FR2729859A1 - Compsns. contg. essential and/or absolute oil for topical anti-inflammatory treatment - Google Patents

Abstract

Use of compsns. contg. an essential and/or absolute oil for topical anti-inflammatory treatment is new.

Description

COMPOSITIONS COMPRISING ESSENTIAL OIL AND / OR A
ABSOLUTE FOR THE TREATMENT, IN TOPICAL APPLICATION, OF
INFLAMMATION
The present invention relates to therapeutic and cosmetic compositions for topical application, said compositions comprising essential and / or absolute oils.

 Essential oils and / or absolute are obtained from raw materials of plant origin. However, the essential oils are obtained, in general, by distillation of said materials with water vapor, while the absolutes are obtained essentially in a two-stage process, a first step consisting of an extraction from the vegetable materials at the first stage. using volatile solvents to obtain a concrete, a second step consisting of a cold decantation after solubilization in alcohol followed by removal of said alcohol.

 Essential and / or absolute oils are mainly known for their fragrance properties.

However, they are known elsewhere in various therapeutic applications, but their effects have been rigorously demonstrated.

 Also, the present invention aims to show a new therapeutic application of essential oils and / or absolute.

 It relates to a composition comprising an essential oil and / or a useful absolute, topically applied, as an anti-inflammatory.

 The following description, which has no limiting character, will better understand how the invention can be put into practice. It should be read with reference to the accompanying drawings, in which Figures 1A to 1D illustrate the effect of a therapeutic treatment by a composition according to the invention, vis-à-vis a solar erythema.

 Inflammation is a response of a living organism to aggression. The nature of this aggression can be of diverse origin, for example mechanical or chemical.

 Inflammation involves complex biochemical reactions that result in activation of different cell types and mediators.

In particular, the inflammation involves neutrophilic leukocytes which release proteases, for example human leukocyte elastase (ELH), and oxygen free radicals, for example the superoxide anion (2).
ELH degrades many connective tissue macromolecules, particularly fibrous elastin, certain types of collagen, proteoglycans and structural glycoproteins. This degradation is at the origin of an alteration of many tissues and in particular the skin which loses its elasticity and its brightness.

 Oxygen free radicals and, in particular, O, O- are highly reactive activated species. At the intracellular level, they mainly induce peroxidation of the polyunsaturated fatty acids of phospholipid membranes, an increase in the amount of irritating and often pro-oxidant free fatty acids, a formation of cytotoxic peroxides, an increase in squalene hydroperoxides, and an activation of carcinogenesis. At the extracellular level, they induce, in particular, a degradation of the main constituents of the extracellular medium, for example macromolecules of the connective tissue, oxidation of the thiol bonds of the proteins, a modification of the permeability and the structure of the tissues in particular cutaneous.Free radicals oxygenates thus contribute to promote the general aging and in particular of the skin which loses then its physicochemical qualities including its brightness.

 According to the invention, a composition comprising an essential oil and / or an absolute is useful as an anti-inflammatory. Also, it is possible to use an essential oil and / or absolute for the preparation of a composition for the therapeutic treatment, in topical application, inflammations.

 For this purpose, the forearm of four different subjects is divided into two zones, a lower treated zone on which a composition is applied comprising between about 0.01% and about 1% or even 5% by weight, for example 0, 25% by weight of an essential oil and / or an absolute twice daily for 10 days and an untreated upper zone on which no application has been made. Then, at time t = 0, irradiation of ultraviolet light of type B (WB) is carried out simultaneously on the two zones. The irradiation dose is adjusted to the cutaneous characteristics of each subject. The evolution of a solar erythema caused by the WB irradiation for each zone of the forearm is then compared for said subjects and at different times.

 The following results are obtained, recorded in Tables 1.1 to 1.4 below, the measurements having been carried out using a Minolta CR300 chromameter, "L" being the representative luminance of the gray level of the skin, the black corresponding to L = 0 and the white corresponding to L = 100, the coefficient "a" being proportional to the red color of the skin, and the coefficient "b" being representative of its "yellow / blue" component.

