A personal care composition proving antioxidant properties

Abstract

The present invention relates to a personal care composition. Particularly, the present invention relates to a personal care composition that provides antioxidant effect. The composition comprises a vitamin B3 compound selected from niacinamide, picolinamide, iso-nicotinamide, n-cyclopropyl niacinamide, n-cyclo-butyl niacinamide, n-cyclo-pentyl niacinamide and mixtures thereof in combination with a gingerol or a source thereof and a compound of formula (1) where, R1, R2, R3, R4 are each, independently, a linear or branched carbon chain having 2 to 6 carbon atoms; and R5 is a carbon chain having 1 to 6 carbon atoms.

Description

[0001] A PERSONAL CARE COMPOSITION

[0002] Field of the invention

[0003] The present invention relates to a personal care composition. Particularly, the present invention relates to a personal care composition that provides antioxidant effect.

[0004] Background of the invention

[0005] People tend to get exposed to stressful conditions e.g. heat, either directly e.g. through the infrared radiations contained in the sunlight; or indirectly e.g. through their day-to-day activities, that involve working or being exposed to elevated temperatures. Exposure to such stressful conditions such as heat often tends to create oxidative stress that is created due to generation of free radicals I reactive oxygen species (ROS). One of the possible mechanisms of such increased ROS generation is contemplated to be increased calcium influx, due to such exposure to heat, into skin cells e.g. keratinocytes. People also tend to get exposed to other stressful conditions e.g. exposure to ultraviolet radiations contained in the sunlight and to pollutants, where ROS; and thereby oxidative stress, also tends to increase.

[0006] A need therefore exists to provide a personal care composition that provides an antioxidant effect and protects the skin from unwanted effects that may be induced by exposure to such direct or indirect heat.

[0007] It is thus an object of the present invention to provide a personal care composition that provides antioxidant benefit.

[0008] It has now been found that a personal care composition comprising a niacinamide compound in combination with a gingerol or a source thereof; and a compound of formula 1 described more particularly hereinbelow, provided synergistic antioxidant effect. It has also been found that a personal care composition comprising said combination, also provides skin brightening effect and anti-aging effect.

[0009] Summary of the invention

[0010] Accordingly, in the first aspect, the present invention relates to a personal care composition comprising: a. from 0.01 to 10 wt% a vitamin B3 compound, b. from 0.001 to 10 wt% a gingerol or a source thereof; and c. from 0.01 to 10 wt% a compound of formula 1 : where, R1 , R2, R3, R4 are each, independently, a linear or branched carbon chain having 2 to 6 carbon atoms; and R5 is a carbon chain having 1 to 6 carbon atoms; and wherein the vitamin B3 compound is selected from niacinamide, picolinamide, isonicotinamide, n-cyclopropyl niacinamide, n-cyclo-butyl niacinamide, n-cyclo-pentyl niacinamide and mixtures thereof.

[0011] Further, in a second aspect, the present invention relates to a method of protecting the skin through providing antioxidant benefit comprising the steps: a. applying the composition of the first aspect; and b. optionally, rinsing the skin with water.

[0012] Further, in a third aspect, the present invention relates to use of the composition of the first aspect for providing antioxidant benefit.

[0013] Detailed description of the invention

[0014] These and other aspects, features and advantages will become apparent to those of ordinary skill in the art from a reading of the following detailed description and the appended claims. For the avoidance of doubt, any feature of one aspect of the present invention may be utilized in any other aspect of the invention. The word "comprising" is intended to mean "including" but not necessarily "consisting of" or "composed of." In other words, the listed steps or options need not be exhaustive. It is noted that the examples given in the description below are intended to clarify the invention and are not intended to limit the invention to those examples per se. Unless specified otherwise, amounts as used herein are expressed in percentage by weight based on total weight of the composition and may be abbreviated as “wt%”. Except in the operating and comparative examples, or where otherwise explicitly indicated, all numbers in this description and claims indicating amounts of material or conditions of reaction, physical properties of materials and / or use are to be understood as modified by the word "about". Numerical ranges expressed in the format "from x to y" are understood to include x and y. When for a specific feature multiple preferred ranges are described in the format "from x to y", it is understood that all ranges combining the different endpoints are also contemplated.

[0015] The composition of the invention is meant to be used for personal care or for cosmetic use and could also be referred to as a cosmetic composition. By a “personal care composition” as used herein, is meant to include a composition for topical application to sun-exposed areas or heat-exposed areas of the skin and / or hair of humans. Such a composition may be classified as leave-on or rinse off (also known as wash-off), and includes any product applied to a human body for improving appearance, cleansing, odor control or general aesthetics. The composition of the present invention can be in the form of a liquid, a lotion, a cream, foam, a stick or a gel. Non-limiting examples of such leave-on personal care compositions include skin lotions, creams, antiperspirants, deodorants, foundations, mascara, sunscreen lotions; and that of wash-off personal care compositions include face wash, hand I body wash compositions, shampoos, conditioners and shower gels. The composition of the present invention is preferably a leave-on composition.

[0016] "Skin" as used herein is meant to include skin on the face and body (e.g., neck, chest, back, arms, underarms, under-eye, hands, legs and scalp) and especially to the sun-exposed or heat-exposed parts thereof. Compositions of the invention is also of relevance to applications on any other keratinous substrates of the human body other than skin e.g. hair, where products may be formulated with specific aim of improving photoprotection. The terms ‘antioxidant benefit’, ‘protection from reactive oxygen species’ and ‘reducing / scavenging reactive oxygen species’ denote the same meaning and may be used interchangeably.

