USE OF A BIXA ORELLANA EXTRACT

Abstract

The present invention relates to the cosmetic use of a Bixa orellana extract for preventing and/or reducing sebum secretion and/or for preventing and/or reducing the unaesthetic and/or unpleasant and/or uncomfortable manifestations of sebum secretion. It also relates to a cosmetic care method, characterized in that it comprises the topical application to at least one area of skin, advantageously of the scalp, of a Bixa orellana extract for preventing and/or reducing sebum secretion and/or for preventing and/or reducing the unaesthetic and/or unpleasant and/or uncomfortable manifestations of sebum secretion. Finally, it relates to a Bixa orellana extract for use in the treatment and/or prevention of a pathological condition associated with sebum hyperproduction chosen from pathological hyperseborrhoea and seborrhoeic eczema and/or any combination thereof.

Claims

1.-17. (canceled)

18. A cosmetic method for preventing and/or reducing sebum secretion and/or for preventing and/or reducing the unaesthetic and/or unpleasant and/or uncomfortable manifestations linked to sebum secretion of an individual who requires or desires same, comprising the following steps: a) identifying on the individual an area of skin and/or hair for which it is desired to reduce sebum secretion and/or the unaesthetic and/or unpleasant and/or uncomfortable manifestations linked to sebum secretion, and b) applying to this area of skin and/or hair a Bixa orellana extract in an effective amount for preventing and/or reducing sebum secretion and/or the unaesthetic and/or unpleasant and/or uncomfortable manifestations linked to sebum secretion on this area of skin and/or hair.

19. The cosmetic method according to claim 18, wherein the unaesthetic and/or unpleasant and/or uncomfortable manifestations of sebum secretion are skin pore visibility and/or blackhead formation and/or the shiny and/or oily appearance of the skin and/or of the hair and/or the thick appearance of the skin.

20. The cosmetic method according to claim 18, wherein the Bixa orellana extract is a seed extract.

21. The cosmetic method according to claim 18, wherein the Bixa orellana extract is obtained by extraction in a protic polar solvent.

22. The cosmetic method according to claim 21, wherein the Bixa orellana extract is spray-dried in the presence of a concentration by weight of maltodextrin of between 20% and 90%, relative to the total weight of the powder obtained.

23. The cosmetic method according to claim 18, wherein the Bixa orellana extract is in the form of a cosmetic composition also comprising a cosmetically acceptable excipient.

24. The cosmetic method according to claim 23, wherein the cosmetic composition is intended for topical application to the skin and/or the hair.

25. The cosmetic method according to claim 24, wherein the Bixa orellana extract is present in the cosmetic composition in a content of between 1×10.sup.−4% to 10% by weight, relative to the total weight of the composition.

26. The cosmetic method according to claim 24, in which the skin is normal, oily, very oily and/or mixed and/or the hair is normal and/or oily.

27. The cosmetic method according to claim 24, in which the skin is Caucasian or African or Asian and/or the hair is Caucasian, African or Asian.

28. The cosmetic method according to claim 23, wherein the cosmetic composition is chosen from the group consisting of a serum, a lotion, a cream, a shampoo, a conditioner, an oil, a milk, an ointment, a paste, a foam, an emulsion, a hydrogel, a shower gel, a mask, a lacquer, a spray, and a wax.

29. (canceled)

30. (canceled)

31. The cosmetic care method according to claim 23, wherein the area of skin for which it is desired to reduce sebum secretion and/or the unaesthetic and/or unpleasant and/or uncomfortable manifestations linked to sebum secreation is a surface of the body chosen from the skin of the face, the cheeks, the nose, the temples, the T zone (forehead, nose and chin), the external auditory canal and/or the chin, the scalp, the neck, the back, the shoulders, the forearms, the chest, the hands and/or the bust.

