Vehicle and composition containing this vehicle and a stabilized cosmetic or dermatological active substance

A stabilized cosmetic or dermatological active composition containing a vehicle comprising not more than 10% by weight of water, at least one amphiphilic oil, at least one polyol or polyol derivative selected from the group consisting of C.sub.2 -C.sub.4 glycols, ether derivatives of a C.sub.2 -C.sub.4 glycol and mixtures thereof, and at least one solvent for oil and water, containing an alcohol functional group.

This application is a continuation of PCT 95/12446 France published 27 Aug. 
1996. 
FILED OF THE INVENTION 
The present invention relates to a vehicle including not more than 10% by 
weight of water, at least one amphiphilic oil, at least one polyol or 
polyol derivative chosen from C.sub.2 -C.sub.4 glycols and ether 
derivatives of a C.sub.2 -C.sub.4 glycol and at least one common solvent 
for water and oil, chosen from primary alcohols and C.sub.5 -C.sub.7 
glycols. This vehicle forms a transparent or translucent fluid which is 
homogeneous and stable although it contains no surfactant or stabilizer. 
The vehicle according to the invention can be employed especially in a 
composition for topical action containing active substances which are 
sensitive to external factors and/or to water, such as dihydroxyacetone, 
vitamin C or enzymes. These active substances remain stable in such a 
vehicle. 
The composition obtained can be employed especially for the cosmetic and/or 
dermatological treatment of the skin, including the scalp. 
The present invention relates to a vehicle forming a medium which is stable 
although free from surfactant and stabilizer, and capable of being 
employed in a composition containing an active substance that is sensitive 
to external factors and/or to water, and to the use of such a composition 
for the cosmetic and/or dermatological treatment of the skin, including 
the scalp. 
DESCRIPTION OF THE BACKGROUND 
It is known to introduce active substances into cosmetic and/or 
dermatological compositions to provide treatments which are specific to 
the skin, for example for combating the dryness, aging or pigmentation of 
the skin, for treating acne or certain skin diseases (eczema, psoriasis), 
for fighting against excess weight, for promoting the restructuring of the 
skin or its cell renewal, and for coloring the skin. 
Ascorbic acid (or vitamin C), for example, is known to stimulate the growth 
of connective tissue such as collagen. It also makes it possible to 
strengthen the defenses of the cutaneous tissue against external attacks 
such as ultraviolet radiation or pollution. It is also employed for 
removing skin marks and pigmentation, and for promoting cicatrization of 
the skin. 
It is also known that the application of retinol or vitamin A makes it 
possible to fight in particular against skin aging and against some skin 
disorders such as acne or keratinization or cicatrization complaints. 
Furthermore, the prior art has for many years taught the involvement of 
dihydroxyacetone in artificial skin coloring (Bobin et al., J. Soc. 
Cosmet. Chem., 35, pages 265-272, 1984). Dihydroxyacetone reacts with the 
amino acids naturally present in the lipid film of the stratum corneum and 
forms melanoids by a Maillard reaction (L. C. Maillard, C. R. Acad. Sci., 
154, 66-68, 1912). The application of dihydroxyacetone to the skin 
therefore makes it possible to give the latter the appearance of a 
suntanned skin without having the disadvantages (burns, risks of cancer) 
encountered on exposure to the sun. 
In addition, it is also known to introduce enzymes into cosmetic 
compositions, and especially proteases and lipases employed because of 
their proteolytic and lipolytic properties. These enzymes are sought after 
in the field of cosmetics because of their smoothing and cleansing power 
and their ability to remove the dead cells from the skin. 
Unfortunately, some active substances, and in particular those referred to 
above, are unstable because of their sensitivity to external factors such 
as light, heat or the presence of oxygen either in air or present in 
water. The stability of dihydroxyacetone, of vitamin C, of vitamin A or of 
enzymes in a composition is thus quite relative: in a composition these 
active substances degrade in the course of time. 
This instability runs counter to the effectiveness which is sought and can, 
furthermore, be a source of unpleasantness for the user; for example, the 
instability of the active substance may lead to color and/or odor changes 
in the composition containing it. 
