Topical antiseptic composition containing a minimal amount of antimicrobial lipids

Abstract

The present invention relates to a topical disinfecting composition comprising: a) a polyhydroxy compound selected from sugars, polyols or combinations thereof; b) an antimicrobial lipid; and c) tetrahydroxypropyl ethylene diamine (THPE), wherein the antimicrobial lipid and THPE are present in a weight ratio of from 1:10,000 to 1:10. The present invention further relates to a method for disinfecting a surface by applying the above topical composition to the surface, and to the use of the composition for disinfecting the skin, hair or oral cavity. The present invention also relates to the use of a polyhydroxy compound selected from sugars, polyols or combinations thereof as an antimicrobial activity promoter.

Description

Technical Field

[0001] The present invention relates to a disinfectant composition for topical use. Background Art

[0002] People try to take good care of their own skin and the skin of their pets. Specific skin-related problems that people are concerned about include: good skin health without infection, good skin color, and sufficient moisturization.

[0003] Similarly, people want their oral cavities (including gums and teeth) to be free of problems such as tooth decay, tartar, gingivitis, dental caries, abnormal breath (also known as "halitosis"), and dental plaque.

[0004] People are also concerned about hair and scalp care. They generally prefer to have thick long hair with minimal hair loss. Dandruff is a common scalp problem involving fungal microorganisms.

[0005] Good health of the skin, oral cavity, and scalp is generally achieved by keeping them free from infection. One way to combat infection is to use an antimicrobial agent to treat it after the infection has occurred. Another approach is to retain a minimal amount of an antimicrobial composition on the surface (such as the skin of the hands) so that any invading microorganisms (such as bacteria) are killed or inactivated, thereby minimizing the spread of disease. The present inventors, with their extensive knowledge in the fields of skin-friendly active substances and antimicrobial activity, have proposed a unique combination of polyhydroxy compounds, antimicrobial lipids, and tetrahydroxypropyl ethylenediamine to provide synergistic antimicrobial activity.

[0006] Various topical antimicrobial compositions are disclosed in the art.

[0007] US3,050,467 (Horowitz et al., 1962) discloses an antimicrobial cleansing composition consisting essentially of a mixture of a water-soluble soap and a silver salt of partially depolymerized alginic acid. This composition provides synergistic antimicrobial activity.

[0008] US2008 / 014247 (Lu et al., 2008) discloses a composition having a metal-containing material, stearic acid, and a pharmaceutically acceptable carrier, which is used for treating conditions caused by Gram-positive, Gram-negative, fungal pathogens, and / or antibiotic-resistant bacteria. It further provides a method for inhibiting the proliferation of biofilms. The metal-containing material can be silver.

[0009] The use of tetrahydroxypropyl ethylenediamine is also known in the art.

[0010] US2009 / 0227683 (Liebel et al., 2009) discloses compositions for providing an analgesic effect to the skin. The examples describe compositions containing tetra-hydroxypropyl ethylenediamine, glycerol, D-panthenol, methylparaben (Nipagin M), and propylparaben (Nipasol M).

[0011] US2016 / 0324754 (Cure et al., 2016) discloses a shaving cream composition comprising: water, carbomer, ethylhexyl palmitate, glycerol, glycerol acrylate / acrylic acid, isododecane, stearic acid, butylene glycol, ethanol, cetearyl alcohol, cetearyl alcohol polyether-20, propylene glycol, Brassica Campestris, phenoxyethanol, ethylhexylglycerol, tetra-hydroxypropyl ethylenediamine, Aloe Barbadensis, carboxymethyl hydroxyethyl cellulose, bisabolol, PEG-45M, and tocopheryl acetate.

[0012] Glycerol and panthenol are polyhydroxy compounds used as humectants in topical compositions.

[0013] WO20126347 (Unilever) relates to an antimicrobial composition having odor and oral biofilm inhibition benefits and provides an antimicrobial composition comprising a. 0.1 to 10% by weight of tetra-hydroxypropyl ethylenediamine (THPE) and b. 0.001 to 10% by weight of at least one compound selected from bisphenols.