Table 1.1: UVB irradiation of 280 mJ / cm2

<tb> time <SEP> ZONE <SEP> PROCESSED <SEP> ZONE <SEP> NO <SEP> PROCESSED
<tb><SEP> in
<tb> hour
<tb><SEP> L <SEP> a <SEP> b <SEP> L <SEP> a <SEP> b
<tb><SEP> 55.87 <SEP> 10.53 <SEP> 17.29 <SEP> 54.84 <SEP> 10.72 <SEP> 20.75
<tb><SEP> 19 <SEP> 57.49 <SEP> 11.45 <SEP> 19.6 <SEP> 54.25 <SEP> 13.82 <SEP> 20.96
<tb><SEP> 24 <SEP> 57.42 <SEP> 11.57 <SEP> 18.43 <SEP> 53.72 <SEP> 14.46 <SEP> 20.75
<tb><SEP> 40 <SEP> 56.32 <SEP> 12.12 <SEP> 20.57 <SEP> 53.1 <SEP> 13.09 <SEP> 20.96
<tb><SEP> 48 <SEP> 57.05 <SEP> 12.28 <SEP> 19.09 <SEP> 54.04 <SEP> 13.43 <SEP> 21.52
<Tb>
Table 1.2: WB irradiation of 380 mJ / cm2

<tb> time <SEP> ZONE <SEP> PROCESSED <SEP> ZONE <SEP> NO <SEP> PROCESSED
<tb><SEP> in
<tb> hour
<tb><SEP> L <SEP> a <SEP> b <SEP> L <SEP> a <SEP> b
<tb><SEP> 0 <SEP> 55.77 <SEP> 8.89 <SEP> 18.42 <SEP> 55.66 <SEP> 8.41 <SEP> 19.64
<tb><SEP> 12 <SEP> 56.81 <SEP> 10.56 <SEP> 20.39 <SEP> 55.87 <SEP> 12.06 <SEP> 21.89
<tb><SEP> 24 <SEP> 58.07 <SEP> 9.38 <SEP> 19.14 <SEP> 55.94 <SEP> 11.57 <SEP> 21.44
<Tb>
Table 1.3: WB irradiation of 280 mJ / cm

<tb> time
<tb><SEP> in <SEP> ZONE <SEP> PROCESSED <SEP> ZONE <SEP> NO <SEP> PROCESSED
<tb> hour
<tb><SEP> L <SEP> a <SEP> b <SEP> L <SEP> a <SEP> b
<tb><SEP> 0 <SEP> 64.22 <SEP> 8.26 <SEP> 13.97 <SEP> 64.31 <SEP> 7.70 <SEP> 15.39
<Tb>

<tb> 17 <SEP> 64.41 <SEP> 9.88 <SEP> 14.49 <SEP> 62.12 <SEP> 15.37 <SEP> 16.55
<tb> 20 <SEP> 63.54 <SEP> 10.16 <SEP> 14 <SEP> 61.67 <SEP> 15.93 <SEP> 16.05
<tb> 24 <SEP> 64.45 <SEP> 10.27 <SEP> 14.93 <SEP> 61.47 <SEP> 15.69 <SEP> 16.33
<tb> 48 <SEP> 62.75 <SEP> 9.55 <SEP> 14.08 <SEP> 60.92 <SEP> 15.13 <SEP> 16.56
<Tb>
Table 1.4: UVB irradiation of 280 mJ / cm2

<tb> time <SEP> ZONE <SEP> PROCESSED <SEP> ZONE <SEP> NO <SEP> PROCESSED
<tb><SEP> in
<tb> hour
<tb><SEP> L <SEP> a <SEP> b <SEP> L <SEP> a <SEP> 7 <SEP><SEP> b
<tb><SEP> 0 <SEP> 64.58 <SEP> 9.36 <SEP> 15.68 <SEP> 61.93 <SEP> 9.25 <SEP> 16.59
<tb><SEP> 14 <SEP> 63.35 <SEP> 9.75 <SEP> 16.87 <SEP> 59.91 <SEP> 13.16 <SEP> 17.9
<tb><SEP> 17 <SEP> 61.50 <SEP> 9.88 <SE> 17.86 <SE> 59.91 <SE> 13.65 <SE> 18.18
<tb><SEP> 25 <SEP> 61.58 <SEP> 9.04 <SEP> 17.38 <SEP> 60.02 <SEP> 12.78 <SEP> 18.84
<Tb>
The curves presented in FIGS. 1A to 1D show the evolution of the coefficient "a" as a function of time for the four aforementioned subjects.

 They show that, in vivo, surprisingly, the evolution of the coefficient a on the treated zone is more limited than on the untreated zone. Also, a prophylactic treatment of the skin with a composition according to the invention protects it against attacks capable of inducing erythema such as solar erythema.