32. A method for the treatment and/or prevention of a pathological condition associated with sebum hyperproduction chosen from pathological hyperseborrhoea and seborrhoeic eczema and/or any combination thereof of an individual who requires or desires the same, comprising the following steps: a) identifying on the individual of an area of akin for which it is desired to treat and/or prevent a pathological condition associated with sebum hyperproduction chosen from pathological hyperseborrhoea and seborrheic eczema and/or any combination thereof, and b) applying to this area of skin a Bix orellana extract in an effective amount for treating and/or preventing a pathological condition associated with sebum hyperproduction chosen from pathological hyperseborrhoea and seborrheic eczema and/or any combination thereof on this area of skin.

33. The method according to claim 32, wherein the extract is a seed extract.

34. The method according to claim 32, wherein the extract is present in a pharmaceutical composition in a content of between 1×10.sup.−4% to 10% by weight relative to the total weight of the composition.

35. The method according to claim 32, wherein the extract is present in a pharmaceutical composition in a content of between 1×10.sup.−4% to 5% by weight, relative to the total weight of the composition.

36. The cosmetic method according to claim 21, wherein the Bixa orellana extract is spray-dried in the presence of a concentration by weight of maltodextrin of between 40 and 80%, relative to the total weight of the powder obtained.

37. The cosmetic method according to claim 21, wherein the Bixa orellana extract is spray-dried in the presence of a concentration by weight of maltodextrin of 60%, relative to the total weight of the powder obtained.

38. The cosmetic method according to claim 21, wherein the Bixa orellana extract is an extract obtained by aqueous extraction.

39. The method according to claim 32, wherein the Bixa orellana extract is an extract obtained by aqueous extraction.

Description

EXAMPLE

Example 1: Different Methods for Preparing the Bixa orellana Extract according to the Invention

[0125] Example 1a): An amount of 10% (w/w relative to the total mixture of water and seeds) of milled Bixa orellana seeds was macerated in water as solvent for one hour at a temperature of 80° C. The crude extract was centrifuged, decanted, then filtered and then spray-dried in the presence of maltodextrin, in a final amount of maltodextrin of 60% by weight relative to the total weight of the final extract.

[0126] Example 1b): An amount of 10% by weight of milled seeds (relative to the total weight of water and seeds) was macerated in water for 2 hours at a temperature of 20° C. The crude extract was centrifuged, decanted and then filtered.

[0127] Example 1c): An amount of 20% by weight of milled seeds (relative to the total weight of water and seeds) was macerated in water for 2 hours at a temperature of 20° C. The extract was then centrifuged, decanted and filtered.

[0128] Example 1d): An amount of 10% by weight of milled seeds (relative to the total weight of the seeds and of the solvent) was macerated in a solvent consisting of an ethanol:water mixture (80:20; v/v), at a temperature of 80° C. for a period of 1 hour. The extract was then centrifuged, decanted, filtered and then spray-dried in the presence of maltodextrin, in a final amount of maltodextrin of 80% by weight relative to the total weight of the final extract.

[0129] Example 1e): An amount of 10% by weight of milled leaves (relative to the total weight of water and leaves) was macerated in water for one hour at a temperature of 80° C. The crude extract was centrifuged, decanted, then filtered and then spray-dried in the presence of maltodextrin, in a final amount of maltodextrin of 60% by weight relative to the total weight of the final extract.

Example 2: Properties of a Bixa orellana Extract according to the Invention on Sebum Secretion

Method

[0130] Human sebocytes were seeded at 2500 cells/centimetre.sup.2 in a complete culture medium (DMEM/HAM F12 with foetal calf serum (FCS) at 10% (w/w in the medium) and incubated for 5 days at 37° C., CO.sub.2 at 5% with a relative humidity of more than 95%. Then the growth culture medium was replaced with a standard culture medium (DMEM) containing human serum (HS) at 1% or IGF1 at 100 ng/ml. The Bixa orellana extract obtained in Example 1a) as obtained before the step of mixing with the maltodextrin was incubated for 5 days at 37° C. at 0.02% or 0.05% by weight/weight relative to the mixture of medium and the extract. The cells are rinsed in a PBS buffer (phosphate buffered saline) and fixed with a formaldehyde solution. The number of sebocytes is determined by DNA staining with Hoechst reagent and the fluorescence is recorded at 465 nm (excitation at 356 nm) while the amount of cellular lipids is determined with Nile Red staining (11). The fluorescence of total lipids is measured at a wavelength of 625 nm (excitation at 520 nm) while the fluorescence of neutral lipids is measured at a wavelength of 530 nm (excitation at 475 nm). The results are expressed as percentage relative to the control without the Bixa orellana extract (the mean basal expression with HS at 1% or IGF1 at 100 ng/mL) and presented as a mean +/−standard deviation (SD). The statistics were evaluated with the SigmaPlot™ software.