[0014] WO18166758 (Unilever) relates to an antimicrobial composition, particularly an antimicrobial composition providing a synergistic anti-dandruff or anti-acne efficacy. This is achieved by an appropriate combination of selected essential oil actives (selected from thymol or terpineol) with certain antimicrobial lipids (selected from sapienic acid, palmitoleic acid, sphingosine, dihydrosphingosine, phytosphingosine, and 6-hydroxysphingosine). These compositions can be provided by many different types of personal care products (e.g., shampoos, conditioners; face or hand washing products; or leave-on creams / lotions).

[0015] Despite efforts made so far, there has been a search for new technologies (e.g., actives or combinations of actives) that provide improved antimicrobial benefits. Additionally, it is preferred to use the minimum amount of known antimicrobial actives.

[0016] Therefore, antimicrobial compositions and actives that provide antimicrobial benefits remain an interesting subject. Summary of the Invention

[0017] The present inventors have developed a topical composition that provides very effective antimicrobial efficacy by combining (i) a polyhydroxy compound selected from sugars, polyols, or combinations thereof, (ii) an antimicrobial lipid, and (iii) tetrahydroxypropyl ethylenediamine, wherein the antimicrobial lipid and THPE are present in a weight ratio of from 1:10,000 to 1:10.

[0018] The topical composition of the present invention is applicable to a method for disinfecting a surface, the method comprising applying the topical composition to the surface.

[0019] The present invention also relates to the use of the topical composition for disinfecting the skin, hair, or oral cavity.

[0020] The present invention also relates to the use of a polyhydroxy compound selected from sugars, polyols, or combinations thereof as an antimicrobial activity promoter in a composition comprising a combination of an antimicrobial lipid and tetrahydroxypropyl ethylenediamine (THPE). Detailed Description

[0021] These and other aspects, features, and advantages will become apparent to those skilled in the art by reading the following detailed description and the appended claims. For the avoidance of doubt, any feature of one aspect of the invention can be used 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 should be noted that the examples given in the following description are intended to illustrate the invention and are not intended to limit the invention to these examples themselves. Similarly, unless otherwise indicated, all percentages are weight / weight percentages and may be abbreviated as "wt%". Except in operating and comparative examples, or where otherwise explicitly indicated, all numbers expressing amounts of materials or reaction conditions, physical properties of materials, and / or uses in this specification are to be understood as being modified by the word "about". Numerical ranges expressed in the format "x to y" should be understood to include x and y. When multiple preferred ranges for a particular feature are described in the format "x to y", it should be understood that all ranges combining different endpoints are also contemplated.

[0022] For the purposes of the present invention, the terms "disinfect" and "antimicrobial" are used interchangeably and have the same meaning.

[0023] Thus, a first aspect of the present invention relates to a topical composition comprising:

[0024] a) a polyhydroxy compound selected from sugars, polyols, or combinations thereof;

[0025] b) an antimicrobial lipid; and

[0026] c) tetra-hydroxypropyl ethylene diamine (THPE), wherein the antimicrobial lipid and THPE are present in a weight ratio of from 1:10,000 to 1:10.

[0027] The polyhydroxy compound according to the present invention refers to a compound containing two or more hydroxy groups. The polyhydroxy compounds useful in the present invention may be selected from sugars or polyols.

[0028] Preferred sugars may be monosaccharides, disaccharides or polysaccharides. Preferred monosaccharides for use in the present invention are one or more of glucose, fructose, galactose, mannose or ribose; more preferably glucose, fructose or galactose. Preferred disaccharides for use in the present invention are selected from one or more of sucrose, lactose, lactulose, maltose, turanose or trehalose; more preferably sucrose, lactose, lactulose or trehalose. The polysaccharide according to the present invention refers to a compound having more than two sugar units and thus also includes oligosaccharides. Preferred polysaccharides for use in the present invention are selected from one or more of fructooligosaccharide, glucooligosaccharide or saccharide isomerate; more preferably saccharide isomerate. Saccharide isomerate may be commercially obtained under the trade name (from DSM), under the trade name "Waterin" (from Clariant), under the trade names "EPS3 Powder", "EPS4 Powder", "EPS5 Powder" and "EPS15 Powder" (all from Codif) and under the trade name "Hyanify" (from Lipotec S.A.).

