Field of Invention
The invention relates to compositions of cosmetic and dermatological use. The invention
particularly relates to synergistic compositions, which comprise essentially of at least one
polyol, al least one silicone and at least one vitamin or their respective derivatives. In
particular the invention relates to synergistic compositions comprising glycerol, vitamin
E derivative and silicone. Most particularly, the invention relates to compositions
comprising a synergistic mix of polyol/s, silicone's and vitamin/s or derivatives thereof
exhibiting an enhanced moisturizing effect.
The invention discloses the stochiometric ratios of the three constituents, which may be
added to achieve a desired potentiation in moisturizing effect.
Background of the invention
The skin protects the human body from the environment. Starting from surface, skin is
made up of three basic layers, the epidermis, the dermis and the hypodermis. The
epidermis is further made up of four constituent layers out of which stratum corneum
forms the outermost layer. The main cell types in the epidermis are the keratinocytes,
which at later stages form corneocytes. The corneoc\tes provide strength and rigidity to
the stratum corneum and together with it maintain the skin barrier against water loss and
entry of foreign matter into skin.
However owing to environmental aggressions, internal changes or external injuries, the
skin barrier might get disrupted. Loss of moisture and entry of foreign particle through
the disrupted stratum corneum thus ensues. It is in such situations particularly, that skin
moisturizers provide relief. Skin moisturization is a desired trait each time cosmetics are
applied to skin surface.
Moisturizers 'moisturisers are among the most used and prescribed products for the skin.
Owing to their wide usage they play a pivotal role in the cosmetic industry and find a
place of significance in pharmaceutical and therapeutic field. When applied topically,
moisturisers cause an increase in the water content of skin epidermis making it softer and
more pliable. They form a physical barrier on the skin surface preventing water loss
thereon. Moisturisers help in repairing skin damage caused by external aggressions or
internal changes. They are also used for repairing or postponing the aging effects on the
skin.
Principally, moisturisers are chemical formulations.These are complex mixtures of
selected chemical compounds and may include one or more naturally occurring skin
lipids or sterols, artificial or natural oils, humactants, emollients, lubricant etc.
Moisturisers can be classified as simple or complex depending upon the ease of
manufacture, number of components included therein and beneficial effects obtained
from them. Glycerine, olive oil and stearates when used individually or in admixture may
be used as simple moisturisers. Complex moisturisers are more varied in composition.
They are designed to meet the specific needs and requirements of individuals per se and
hence their compositions are more need specific.
Thus complex moisturisers are defined for different skin types such as oily skin, dry skin,
mixed skin types, skin types which are more prone to acne, sensitive skins, baby skins
etc.and there are moisturisers defined as per the skin condition as for damged and healthy
skin. Composition for moisturisers also vary depending on other factors, viz the time of
application as in day time application or night time application or the age group of
people.
Depending upon the specifications complex moisturisers may include humectants such as
polyols, glycerin, urea, lactic acid, sorbitol, etc. natural moisturising factors (NMF) such

as ammonia, aminoacids. glucosamine, creatinine, citrate, sodium, potassium, chloride,
phosphate, calcium, magnesium etc., emollients such as lanolin, octyl dodecanol, hexyl
decanol. oleyl alcohol, decyl oleate, isopropyl stearate, isopropyl palmitate. isopropyl
myristate. hexyl laureate, dioctyl cyclohexane. etc. emulsifiers. thickners. vehicles,
cleaners, actives, fragrance, colours, preservatives, antioxidants, desenitizers, UV
absorbers, chelating agents, sunscreens, in differing concentrations.
Various compositions of moisturisers prepared by selecting known chemical components
or by varying their concentrations or by replacing one with another are available in the
market. Such selection may however cause a number of adverse effects, including
allergic reactions to some of the components, skin irritation caused by overdose of any of
the selected components, contact dermatitis, characterised by redness, itching, burning
and stinging sensations, or even may cause a contrary effect to the desired, i.e. it may
actually increase dehydration. When used near sensitive spots, such as the eyes, lips and
genitals, these effects may be exaggerated in some persons. Use of plant extracts, some
alcohols and proteins may increase the danger of adverse effects. Even glycols, which
form a part of most cosmetic formulations, when added in higher concentrations are
known to exhibit undesirable effects such as an oily and sticky feel.
All in all there is a standing requirement for cosmetic formulations, which, in terms of
input components, delivers more from less. Hence, research is in progress continually for
formulations which are safe, stable, effective, easy to manufacture and are an ideal mix of
quality with quantity.
WO2006069426 relates to cosmetic compositions comprising (a) a wetting agent
(glycerin), (b) an emollient, (c) an emulsifying system, (d) a silicone system and (e) an
oiliness adsorbing system. The publication relates particularly to a system exhibiting
reduction in oily/sticky texture and rapid absorption. It discloses of a composition
wherein the quantities of each of the components added are significantly high.