Results

1. Activation with 1% HS

Asian Sebocytes, 25 Years Old

[0131]

TABLE-US-00001 N = 3 HS at 1% without HS Control Extract at 0.02% Number of cells (DNA) 61 +/− 27 100 +/− 6 83 +/− 4 Total lipids 50 +/− 14 100 +/− 4 84 +/− 7 p < 0.001 Neutral lipids 74 +/− 24 100 +/− 5  76 +/− 24 p < 0.001

[0132] The Bixa orellana extract according to the invention significantly reduced sebocyte proliferation and the synthesis of total lipids in sebocytes treated with 1% HS.

2. Activation with IGF-1 100 ng/ml

2.1. Caucasian Sebocytes, 25 Years Old

[0133]

TABLE-US-00002 IGF at 100 ng/ml without IGF Control Extract 0.05% Number of cells 81 +/− 6 100 +/− 8 48 +/− 3 (DNA) p < 0.001 Total lipids  77 +/− 11 100 +/− 7 33 +/− 3 p < 0.001 Neutral lipids 94 +/− 1 100 +/− 3 86 +/− 2 p < 0.01 

[0134] The Bixa orellana extract according to the invention, at a concentration of 0.05%, significantly reduced sebocyte proliferation and the synthesis of total and neutral lipids in sebocytes treated with IGF-1. Similar results were obtained at 0.02% of extract according to the invention.

2.2. Asian Sebocytes, 25 Years Old

[0135]

TABLE-US-00003 IGF at 100 ng/ml without IGF Control Extract 0.05% Number of cells 89 +/− 5  100 +/− 8  69 +/− 9  (DNA) p < 0.05 Total lipids 88 +/− 10 100 +/− 11 53 +/− 11 p < 0.01

[0136] The Bixa orellana extract according to the invention, at a concentration of 0.05%, significantly reduces sebocyte proliferation and the synthesis of total lipids in sebocytes treated with IGF-1.

Example 3: Induction of the IGH-Binding Protein: IGFBP3 Protein

[0137] The BP3 protein is dedicated to blocking the binding of IGF-1 to its respective receptor IGF1R; it will therefore block the IGF1-IGF1R pathway and therefore obstruct keratinocyte hyperproliferation and differentiation. By activating this protein, the Bixa orellana extract slows down the hyperkeratinization observed in oily skin. The Bixa orellana extract according to the invention increases the synthesis of the IGFBP3 protein.

Materials and Methods

[0138] Normal human keratinocytes were cultured up to 70% confluence, then treated for 24 h with IGF-1 at 100 ng/ml or the Bixa orellana extract obtained according to Example 1a) before mixing with maltodextrin and spray-drying at 0.1% or 0.05% (w/w in the total medium) for 24 h. The cells are lysed for assaying the DNA, and the supernatant is used for the quantification of the IGFBP3 protein by ELISA according to the protocol of the supplier of the ELISA kit (LSBio Human IGFBP3 ELISA Kit ref LS-F24538 lot 103180).

Results

[0139] The results are related to non-treated cells. A statistical t-test test is carried out, and the means are compared.

TABLE-US-00004 Mean deviation Statistic Non-treated 100 19.3937 IGF-1 128.195 25.6252 NS extract 0.1% 147.769 25.3724 P < 0.01  extract 0.05% 174.824 24.9337 P < 0.001

[0140] The Bixa orellana extract according to the invention increased the amount of IGFBP3 protein.