Accordingly, various means have been envisaged for stabilizing these active 
substances. When the active substance comprises a reactive site, 
especially in the case of vitamins and of dihydroxyacetone, one of the 
means for stabilizing it consists, for example, in blocking this site by 
esterification, especially with phosphated, sulphated or alkylated 
derivatives and in employing these derivatives instead of the free active 
substance. Unfortunately, the activity exhibited by these derivatives is 
less good than that of the free active substance. 
It has also been envisaged to employ precursors of such active substances, 
which, after application to the skin, are broken down by the skin enzymes 
and then release the free active substance (see EP-A-487404). However, the 
use of such derivatives does not always permit a release of active 
substance which is rapid and in sufficient quantity at the skin surface. 
In addition, it has been envisaged to put an active substance, especially 
an enzyme, in a pulverulent composition (see JP-A-63-130514). It has also 
been envisaged to employ these active substances, and especially enzymes, 
in an immobilized form on polymeric bases (see JP-A-61-207499) or in 
microcapsules (see JP-A-61-254244). Unfortunately, these means require 
special processing, and this increases the cost and the time of 
preparation of the composition. 
When the active substances are water-sensitive, another solution consists 
in incorporating them into an anhydrous liquid medium (see U.S. Pat. No. 
5,322,683). Unfortunately, this solution limits the galenic form of the 
composition and does not permit the incorporation of hydrophilic active 
substances. 
A need therefore continues to exist for a composition in which sensitive 
cosmetic and/or dermatological active substances would retain all their 
properties and therefore their effectiveness in the course of time. 
SUMMARY OF THE INVENTION 
A vehicle which comprises not more than 10% by weight of water, at least 
one amphiphilic oil, at least one polyol or polyol derivative selected 
from the group consisting of C.sub.2 -C.sub.4 glycols, ether derivatives 
of a C.sub.2 -C.sub.4 glycol and mixtures thereof, and at least one 
solvent for oil and water, containing an alcohol functional group. 
The applicant has now found unexpectedly that a vehicle including not more 
than 10% by weight of water, an amphiphilic oil, a C.sub.2 -C.sub.4 glycol 
or an ether derivative of a C.sub.2 -C.sub.4 glycol, mixed with a primary 
alcohol and/or a C.sub.5 -C.sub.7 glycol is capable of maintaining the 
activity of an active substance which is sensitive to the external factors 
and/or to water and of preventing the degradation of this active 
substance. 
DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS 
The present invention provides a vehicle that includes 
not more than 10% by weight of water, 
at least one amphiphilic oil, at least one polyol or polyol derivative 
chosen from C.sub.2 -C.sub.4 glycols, the ether derivatives of a C.sub.2 
-C.sub.4 glycol and mixtures thereof, and 
at least one solvent for oil and water, containing an alcohol functional 
group. The composition is further free of surfactants. 
Water in the vehicle according to the invention is preferably present in a 
quantity ranging from 1 to 10% by weight relative to the total weight of 
the vehicle. 
The solvent containing an alcohol functional group may be especially a 
C.sub.2 -C.sub.8 primary alcohol, a C.sub.5 -C.sub.7 glycol or a mixture 
of both primary alcohol and of C.sub.5 -C.sub.7 glycol. 
Although free from surfactant and stabilizer, the vehicle according to the 
invention is in the form of a transparent or translucent fluid, exhibiting 
good stability. The absence of surfactant has the advantage of making the 
vehicle less irritating. 
According to the invention, "amphiphilic oil" is intended to mean an oil 
which has affinities with water. It may involve in particular esters or 
ethers containing an oxygen atom which have affinities with water and 
which have an HLB (hydrophilic lipophilic balance) of 6 to 12, and 
preferably an HLB of approximately 10. Amphiphilic oils usable in the 
present invention preferably include laureth-2 benzoate, glycereth-7 
benzoate, diethylene glycol dioctanoate/diisononanoate, 
polyoxypropylene-15 stearyl ether, 2-ethylhexyl malate, isopropyl adipate, 
the copolymer of PPG-7 and of succinic acid and neopentyl glycol 
dioctanoate. 
The amphiphilic oil is preferably present in the vehicle of the invention 
in a quantity ranging from 10 to 55% by weight, and more preferably from 
20 to 30% by weight, relative to the total weight of the vehicle. 
