NOVEL COMPOSITIONS

Abstract

The present invention relates to emulsions containing at least one sunscreen active agent and having improved sun protection factor (SPF) properties, as well as methods of improving sun protection factor (SPF) properties.

Claims

1. An emulsion composition with a phosphate ester emulsifier, wherein the emulsion composition comprises at least one sunscreen active agent and at least one human milk oligosaccharide.

2. The composition according to claim 1, wherein the at least one human milk oligosaccharide is present in an amount effective to increase SPF of the composition.

3. The composition according to claim 1, wherein the total amount of human milk oligosaccharides in the composition is selected in the range from 0.2 to 5 wt.-%, based on the total weight of the composition.

4. The composition according to claim 1, wherein the at least one human milk oligosaccharide is selected from the group consisting of 2-fucosyllactose, 3-fucosyllactose, difucosyllactose, lacto-N-fucopentaose I, 3sialyllactose sodium salt, 6sialyllactose sodium salt, lacto-N-neotetraose and lacto-N-tetraose; or a mixture thereof.

5. The composition according to claim 1, wherein the amount of the phosphate ester emulsifier in the composition is selected in the range from 0.1 to 10 wt. %, based on the total weight of the composition.

6. The composition according to claim 1, wherein the phosphate ester emulsifier is a C8-C25 alkyl phosphate.

7. The composition according to claim 1, wherein the total amount of the at least one sunscreen active agent in the composition is selected in the range from 1 to 50 wt.-%, preferably from 3 to 40 wt. %, most preferably from 5 to 30 wt.-%, based on the total weight of the composition.

8. The composition according to claim 1, wherein the at least one sunscreen active agent is homosalate, ethylhexyl salicylate, polysilicone-15, ethylhexyl 2 methoxycinnamate, octocrylene, phenylbenzimidazole sulphonic acid or a salt thereof, bis-ethylhexyloxyphenol methoxyphenyl triazine, ethylhexyl triazone, diethylhexyl butamido triazone, methylene bisbenzotriazolyl tetramethylbutylphenol, tris-biphenyl triazine, butyl methoxydibenzoylmethane, diethylamino hydroxybenzoyl hexyl benzoate, or a mixture thereof.

9. The composition according to claim 1, wherein the composition comprises a carrier consisting of at least 30 wt. % of water.

10. The composition according to claim 1, wherein the composition is an O/W emulsion.

11. The composition according to claim 1, wherein the composition comprises the phosphate ester emulsifier as co-emulsifier together with one or more further emulsifiers.

12.-13. (canceled)

14. A method for increasing the sun protection properties (SPF) of an emulsion composition with a phosphate ester surfactant comprising at least one sunscreen active agent, said method comprising adding at least one human milk oligosaccharide to the composition in an amount effective to increase the SPF of the composition.

15. A method of preparing an emulsion composition with a phosphate ester emulsifier comprising adding at least one sunscreen active agent and at least one human milk oligosaccharide to the composition during preparation of the emulsion composition.

16. (canceled)

17. The composition according to claim 4, wherein the at least one human milk oligosaccharide is selected from the group consisting of 2-fucosyllactose, difucosyllactose, 3sialyllactose sodium salt, 6sialyllactose sodium salt, lacto-N-neotetraose and lacto-N-tetraose; or a mixture thereof.

18. The composition according to claim 5, wherein the amount of the phosphate ester emulsifier in the composition is selected in the range from 0.5 to 4 wt.-%, based on the total weight of the composition.

19. The composition according to claim 6, wherein the C8-C25 alkyl phosphate is a C20-22 alkyl phosphate or a cetyl phosphate.

20. The composition according to claim 7, wherein the total amount of the at least one sunscreen active in the composition is selected in the range of 5 to 30 wt.-%, based on the total weight of the composition.

21. The composition according to claim 9, wherein the composition comprises a carrier consisting of at least 45 wt.-% of water.

22. The composition according to claim 11, wherein the one or more further emulsifiers comprises polyglyceryl-6 stearate, polyglyceryl-6 behenate, PEG-100 stearate, glyceryl stearate citrate, or a mixture thereof.