Example 4: Increase in Collagen IV Synthesis by the Extract according to the Invention

Method

[0141] “Normal” human keratinocytes originating from the breast of a healthy 24-year-old donor were cultured in a defined medium (KSFM) for a period of 48 hours until confluence (100%) in the presence of 3 different final concentrations of the B. orellana extract prepared according to Example 1a), before the mixing and spray-drying, then the culture medium is removed. The cell layer obtained is then lysed with an ammonium hydroxide solution. A part of the lysate was used to assay the DNA. The collagen IV was assayed with an anti-collagen IV antibody (Acris, R1041) diluted to 1/2500 in a PBS buffer solution containing bovine serum albumin (BSA). After a period of 60 minutes, the secondary antibody (PerkinElmer, AD0105) diluted to 1/25000 is applied for a period of 1 hour in darkness. The fluorescence was measured (ENVision, PerkinElmer).

Results

[0142] The fluorescence results were standardized relative to the fluorescence obtained with the same cell medium in the absence of the B. orellana extract (Control) and were related to the percentage of DNA obtained under each condition. The results presented correspond to the mean of the assays. (SD: Standard deviation).

TABLE-US-00005 Mean Standard deviation statistic Non-treated 100.00 7.53 extract 0.025% 144.08 8.67 p < 0.001 Extract 0.05% 157.83 7.77 p < 0.001 Extract 0.1% 159.83 14.64 p < 0.001

[0143] The Bixa orellana extract according to the invention increases collagen IV synthesis in the keratinocytes and thus makes it possible to tighten the pores of the skin.

Example 5: Clinical Study of a Bixa orellana Extract according to the Invention on Sebum Secretion

Method

[0144] A clinical study was carried out double blind, in a half-face test, one part with the placebo and one part with the Bixa orellana extract according to the invention at 0.25% as obtained in Example 1a) and formulated in the composition described below (Formula according to the invention).

[0145] The study was carried out on 35 Asian women aged from 20 to 45 years old, with a lipid index, measured using a sebumeter (Sebumeter™ SM 815), ≥150 micrograms of sebum per cm.sup.2 (very oily skin) and including a maximum of 10 volunteers with a lipid index, measured using a sebumeter (Sebumeter™ TM SM 815), ranging from 120 to 149 micrograms of sebum per cm.sup.2 (oily skin). The treatment was applied twice a day for 56 days.

TABLE-US-00006 Formula Placebo according to the Formula invention Brand name INCI (% w/w) (% w/w) Eumulgin ® Sodium stearoyl 0.5 0.5 SG glutamate 10% Citric acid Citric acid, aqua 0.7 0.65 solution Cosmedia ® Sodium polyacrylate 0.7 0.7 SP Cutina ® PES Pentaerythrityl 1 1 distearate Glycerine 99-5 Glycerin 2 2 Elestab ™ 388 Propylene glycol, 2.5 2.5 phenoxyethanol, chlorphenesin, methylparaben Emulgade ™ Sucrose polystearate, 3 3 Sucro Plus cetyl palmitate Miritol ™ 318 Caprylic/capric 3 3 triglyceride Cetiol ® C-5-C Coco-caprilate/caprate 3 3 Cetiol ® CC Caprylyl carbonate 3 3 Extract according Bixa orellana 0 0.25 to the invention according to Ex 1a) Water Aqua qs qs

[0146] The compositions were prepared by mixing according to the methods known by those skilled in the art.

[0147] Samples were taken using the Sebutape® patch and made it possible to measure the activity of the sebaceous glands by measuring the amount of sebum before (D0) and after treatment at 28 and 56 days. The size of the pores on the cheeks, evaluated at the start between 2 and 4, was evaluated by a clinical calculation carried out by a trained referent individual. The moisturization of the skin was measured using the corneometry method. A questionnaire was filled in by the volunteers at 28 and 56 days.