Additionally it mandates the use of an oiliness adsorbing system in its composition thus
adding to the number of constituents required to make the composition and net cost for its
preparation. The publication states a composition characterized by the presence of
nylon 12 as oiliness reducing substance in a concentration of 2 to 6 parts by weight and
glycerin in the proportions of 8 to 13 parts by weight. The publication further discloses a
multistep procedure for the preparation of the disclosed composition, which is essentially
complex and difficult to apply on a commercial scale. It does not state any synergism
between silicones, polyols and vitamins.
US 6,861,061 discloses a water-in-oil (W/O) emulsion with a linear silicone polyether,
an .a.,.?. -diene crosslinked silicone elastomer, and a nonionic organic emulsifier. The
emulsion further contains a water-soluble or oil soluble active ingredient such as a
vitamin and particularly refers to stabilization of vitamins in water in oil emulsions. The
patent does not state whatsoever any synergistic possibility between the polyols. vitamins
and silicones affecting the moisturizing effect of a composition. The patent further states
that Vitamin E typically is known to exhibit signs of degradation and instability in W/O
systems. Particularly so W/O films tend to be immiscible in water, are not water
washable, do not absorb water, are occlusive, and may be "greasy" and find less cosmetic
acceptance amongst customers.
US 6,498,197 discloses micro emulsion comprising a non-aqueous polar solvent, a non-
polar solvent immiscible with it and an oxyalkylene-containing polydiorganosiloxane for
delivery of active ingredients such as Vitamin E. However microemulsions have certain
inherent complications related to their composition, which necessarily include the use of
high proportion of surfactants in their compositions. This leads to intolerance and results
in a sticky feel during application to the skin. Furthermore, the formulation range of
microemulsions is generally very narrow and their temperature stability very limited.
Moreover, the preparation of microemulsions is time consuming and requires the expert
guidance of one skilled in the art at all instances of product formation in lab or pilot scale,
adding to the total cost of the product. The patent makes no reference of the synergistic
effect shown in moisturization by composition containing a mix of polyols, silicones and
vitamins.
US 6.159,480 also states a water-in-silicone cosmetic makeup composition includes a
hydroxy acid, a sunscreen agent, a moisturizing agent, an antioxidant, a cosmetically
acceptable pigment, an emulsifier, a silicone-containing compound and water. The patent
discloses a complex and multi-step procedure for the preparation of the composition. The
patent relates to water in oil type films that find low cosmetic acceptance amongst
customers. It is also noteworthy that it is difficult to obtain highly stable water-in-oil type
emulsion cosmetic that comprises silicone oil as a base. The final product may thus lack
in commercial and industrial utility. The patent does not disclose any synergism between
silicones, vitamins and polyols.
US 20050249763 relates to kits for formulating cosmetic products, which contain an
aqueous composition and a water-soluble anhydrous film. The aqueous composition
amongst other components comprises glycerol, volatile silicone oil and Vitamin E.
However, the publication does not refer to moisturizing compositions and does not state
of any possible synergism between the three constituents to enhance such an effect.
US20020192170 relates to a liquid for lip care and lip coloring, comprising: water, a
moisture retainer, and a polyoxyethylene glycerin fatty acid ester. The application further
states the presence of vitamin E in the composition. However, the application does not
make any reference to the moisture enhancing capabilities of polyols, silicones and
vitamins when added together to a composition.
Owing to their varied usage, polyols, silicones and vitamins are used widely in most
cosmetic and dermatological preparations. These therefore form a part of most patents
describing such compositions as in W09811873, WO0062737, EP0920300. US
6,440.432, US 6,649,176, US 6,548,075, US 5,989,528, US 6,136,330 US 6,132,742, US
6.517,816, US20050192187, US20060182699 which even though state the use of the
three constituents jointly, do not refer to any possibility of synergism between them
towards enhancement in moisturization effect.
The dispersion of oil droplets in water (O/W) or water droplets in oil (W/O) is a
complicated procedure more so when the preparations are required in large quantities.
Meeting all desired specifications by including the various desired ingredients often
becomes a challenge when inventions are practised on a commercial scale. Even so the
final product may cause adverse effect and allergic reaction owing to its constituents.
Hence, a need remains to simplify cosmetic preparations and to deliver a moisturizing
composition preferably with fewer constituents and exhibiting more pronounced effects.
A composition, wherein two or more components, while exhibiting their individual
unrelated effects add to the net moisturing effect shown by it. is much needed.
Objects of the Invention
The main objective of the invention is to provide composition comprising polyols.
silicones and vitamins, exhibiting synergism when present in specified quantities.