[0029] The most preferred sugar for use in the compositions of the present invention is selected from one or more of fructose, sucrose, trehalose or saccharide isomerate.

[0030] The polyol according to the present invention is a compound containing more than one alcohol group. Preferred polyols according to the present invention are glycerol or panthenol.

[0031] Panthenol (2,4-dihydroxy-N-(3-hydroxypropyl)-3,3-dimethylbutyramide) is an alcohol analogue of pantothenic acid (vitamin B5).

[0032] The term "antimicrobial lipid" as used herein refers to fatty acids, glycerol monoesters, sphingolipids and ceramides containing a straight-chain C 10-24 saturated or unsaturated aliphatic chain, which aliphatic chain may be substituted with one or more hydroxy groups.

[0033] The term "sphingolipid" as used herein refers to an aliphatic amine which contains two or three hydroxy groups and which usually has a unique trans double bond in the 4-position.

[0034] As used herein, the term "ceramide" refers to a fatty acid ester of a sphingolipid in which the amino group of a sphingoid base is N-acylated with a fatty acid moiety.

[0035] Examples of sphingolipids that can be used as antimicrobial lipids according to the present invention include sphingosine, dihydrosphingosine, phytosphingosine, 6-hydroxysphingosine. Most preferably, the sphingosine used is phytosphingosine.

[0036] Examples of antimicrobial fatty acids that can be used according to the present invention include lauric acid, myristic acid, palmitic acid, stearic acid, arachidic acid, myristoleic acid (9-cis-tetradecenoic acid), palmitoleic acid (9-cis-hexadecenoic acid), hexadecenoic acid (cis-6-hexadecenoic acid), oleic acid and vaccenic acid (cis-11-octadecenoic acid). Preferred antimicrobial fatty acids are monounsaturated fatty acids. Most preferably, the antimicrobial fatty acid is selected from palmitoleic acid, hexadecenoic acid and combinations thereof.

[0037] Examples of antimicrobial monoglycerides that can be used according to the present invention include monoglycerides containing fatty acid residues selected from lauric acid, myristic acid, palmitic acid, stearic acid, arachidic acid, myristoleic acid, palmitoleic acid, hexadecenoic acid, oleic acid and vaccenic acid. Preferred antimicrobial monoglycerides are monopalmitolein, monoglyceryl hexadecenoate and combinations thereof.

[0038] Preferably, the antimicrobial lipid used according to the present invention is selected from fatty acids, sphingolipids and combinations thereof.

[0039] According to a particularly preferred embodiment, the antimicrobial lipid used according to the present invention is preferably selected from hexadecenoic acid, sphingosine, dihydrosphingosine, phytosphingosine, 6-hydroxysphingosine, palmitoleic acid and combinations thereof. Most preferably, the antimicrobial lipid is phytosphingosine.

[0040] The antimicrobial lipid is preferably included in the topical composition at a concentration of from 0.0001 to 5% by weight, more preferably from 0.0005 to 1% by weight, and most preferably from 0.001 to 0.1% by weight.

[0041] The polyhydroxy compound is preferably present in the topical composition at a concentration of from 0.01 to 25% by weight, more preferably from 0.1 to 10% by weight, and most preferably from 0.3 to 3% by weight.

[0042] THPE is preferably present in the topical composition at a concentration of from 0.01 to 10% by weight, more preferably from 0.05 to 5% by weight, and most preferably from 0.1 to 2% by weight.

[0043] The polyhydroxy compound and THPE are preferably present in the topical composition in a weight ratio in the range of 1:20 to 20:1, more preferably in the range of 1:10 - 10:1, and most preferably in the range of 1:5 - 5:1.

[0044] Preferably, the antimicrobial lipid and THPE are present in a weight ratio in the range of 1:10000 to 1:10, more preferably in the range of 1:5000 to 1:20, even more preferably in the range of 1:5000 to 1:50, further more preferably in the range of 1:2500 to 1:75, and most preferably in the range of 1:1000 to 1:100.

