COSMETIC COMPOSITION COMPRISING A COMBINATION OF PONGAMIA OIL AND 4-T-BUTYLCYCLOHEXANOL FOR THE TREATMENT OF ROSACEA

20190350875 · 2019-11-21

Assignee

Inventors

Cpc classification

International classification

Abstract

The present invention relates to the novel combination of pongamia oil and 4-t-butylcyclohexanol, and to the uses thereof in the fields of cosmetics and dermatology to combat redness.

More specifically, the present invention relates to the cosmetic use of a composition comprising said combination to combat rosacea.

Claims

1-12. (canceled)

13. Method for treating rosacea or skin redness comprising the administration to a patient in need thereof, of a combination comprising pongamia oil and 4-t-butylcyclohexanol, wherein the 4-t-butylcyclohexanol is solubilized in 1,5-pentanediol.

14. Method according to claim 13, wherein the rosacea is selected from the group consisting of erythematotelangiectatic rosacea, papulopustular rosacea, phymatous rosacea, ocular rosacea.

15. Method according to claim 13, wherein the administration is topical.

16. Dermatological or dermocosmetic composition comprising a combination pongamia oil and 4-t-butylcyclohexanol, wherein the 4-t-butylcyclohexanol is solubilized in 1,5-pentanediol, in association with at least one dermatologically or dermocosmetically acceptable excipient.

17. Dermatological or dermocosmetic composition according to claim 16, wherein it comprises 0.01 to 5 wt %, preferably 0.05 to 2 wt % pongamia oil based on the total weight of the composition.

18. Dermatological or dermocosmetic composition according to claim 16, wherein it comprises 0.01 to 5 wt %, preferably 0.05 to 2 wt %, 4-t-butylcyclohexanol solubilized in 1,5-pentanediol based on the total weight of the composition.

19. Dermatological or dermocosmetic composition according to claim 16, wherein it is in a form suitable for topical application.

Description

EXAMPLE 1: PHARMACOLOGICAL TEST OF THE COMBINATION OF PONGAMIA OIL AND 4-T-BUTYLCYCLOHEXANOL IN PENTYLENE GLYCOL

[0090] The purpose of this study is to evaluate the effects of the combination of pongamia oil and 4-t-butylcyclohexanol in pentylene glycol on the inflammatory response of normal human epidermal keratinocytes in a rosacea environment.

[0091] The rosacea environment is mimicked by the mixture of three agonists; an inflammation mediator, an innate immunity mediator and a bacterial component selected from TNF activators, toll-like receptor (TLR2) activators and TRP activators (TRPV1, TRPA1), LL37 peptide, as described in Steinhoff et al. 2013, JAAD.

[0092] Protocol

[0093] Pongamia oil is evaluated at 10 g/ml (corresponding to 0.001%), pentylene glycol 4-t-butylcyclohexanol is evaluated at 300 M (corresponding to 47 g/ml of 4-t-butylcyclohexanol, and therefore 0.0047%). An IKK inhibitor evaluated at 10 M was used as positive control.

[0094] Human epidermal keratinocytes in a rosacea environment were exposed to the compounds for 25 hours.

[0095] The culture supernatant is then removed, centrifuged and frozen at 20 C. IL8 production is quantified by ELISA, according to the supplier's instructions (R&D Systems). A percentage inhibition of IL8 secretion after exposure to the various compounds tested is calculated. The statistical analysis is performed using a one-way analysis of variance (ANOVA) followed by Dunnett's test.

[0096] Seven independent experiments are performed and averaged.

[0097] Results

[0098] The results are summarized in the table below:

TABLE-US-00001 [IL8] (pg/mL) SEM % inh p Vehicle (DMSO) Control 69.1 5 Vehicle (DMSO) Rosacea 3267.0 177 ### IKK 10 MM 515.2 41 86 *** Pongamia oil 10 g/mL 2739.5 173 16 * PG4B 300 M 2381.8 242 28 ** PG4B + pongamia oil 300 M + 1667.0 199 50 *** 10 g/mL Inh: inhibition PG4B: pentylene glycol 4-t-butylcyclohexanol * p < 0.05, ** p < 0.01, *** p < 0.001 versus rosacea group, ### p < 0.001 versus control.

[0099] When the keratinocytes are in a rosacea environment, a very clear secretion of IL8 is observed, going from 695 g/mL under control conditions (0.1% DMSO) to 3267177 g/mL. The reference inhibitor IKK, which blocks the NFB pathway, strongly inhibits this IL8 secretion (86% inhibition), thus validating the pharmacological test used.