Summary of Invention
One embodiment of the invention provides a synergistic cosmetic composition
comprising at least a polyol, at least a silicone and at least a vitamin.
Another embodiment of the invention provides a composition comprising a synergistic
composition of a polyol. a silicone and vitamin derivative.
Brief description of accompanying drawings
Figure 1 describes a comparative study of skin moisturization efficacy of glycerol (G),
cyclopentasiloxane (S). vitamin E acetate (V), their binary (G+S. S+V and G+V) and
synergistic (G+S+V) mixture of the three compounds.
Detailed description of invention
The instant invention describes compositions comprising polyols. silicones and vitamin
derivatives and exhibiting synergism among themselves, which when added together to
any other composition lead to a pronounced enhancement in the moisturizing effect
shown by it. Preferably the said components are present in defined amount to provide the
synergism and enhance the moisturizing effect when present in a moisturizing
composition.
The term "composition" as used herein refers to a mixture of chemical components of
various usage and properties
The terms, "synergistic", "synergism" as used in the present invention refers to
moisturizing effect created from the application of two or more agents to produce a
moisturizing effect that is greater than the sum of the moisturizing effects produced by
the application of the individual agents.
The term "moisturizing effect" as used herein refers to effects shown by moisturizers on
application to skin surface such as repair of skin barrier, retentioa/increase in water
content, reduction in TEWL i.e. transepidermal water loss, restoration of the lipid
barriers' ability to attract, hold and redistribute water and maintenance of skin integrity
and appearance.
The term "moisturizer or moisturiser" as used herein refers to chemical compositions
comprising varying combinations of emollients, occlusives, and humectants. The
composition may further comprise of chemicals added to suit the specific needs of
customers and may be selected from the group comprising cleansers, age masking
factors, sunscreens, antioxidants and the like. The term includes compositions that are
used to restore the barrier function of the epidermis, to cover tiny fissures in the skin,
provide a soothing protective film and increase the water-content of the epidermis. The
term also includes compositions, which slows down evaporation of the skin's moisture,
thereby maintaining hydration and improving the appearance and tactile properties of dry
and aging skin.
The term "humectants" as used herein refers to hygroscopic materials, which have
property of absorbing water vapour from moist air until a certain degree of dilution is
attained for example, polyols, gelatin, hyaluronic acid, honey, panthenol. propylene
glycol, sodium and ammonium lactate and the like
The term "polyol" as used herein refers to chemical compounds containing multiple
hydroxyl groups. Examples of polyol compounds suitable for use in the instant invention
include, but are not limited to. glycerol, ethylene glycol, propylene glycol,
pentaerythritol, diglycerol, and polyglycerol.
As used herein the term "glycerol", referred at some instances in the instant invention as
G, refers to a chemical compound with the formula HOCH2CH(OH)CH2OH that is also
known as glycerin or glycerine or its derivatives thereof.
The term "emollient" is used interchangeably with "occlusives" and as used herein refers
to a materials which has been designed to soften the skin to touch and make the surface
look smoother to the eye for example cyclomethicone, dimethicone. castor oil. isopropyl
isostearate. etc. These emollients mostly work by forming a layer on the skin thus
preventing the loss of water from the skin surface.
The term "occlusives" as used herein refers to chemical compounds which when applied
topically reduce TEWL by creating a hydrophobic barrier over the skin and contributing
to the matrix between corneocytes for example petroleum jelly. lanolin, mineral oil, and
silicones (e.g., dimethicone). etc.
As used herein the term, "silicones, or polysiloxanes", referred at some instances in the
instant invention as S. refers to inorganic-organic polymers with the chemical formula
[R2SiO]n, where R= organic groups such as methyl, ethyl, and phenyl. These materials
consist of an inorganic silicon-oxygen backbone (...-Si-O-Si-O-Si-O-...) with organic side
groups attached to the silicon atoms, which are four-coordinate. In some cases organic
side groups can be used to link two or more of these -Si-O- backbones together.
Examples of silicone compounds suitable for use in the instant invention include, but are
not limited to, silicone oil, volatile and non volatile silicones, linear and branched chain
silicones, alone or in combination and may be selected from the group comprising
dimethicone copolyol, dimethylpolysiloxane, diethylpolysiloxane, high molecular weight
dimethicone. mixed C1-C30 alkyl polysiloxane. phenyl dimethicone, dimethiconol,
cyclopentasiloxane. dimethicone, dimethiconol, mixed C1-C30 alkyl polysiloxane, and
mixtures thereof.