[0045] Preferred combinations of a) a polyhydroxy compound selected from sugars, polyols or combinations thereof; b) an antimicrobial lipid; and c) tetra-hydroxypropyl ethylenediamine (THPE) are as follows:

[0046] - glycerol + phytosphingosine + THPE,

[0047] - panthenol + phytosphingosine + THPE,

[0048] - glycerol + panthenol + phytosphingosine + THPE,

[0049] - glycerol + lauric acid + THPE,

[0050] - fructose + lauric acid + THPE,

[0051] - fructose + phytosphingosine + THPE,

[0052] - sucrose + phytosphingosine + THPE,

[0053] - sucrose + lauric acid + THPE,

[0054] - fructooligosaccharide (FOS) + lauric acid + THPE,

[0055] - FOS + phytosphingosine + THPE.

[0056] In addition to the polyhydroxy compound, the antimicrobial lipid and THPE, the topical composition may contain other cosmetically acceptable ingredients such as solvents, thickeners, gelling agents, emollients, UV absorbers, humectants, penetration enhancers, essential oils, preservatives, antioxidants, surfactants, vitamins, pigments and fragrances.

[0057] According to a preferred embodiment, the topical composition is water-based. Preferably, the topical composition contains 0.1 to 99.9% by weight of water, more preferably 1 to 99% by weight of water, and most preferably 5 to 95% by weight of water.

[0058] The topical composition of the present invention is preferably a lotion, cream, deodorant, hand sanitizer or body spray.

[0059] The composition can be delivered to the topical surface of the body as a leave-on product or a rinse-off product. A leave-on product is a product that is applied to the topical surface of the body and remains thereon to provide its desired function until it is typically substantially removed by washing and / or rinsing during the next personal cleansing event, such as a shower or bath. A rinse-off product is a personal cleansing product that contains a sufficient amount of surfactant and is designed to assist in cleaning the body with a large amount of water. After application of such a product to the skin, it is usually accompanied by a large amount of foam, and the topical surface can be rinsed with a sufficient amount of water to make it substantially free of the product.

[0060] The composition according to the present invention is preferably a leave-on product.

[0061] The composition of the present invention can be used in rinse-off products for cleaning the oral cavity, skin or hair, such as those formulated as toothpaste, tooth powder, mouthwash, shampoo, conditioner, soap bar, body or facial wash in the form of a gel, emulsion or liquid. Preferably, the composition is formulated as a leave-on product for skin care or a deodorant product for axillary application. Preferably, the composition of the present invention comprises a cosmetically acceptable matrix. The cosmetically acceptable matrix for providing a skin care product or a deodorant product may have the following optional components.

[0062] Skin care

[0063] The composition of the present invention can be used for skin care. Skin care means applying the composition to the skin and leaving it on the skin until one typically takes a shower or bath several hours or about a day later. The cosmetically acceptable matrix is usually present in an amount in the range of 10 to 99.9% by weight of the composition, more preferably in the range of 40 to 85% by weight. Particularly preferably, the cosmetically acceptable matrix includes water. Water is preferably included in an amount of 30 to 90% by weight, more preferably 30 to 85% by weight, and most preferably 30 to 80% by weight. In addition to water, suitable carrier types include silicones, polyols, hydrocarbons, triglycerides and thickening powders.

[0064] The skin care composition of the present invention can be in any form suitable for topical application to the skin, including toner, lotion, cream, mousse, scrub, serum or gel. Preferably, the composition is a skin lotion or cream.

[0065] The composition may comprise an emollient oil used as a co-solvent. Suitable emollient oils include, for example, esters of alkoxylated aromatic alcohols and fatty carboxylic acids, esters of polyglycols or diols and fatty carboxylic acids (such as triglyceride caprylate / caprate), esters of fatty alcohols and fatty acids, alkoxylated derivatives of benzyl alcohol, and mixtures thereof. Preferably, the emollient oil is triglyceride caprylate / caprate.