[0100] 4-t-Butylcyclohexanol at 300 M in pentylene glycol statistically significantly inhibits IL8 production. Pongamia oil at 10 g/mL has a lower inhibitory effect on IL8 secretion, but still in a statistically significant manner. On the other hand, the combination of pentylene glycol 4-t-butylcyclohexanol and pongamia oil at the same concentrations as above inhibits IL8 secretion to a greater extent than with the compounds taken individually, whether with pentylene glycol 4-t-butylcyclohexanol (p<0.05) or pongamia oil (p<0.001). Thus, the inventors have demonstrated a real synergy on the inhibition of IL8 production with the combination of pentylene glycol 4-t-butylcyclohexanol and pongamia oil. With such activity, this combination has very promising soothing and calming properties.

EXAMPLE 2: EXEMPLARY COMPOSITION ACCORDING TO THE INVENTION

[0101]

TABLE-US-00002 Pongamia oil 0.1 to 1% 4-t-Butylcyclohexanol in pentylene glycol 0.1 to 1% Sodium hydroxide 0.1 to 0.5% Capric caprylic/triglyceride 1 to 5% Poloxamer 0.5 to 2% Benzoic acid 0.1 to 0.2% Sodium EDTA 0.05 to 0.6% C12-C15 benzoate 1 to 10% Acrylates/C10-30 alkyl crosspolymer 0.1 to 2% Carbomer 0.05 to 0.3% Chlorphenesin 0.1 to 0.3% C14-22 alkyl alcohol 0.1 to 2% Avene water qs

EXAMPLE 3: EXEMPLARY COMPOSITION ACCORDING TO THE INVENTION

[0102]

TABLE-US-00003 Pongamia oil 0.1 to 1% 4-t-Butylcyclohexanol in pentylene glycol 0.1 to 1%. Sodium hydroxide 0.1 to 0.5% Tocopheryl acetate 0.1 to 2% Octyl dodecanol 2 to 15% Hesperidin methyl chalcone 0.05 to 0.5% Glycerin 3 to 10% Sodium EDTA 0.05 to 0.6% Acrylates/C10-30 alkyl crosspolymer 0.1 to 2% Hexanediol caprylyl glycol tropolone 0.2 to 4% Dyes qs Avene water qs

EXAMPLE 4: EXEMPLARY COMPOSITION ACCORDING TO THE INVENTION

[0103]

TABLE-US-00004 Pongamia oil 0.1 to 1% 4-t-Butylcyclohexanol in pentylene glycol 0.1 to 1%. Acrylate polymer 1 to 2% C12-C15 benzoate 2 to 10% Butyl methoxy dibenzoylmethane 1 to 4% Cetrimonium bromide 0.01 to 0.5% Potassium cetyl phosphate 1 to 5% Coco-caprylate/caprate 2 to 10% Dextran sulfate 0.2 to 0.5% Dicaprylyl carbonate 2 to 10% Sodium EDTA 0.05 to 0.6% Ethylhexyloxyphenol methoxyphenyl 1 to 5% Glycerin 3 to 10% Shea butter 1 to 4% Methicone 0.5 to 4% Methyl gluceth 1 to 4% Titanium oxide 0.2 to 2% Pentylene glycol 1 to 5% Sorbitol 1 to 5% Glyceryl stearate 1 to 3% Tocopheryl glucoside 0.01 to 0.5% Ethylhexyl triazone 1 to 5% Fragrances qs Dyes qs Avene water qs

EXAMPLE 5: EXEMPLARY COMPOSITION ACCORDING TO THE INVENTION

[0104]

TABLE-US-00005 Pongamia oil 0.1 to 1% 4-t-Butylcyclohexanol in pentylene glycol 0.1 to 1%. C12-C15 benzoate 2 to 10% Aluminum starch octenylsuccinate 1 to 3% Butyl methoxy dibenzoylmethane 1 to 4% Carbomer 0.05 to 0.3% Cetrimonium bromide 0.01 to 0.5% Potassium cetyl phosphate 1 to 5% Coco-caprylate/caprate 2 to 10% Dextran sulfate 0.2 to 0.5% Dicaprylyl carbonate 2 to 10% Sodium EDTA 0.05 to 0.6% Ethylhexyloxyphenol methoxyphenyl 1 to 5% Ethylhexyl salicylate 2 to 5% Glycerin 3 to 10% Methicone 0.5 to 4% Methyl gluceth 1 to 4% Titanium oxide 0.2 to 2% Pentylene glycol 1 to 8% Sorbitol 1 to 5% Glyceryl stearate 1 to 3% Tocopheryl glucoside 0.01 to 0.5% Ethylhexyl triazone 1 to 5% Fragrances qs Dyes qs Avene water qs