As used herein the term "vitamins" refers to biomolecules that act both as catalysts and
substrates in biochemical reactions and to those organic compounds, which are required
in tiny amounts for essential metabolic reactions in living organisms. Vitamins are
generally added to topical compositions in the form of vitamin derivatives since these are
prone to degradation. Once the composition is applied to skin, the derivatives break to
release vitamins that are then topically absorbed. As used in the current specification the
term vitamin derivative is hence equivalent to the term vitamin.
The percentages stated in the instant invention unless specified otherwise, are
weight/weight.
By virtue of their physicochemical properties, polyols are well known for their
moisturizing capabilities. However, large amounts of polyols cannot be added to a
cosmetic or dermatological composition without running the risk of obtaining a sticky
composition, which discourages users from using the composition. In addition, the
duration of the moisturization provided by the polyols is limited in time. Of late silicones
have proved their potential as occlusive agents and have been widely used in cosmetic
preparations. However, their properties of providing moisturization to skin are only
limited.
Vitamin derivatives, referred at some instances in the instant invention as V, have been
known to provide essential nutrients to the skin. Vitamin E acetate in particular is
commonly used in skin care formulations for its ability to reduce the damage caused by
free radicals. However, vitamins do not whatsoever have any direct effect on the
moisturization of the surface whereon they are applied.
Whereas the invention does not negate the possibility of achieving improved
moisturization by combining occlusive with humectants, it was found by the applicants of
the instant invention that when silicones, which are occlusives by nature, are mixed with
glycerol, a humectants. the moisturizing effect shown by the composition is decreased.
On the contrary when vitamins, which are antioxidants by nature and show whatsoever
no moisturizing effect on their own, are added to the composition containing a
combination of silicone and humectants, the moisturizing effect of the resultant
composition is improved markedly. Further the effect so obtained is much more than the
sum of the three individual ingredients put together. As expected and as is evident from a
separate experiment vitamins when added to glycerol decrease the moisturizing effect
shown by it. Hence the presence of all three constituents is required jointly to achieve an
increase in moisturisation.
In a preferred embodiment the invention relates to a composition comprising polyols.
vitamins and silicones and/or their derivatives in stoichiometrically derived ratios.
In a preferred embodiment the invention relates to compositions wherein the
concentrations of polyol compounds varies from about 0.1 to 10.0 percent; preferably
between 0.5 and 5.0 percent, most preferably between 1.0 and 4.0 percent.
The polyols used are selected from glycerol, ethylene glycol, propylene glycol,
pentaerythritol, diglycerol. polyglycerol. their derivatives and combinations thereof.
The concentration of silicones is about 0.01 to 5.0 percent; preferably about 0.1 to 3.0
percent, more preferably about 0.5 to 2.0 percent.
The silicone used in the invention is selected from linear, branched, crosslinked, silicone
oils, volatile and non volatile silicones such as dimethicone copolyol,
dimethylpolysiloxane, diethylpolysiloxane, high molecular weight dimethicone, mixed
C1-C30 alkyl polysiloxane, phenyl dimethicone, dimethiconol. cyclopentasiloxane,
dimethicone, dimethiconol. mixed Cl-C30 alkyl polysiloxane, and mixtures thereof.
The concentrations of the vitamin and/or its derivative(s) may be about 0.01 to 5.0
percent; preferably about 0.05 and 3.0 percent, and more preferably between 0.5 and 2.0
percent.
The vitamin used in the composition is selected from a group comprising vitamin A.
vitamin B (1-12), vitamin C, vitamin D (2-4), vitamin E, vitamin K, their derivatives,
such as acetates, propionates, palmitates, phosphates, alone on in combinations thereof.
In a preferred embodiment, the invention relates to compositions comprising glycerol,
cyclopentasiloxane and vitamin E acetate in proportions of about 3%. about 1.5% and
about 1%. Mixtures of one or more polyols, one or more silicones and one or more
vitamins and/or their derivative(s) are encompassed by the present invention.
Preferably the invention relates to body and face moisturizers, day and night time
moisturizers, anti-aging preparations to be used during day or night time, cosmetic
preparations applicable to children, anti-perspirants, aftershave lotions, hydroalcoholic
skin disinfectants, therapeutic creams, after shower day care preparations, preparations
for localized-action as under eye marks and regions, sunscreens and the like comprising
synergistic mix of silicones, vitamins and polyols or their derivatives disclosed in the
instant invention. These and similar compositions and formulations may be applied
topically to the skin or to the various mucous membranes of the body, including but not
limited to those of the oral, nasal, vaginal or rectal cavities. The synergistic combination
of the instant invention may be added to compositions of cosmetic, dermatological,
topical, pharmaceutical and therapeutic uses.