[0017] Niacinamide Compounds

[0018] A personal care composition of the present invention (the composition) comprises a niacinamide compound. The niacinamide compound is selected from niacinamide (also known as nicotinamide or vitamin B3), picolinamide, iso-nicotinamide, n-cyclopropyl niacinamide, n- cyclobutyl niacinamide, n-cyclopentyl niacinamide and mixtures thereof. More preferably, the niacinamide compound is selected from niacinamide, picolinamide, iso-nicotinamide and mixtures thereof. Even more preferably, the niacinamide compound is selected from niacinamide, picolinamide and mixtures thereof; with niacinamide as the most preferred niacinamide compound.

[0019] A niacinamide compound may also be selected from nicotinic acid esters, non-vasodilating esters of nicotinic acid, nicotinyl amino acids, nicotinyl alcohol esters of carboxylic acids, nicotinic acid N-oxide, niacinamide N-oxide and mixtures thereof.

[0020] The composition comprises from 0.01 to 10 wt%, preferably from 0.05 to 9 wt%, preferably from 0.1 to 8 wt%, preferably 0.5 to 7 wt%, preferably 1 to 6 wt%, preferably 2 to 5 wt%, preferably 3 to 5 wt% of one or more niacinamide compounds described above.

[0021] Gingerols and sources thereof

[0022] The composition comprises gingerols or a source thereof. Preferably, the gingerols are selected from 6-gingerol, 8-gingerol, 10-gingerol, 12-gingerol and combinations thereof.

[0023] Alternatively, but equally preferably, gingerols may be added to the composition using sources thereof. Preferably, plants of Zingiberaceae family are used as sources of gingerols. Preferably, extracts of roots of plants of Zingiberaceae family may be used as a source of gingerols. An example of such plants is Zingiberaceae officinale (commonly known as Ginger). Thus, an extract of roots of ginger may preferably be used as a source of gingerols.

[0024] The composition comprises from 0.001 to 10 wt%, preferably from 0.01 to 9 wt%, preferably from 0.1 to 8 wt%, preferably from 0.5 to 7 wt%, preferably from 1 to 5 wt%, preferably from 2 to 3 wt% of one or more gingerols or a source thereof described above.

[0025] If a source of gingerol is used e.g. an extract of plants of the Zingiberaceae family, then it is preferably added in amounts so that the total amount of gingerols that may be contained the composition is in amounts as described above. A compound of formula 1

[0026] The composition comprises a compound of formula 1 : where, Ri, R2, R3, R4 are each, independently, a linear or branched carbon chain having 2 to 6 carbon atoms; and Rs is a carbon chain having 1 to 6 carbon atoms.

[0027] Examples of a compound of formula 1 includes: a. N,N,N',N'-Tetrakis(2-hydroxyethyl)ethylenediamine, where RI=R2=R3=R4=C2; and Rs=C2 (abbreviated as THEE), b. N,N,N',N'-Tetrakis(2-hydroxypropyl)ethylenediamine, where RI=R2=R3=R4=C3; and Rs=C2 (abbreviated as THPE); and c. N,N,N',N'-Tetrakis(2-hydroxypentyl)ethylenediamine, where RI=R2=R3=R4=C5; and Rs=C2 (abbreviated as THPyE).

[0028] Preferably, a compound of formula 1 is selected from THEE, THPE, THPyE and mixtures thereof. More preferably, a compound of formula 1 is THPE.

[0029] Additional examples a compound of formula 1 include:

[0030] 1 ,T,T',T"-(1 ,3-Propanediyldinitrilo)tetrakis[2-propanol] (Registry number 69666- 46-2),

[0031] 2-Propanol, 1 , 1 ', 1 ", 1 "'-(1 , 5-pentanediy Id i n itri Io) tetrakis- (Registry number 104867- 12-1); and

[0032] 1 , 1 ', 1 " , 1 "'-(1 ,6-Hexanediyldinitrilo)tetrakis[2-propanol] (Registry number 16607- The composition comprises from 0.01 to 10 wt%, preferably from 0.1 to 8 wt%, preferably from 0.25 to 7 wt%, preferably from 0.5 to 6 wt%, more preferably from 1 to 6 wt%, more preferably 1 to 5 wt% and more preferably from 2 to 5 wt% of a compound of formula 1 . It will be understood that in case, the composition comprises one or more compounds of general formula 1 , then the composition comprises such one or more compounds of general formula 1 in amounts described hereinabove.

[0033] It has been found that when the composition contained a niacinamide compound e.g. niacinamide, in combination with a gingerol e.g. 10-gingerol; and a compound of formula 1 e.g. THPE, a synergistic antioxidant benefit was obtained. Preferably, other combinations that may be comprised in the composition include: niacinamide, 6-gingerol and THPE, picolinamide, 10-gingerol and THPE; and niacinamide, 10-gingerol, and THEE.

[0034] It has also been found that a personal care composition comprising said combination, also provides skin brightening effect and anti-aging effect.