Propylene glycol and butylene glycol are preferred C.sub.2 -C.sub.4 glycols 
usable according to the invention. Furthermore, "ether derivative of a 
C.sub.2 -C.sub.4 glycol" is intended to mean the glycols obtained by 
condensation of two C.sub.2 -C.sub.4 glycols with formation of an ether 
bond, such as dipropylene glycol, and their derivatives such as the 
ethoxydiglycol (for example, sold under the name of TRANSCUTOL by 
Gattefosse). 
Preferred C.sub.5 -C.sub.7 glycols usable according to the invention 
include 1,2-pentanediol (for example, sold under the name HYDROLITE-5 by 
Dragoco). 
A preferred primary alcohol usable in the vehicle of the invention is ethyl 
alcohol. 
The vehicle according to the invention may contain from 10 to 20% by weight 
of one or more C.sub.2 -C.sub.4 glycols and/or of one or more ether 
derivatives of a C.sub.2 -C.sub.4 glycol and preferably from 15 to 18% by 
weight relative to the total weight of the vehicle. 
Furthermore, the vehicle according to the invention may contain from 5 to 
60% by weight, and preferably from 15 to 55% by weight, of one or more 
primary alcohols and/or of one or more C.sub.5 -C.sub.7 glycols. The 
quantity of C.sub.5 -C.sub.7 glycol advantageously changes from 5 to 10% 
by weight when the vehicle contains a primary alcohol. 
The vehicle of the invention may advantageously be employed in a 
composition with topical action containing active substances that are 
sensitive to external factors such as light and heat and/or to water. 
These active substances surprisingly remain stable in the composition 
according to the invention. 
In another embodiment, the present invention provides a composition 
containing an active substance with topical action, sensitive to external 
factors and/or to water, which contains a vehicle as defined above. 
The active substances with topical action which are sensitive to external 
factors and/or to water and to which the invention can be applied may be 
especially enzymes and active substances containing at least one hydroxyl 
functional group. 
Lipases and proteases may be mentioned, for example, as enzymes. Among 
proteases there may be mentioned, for example, that sold under the trade 
name SUBTILISINE SP 544 by the company Novo Nordisk and that sold under 
the trade name LYSOVEG by Laboratoires Serobiologiques of Nancy. 
As active substances containing at least one hydroxyl functional group 
there may be mentioned in particular the esterifiable vitamins such as 
retinol (vitamin A) and its derivatives, ascorbic acid (vitamin C) and its 
derivatives, and hydroxylated ketones such as dihydroxyacetone. 
These active substances are advantageously present in the composition 
according to the invention in a quantity ranging from 0.5 to 10% by 
weight, and more particularly from 1 to 5% by weight, relative to the 
total weight of the composition. 
For a topical application the composition according to the invention must 
contain a topically acceptable medium, that is to say compatible with the 
skin and/or the hair and/or the mucosae. 
Depending on the active substance which it contains, the composition 
according to the invention can be employed for the cosmetic and/or 
dermatological treatment of the skin and/or of hair. 
The composition according to the invention may in particular constitute 
cleansing, protective, treatment or care compositions for the face, for 
the neck, for the hands or for the body, artificial tanning products or 
products for the hair and especially for the care of the scalp, for 
example in the form of treating lotions. 
In the particular case of ascorbic acid, the composition may be intended, 
for example, for the depigmentation of the skin or for the treatment of 
acne. The latter may also be treated with a composition containing 
retinol. 
Accordingly, another embodiment of the invention is the use of the 
composition as defined above for the depigmentation of the skin, the 
active substance being ascorbic acid. 
Another embodiment of the invention is the use of the composition as 
defined above for preparing a salve or a dermatological ointment intended 
for the therapeutic treatment of acne, the active substance being ascorbic 
acid and/or retinol. 
When it contains dihydroxyacetone, the composition according to the 
invention may constitute a tanning composition. 
Accordingly, another embodiment of the invention is the use of the 
composition as defined above for coloring the skin, the active substance 
being dihydroxyacetone. 
The dihydroxyacetone is preferably employed in a quantity ranging from 1 to 
8% by weight and, better, from 1 to 5% by weight relative to the total 
weight of the composition. 