[0066] Typically, such compositions comprise a co-solvent in an amount of 0.01 to 10%, more preferably 0.1 to 8%, most preferably 1 to 6% based on the total weight of the sunscreen composition, and include all ranges therebetween.

[0067] The composition may additionally comprise a sunscreen agent, such as an inorganic sunscreen agent or an organic sunscreen agent. Examples of organic sunscreen agents are zinc oxide, titanium dioxide, iron oxide, silica (such as fumed silica). The composition of the present invention may comprise a UV-A sunscreen agent selected from dibenzoylmethane derivatives, triazine derivatives, benzophenone derivatives, and mixtures thereof. The composition of the present invention may also comprise a UV-B sunscreen agent. Suitable UV-B sunscreen agents of the present invention are selected from benzophenone, anthranilate, salicylate, cinnamate, camphor, benzylidenemalonate, triazolone, and derivatives thereof.

[0068] Skin lightening agents may also be incorporated into the composition of the present invention.

[0069] The skin care product further includes a disinfectant that ensures almost immediate killing of microorganisms present on the skin. The disinfectant preferably comprises 20 to 90% by weight, preferably 30 to 80% by weight of a C2 to C4 monohydric alcohol, wherein the monohydric alcohol is selected from ethanol, isopropanol, or a combination thereof. The disinfectant composition may comprise a combination of ethanol and isopropanol. Even more preferably, the composition comprises 40 to 75% by weight, still more preferably 55 to 70% by weight and most preferably 60 to 70% by weight of a C2 to C4 monohydric alcohol.

[0070] Preferably, the disinfectant composition may contain 30 to 80% by weight, more preferably 40 to 70% by weight, even more preferably 50 to 68% by weight, most preferably 60 to 65% by weight of ethanol. The disinfectant may include certain additional polyhydric alcohols. The additional polyhydric alcohols in the composition according to the present invention are preferably sorbitol, glycerol, polyethylene glycol, propylene glycol, and combinations thereof.

[0071] The disinfectant preferably comprises 0.01 to 1% by weight of a thickening agent. More preferably, the composition comprises 0.05 to 0.8% by weight of a thickening agent, most preferably 0.08 to 0.2% by weight of a thickening agent. Water is generally present in the disinfectant composition in an amount of 10 to 40% by weight. More preferably, the composition comprises 12 to 35% by weight of water, most preferably 25 to 30% by weight of water.

[0072] Deodorant product

[0073] A particular type of skin care composition is the so-called deodorant composition. These compositions are typically applied to skin areas where body odor is produced, such as the axillary area. These products act by masking the odor or by ensuring that odor-causing molecules are not produced or by killing or inactivating odor-causing microorganisms. One class of such products is also known as antiperspirant products because they reduce or minimize the amount of sweat produced by a person.

[0074] Broadly speaking, these products can be applied cosmetically and topically to the skin by one of two methods. In one method (sometimes called the contact method), the composition is spread on the skin surface, thereby depositing a portion of the composition as it passes. In the second method (sometimes called the non-contact method), the composition is sprayed from a dispenser that is held close to the skin. The spray can be formed by mechanical means that create pressure on the contents of the dispenser (such as a pump or squeezable sidewalls) or by internal pressure created by the evaporation of a portion of a liquefied propellant, and such a dispenser is commonly referred to as an atomizer.

[0075] Broadly speaking, there are two types of contact compositions, one type being liquid and typically applied with a roll-on dispenser or possibly absorbed into or onto a wipe, and in the second type, the desired active substance is distributed in a carrier liquid that forms a gelled continuous phase. In one variant, the carrier liquid contains a solvent for the desired active substance, and in a second variant, the active substance remains as a particulate solid suspended in an oil (usually a mixture of oils).

[0076] Stick or soft solid compositions:

[0077] Many different materials have been proposed as gelling agents for the continuous oil phase, including waxes, small molecule gelling agents, and polymers. They each have their advantages, and one of the most popular classes of gelling agents includes waxes, at least in part because they are readily available and easy to process, particularly including straight-chain fatty alcohol wax gelling agents. The gelled deodorant compositions are applied topically to the skin by spreading on the skin and contacting the skin, thereby depositing a film on the skin.