In preferred embodiment the invention relates to oil in water emulsion compositions
comprising, besides the three essential ingredients i.e. silicones, vitamin derivatives and
polyols. other optional ingredients like acceptable vehicles, structurants, emollient/s,
gelling agent/s, a thickening agent/s, a hydrophilic or hydrophobic polymer/s, an
emulsifying agent/s, alcohol/s etc. Examples of these ingredients include but are not
limited to such substances as binders, emollients, preservatives (such as methyl paraben).
colorants, perfumes, skin-lightening agents, anti-wrinkle agents, antimicrobials and the
like.
Emulsifying agents which may be optionally added to the compositions of the present
invention include but are not restricted to oxyalkylenated fatty acid esters of polyols, for
example polyethylene glycol stearates, for instance PEG-100 stearate, PEG-50 stearate
and PEG-40 stearate; and mixtures thereof, mixture of glyceryl monostearate and of
polyethylene glycol stearate (100 EO) (Simulsol 165), oxyalkylenated fatty acid esters of
sorbitan comprising, for example, from 20 to 100 EO such as Tween 20 or Tween 60,
oxyalkylenated (oxyethylenated and/or oxypropylenated) fatty alcohol ethers;
alkoxylated or non-alkoxylated sugar esters, such as sucrose stearate and PEG-20
methylglucose sesquistearate; sorbitan esters such as the sorbitan palmitate ( Span 40).
esters of diacid and of fatty alcohol, such as dimyristyl tartrate; mixtures of these
emulsifiers, for instance the mixture of glyceryl stearate and of PEG-100 stearate(ArIacel
165). and mixtures comprising these emulsifiers, such as the mixture of dimyristyl
tartrate, cetearyl alcohol. Pareth-7 and PEG-25 laureth-25. (Cosmacol PSE). steareth - 2.
steareth 21, PPG-15 stearyl ether.
Thickeners when used in the instant invention include but are not restricted to
alkyloamides, carbomer 934,940,941,960,961, cetearyl alcohol, cetyl alcohol, gelatin,
gums, magnesium aluminium silicates, ozocarite, paraffin, tragacanth, sodium alginate,
Tinovis ADM and the like.
Structurants when used in compositions of the present invention include those materials
which are well known in the art and include fatty acids, fatty alcohols, fatty acid esters,
and fatty acid amides, having fatty chains of from 8 to 30 carbons atoms. Preferably the
structurant used is stearic acid.
Various emollients as are known to a person skilled in the art and as are available in the
market can be employed as an optional constituent in the instant invention. These include
but are not restricted to the group consisting of lanolin. octyl dodecanol, hexyl decanol,
oleyl alcohol, decyl oleate. isopropyl stearate. isopropyl palmitate, isopropyl myristate,
hexyl laureate, dioctyl cyclohexane, PPG-15 stearyl ether, isohexadecane, stearic acid,
cetyl alcohol, mineral oil etc
Various chelating agents when used as optional constituents of the instant invention may
be selected from a group consisting of but not limited to Dimercaptosuccinic acid
(DMSA). Dimercapto-propane sulfonate (DMPS). Alpha lipoic acid (ALA). Calcium
disodium versante (CaNa2-EDTA), Disodium EDTA, Dimercaprol (BAL).
Various cosmeticaly and dermatologically suitable preservatives may be added to the
instant composition. These may be selected from the group consisting of but not
restricted to 2-phenoxyethanol. para-hydroxybenzoic acid esters, also known as parabens.
for instance methyl para-hydroxybenzoate (methyl paraben), ethyl para-hydroxybenzoate
(ethyl paraben) and propyl para-hydroxybenzoate (propyl paraben) and mixtures thereof;
formaldehyde-releasing agents, for instance imidazolidinylurea or diazolidinylurea;
haloalkynyl carbamates, for instance 3-iodo-2-propynyl butyl carbamate (IPBC); caprylyl
glycol, also known as 1,2-octanediol; sodium benzoate; N-(3-chloroallyl)-hexaminium
chloride (or Quaternium-15); polyhexamethylene biguanide hydrochloride (CTFA name:
polyaminopropyl biguanide); alkyltrimethylammonium bromides, for instance
dodecyltrimethylammonium bromide, myristyltrimethylammonium bromide and
hexadecyltrimethylammonium bromide, and mixtures thereof.
Anti-ageing active agents which may optionally added to the compositions of the instant
invention may be chosen from free-radical scavengers, keratolytic agents, vitamins, anti-
elastase and anti-collagenase agents, proteins, fatty acid derivatives, steroids, trace
elements, bleaching agents, algal and plankton extracts, enzymes and coenzymes,
flavonoids, ceramides. tensioning agents and muscle relaxants, and mixtures thereof.