In addition, another embodiment of the invention is a tanning composition 
based on dihydroxyacetone, characterized in that it includes not more than 
10% of water, at least one amphiphilic oil, at least one polyol or polyol 
derivative chosen from C.sub.2 -C.sub.4 glycols, ether derivatives of a 
C.sub.2 -C.sub.4 glycol and mixtures thereof, and at least one solvent for 
oil and water, containing an alcohol functional group. 
In a known manner, the composition according to the invention may also 
contain adjuvants which are usual in the cosmetic or dermatological field, 
such as preservatives, antioxidants, perfumes, sunscreens, gelling agents, 
sequestrants, essential oils, colorants and hydrophilic or lipophilic 
active substances other than those indicated above. 
Gelling agents which may be mentioned are, for example, polysaccharides 
such as hydroxypropyl celluloses. 
Hydrophilic active substances which may be employed are, for example, 
proteins or protein hydrolysates and amino acids. 
Lipophilic active substances which may be employed are, for example, 
tocopherol (vitamin E) and its derivatives, essential fatty acids, 
ceramides and essential oils. 
The quantities of the various constituents of the composition according to 
the invention are those conventionally employed in the fields being 
considered.

EXAMPLES 
Having generally described this invention, a further understanding can be 
obtained by reference to certain specific examples which are provided 
herein for purposes of illustration only and are not intended to be 
limiting unless otherwise specified. 
The quantities shown are percentages by weight. 
In all the examples the compositions are prepared in the following manner: 
if a gelling agent is present, it is dispersed when cold in the solvent 
containing an alcohol functional group (ethyl alcohol) with continuous 
stirring, and the various constituents are then added one after the other, 
after preliminary dilution of the active substances in water. 
______________________________________ 
Example 1: Tanning fluid 
______________________________________ 
Ethyl alcohol 43.4% 
Hydroxypropyl cellulose 0.7% 
Vitamin E 0.5% 
Butylene glycol 10% 
Dipropylene glycol 5% 
Laureth-2 benzoate (DERMOL 126 sold by 
12.5% 
Alzo) 
Glycerth-7 benzoate (DERMOL G76 sold 
7.5% 
by Alzo) 
Diethylene glycol dioctanoate/ 
5% 
diisononanoate (DERMOL 489 sold by 
Alzo) 
Dihydroxyacetone 5% 
Perfume 0.4% 
Water 10% 
______________________________________ 
The fluid obtained is in the form of a transparent liquid, stable with 
time, pleasant to apply. It permits uniform tanning of the face and of the 
body by daily application for at least one week. 
A use test was performed on a panel of 40 women who applied the tanning 
fluid to the face for 10 days. 
The users assessed the transparency of the fluid and indicated that it was 
easy to apply and particularly cool when applied to the skin. After the 10 
days' use, they judged that the tanning had been obtained more quickly 
than with the usual compositions and that the coloring obtained was 
uniform. 73% of the users declared they were prepared to buy it. 
______________________________________ 
Example 2: Tanning fluid 
______________________________________ 
Ethyl alcohol 33.2% 
Hydroxypropyl cellulose 0.7% 
Vitamin E 0.5% 
Butylene glycol 10% 
Dipropylene glycol 7.5% 
Laureth-2 benzoate (DERMOL 126 sold by 
10% 
Alzo) 
Diethylene glycol dioctanoate/ 
8% 
diisononanoate (DERMOL 489 sold by 
Alzo) 
Polyoxypropylene-15 stearyl ether 
4.5% 
(ARLAMOL E sold by ICI) 
1,2-Pentanediol (HYDROLITE-5 sold by 
10% 
Dragoco) 
Dihydroxyacetone 5% 
Perfume 0.6% 
Water 10% 
______________________________________ 
The fluid obtained has the same characteristics as that in Example 1. 
______________________________________ 
Example 3: Tanning fluid 
______________________________________ 
Ethyl alcohol 53.8% 
Hydroxypropyl cellulose 0.5% 
Vitamin E 0.5% 
Butylene glycol 15% 
Diethylene glycol dioctanoate/ 
20% 
diisononanoate (DERMOL 489 sold by 
Alzo) 
Dihydroxyacetone 5% 
Perfume 0.2% 
Water 5% 
______________________________________ 
The fluid obtained has the same characteristics as that in Example 1. 