Description

EXAMPLES

Short Description

[0147] The HMO's 2FL, 3SL, LNT and LNnT were evaluated for their SPF boosting effect. For this purpose various sunscreens were prepared according to standard methods in the art as outlined in tables 1a, 2a and 3a.

In Vitro SPF Measurement

[0148] The in vitro SPF test was performed on PMMA plates (HD6 plates from Helioscreen, 5 cm5 cm, roughness of Sa=6 m): 32.5 mg of the respective formulation (i.e. 1.3 mg/cm.sup.2) were applied homogenously onto the PMMA plates and dried for 15 minutes.

[0149] The in vitro SPF was determined using a Labsphere 2000 UV Transmittance Analyzer: each PMMA plate was measured 9 times at different points on the plate resulting in 27 data points. The result is calculated as the average of these 27 data points.

TABLE-US-00002 TABLE 1a Formulation 1 Conc. Trade name INCI name [wt.-%] Lexfilm Sun Natural MB Capryloyl Glycerin/Sebacic Acid Copolymer 1.5 Lanette O Cetearyl Alcohol 1.0 TEGIN M Pellets MB Glyceryl Stearate 0.4 AMPHISOL K Potassium Cetyl Phosphate 0.5 Cetiol B Dibutyl Adipate 9.5 DL-alpha-Tocopheryl Tocopheryl Acetate 0.5 Acetate Uvinul A Plus Diethylamino Hydroxybenzoyl Hexyl 5.0 Benzoate PARSOL EHT Ethylhexyl Triazone 1.5 PARSOL Shield Bis Ethylhexyloxyphenol Methoxyphenyl 2.0 Triazine PARSOL MCX Ethylhexyl Methoxycinnamate 4.0 PARSOL SLX Polysilicone-15 2.0 Uvasaorb HEB Diethylhexyl Butamido Triazone 1.5 X-Tend 226 Phenethyl Benzoate 5.5 Dermosoft GMCY MB Glyceryl Caprylate 0.5 TEGO CARE PBS 6 MB Polyglyceryl-6 Stearate; Polyglyceryl-6 4.0 Behenate HMO See table 1b table 1b HYA-ACT TM M Sodium Hyaluronate 0.1 Phenethylalcohol Nat. Phenethyl Alcohol 1.0 PARSOL MAX Methylene Bis-Benzotriazolyl 4.0 Tetramethylbutylphenol; Aqua; Decyl Glucoside; Propylene Glycol; Xanthan Gum Water Dem Aqua Ad 100 Rheocare XGN XANTHAN GUM 0.4 TILAMAR PDO with PROPANEDIOL 2.0 NVISTA

TABLE-US-00003 TABLE 1b Results SPF HMO Conc. HMO SPF in vitro boosting Reference 64.1 Sialyllactose (3SL) 1% 75.9 +18% Lacto-N-Neotetraose (LNnT) 1% 85.7 +34%

TABLE-US-00004 TABLE 2a Formulation 2 Conc. Trade name INCI name [wt.-%] AMPHISOL K Potassium Cetyl Phosphate 2.0 Lanette O Cetearyl Alcohol 3.0 PARSOL 1789 Butyl Methoxydibenzoyl Methane 4.0 PARSOL EHS Ethylhexyl Salicylate 5.0 PARSOL 340 Octocrylene 8.0 PARSOL SHIELD Bis Ethylhexyloxyphenol 1.5 Methoxyphenyl Triazine Finsolv TN C12-15 Alkyl Benzoate 3.0 Dub DIS Diisopropyl Sebacate 2.0 Myritol 318 Caprylic/Capric Triglyceride 10.0 WATER DEM. Aqua Ad 100 Edeta BD Disodium EDTA 0.2 Keltrol CG-T Xanthan Gum 0.2 Glycerin 99.5% Glycerin 3.0 Triethanolamine Care Triethanolamine 0.1 HMO See table 2b table 2b Euxyl PE 9010 Phenoxyethanol; Ethylhexylglycerin 1.0

TABLE-US-00005 TABLE 2b Results Conc. HMO HMO [wt.-%] SPF in vitro SPF boosting Reference 5.3 Fucosyllactose (2FL) 1% 10.0 +89% 3% 15.2 +187% Lacto-N-tetraose (LNT) 1% 15.6 +194%