Free-radical scavengers and antioxidants which may be optionally added to the
compositions of the instant invention include but are not restricted to phosphonic acid
derivatives such as ethylenediaminetetra (methylenephosphonic acid), methylene
phosphonic acid, methylenephosphonic acid and salts thereof, in particular the sodium
salts thereof; ethylenediaminetetraacetic acid and its salts, such as the sodium salt;
guanosine; superoxide dismutase; tocopherol (vitamin E) and its derivatives (acetate);
ethoxyquine; lactoferrin; lactoperoxidase, and nitroxide derivatives; superoxide
dismutases; glutathione peroxidase; plant extracts with free-radical-scavenging activity,
such as the aqueous extract of wheatgerm (Detoxiline). green tea. and mixtures thereof.
Various cosmetically acceptable vehicles may be used for the preparation of
compositions as per the instant invention. These may be selected from the group
consisting of but not restricted to water, alcohols, oils and combinations therof.
Accordingly, when the surface contemplated is skin, the composition of this invention
may contain ingredients, which are added to known creams, lotions, ointments, gels or
medicaments, which are physiologically acceptable to skin and which do not contain
ingredients, which will reverse or retard the action of skin-moisturizing agent(s).
Certain preferred embodiments of the invention comprise, for example but not by way of
limitation, one or more of the following: a polyol such as glycerol, a silicone such as
cyclopentasiloxane, a vitamin derivative, such as vitamin E acetate, one or more
emulsifiers such as ethoxylated and propoxylated fatty alcohols, sugar esters such as
sorbitan stearate, sucrose cocoate, polyol esters of fatty acids such as glyceryl stearate,
PEG-20 stearate, PEG-100 strearate; one or more of the emollients such as mineral oil.
petroleum jelly, isohexadecane, PPG-15 stearyl ether, Isopropyl palmitate, emollient,,
PPG-10 cetyl ether, PPG-50 cetyl ether, PPG-3 Myristyl ether. PPG-3 benzyl ether
microstate PEG 20 Almond Glycerides, hydroxylated milk glycerides; structurants and
emollients such as strearic acid, cetyl alcohol, thickeners and emulsion stabilizers such as
acrylate/acrylamide copolymer, sodium acrylate copolymer, carbopol, one or more
thickeners such as polymeric quaternary ammonium salts of hydroxyethyl cellulose
reacted with trimethyl ammonium substituted epoxide (Polyquaternium). hydroxypropyl
methyl cellulose.
In preferred embodiments, the invention relates to compositions comprising water
present in a concentration of about 10-90%, thickeners and/or gelling agents present in
concentrations of about 0.05-5.0%, emulsifiers present in concentrations of about 0.5-
7.0% and emollients present in concentrations of about 0.1-65 %.
In certain non-limiting embodiments of the invention, the composition may be added to
pre-existing formulations provided that the ingredients in those formulations do not
prevent or retard the activity of the claimed composition. In a preferred embodiment, the
instant composition can be added to cosmetic and therapeutic compositions, which are
commercially available.
Process of preparation of cosmetic products
All ingredients are segregated as per their boiling points and their ease of degradation at
elevated temperatures. Ingredients that have a low boiling point or are prone to
degradation at elevated temperatures (eg: Silicones and vitamins) are weighed separately
and kept aside. Rest of the ingredients are weighed individually and added to water or oil
phase as per their solubility or as required. The water phase and the oil phase are heated
to a temperature of 75°C. The oil phase is then slowly added to the water phase with
homogenization to get an emulsion. The emulsion is stirred and allowed to cool to
temperature of about 40°C. Ingredients that have a low boiling point or are prone to
degradation at elevated temperatures and that had been kept aside initially are then added
to the cooled emulsion to obtain the final product.
The invention provides for methods of using the foregoing compositions to achieve a
moisturizing effect, comprising applying an effective amount of the composition to the
surface. A moisturizing effect significantly diminishes the risk of drying of the skin or
progression of existing skin dryness. Often substantially in few instances substantial
increase in skin moisturization is achieved. While increase from 10 - 50% or more may
be considered normal, it would not be unusual to have moisturization extend to 200% in
this instance. Examples of the surface on which the said composition could have
moisturization benefit include, skin or the various mucous membranes of the body,
including but not limited to those of the oral, nasal, vaginal or rectal cavities.
The following are specific, non-limiting examples of formulations prepared as per the
present invention.
Example 1 A
The composition of the present invention is formulated into moisturizing cream with the
components as in Table 1.
Table 1: Moisturizing Cream

Example 1 B
The composition of the present invention is formulated into winter cream with the
components as in Table 2.
Table 2: Winter Cream

Example 1 C
The composition of the present invention is formulated into moisturizing lotion with the
components as in Table 3.
Table 3: Moisturizing Lotion

Example 1 D
The composition of the present invention is formulated into Body Lotion with the
components as in Table 4.