______________________________________ 
Example 4: Tanning fluid 
______________________________________ 
Ethyl alcohol 53.8% 
Hydroxypropyl cellulose 0.5% 
Butylene glycol 15% 
Diethylene glycol dioctanoate/ 
15.5% 
diisononanoate (DERMOL 489 sold by 
Alzo) 
Polyoxypropylene-15 stearyl ether 
5% 
(ARLAMOL E sold by ICI) 
Dihydroxyacetone 5% 
Perfume 0.2% 
Water 5% 
______________________________________ 
The fluid obtained has the same characteristics as that in Example 1. 
______________________________________ 
Example 5: Tanning fluid 
______________________________________ 
Ethyl alcohol 37.2% 
Hydroxypropyl cellulose 0.1% 
Butylene glycol 15% 
Diethylene glycol dioctanoate/ 
30% 
diisononanoate (DERMOL 489 sold by 
Alzo) 
Polyoxypropylene-15 stearyl ether 
5.5% 
(ARLAMOL E sold by ICI) 
Dihydroxyacetone 7% 
Perfume 0.2% 
Water 5% 
______________________________________ 
The fluid obtained has the same characteristics as that in Example 1. 
______________________________________ 
Example 6: Tanning fluid 
______________________________________ 
Ethyl alcohol 28.8% 
Vitamin E 0.5% 
Butylene glycol 15% 
Diethylene glycol dioctanoate/ 
50% 
diisononanoate (DERMOL 489 sold by 
Alzo) 
Dihydroxyacetone 3% 
Perfume 0.2% 
Water 2.5% 
______________________________________ 
The fluid obtained has the same characteristics as that in Example 1. 
______________________________________ 
Example 7: Tanning fluid 
______________________________________ 
Ethyl alcohol 54.3% 
Butylene glycol 15% 
Polyoxypropylene-15 stearyl ether 
20.5% 
(ARLAMOL E sold by ICI) 
Dihydroxyacetone 5% 
Perfume 0.2% 
Water 5% 
______________________________________ 
The fluid obtained has the same characteristics as that in Example 1. 
______________________________________ 
Example 8: Tanning fluid 
______________________________________ 
Ethyl alcohol 34.2% 
Hydroxypropyl cellulose 0.1% 
Vitamin E 0.5% 
Butylene glycol 10% 
Dipropylene glycol 7.5% 
Laureth-2 benzoate (DERMOL 126 sold by 
5% 
Alzo) 
Diethylene glycol dioctanoate/ 
12.1% 
diisononanoate (DERMOL 489 sold by 
Alzo) 
Polyoxypropylene-15 stearyl ether 
5% 
(ARLAMOL E sold by ICI) 
2-Ethylhexyl malate 5% 
Ethoxydiglycol 10% 
Dihydroxyacetone 5% 
Perfume 0.6% 
Water 5% 
______________________________________ 
The fluid obtained has the same characteristics as that in Example 1. 
______________________________________ 
Example 9: Depigmenting fluid 
______________________________________ 
Ethyl alcohol 33.5% 
Hydroxypropyl cellulose 0.7% 
Vitamin E 0.5% 
Butylene glycol 10% 
Dipropylene glycol 7.5% 
Diethylene glycol dioctanoate/ 
10% 
diisononanoate (DERMOL 489 sold by 
Alzo) 
Laureth-2 benzoate (DERMOL 126 sold by 
10% 
Alzo) 
Polyoxypropylene-15 stearyl ether 
7.5% 
(ARLAMOL E sold by ICI) 
1,2-Pentanediol (HYDROLITE-5 sold by 
10% 
Dragoco) 
Ascorbic acid 5% 
Perfume 0.3% 
Water 5% 
______________________________________ 
The fluid obtained is in the form of a stable, transparent liquid which is 
pleasant to apply. Its regular application allows marks to be removed from 
the skin. 
______________________________________ 
Example 10: Cleansing fluid 
______________________________________ 
Ethyl alcohol 33.8% 
Hydroxypropyl cellulose 0.7% 
Butylene glycol 10% 
Dipropylene glycol 7.5% 
Diethylene glycol dioctanoate/ 
10% 
diisononanoate (DERMOL 489 sold by 
Alzo) 
Laureth-2 benzoate (DERMOL 126 sold by 
10% 
Alzo) 
Polyoxypropylene-15 stearyl ether 
8% 
(ARLAMOL E sold by the company ICI) 
1,2-Pentanediol (HYDROLITE-5 sold by 
10% 
Dragoco) 
Enzyme (SUBTILISINE SP 544 by 
0.1% 
Novo Nordisk) 
Water 9.9% 
______________________________________ 
A transparent fluid is obtained, intended for cleansing the skin of the 
face and of the body. 