 In other words, a composition comprising an essential oil and / or an absolute is useful, in topical application, against erythema especially solar and it is possible to use an essential oil and / or an absolute for the preparation of a composition for the therapeutic treatment of erythema especially solar.

 On the other hand, the invention has made it possible to highlight the fact that, among all the complex biochemical reactions induced during an inflammation, the reactions involving the action of ELH and oxygenated free radicals are inhibited by the presence of essential oils and / or absolutes.

 Also, according to the invention a composition comprising an essential oil and / or an absolute is useful as anti-elastase. It is therefore possible to use an essential and / or absolute oil for the preparation of a composition for the therapeutic treatment of pathologies that induce an increase in the activity of human leukocyte elastase.

 For this purpose, the following tests were carried out in vitro. The influence of the presence of an essential oil and / or an absolute on the activity of the ELH in buffer solution is monitored. A synthetic substrate, N-methoxysuccinylalanine-alanine-proline-valine-β-nitroanilide, is used as the substrate of the ELH. ELH hydrolyzes the aforementioned substrate and releases a colored product: β-nitroanilide. The kinetics of the enzymatic reaction are monitored by spectrophotometry at 410 nm. The anti-elastase effect is calculated with respect to a control curve, in the absence of essential oil and / or absolute.

 The essential oil and / or the absolute is incubated for 15 minutes in the presence of ELH before adding the aforementioned substrate.

By way of illustration, in a first test, 50 μl of an emulsion of essential oil of Roman chamomile was used at a concentration of 0.2 g / ml in Tween 20. This essential oil complies with the AFNOR standard. T75-253. Its composition in principal constituents is given in table 2 following
Table 2

<tb><SEP> Constituent <SEP> Minimum <SEP> (in <SEP> Maximum <SEP> (in
<tb><SEP>%<SEP> in <SEP> weight) <SEP>% <SEP> in <SEP> weight)
<tb><SEP> a-pinene <SEP> 1.5 <SEP> 5.0
<tb><SEP> n-butyrate <SEP> Isobutyl <SEP> 2 <SEP> 9.0
<tb><SEP> Isobutyl methacrylate <SEP><SEP> 1 <SEP> 3
<tb><SEP> Isobutyrate <SEP> Isoamylate <SEP> 3 <SEP> 5
<tb><SEP> Methacrylate <SEP> of <SEP> 2-methyl <SEP> 0.5 <SEP> 1.5
<tb><SEP> butyl
<tb><SEP> Isobutyl Angela <SEP><SEP> + <SEP> 30 <SEP> 45
<tb><SEP> isoamyl methacrylate <SEP>
<tb><SEP> Angelate <SEP> of <SEP> methyl <SEP> allyl <SEP> 6 <SEP> 10
<tb> Angélate <SEP> of <SEP> 2-methyl <SEP> butyl <SEP> 3 <SEP> 7
<tb><SEP> Isoamyl <SEP> Angelate <SEP> 12 <SEP> 22
<tb><SEP> Pinocarvone <SEP> 1.3 <SEP> 4
<tb><SEP> Trans-pino-carveol <SEP> 2 <SEP> 5
<Tb>
At the same time, the same experimental procedure was carried out on a control containing no essential oil, but tween 20 only.

 It was then shown that, for a concentration of 0.5 mg / ml of essential oil of Roman chamomile, the inhibition of the action of ELH is 12% and that, for a concentration of 1.25 mg / ml, the inhibition is 27%.

In a second test, 50 μl of an emulsion of hay absolute present in cremophor was used.
RH 40 at a concentration of 50 mg / ml. This absolute was obtained by a classical way from hay, by obtaining a concrete.

 The results obtained clearly show that, compared to a control containing no absolute but only RH40 cremophor, the presence of hay absolute inhibits the action of ELH. For a concentration of 0.083 mg / ml of absolute, the inhibition is 45% and, for a concentration of 1.25 mg / ml, it is 75%.

 Furthermore, according to the invention, a composition comprising an essential oil and / or an absolute is useful, in topical application, as an antioxidant.

Also, it is possible to use an essential oil and / or absolute for the preparation of a composition for the treatment of conditions that induce oxidation of skin tissue.

