100 Ammonium laureth sulfate 10.00 Ammonium lauryl sulfate 5.00 Glycol distearate 1.00 Dimethicone 1.00 Cetyl alcohol 0.50 Cocamide MEA 3.00 Erythrulose 0.8 ZPT 0.50 Guar hydroxypropyltrimonium chloride 0.20 Hydrogenated polydecene 1.00 Polyquaternium 10 0.30 PEG 7m 0.50 Trimethylpropane tricaprylate/tricaprate 1.00 Preservative q.s. Fragrance 0.30 E 104, E 110, E 132 0.02 p-Hydroxyacetophenone 0.7

EXAMPLE 10: CLEAR SHAMPOO WITH PLANT EXTRACTS

(18) TABLE-US-00012 INCI Nomenclature wt. % Aqua (water) Ad 100 Sodium laureth sulfate 10.00 Lauryl glucoside 6.00 Cocamidopropyl betaine, 2.00 Propylene glycol 2.00 Perfume oil 1.25 Sodium citrate 0.25 Sodium benzoate 0.20 Panthenol 1.00 Sodium formate 0.20 Polyquaternium-10 0.20 Hydroxypropyl guar 0.05 hydroxypropyltrimonium chloride Erythrulose 0.2 PEG-35 castor oil 1.00 Maris sal 1.25 Polysorbate 20 1.00 Tocopheryl acetate 0.20 Prunus armeniaca 0.20 Echinacea purpurea 0.05 Tocopherol 0.05 Linoleic acid 0.20 Preservative 1.00 CI77891 0.02 p-Hydroxyacetophenone 0.6

EXAMPLE 11: RINSE-OFF HAIR AND SCALP CONDITIONER

(19) TABLE-US-00013 INCI Nomenclature wt. % Aqua (water) Ad 100 Stearyl alcohol 2.50 Cetyl alcohol 2.50 Behentrimonium chloride 1.30 Dimethicone 2.00 Erythrulose 0.3 Fragrance 0.50 Butylene glycol 2.00 Methyl parabene 0.30 p-Hydroxyacetophenone 0.3