[0035] Fatty acids

[0036] Preferably, the composition comprises 3 to 25 wt% fatty acid. The fatty acid is preferably a C10 to C22 fatty acid, more preferably a C16 to C18 fatty acid. Examples of such fatty acid include capric acid, lauric acid, myristic acid, palmitic acid, stearic acid, arachidic acid and behenic acid. More preferably, the fatty acids are selected from stearic acid or palmitic acid or a mixture thereof. The fatty acid is often hystric acid which is substantially (generally about 90 to 95 %) a mixture of stearic acid and palmitic acid. Preferred hystric acid are ones having 40 to 65 wt% C16 and 34 to 58 wt% C18; or ones having 52 to 58 wt% C16 and 40 to 47 wt% C18 fatty acids.

[0037] It is particularly preferred that the composition comprises 4 to 23 %, more preferably 5 to 20 %, even more preferably 6 to 17% fatty acid by weight of the composition.

[0038] Humectants

[0039] Preferably, the composition further comprises humectants. Preferably the humectant is at least one of propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol, sorbitol, hydroxypropyl sorbitol, hexylene glycol, 1 ,3-butylene glycol, isoprene glycol, 1 ,2,6- hexanetriol, glycerol, ethoxylated glycerol, and propoxylated glycerol. Preferred humectants are selected from one or more of glycerol, sorbitol, propylene glycol and 1 ,3-butylene glycol. Glycerol is the most preferred humectant. It is preferred that the amount of humectant is from 0.1 to 10 wt%, preferably 1 to 8 wt%, preferably 2 to 5 wt%.

[0040] Oil-soluble sunscreen

[0041] Preferably, the composition further comprises from 0.1 to 25 wt% of an oil-soluble sunscreen. By ‘oil-soluble’, it is meant those organic sunscreens which have a solubility in water of less than 10 g / l, preferably less than 5 g / l, more preferably less than 2 g / l, at 25°C. Oil-soluble sunscreens could be of the IIV-B type or of the IIV-A type and may be selected from those described below.

[0042] It is preferred that the composition comprises 0.1 to 20 wt%, preferably 1 to 15 wt%, preferably 3 to 12 wt%, preferably 5 to 10 wt% of a UVB oil soluble sunscreen. It is further preferred that the composition of the invention comprises 0.1 to 5 wt%, preferably 1 to 4 wt% of a UVA oil soluble sunscreen.

[0043] When an oil soluble UVB sunscreen is included, it is preferably one or more of octyl salicylate, 3,3,5-trimethylclohexyl 2-hydroxybenzoate, ethylhexyl salicylate, 2-ethylhexyl 2-cyano-3,3- diphenyl-2-propenoate which is also known as octocrylene, 2-ethylhexyl-4-methoxycinnamate or octylmethoxycinnamate, ethylhexyl triazone, 3-benzylidene camphor, cinoxate, diethylhexyl butamido triazone, para amino benzoic acid (PABA), ethyl dihydroxypropyl PABA, ethylhexyl dimethoxy benzylidene dioxoimidazoline propionate, isoamyl p-methoxycinnamate, isopentyl trimethoxycinnamate trisiloxane, isopropyl benzyl salicylate, isopropyl methoxycinnamate, 4- methylbenzylidene camphor, PEG-25 PABA, and pentyl dimethyl PABA. More preferred oilsoluble UVB sunscreens are selected from one or more of octyl salicylate, 3,3,5- trimethylclohexyl 2-hydroxybenzoate, ethylhexyl salicylate, 2-ethylhexyl 2-cyano-3,3- diphenyl-2-propenoate, and 2-ethylhexyl-4-methoxycinnamate and further more preferred are selected from one or more of 2-ethylhexyl-4-methoxycinnamate, ethylhexyl salicylate and 2- ethylhexyl 2-cyano-3,3-diphenyl-2-propenoate. Some of the well known brands under which the above sunscreens are sold are Octisalate®, Homosalate®, Neo Heliopan®, Neo Heliopan® AV, Neo Heliopan® OS, Octocrylene® and Parsol® MCX. The oil-soluble IIV-B sunscreen has Amax from 280 to 320 nm.

[0044] Composition of the invention may comprise an organic oil-soluble UVA sunscreen. When included, it is selected from one or more of a dibenzoylmethane compound, diethylamino hydroxybenzoyl hexyl benzoate and menthyl anthranilate. A dibenzoyl methane compound is most preferred for an oil-soluble UVA-sunscreen. Suitable dibenzoyl methane compounds are selected from one of more of t-butylmethoxy dibenzoylmethane, 2-methyldibenzoylmethane, 4-methyl-dibenzoyl-ethane, 4-isopropyldibenzoyl-methane, 4-tert-butyldibenzoylmethane, 2,4-dimethyldibenzoylmethane, 2,5-dimethyldibenzoylmethane, 4,4'-diisopropyl- dibenzoylmethane, 2-methyl-5-isopropyl-4'-methoxydibenzoylmethane, 2-methyl-5-tert-butyl- 4'-methoxy-dibenzoyl methane, 2,4-dimethyl-4'-methoxy dibenzoylmethane and 2,6-dimethyl- 4-tert-butyl-4'-methoxy-dibenzoylmethane. The most preferred dibenzoyl methane compound is t-butylmethoxy dibenzoylmethane. Commercially available as Parsol 1789.