Table 4: Body Lotion

In all the above formulation the moisturizing properties were present
Example 2
Formulations containing only single ingredients that is a polyol such as glycerol (G), a
silicone such as cyclopentasiloxane (S), and a vitamin derivative such as vitamin E
acetate (V)] their binary combinations [such as G+S, G+V and S+V] and the combination
of all the three (G+S+V) were prepared in a cream base as shown in table 5. The same
cream base devoid of all three ingredients-G, S or V was formulated and used as a
Placebo.
Table-5: Formulations comprising the three constituents in varying combinations

Table 6: Formulation 1 comprising none of the three constituents out of vitamins,
silicones and polvols

Measurement of skin moisturization using Corneometer
The measurement of skin moisture is based on the measurement of capacitance. This
method is based on the fact that the dielectric constant of water (81) is different when
compared to other substances (<7). The measuring capacitor in the probe when placed on
the skin shows a change in the capacitance depending on the moisture content. The probe
head contains gold metallic tracks one of which develops a positive charge where as the
other builds up a negative charge. An electric field between the tracks with alternating
attraction develops. During the measurement the scatter field penetrates the very first
layer of the skin and determines the dielectricity.
Sample pre-conditioning: It is important to ensure that all the samples that have been
fielded for evaluation have been subjected to pre-conditioning. This was achieved by
storing overnight, all the samples in an area with similar temperature and humidity until
the samples equilibrate to these conditions.
Skin Preconditioning: Six human volunteers were included in the study panel. The
panelists were advised not to use lotions, creams, or any other topical products to the
volar forearms for approximately 4 hours before the evaluation session.
Site Preparation: The subjects washed their volar forearms with plain water and dried
them. The subjects were then allowed to acclimatize in a room maintained at a
temperature of 22 ± 3oC and a relative humidity of 40-60%. These conditions were
maintained throught the study. Test sites (diameter: 2-inch) chosen on the volar forearm
were then marked with indelible ink.
Skin Moisture Measurement: Skin moisture measurements were taken using the
Corneometer® 825 (Courage + Khazaka, Germany) as per the standard procedure3. The
probe was placed perpendicular to the test site and gently pressed against the skin. Three
readings were taken at different locations on a single site and the mean reading was
recorded as the Baseline reading (B). The desired formulation (x gm) was then applied to
the test site and rubbed into the skin and allowed to get absorbed for 10 min. The
formulations were alternatively applied in duplicates on the volar forearms of the panel
members. Skin moisture measurement at the test site was similarly taken and recorded as
the Test reading (T). The difference in the readings gives a measure of the increase in the
skin moisturization due to that particular test formulation.
Calculations:
The increase in the skin moisturization due to the application of a particular formulation
was measured by using the formula:
Mx = Tx-Bx
Where.
Mx: Increase in skin moisturisation (Corneometer units) due to application of the cream.
containing ingredient X.
Bx: Corneometer reading (Corneometer units) before application of the cream, containing
ingredient X (Baseline reading)
Tx: Corneometer reading (Corneometer units) after application of cream, containing
ingredient X (Test reading)
The increase in the skin moisturization due to cream containing ingredient X (Mx) was
calculated for every subject and the mean increase in moisturization for all the subjects
(MMx) was calculated. Similar study was carried out with all the formulations and their
MM values were calculated
These MMx values would give information about the increase in the skin moisturization
after applying the cream (which is a combination of the cream base and the ingredient(s)
incorporated into it). To nullify the moisturizing effect of the cream base, and to
understand the true moisturizing activity of individual cosmetic ingredient or their
combinations, a new term moisturizing efficacy (ME) was coined. Moisturizing efficacy
(ME) of an ingredient(s) in a formulation is defined as the difference between the mean
increase in skin moisturization due to application of the cream containing that
ingredient(s) and the mean increase in skin moisturization due to the application of the
cream base (without the ingredient(s)).
MEX = MMX - MMP
Where,
MEX: Moisturizing efficacy of the ingredient X.
MMx: Mean increase in skin moisturisation (Corneometer units) due to cream containing
ingredient X.
MMp: Mean increase in skin moisturisation (Corneometer units) due to the cream base
(Placebo)
The Moisturizing efficacy (MEx) values is calculated for all the ingredients and their
combinations and this is used for comparing their moisturizing efficacies.