Results

[0148] At 28 days of treatment with the Bixa orellana extract according to the invention at 0.25%, the number of spots (secreted sebum) significantly decreases by 22% versus D0, and significantly by 14% versus placebo.

[0149] At 56 days of treatment with the Bixa orellana extract according to the invention at 0.25%, the number of spots (secreted sebum) significantly decreases by 37% versus D0, and significantly by 25% versus placebo.

[0150] At 28 days with the Bixa orellana extract according to the invention at 0.25%, the area of the spots significantly decreases by 46% versus D0, and significantly by 31% versus placebo.

[0151] At 56 days of treatment with the Bixa orellana extract according to the invention at 0.25%, the number of spots (secreted sebum) significantly decreases by 62% versus D0, and significantly by 36% versus placebo.

[0152] At 28 days of treatment with the Bixa orellana extract according to the invention at 0.25%, the size of the pores decreases visually and significantly by 3% versus D0. At 56 days of treatment with the Bixa orellana extract according to the invention at 0.25%, the size of the pores significantly decreases by 9% versus D0, and by 3% versus placebo.

[0153] After 28 and 56 days of treatment, the Bixa orellana extract according to the invention at 0.25% significantly increases the corneometer value by 3% versus D0.

Example 6: Cosmetic Composition according to the Invention

[0154] The extract used is that obtained in Example 1a) (after mixing with maltodextrin and spray-drying) in powder form.

Example 6a): Tonic Care for Refining the Grain of the Skin

[0155]

TABLE-US-00007 Amount (% by Phase Name total weight) A Water 87.65 A Glycerin 4.00 A Disodium EDTA 0.05 A Preservative qs A Polysorbate 20 1.00 A Poloxamer 184 2.00 A Zinc gluconate 0.05 B water 3 B Bixa orellana extract according to Example 1a) 0.25 B pH adjuster (citric acid) qs C PEG-7 glyceryl cocoate 0.5 H Fragrance 0.1

[0156] The tonic care is prepared by the usual methods in the field well known to those skilled in the art, by mixing the 3 phases and by adjusting the composition to a pH of 5.1.

Example 6b): Matifying Cream

[0157]

TABLE-US-00008 Amount (% by Phase Name total weight) A Sucrose polystearate, cetyl palmitate 3.00 A Pentaerythrityl distearate 1.00 A Caprylic/capric triglyceryl 3.00 A Coco-caprylate/caprate 3.00 A Dicaprylyl carbonate 3.00 A Sodium polyacrylate 0.70 B water 80.90  B glycerin 2.00 B Sodium stearoyl glutamate 0.50 B preservative qs C Bixa orellana extract according to Example 1a) 0.25 C Water 2.00 D Fragrance qs E pH adjuster (citric acid) qs

[0158] The cream is prepared by the usual methods in the field well known to those skilled in the art, by mixing phases A and B preheated to 75° C., and then by adding phases C and D while mixing and while adjusting the composition with phase E to a pH of 6.2 and to a viscosity of 15000 mPas (measured with a Brookfield instrument (RVT; 23° C., spindle TC; 20 rev per min)).

Example 6c): Shampoo

[0159]

TABLE-US-00009 Amount (% by Phase Name total weight) A Water 60.3 A Xanthan gum 1.2 B Decyl glucoside 14 B Dicaprylyl ether, decyl glucoside, glyceryl oleate 5 B Sodium cocoyl glutamate 12 B Coco-glucoside, glyceryl oleate 2 B Glycerin 3 B Preservative qs C pH adjuster (citric acid) qs D Fragrance 0.5 D Bixa orellana extract according to Example 2a) 0.01-10

[0160] The shampoo is prepared by the usual methods in the field well known to those skilled in the art, by mixing the 4 phases and by adjusting the composition to a pH of 5.2 and to a viscosity of 2200 mPas (measured with a Brookfield instrument (RVT; 23° C., spindle 5; 50 rev per min)).