[0045] The composition may comprise both an organic oil-soluble UVB and an organic oil-soluble UVA sunscreen. Alternately, there are certain oil soluble sunscreens which have both a UVA and UVB screening efficacy. It is selected from one or more bis-ethylhexyloxyphenol methoxyphenyl triazine, drometrizole trisiloxane, benzophenone and its derivatives. The most preferred one is bis-ethylhexyloxyphenol methoxyphenyl triazine, commercially available as Tinosorb S.

[0046] Water-soluble sunscreen

[0047] Preferably, the composition further comprises from 0.1 to 5 wt% of a water-soluble sunscreen. By water soluble sunscreen, whether of the UVA type, or of the UVB type, is meant that the solubility in water of the organic sunscreen is higher than 10 g / l preferably higher than 50 g / l at 25 °C.

[0048] The preferred water-soluble UVB sunscreen for use in the present invention is phenyl benzimidazole sulphonic acid (PBSA), benzophenone-4 or benzylidene camphor sulfonic acid, preferably PBSA. PBSA also known as Ensulizole is commercially available as Eusolex 232 (from Merck KGaA). PBSA is also available under the brand names Neo Heliopan Hydro (from Symrise), Parsol HS (from DSM) and Sunsafe ES (from Uniproma). There are certain water-soluble sunscreens which have both a UVA screening efficacy as well as a UVB screening efficacy. Such sunscreens provide both UVA and UVB protection e.g. benzophenone-4 (sold as Sulisobenzone). However, for the purposes of the present invention benzophenone- 4 may be included as a water-soluble UV-B sunscreen.

[0049] The preferred UVA sunscreen for use in the present invention is one or more of disodium phenyl dibenzimidazole tetrasulfonate (Neoheliopan AP) or terephthalylidene dicamphor sulfonic acid (TDSA). Di sodium phenyl dibenzimidazole tetra sulfonate is also known as bisdisulizole disodium. This is commercially available as Neo heliopan AP (from Symrise Shanghai Ltd) or as Sunsafe DPDT (from Uniproma)

[0050] Terephthalylidene dicamphor sulfonic acid (TDSA) is also known as Ecamsule. This is commercially available as Mexoryl SX (US4585597) by L’ Oreal or Sunsafe TDSA (from Uniproma). It can be used as parent acid or its salts to deliver the desired benefit.

[0051] Preferably, the composition comprises 0.1 to 5 wt%, preferably 1 to 4 wt%, preferably 1.5 to 3, preferably 2 to 3 wt% of a water-soluble UVA sunscreen.

[0052] Non-ionic surfactant

[0053] Preferably, the composition further comprises a non-ionic surfactant having an HLB value in the range of 9 to 20. More preferably, the nonionic surfactant is selected from those having HLB value in the range 12 to 20, further more preferably 12 to 18.

[0054] HLB is calculated using the Griffin method wherein HLB = 20 x Mh / M wherein Mh is the molecular mass of the hydrophilic portion of the molecule and M is the molecular mass of the whole molecule, giving a result on an arbitrary scale of 0 to 20.

[0055] Preferably, the nonionic surfactant having HLB value in the range 9 to 20 is selected from one or more of fatty alcohol ethoxylates, fatty acid ethoxylate, alkyl phenol ethoxylates, and polyoxyethylene sorbitan alkyl esters.

[0056] Examples of fatty alcohol ethoxylates that may be used as nonionic surfactants in the composition include polyoxyethylene lauryl ether (HLB= 16.9; commercially available as Brij® 35), polyoxyethylene (20) cetyl ether (HLB=16; commercially available as Brij® 58), polyethylene glycol octadecyl ether (HLB= 18.8; commercially available as Brij® 700) and Laureth - 9 (C12EO9; HLB=14.3; commercially available as Brij® L9).

[0057] Examples of alkyl phenol ethoxylates that may be used as nonionic surfactant in the composition include octylphenol ethoxylate (HLB=15.5; commercially available as Triton™ X165), octylphenol ethoxylate (HLB=17.6; commercially available as Triton™ X405) and octylphenol ethoxylate (HLB=18.4; commercially available as Triton™ X705).

[0058] Examples of polyoxyethylene sorbitan alkyl esters that may be used as the nonionic surfactant in the composition include polyoxyethylenesorbitan monolaurate (HLB=13.3; commercially available as Tween® 21), polyoxyethylenesorbitan monolaurate (HLB=16.7; commercially available as Tween® 20), Polyoxyethylenesorbitan monopalmitate (HLB=15.6; commercially available as Tween® 40) and polyoxyethylene sorbitan monostearate (HLB= 14.9; commercially available as Tween® 60).

[0059] Fatty acid ethoxylates are available under the Myrj class. Suitable examples of commercially available non-ionic surfactants for use in the composition of this class are Myrj S40 (PEG-40 stearate), Myrj S50 (PEG-50 stearate), or Myrj 59 (PEG-100 stearate).

[0060] Preferably, the composition comprises 0.2 to 5 wt%, more preferably 0.5 to 4 wt%, even more preferably from 1 to 3 wt% nonionic surfactant having HLB in the range 9 to 20.

[0061] A polymer

[0062] Preferably, the composition further comprises 0.25 to 5 wt% of a polymer selected from one or more of (a) dimethicone / vinyldimethicone crosspolymer and b) hydrophobically modified silica. The dimethicone / vinyldimethicone crosspolymer could be with or without silica. Such polymers provided the required sensory properties to the composition.