TABLE-US-00006 TABLE 3a Formulation 3 Conc. Trade name INCI name [wt.-%] AMPHISOL K Potassium Cetyl Phosphate 2.0 Lanette O Cetearyl Alcohol 3.0 PARSOL 1789 Butyl Methoxydibenzoyl Methane 4.0 PARSOL EHS Ethylhexyl Salicylate 5.0 PARSOL 340 Octocrylene 8.0 PARSOL Bis Ethylhexyloxyphenol 1.5 SHIELD Methoxyphenyl Triazine Finsolv TN C12-15 Alkyl Benzoate 3.0 Dub DIS Diisopropyl Sebacate 2.0 Myritol 318 Caprylic/Capric Triglyceride 5.0 WATER DEM. Aqua Ad 100 Edeta BD Disodium EDTA 0.2 Keltrol CG-T Xanthan Gum 0.2 Glycerin 99.5% Glycerin 3.0 Triethanolamine Triethanolamine 1.3 Care PARSOL HS Phenylbenzimidazole Sulfonic Acid 2.0 WATER DEM. Aqua 10.0 HMO see table 3b table 3b Euxyl PE 9010 Phenoxyethanol; 1.0 Ethylhexylglycerin

TABLE-US-00007 TABLE 3b Results Conc. HMO HMO [wt.-%] SPF in vitro SPF boosting Reference 11.4 Fucosyllactose (2FL) 1% 21.2 +86% 3% 23.3 +104% Lacto-N-tetraose (LNT) 1% 29.2 +156%

[0150] As shown in the tables 1 b, 2b and 3b the HMO's 2FL, 3SL, LNT and LNnT boost the in vitro SPF between 34% and 194%.

TABLE-US-00008 TABLE 4 Formulation 4 Trade name INCI Name 1 (Control) 2 Sensanov WR C20-22 Alkyl Phosphate 2.0 2.0 Lanette O Cetearyl alcohol 3.0 3.0 PARSOL 1789 Butylmethoxydibenzoyl 4.0 4.0 methane Parsol EHT Ethylhexyl Triazone 3.0 3.0 PARSOL 340 Octocrylene 8.0 8.0 HMS Homosalate 5.0 5.0 Finsolv TN C12-15 Alkyl benzoate 3.0 3.0 Dub DIS Diisopropyl sebacate 2.0 2.0 Myritol 318 Caprylic/Capric trigylceride 10.0 10.0 WATER DEM. Aqua 53.6 52.6 Edeta BD Disodium EDTA 0.2 0.2 Keltrol CG-T Xanthan Gum 0.2 0.2 Glycerin 99.5% Glycerin 3.0 3.0 6SL Sialyllactose 1.0 Euxyl PE 9010 Phenoxyethanol, 1.0 1.0 Ethylhexylglycerin SPF in vitro 21.8 27.1 SPF boosting +24.6%

TABLE-US-00009 TABLE 5 Formulation 5 (no phosphate ester emulsifier) - Comparative example 3 Tradename INCI Name (Control) 4 Tegocare 450 Polyglyceryl-3 Methylglucose 3.0 3.0 Distearate Lanette O Cetearyl alcohol 3.0 3.0 Uvinul A Plus Diethylamino Hydroxybenzoyl 5.0 5.0 Hexyl Benzoate Parsol MCX Ethylhexyl Methoxycinnamate 8.0 8.0 Parsol SLX Polysilicone-15 3.0 3.0 Uvasrob HEB Diethylhexyl Butamido Triazone 4.0 4.0 Finsolv TN C12-15 Alky benzoate 3.0 3.0 Dub DIS Diisopropyl sebacate 2.0 2.0 Myritol 318 Caprylic/capric triglyceride 8.0 8.0 WATER DEM. Aqua Ad 100 Ad 100 Edeta BD Disodium EDTA 0.2 0.2 Keltrol CG-T Xanthan Gum 0.2 0.2 Glycerin 99.5% Glycerin 3.0 3.0 3-Sialyllactose Sialyllactose 1.0 Euxyl PE 9010 Phenoxyethanol, 1.0 1.0 Ethylhexylglycerin SPF in vitro 12.3 12.7 SPF boosting +3.3%