An analytical test was carried out to determine the stability of 
dihydroxyacetone after storage at 45C for a certain time, for two 
compositions according to the invention (Examples 11 and 12) and two 
comparative compositions (Counterexamples 1 and 2), the dihydroxyacetone 
content being initially 5% in all the compositions. 
The compositions tested were the following: 
______________________________________ 
Example 11: Tanning fluid according to the invention 
______________________________________ 
Ethyl alcohol 59.3% 
Vitamin E 0.5% 
Butylene glycol 15% 
Diethylene glycol dioctanoate/ 
10% 
diisononanoate (DERMOL 489 sold by 
Alzo) 
Dihydroxyacetone 5% 
Perfume 0.2% 
Water 10% 
______________________________________ 
______________________________________ 
Example 12: Tanning fluid according to the invention 
______________________________________ 
Ethyl alcohol 54.3% 
Vitamin E 0.5% 
Butylene glycol 15% 
Diethylene glycol dioctanoate/ 
15% 
diisononanoate (DERMOL 489 sold by 
Alzo) 
Polyoxypropylene-15 stearyl ether 
5% 
(ARLAMOL E sold by ICI) 
Dihydroxyacetone 5% 
Perfume 0.2% 
Water 5% 
______________________________________ 
______________________________________ 
Comparative Example 1: Tanning gel 
______________________________________ 
Methyl vinyl ether/maleic anhydride 
0.5% 
copolymer crosslinked with 1,9-decadiene 
(STABILEZE 06 sold by ISP) 
2-Amino-2-methyl-1-propanol 
0.25% 
Ethyl alcohol 45% 
Butylene glycol 15% 
Diethylene glycol dioctanoate/ 
20% 
diisononanoate (DERMOL 489 sold by 
Alzo) 
Hydrogenated castor oil PEG-60 
0.5% 
(CREMOPHOR RH60 sold by BASF) 
Dihydroxyacetone 5% 
Perfume 0.2% 
Water 13.55% 
______________________________________ 
The gel of Comparative Example 1 is translucent and not very fluid. It 
differs from the compositions of the invention in a higher water content. 
______________________________________ 
Comparative Example 2: Tanning microemulsion 
______________________________________ 
Isohexadecane (ARLAMOL HD sold by the 
44% 
company ICI) 
Dimethicone (DOW CORNING 200 FLUID sold 
18.8% 
by Dow Corning) 
Mixture of PEG-8 OE and glyceryl laurate 
21.6% 
(surfactant) 
Lauric Plurol (surfactant) 
5.4% 
Dihydroxyacetone 5% 
Perfume 0.2% 
Water 5% 
______________________________________ 
A transparent microemulsion is obtained which differs from the compositions 
of the invention in the fact that the oils employed are not amphiphilic 
and in the presence of surfactant. 
The results of Examples 11 and 12 and of Comparative Examples 1 and 2 are 
shown in the following table: 
______________________________________ 
Number 
of days 
Example 11 
Example 12 Comparative 
Comparative 
at 45.degree. C. 
(invention) 
(invention) 
Example 1 
Example 2 
______________________________________ 
30 3.9 4.8 3.7 1.9 
50 4.2 4.7 1.5 2.0 
______________________________________ 
With the quantity of dihydroxyacetone at TO being 5%, these results clearly 
show that the compositions according to the invention maintain the 
activity of dihydroxyacetone for a longer time than their comparative 
products. From this it follows that the stability of dihydroxyacetone in 
the compositions according to the invention is markedly higher than that 
of the prior art. 
Having now fully described the invention, it will be apparent to one of 
ordinary skill in the art that many changes and modifications can be made 
thereto without departing from the spirit or scope of the invention as set 
forth herein. 
This application is based on French application 95-12446, filed Oct. 23, 
1995. The full text of that priority is incorporated herein by reference.