[0063] Various polymers of the above types could be used in the present invention. Dimethicone / vinyl dimethicone crosspolymer which is a preferred polymer as per the invention is available as KM-9729, DOWSIL™ EP-9215, SeraSnowSP 13, DOWSIL™9506 Powder, SpecsilSPD. An even more preferred polymer as per the invention is Dimethicone / Vinyl Dimethicone Crosspolymer (and) Silica which is available as DOWSIL™9701 Cosmetic Powder. Other suitable polymers which may be used are listed below: Dimethicone / Vinyl Dimethicone Crosspolymer(and) Silica (and) Butylene Glycol available as DOWSIL™ EP-9801 Hydro Cosmetic Powder

[0064] Dimethicone (and) Dimethicone / Vinyl Dimethicone Crosspolymer(and) Dimethicone Crosspolymer(and) Beeswax (and) Silica (and) Silica Silylate available as DOWSIL™9576 Smooth Away Elastomer

[0065] Dimethicone / Vinyl Dimethicone Crosspolymer(and) Polymethylsilsesquioxane(and) Silica Dimethyl Silylate Available as SSP100

[0066] Dimethicone / Vinyl Dimethicone Crosspolymer(and) LauroylLysine available as DOWSIL™ EP-9289 LL

[0067] Hydrophobically modified silica is preferably selected from Silica Silylate available as DOWSIL™ VM-2270 Aerogel Fine Particles, HDK® H2000 and

[0068] Silica dimethyl silylate available as HDK® H15, HDK® H20, HDK® H30, HDK® H18

[0069] Preferably, the polymer is included in 0.25 to 5%, preferably 0.5 to 4%, more preferably 1 to 3% by weight of the composition.

[0070] The composition may optionally include polymers as spherical microporous particles. Preferred particles of this type are of the acrylate crosspolymer type. One especially preferred particle is available as Ganzpearl 820 GMP. It is included in the composition to get a smooth creamy feel and to achieve high oil absorbency. Other polymeric particles which may be included are styrene / acrylates copolymer which are available under the brand name of SunSpheres™ Powder, SunSpheres™ PGL and SunSpheres™ LOG from Dow.

[0071] Other Polymers

[0072] Preferably, the composition further comprises a polymer other than those described above. The polymer acts as thickener in the composition and improves sensorial properties of the composition. The polymer is preferably selected from the following classes: • acrylate I R-methacrylate copolymer e.g. acrylates / steareth-20 methacrylate copolymer (commercially available as AculynTM 22) and acrylates / beheneth-25 methacrylate copolymer (commercially available as AculynTM 28),

[0073] • acrylate I R-methacrylate crosspolymer e.g. acrylates / steareth-20 methacrylate crosspolymer (commercially available as AculynTM 88),

[0074] • acrylates copolymer (commercially available as AculynTM 33),

[0075] • acrylate / R-alkyl acrylate crosspolymer e.g. acrylates / C10-C30 alkyl acrylate crosspolymer (commercially available as PemulenTM TR-2),

[0076] • copolymer of ammonium acryloyldimethyltaurate with vinyl pyrrolidone (commercially available as Aristoflex® AVC),

[0077] • copolymer of sodium acryloyldimethyltaurate with vinyl pyrrolidone (commercially available as Aristoflex® A VS); and

[0078] • crosspolymer of acryloyldimethyltaurate with R-alkyl acrylate and methyacrylate e.g. Ammonium acryloyldimethyltaurate / beheneth-25 methacrylate crosspolymer (commercially available as Aristoflex® HMB and Aristoflex® BLV); and mixtures thereof.

[0079] Alternatively, the composition may comprise cellulose-based thickeners such as hydroxyethyl cellulose, hydroxypropyl methyl cellulose and mixtures thereof. More preferably, the polymer is selected from acrylate I R-methacrylate copolymer, acrylates copolymer and mixtures thereof. Preferably, the composition comprises 0.1 to 5 wt%, more preferably 0.5 to 4.5 wt%, even more preferably 1 to 4 wt%, further more preferably from 1.5 to 3.5 wt%, still more preferably from 2 to 3 wt% of these polymers.

[0080] Water

[0081] Water is preferably included in 35 to 90 %, more preferably 50 to 85 %, further more preferably 50 to 80 % by weight of the composition.

[0082] Preferably, the composition further comprises an emollient. These may be in the form of silicone oils, ester emollients, and hydrocarbons. Amounts of the emollients may range anywhere from 0.1 to 25 %, preferably between 1 and 10 % by weight of the composition. Silicone oils may be divided into the volatile and nonvolatile variety. The term "volatile" as used herein refers to those materials which have a measurable vapor pressure at ambient temperature. Volatile silicone oils are preferably chosen from cyclic (cyclomethicone) or linear polydimethylsiloxanes containing from 3 to 9, preferably from 5 to 6, silicon atoms.

[0083] Nonvolatile silicone oils useful as an emollient material include polyalkyl siloxanes, polyalkylaryl siloxanes and polyether siloxane copolymers. The essentially nonvolatile polyalkyl siloxanes useful herein include, for example, polydimethyl siloxanes with viscosities of from 5 x 10"6to 0.1 m2 / s at 25 °C. Among the preferred nonvolatile emollients useful in the present compositions are the polydimethyl siloxanes having viscosities from 1 x 105to 4 x 104m2 / s at 25 °C.