As generally known glycerol has the maximum moisturizing efficacy amongst the three
ingredients. Cyclopentasiloxane and vitamin E acetate show no moisturizing effect
individually. Binary combinations of these ingredients (G+S, S+V and G+V) do not show
synergy in their moisturizing efficacy. Infact, the moisturizing effect of glycerol is visibly
reduced in presence of cyclopentasiloxane or vitamin E acetate when mixed with it
individually. Yet. it has been found that there exists a synergy between glycerol,
cyclopentasiloxane, and vitamin E acetate in its moisturizing efficacy. The formulation
containing all the three ingredients shows an unprecedented synergy in their moisturizing
efficacies. The moisturizing efficacy of the G+S+V combination obtained is even more
than the sum of the individual moisturizing efficacies of G, S and V.
The mean increase in moisturization (MMx) due to creams (a) containing none of G, S or
V {Placebo}, (b) containing only G, S or V, (c) their binary combinations G+S, S+V and
G+V and a (d) combination of all the three (G+S+V) as recorded for a set of six human
volunteers (in duplicates) and the moisturizing efficacies (ME\) of these Ingredients or
their combinations is presented in Figure-1. On the X axis of figure 1, compositions
comprising only glycerol, cyclopentasiloxanes or vitamin derivatives, marked as G, S. V
are stated along with their binary combinations i.e. combinations of glycerol and
cyclopentasiloxane, G+S; combination of cyclopentasiloxane and vitamin, S+V; and
combination of glycerol and vitamin G+V; and further against a composition comprising
a three-in-one combination of glycerol, cyclopentasiloxane and vitamin, G+S+V. On the
Y axis the moisturizing efficacy of the each of the compositions ranked in corneometer
units is marked. The increase in moisturization efficacy owing to evident synergism
between glycerol, cyclopentasiloxane and vitamin is self-explanatory.
A combination of all the three ingredients in a cosmetic formulation decreases the
quantity of glycerin required to obtain a moisturizing effect. Additionally, vitamins and
silicones besides showing their individual effects add to the moisturizing effect of the
composition.
Other variations as may be obvious to one skilled in the art may be made in compounds,
compositions, and methods described herein without departing from the essential features
of the invention and therefore must be held non restrictive to the scope of the instant
invention. The embodiments of the invention specifically illustrated herein are exemplary
only and may not in any way be intended as limitations in its scope.
We claim
1. A composition comprising at least one polyol, at least one silicone and at least
one vitamin.
2. A composition comprising at least one polyol. at least one silicone and at least
one vitamin derivative
3. The composition as claimed in any of claims 1 or 2 wherein the at least one polyol
is present in an amount of from about 0.1 to about 10.0 % by weight.
4. The composition as claimed claim 3 wherein the at least one polyol is selected
from the group comprising glycerol, ethylene glycol, propylene glycol,
pentaerythritol, diglycerol. polyglycerol, their derivatives and combinations
thereof.
5. The composition as claimed in any of the preceding claims wherein the at least
one silicone is present in amount of from about 0.01 to about 5.0% by weight..
6. The composition as claimed in claim 5 wherein the at least one silicone is selected
from the group comprising linear, branched, crosslinked, silicone oils, volatile and
non volatile silicones such as dimethicone copolyol, dimethylpolysiloxane,
diethylpolysiloxane. high molecular weight dimethicone, mixed C1-C30 alkyl
polysiloxane, phenyl dimethicone, dimethiconol. cyclopentasiloxane,
dimethicone, dimethiconol, mixed C1-C30 alkyl polysiloxane, and mixtures
thereof.
7. The composition as claimed in any preceding claims wherein the at least one
vitamin is present in an amount of from about 0.01 to 5.0% by weight..
8. The composition as claimed in any of the preceding claims wherein the at least
one vitamin derivative is present in an amount of from about 0.01 to about 5.0%
by weight.
9. The composition as claimed in claim 7 wherein the at least one vitamin is selected
from a group comprising vitamin A, vitamin B (1-12), vitamin C, vitamin D (2-4),
vitamin E, vitamin K alone and in combinations thereof.
10. The composition as claimed in claim 8 wherein the at least one vitamin derivative
is selected from a group comprising vitamin acetates, vitamin propionates,
vitamin palmitates, vitamin phosphates alone and in combinations thereof.
11. The composition as claimed in any of the preceding claim comprising glycerol,
cyclopentasiloxane and vitamin E acetate in proportions of 3%. 1.5% and 1%
respectively.
12. The composition as claimed in any preceding claim optionally comprising
acceptable vehicles, structurants, emollient/s, gelling agent/s, thickening agent/s, a
hydrophilic or hydrophobic polymer/s. emulsifying agent/s. alcohol/s and
mixtures thereof

The present invention discloses a composition comprising at least one polyol. at least one
silicone and at least one vitamin. In particular the invention discloses compositions
comprising synergistic combinations of at least one polyol, at least one silicone and at
least one vitamin derivative. The combination may be used suitably in cosmetic and
dermatological compositions and in compositions of topical, pharmaceuticals or
therapeutic use.