 To show the antioxidant effect of essential and / or absolute oils, the inhibition of cytochrome C reduction by the superoxide anion (2 -) in vitro was measured. For this purpose, in a reaction medium comprising 137 ml of 50 mM phosphate buffer and 0.1 mM EDTA at a pH of 7.8, 1.5 ml of 10-3 M oxidized cytochrome C were brought together. and 1.5 ml of 5,10'3 M xanthine, demineralized water and / or a sample to be assayed with an essential oil and / or an absolute solubilized at 5% in 10% cremophor RH40 and / or xanthine oxidase according to the following Table 3.

The action of xanthine oxidase on xanthine generates O2 - O which, in the absence of a molecule capable of capturing said 02 "-, leads to a reduction of reduced cytochrome C cytochrome C. is followed spectrophotometrically at 550 nm.

Table 3

<tb><SEP> white <SEP> control <SEP> test
<tb> Medium <SEP> reaction <SEP> (in <SEP> 1,4 <SEP> 1,4 <SEP> 1,4
<tb> ml)
<Tb>

<tb> H2O <SEP> demineralized <SEP> (in <SEP> ml) <SEP> 0.100 <SEP> 0.050 <SEP><SEP> - <SEP>
<tb> Sample <SEP> to <SEP> assay <SEP> - <SEP> 0.050
<tb> Xanthine <SEP> oxidase <SEP> (in <SEP> ml) <SEP> - <SEP> 0.050 <SEP> 0.050
<Tb>
The results obtained show that the essential oils of rose, marjoram, lavender and chamomile have anti-free radical properties, especially with respect to free radicals oxygenated, interesting since they generate, at a rate of 1.67 mg / ml a decrease in the oxidative activity of 1 '2 in general, greater than 10%, as confirmed in Table 4 below
Table 4

<tb> oil <SEP> essential <SEP> Activity
<tb> Chamomile <SEP> - <SEP> 12 <SEP>%
<tb> Lavender <SEP> - <SEP> 14 <SEP>%
<tb> pink <SEP> Turkish <SEP> - <SEP> 18 <SEP>%
<tb> marjoram <SEP> - <SEP> 27 <SEP>%
<Tb>
It will be noted that the abovementioned essential oils are all accessible to those skilled in the art. They are obtained by conventional distillation methods.

For example, the essential oil of rose is obtained according to standard NF T75-345 and has a composition defined in Table 5 below.

Table 5

<SEP> Constituent <SEP> Minimum <SEP> (in <SEP> Maximum <SEP> (in
<tb><SEP>%<SEP> in <SEP> weight) <SEP>% <SEP> in <SEP> weight)
<tb> Citronellol <SEP> 34 <SEP> I <SEP> 44
<Tb>

<tb><SEP> Nérol <SEP> 6 <SEP> 9
<tb><SEP> Geraniol <SEP> 12 <SEP> 18
<tb><SEP> Phenylethyl alcohol <SEP><SEP> 2 <SEP>
<Tb>
Of course, the present invention is not limited to the prophylactic treatment of solar erythema. Indeed, it aims a treatment against all types of aggressions capable of inducing inflammation.

This concerns, in particular, skin damage due to the presence, in the environment, of oxidizing gases such as carbon monoxide, sulfur and nitrogen oxides, as well as mechanical stress induced by for example, by irritating microparticles.

 Moreover, the invention aims not only at the prophylactic treatment, in topical application, of all the skins, but it aims, more particularly, the treatment of sensitive skins, in particular blotchy skin, as well as the soothing of the allergies which are manifested in the skin. the case of sensitive skin, by inflammatory reactions.

 Furthermore, it should be noted that the invention goes against the prejudices of a person skilled in the art who is well aware that perfumes, comprising essential and / or absolute oils in large quantities, greater than 5% by weight, are known to be allergenic.

 The following examples will make it possible to better appreciate the diversity of the compositions according to the invention. In these examples, the complex of essential oils and / or absolutes is a complex preferably composed of one or more essential oils among the essential oils of rose, chamomile and marjoram, and / or hay absolute.

On the other hand, ceramisomes are liposomal-type skin penetration vectors whose vesicular walls comprise phospholipids and plant ceramides and which comprise, according to the invention, essential and / or absolute oils.