[0084] Another class is of ester emollients, which are alkyl esters of saturated fatty acids having 10 to 24 carbon atoms. Examples thereof include behenyl neopentanoate, isononyl isonanonoate, isopropyl myristate and octyl stearate. Alternatively, they are ether-esters such as fatty acid esters of ethoxylated saturated fatty alcohols. Further alternatively they are polyhydric alcohol esters such as ethylene glycol mono and di-fatty acid esters, diethylene glycol mono- and di-fatty acid esters, polyethylene glycol (200-6000) mono- and di- fatty acid esters, propylene glycol mono- and di-fatty acid esters, polypropylene glycol 2000 monostearate, ethoxylated propylene glycol monostearate, glyceryl mono- and di-fatty acid esters, polyglycerol poly-fatty esters, ethoxylated glyceryl mono-stearate, 1 ,3-butylene glycol monostearate, 1 ,3-butylene glycol distearate, polyoxyethylene polyol fatty acid ester, sorbitan fatty acid esters, and polyoxyethylene sorbitan fatty acid esters are satisfactory polyhydric alcohol esters. Particularly useful are pentaerythritol, trimethylolpropane and neopentyl glycol esters of C1-C30 alcohols. Alternatively, there are wax esters such as beeswax, spermaceti wax and tribehenin wax. Yet further alternatively they are sugar esters of fatty acids such as sucrose polybehenate and sucrose polycottonseedate. Further alternatively there are ester emollients principally based upon mono-, di- and tri- glycerides. Representative glycerides include sunflower seed oil, cottonseed oil, borage oil, borage seed oil, primrose oil, castor and hydrogenated castor oils, rice bran oil, soybean oil, olive oil, safflower oil, shea butter, jojoba oil and combinations thereof. Amounts of such esters may range from 0.1 to 20 % by weight of the compositions. Another example of emollients includes lanolin oil and lanolin derivatives. Hydrocarbons, which are suitable cosmetically acceptable carriers include petrolatum, mineral oil, C8-Ci8 isoparaffins, polybutenes and especially isohexadecane, available commercially as Permethyl® 101 A from Presperse Inc.

[0085] Fatty alcohols having from 10 to 30 carbon atoms are another useful category of cosmetically acceptable carrier. Illustrative of this category are stearyl alcohol, lauryl alcohol, myristyl alcohol, oleyl alcohol and cetyl alcohol and mixtures thereof. Thickeners can be utilized as part of the cosmetically acceptable carrier of compositions according to the present invention. Typical thickeners include crosslinked acrylates (e.g. Carbopol® 982 and Carbopol® llltrez 10), hydrophobically-modified acrylates (e.g. Carbopol 1382(R)), polyacrylamides (e.g. Sepigel® 305), acryloylmethylpropane sulfonic acid / salt polymers and copolymers (e.g. Aristoflex® HMB and AVC), cellulosic derivatives and natural gums. Among useful cellulosic derivatives are sodium carboxymethylcellulose, hydroxypropyl methocellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, ethyl cellulose and hydroxymethyl cellulose. Natural gums suitable for the present invention include guar, xanthan, sclerotium, carrageenan, pectin and combinations of these gums. Inorganics may also be utilized as thickeners, particularly clays such as bentonites and hectorites, fumed silicas, talc, calcium carbonate and silicates such as magnesium aluminum silicate (Veegum®). Amounts of the thickener may range from 0.0001 to 10 %, usually from 0.001 to 2.5 %, optimally from 0.01 to 1 % by weight of the composition. Preferred are emollients that can be used, especially for products intended to be applied to the face, to improve sensory properties and are chosen from the group of oils that do not form stiff gels with 12HSA; these include polypropylene glycol-14 butyl ether otherwise known as Tegosoft® PBE, or PPG 15 stearyl ether such as Tegosoft® E, other oils such as esters, specifically, isopropyl myristate, isopropyl palmitate, other oils could include castor oils and derivatives thereof.

[0086] Preferably, the composition further comprises a skin brightening compound. Illustrative substances are lactic acid, vitamin C or derivatives thereof, arbutin, kojic acid, ferulic acid, hydroquinone, resorcinol and derivatives including 4-substituted resorcinols e.g. 4-ethyl resorcinol, 4-hexyl resorcinol and combinations thereof. More preferably, such skin brightening compound is a tyrosinase inhibitor, to complement the melanogenesis inhibition activity of the substituted monoamines, most preferably a compound selected from the group consisting of kojic acid, hydroquinone and said 4-substituted resorcinol. Also, dicarboxylic acids represented by the formula HOOC-(CxHy)-COOH where x=4 to 20 and y=6 to 40 such as azelaic acid, sebacic acid, oxalic acid, succinic acid, fumaric acid, octadecenedioic acid or their salts or a mixture thereof, most preferably fumaric acid or salt thereof, especially disodium salt.

[0087] Amounts of these skin brightening compounds may range from 0.1 to 10 wt%, preferably from 0.5 to 8 wt%, preferably from 1 to 7 wt%, preferably from 2 to 6 wt%, preferably from 3 to 5 wt% in the composition.

[0088] Another preferred ingredient of the inventive compositions is a retinoid. As used herein, "retinoid" includes all natural and / or synthetic analogs of Vitamin A or retinol-like compounds which possess the biological activity of Vitamin A in the skin as well as the geometric isomers and stereoisomers of these compounds. The retinoid is preferably retinol, retinol esters (e.g., C2 -C22 alkyl esters of retinol, including retinyl palmitate, retinyl acetate, retinyl propionate), retinal, and / or retinoic acid (including all-trans retinoic acid and / or 13-cis-retinoic acid), more preferably retinoids other than retinoic acid. These compounds are well known in the art and are commercially available from a number of sources, e.g., Sigma Chemical Company (St. Louis, Mo.), and Boerhinger Mannheim (Indianapolis, Ind.). Preferred retinoids are retinol, retinyl palmitate, retinyl acetate, retinyl propionate, retinal and combinations thereof. The retinoid is preferably substantially pure, more preferably essentially pure.

[0089] Colorants, opacifiers and abrasives may also be included in compositions of the present invention. Each of these substances may range from 0.05 to 5 %, preferably between 0.1 and 3 % by weight of the composition.

[0090] Preservatives could be incorporated into the compositions of this invention to protect against the growth of potentially harmful microorganisms. Suitable traditional preservatives for compositions of this invention are alkyl esters of para-hydroxybenzoic acid. Other preservatives which have come into use include hydantoin derivatives, propionate salts, and a variety of quaternary ammonium compounds. Cosmetic chemists are familiar with appropriate preservatives and routinely choose them to satisfy the preservative challenge test and to provide product stability. Particularly preferred preservatives are iodopropynyl butyl carbamate, phenoxyethanol, caprylyl glycol, C1-6 parabens (especially, methyl paraben and / or propyl paraben), imidazolidinyl urea, sodium dehydroacetate and benzyl alcohol. The preservatives should be selected having regard for the use of the composition and possible incompatibilities between the preservatives and other ingredients in the emulsion.

[0091] Preservatives are preferably employed in amounts ranging from 0.01 % to 2 % by weight of the composition, including all ranges subsumed therein. An especially preferred combination is octocrylene and caprylyl glycol, since caprylyl glycol has been disclosed to enhance UVA and UVB protection. The compositions of the present invention can comprise a wide range of other optional components. The CTFA Cosmetic Ingredient Handbook, Second Edition, 1992, which is incorporated by reference herein in its entirety, describes a wide variety of non-limiting cosmetic and pharmaceutical ingredients commonly used in the skin care industry, which are suitable for use in the compositions of the present invention. Examples include antioxidants, binders, biological additives, buffering agents, colorants, astringents, fragrance, opacifying agents, conditioners, exfoliating agents, pH adjusters, essential oils, skin sensates, skin soothing agents and skin healing agents.

[0092] Further, in a second aspect, the present invention relates to a method of protecting the skin through providing antioxidant benefit comprising the steps: a. applying the composition of the first aspect; and b. optionally, rinsing the skin with water.

[0093] Alternatively, in this second aspect, the invention relates to the composition of the first aspect wherein the skin is protected from reactive oxygen species by: a. applying the composition of the first aspect; and b. optionally, rinsing the skin with water.

[0094] Preferably, the method is non-therapeutic or cosmetic in nature.

[0095] The method further comprises an optional step, step b., where the skin is rinsed with water. If carried out, because of step b., the composition so applied in the preceding step a., is removed as the skin is rinsed with water. If carried out, the step b., may be carried out within 30 minutes, preferably within 25 minutes, preferably within 20 minutes, preferably within 15 minutes, preferably within 10 minutes, preferably within 5 minutes, preferably within 1 minute from carrying out the step a. Such step b., is carried out if the composition is formulated as a wash- off composition. Preferably, the method is non-therapeutic or cosmetic in nature.

[0096] In use, a small quantity of the composition, for example from 1 to 5 ml, is applied to exposed area of the skin, from a suitable container or applicator and, if necessary, it is then spread over and / or rubbed into the skin using the hand or fingers or a suitable device.

[0097] Further, in a third aspect, the present invention relates to use of the composition of the first aspect for providing antioxidant benefit. Preferably, the use is non-therapeutic or cosmetic in nature. Alternatively, in this third aspect, the present invention relates to the composition of the first aspect for use in protecting the skin through providing antioxidant benefit.

[0098] While the above summarizes the present invention, it will become apparent to those skilled in the art that modifications, variations and alterations may be made without deviating from the scope and spirit of the present invention as described and claimed herein. The invention will now be further illustrated in the following non-limiting examples.

[0099] Examples

[0100] 1,1-Diphenyl-2-picrylhydrazyl (DPPH; Sigma Aldrich cat. no.: D9132), Vitamin B3 I Niacinamide (Sigma Aldrich cat. no.: N0636), Picolinamide (Sigma Aldrich cat. no.: 104051), THPE (Neutrol®TE- BASF), THEE (Sigma Aldrich cat. no.: 87600), 6-gingerol (Sigma Aldrich cat. no.: G1046), 10-gingerol (Sigma Aldrich cat. no.: G5798) and Ginger extract (Code: 4334000G- Lot no: 24273401 from Provital, source of ginger: Sri Lanka / China) were used in the experiments.

[0101] Cell culture: HaCaT Keratinocytes were used in the experiments.

[0102] Actives preparation:

[0103] DPPH (1 mM) was prepared in 100 % ethanol by vortexing and covered with aluminum foil to avoid light exposure. Niacinamide 3% and THPE 1% stock was made in distilled water and subsequent dilutions were made in 100% ethanol. Ginger extract 10 % was made in 100% ethanol.