Example 1 Anti-Aging Cream, Anti
inflammatory, for sensitive skin, in water emulsion
in oil
% in weight
Propylene glycol 2.00
Sodium Chloride 1.00
Magnesium sulphate7H2O 1.00
Conservatives' 0.30
Vegetable oil 2.00
Mineral oil 13,00
Polyglyceryl - 3 diisostearate 3.00
Isostearyl isostearate 4.00
Complex of essential oils from 0.05 to 0.50
Perfume 0.30
Demineralized and sterile water qs 100
Example 2: Soothing anti-inflammatory lotion for
sensitive skins
% in weight
Propylene glycol 3.00
Urea 1.00
Sodium lactate 0.50
Lactic acid 0.50
0.02 sodium hyaluronate
Vegetable hydroglycolic extract 5.00
Conservatives 0.30
Complex of essential oils from 0.05 to 0.50
Castor oil hydrogenated 1,00
Perfume 0.20
Demineralized and sterile water qs 100
Example 3: Soothing lip balm for lips
sensitive and fragile
% in weight
Beeswax 5,00
Carnauba wax 5.00
Candellila wax 5,00
Castor oil 40.00
Myristyl lactate 30.00
Bentone 0.50
Glycerin 5.00
Conservatives 0.30
Perfume 0.30
Complex of essential oils from 0.05 to 0.50
Monoricinoleate of propylene glycol qs 100
Example 4: Foaming gel for skin cleanser
sensitive
% by weight Propylene glycol 2.00
Carboxymethyl cellulose 0.80
Acylglutamate 5.00 Glyceryl cocoate and sulfate 10.00
Polysorbate 20 2.00
Decyl glucoside 4.00
Conservatives 0.30
Perfume 0,50
Complex of essential oils from 0.05 to 0.50
Demineralized and sterile water qs 100
Example 5 Anti-Aging and Anti-Inflammatory Cream
for sensitive skin, in oil-in-water emulsion
% in weight
Propylene glycol 4.00
Carbopol 934 0.30
Cetearyl glucoside 4.00
Glyceryl stearate 1.50
Vegetable oil 3,00
Silicone oil 3.00
Beeswax 0.50
Perhydrosqualene 5.00
Triethanolamine 0.30
Conservatives 0.30
0.03 sodium hyaluronate
Ceramisomes essential oils from 0.50 to 5.00
Perfume 0.30
Demineralized and sterile water qs 100
Example 6 Anti-Aging and Anti-Inflammatory Gel for
sensitive skins
% in weight
Propylene glycol 4.00
Polyacrylamide copolymer 1.50
Carboxymethyl cellulose 0.20
Polyethylene Glycol 400 2.00
Vegetable oil 2.00
Conservatives 0.30
0.02 sodium hyaluronate
Ceramisome essential oils from 0.50 to 5.00
Perfume 0.30
Demineralized and sterile water qs 100

Claims (18)

 1. Composition comprising an essential oil and / or a useful absolute, in topical application, as anti-inflammatory.  2. Composition according to claim 1, useful as anti-elastase.  3. Composition according to one of claims 1 or 2, useful as an antioxidant.  4. Composition according to claim 3, useful as oxygenated free radical scavengers.  5. Composition according to one of the preceding claims, useful against erythema.  6. Composition according to claim 5, useful against solar erythemas.  7. Composition according to one of the preceding claims, characterized in that the essential oil and / or the absolute is selected from the essential oil of chamomile, lavender, rose, marjoram, and hay absolute .  8. Composition according to one of the preceding claims, characterized in that it acts prophylactically.  9. Composition according to one of the preceding claims, characterized in that it comprises between about 0.01 and about 1% by weight of essential oil and / or absolute.  10. Use of an essential oil and / or an absolute for the preparation of a composition for the therapeutic treatment, in topical application, of inflammations.  11. Use according to claim 10 for the preparation of a composition for the therapeutic treatment of pathologies that induce an increase in the activity of human leukocyte elastase.  12. Use according to one of claims 10 or 11 for the preparation of a composition for the therapeutic treatment of pathologies that induce oxidation of skin tissue.  13. Use according to claim 12, for the preparation of a composition for the therapeutic treatment of pathologies induced by the presence of oxygen free radicals.  14. Use according to one of claims 10 to 13, for the preparation of a composition for the treatment of erythema.  15. Use according to claim 14, for the preparation of a composition for the treatment of solar erythemas.  16. Use according to one of claims 10 to 15, characterized in that the essential oil and / or the absolute is selected from the essential oil of chamomile, lavender, rose, marjoram, and the absolute hay.  17. Use according to one of claims 10 to 16, characterized in that the treatment is a prophylactic treatment.  18. Use according to one of claims 10 to 17, characterized in that the composition for the therapeutic treatment comprises between about 0.01 and about 1% by weight of essential oil and / or absolute.