[0104] ROS scavenging obtained by control and the inventive composition were assayed using the DPPH assay. The DPPH assay was carried out in 96 well plate with 200 pl of total rection volume. Required concentration of actives were added in to 96 well plate and volume was made up to 180 pl with 100 % ethanol. The reaction was initiated by adding 20 pl of 1 mM DPPH to get the final concentration of 0.1 mM DPPH in the reaction mix. The reaction was incubated at room temperature in dark condition for 30 min and read @ 517 nm which is expressed in terms of percentage DPPH scavenged. A higher percentage indicates greater antioxidant benefit.

[0105] Vitamin B3 + Ginger extract + THPE showed synergistic benefit in scavenging free radical DPPH as shown in table 1 below: Table 1 :

[0106] Further, Vitamin B3 + 10-gingerol + THPE showed synergistic benefit in scavenging free radical DPPH as shown in table 2 below: Table 2:

[0107] Further, Vitamin B3 + 6-gingerol + THPE showed synergistic benefit in scavenging free radical

[0108] DPPH as shown in table 3 below: Table 3: Further, picolinamide + 10-gingerol + THPE showed synergistic benefit in scavenging free radical DPPH as shown in table 4 below: Table 4:

[0109] Further, Vitamin B3 + 10-gingerol + THEE showed synergistic benefit in scavenging free radical DPPH as shown in table 5 below: Table 5:

[0110] It is to be understood that the experiments described above were conducted in an in-vitro assay to evaluate the technical effect. It is expected that the concentrations to be actually used to prepare a composition for topical use would be vastly different. The concentrations could be orders of magnitude higher due to the following reasons that affect the difference in concentration in the bulk as compared to that at the cellular level. The composition may be formulated as an emulsion or a gel with very many additional ingredients. The concentration of the desired actives in the oil phase and in the water phase, is expected to be very different. They may also have very different physical and hydrodynamic properties like partition coefficients, diffusional rates, convective transport rates, rheological properties etc. Therefore, it is expected that the concentrations to be used when formulated as a composition would be very different from that at the cellular level.

Claims

Claims1. A personal care composition comprising: a. from 0.01 to 10 wt% a vitamin B3 compound, b. from 0.001 to 10 wt% a gingerol or a source thereof; and c. from 0.01 to 10 wt% a compound of formula 1:where, R1 , R2, R3, R4 are each, independently, a linear or branched carbon chain having 2 to 6 carbon atoms; and R5 is a carbon chain having 1 to 6 carbon atoms; and wherein the vitamin B3 compound is selected from niacinamide, picolinamide, isonicotinamide, n-cyclopropyl niacinamide, n-cyclo-butyl niacinamide, n-cyclo-pentyl niacinamide and mixtures thereof.

2. The composition as claimed in claim 1 wherein the vitamin B3 compound is selected from niacinamide, picolinamide, iso-nicotinamide and mixtures thereof.

3. The composition as claimed in claims 1 or 2 wherein the vitamin B3 compound is niacinamide.

4. The composition as claimed in any one of claims 1 to 3 wherein the gingerol is selected from 6-gingerol, 8-gingerol,10-gingerol, 12-gingerol and mixtures thereof.

5. The composition as claimed in any one of claims 1 to 4 wherein the gingerols are sourced from a plant of the Zingiberaceae family.

6. The composition as claimed in any one of claims 1 to 5 wherein the compound of formula 1 is selected from:a. N,N,N',N'-Tetrakis(2-hydroxyethyl)ethylenediamine, where R1=R2=R3=R4=C2; and R5=C2, b. N,N,N',N'-Tetrakis(2-hydroxypropyl)ethylenediamine, where R1=R2=R3=R4=C3; and R5=C2; and c. N,N,N',N'-Tetrakis(2-hydroxypentyl)ethylenediamine, where R1=R2=R3=R4=C5; and R5=C2; and mixtures thereof.

7. The composition according to any one of claims 1 to 6 wherein the compound of general formula 1 is N,N,N',N'-Tetrakis(2-hydroxypropyl)ethylenediamine, where R1=R2=R3=R4=C3; and R5=C2.

8. The composition as claimed in any one of claims 1 to 7 wherein the composition further comprises a C10-C22 fatty acid.

9. The composition as claimed in any one of claims 1 to 8 wherein the composition further comprises a humectant preferably selected from one or more of a propylene glycol, dipropylene glycol, polypropylene glycol, polyethylene glycol, sorbitol, hydroxypropyl sorbitol, hexylene glycol, 1,3-butylene glycol, isoprene glycol, 1,2,6-hexanetriol, glycerol, ethoxylated glycerol and propoxylated glycerol.

10. The composition as claimed in any one of claims 1 to 9 wherein the composition further comprises an oil-soluble organic sunscreen.

11. The composition as claimed in claim any one of claims 1 to 10 wherein composition further comprises a water-soluble organic sunscreen.

12. The composition as claimed in any one of claims 1 to 11 wherein the non-ionic surfactant has an HLB value in the range of 9 to 20.

13. The composition as claimed in any one of clams 1 to 12 wherein the composition is in the form of a leave-on composition or a wash-off composition.

14. A method of protecting the skin through providing antioxidant benefit comprising the steps:a. applying the composition as claimed in any one of claims 1 to 13; and b. optionally, rinsing the skin with water.

15. Use of the composition as claimed in any one of claims 1 to 13 for providing antioxidant benefit.

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