[0078] Roll-on:

[0079] Broadly speaking, liquid compositions suitable for roll coating can be divided into two categories, namely those in which the active substance is suspended in a hydrophobic carrier (such as a volatile silicone) and those in which the active substance is dissolved in a carrier liquid. The latter have proven to be more popular. There are two main types of carrier liquids for dissolution, namely carriers that are mainly alcohols, that is, a major part of the carrier liquid for dissolution contains ethanol, and a second type in which the carrier liquid is mainly water. The former is very popular because ethanol itself is a mild bactericide, but its popularity has gradually waned because it has a stinging sensation, especially when the surface to which the composition is applied is damaged or cut, such as may easily occur during shaving or other hair removal operations.

[0080] The second type of formulation as an alternative to alcohol-based preparations contains a dispersion of water-insoluble or very poorly water-soluble components in an aqueous solution of the active substance. In this article, such a combination is referred to as an emulsion. Roll-on emulsions typically contain one or more emulsifiers to maintain the distribution of water-soluble components.

[0081] Aerosol compositions:

[0082] Deodorant compositions can be delivered by aerosol, which contains a propellant in addition to the other ingredients mentioned above.

[0083] The propellants in this article generally conform to one of three categories: i) low-boiling gases liquefied by compression, ii) volatile ethers, and iii) compressed non-oxidizing gases.

[0084] Category i) conveniently consists of low-boiling materials, typically having a boiling point below -5°C, and usually below -15°C, and especially alkanes and / or halogenated hydrocarbons. Such propellants are usually liquefied and evaporated under the pressure in an aerosol can to generate the pressure to expel the composition from the can. Examples of suitable alkanes particularly include propane, butane, or isobutene. The second type of propellant contains very volatile ethers, and the most widely used ether to date is dimethyl ether. This propellant can advantageously be used at a relatively low weight ratio of propellant to base formulation, for example as low as 5:95. It can also be used in combination with, for example, compressible / liquefiable alkane gases. The third type of propellant includes compressed non-oxidizing gases, especially carbon dioxide or nitrogen. Inert gases (such as neon) are theoretical alternatives.

[0085] Skin care compositions can also contain other ingredients commonly used in the art to enhance physical properties and performance. Suitable ingredients include, but are not limited to, humectants, thickeners, sunscreens, adhesives, colorants and pigments, pH regulators, preservatives, optics, fragrances, viscosity regulators, biological additives, buffers, conditioners, essential oils, and skin-beneficial agents (including anti-inflammatory agents, cooling agents, antiperspirants, anti-aging agents, anti-acne agents, anti-microbial agents, and antioxidants).

[0086] Another aspect of the present invention relates to a method for disinfecting a surface, which comprises the step of applying a topical composition as described above to the surface. The topical composition can be applied, for example, by spraying, brushing or rubbing.

[0087] Generally, the topical composition is applied in an amount of 0.01 - 100 mg / cm 2 , more preferably in an amount of 0.1 - 10 mg / cm 2 , and most preferably in an amount of 1 - 5 mg / cm 2 .

[0088] According to an advantageous embodiment of the method, the surface to which the topical composition is applied is the skin or hair.

[0089] According to another advantageous embodiment, the surface to which the topical composition is applied is selected from the inner wall of the oral cavity, the tongue and the teeth.

[0090] Yet another aspect of the present invention relates to the use of the topical composition as described above for disinfecting the skin, hair or oral cavity.

[0091] Preferably, the above - mentioned use comprises the topical application of the composition.

[0092] The methods and uses claimed in the present invention can be used for therapeutic or non - therapeutic applications, preferably for non - therapeutic applications.

[0093] In a further aspect, the present invention relates to the use of a polyhydroxy compound selected from sugars, polyols or combinations thereof as an antimicrobial activity promoter in a composition comprising a combination of an antimicrobial lipid and tetra - hydroxypropyl ethylenediamine (THPE). These polyhydroxy compounds surprisingly enhance the antimicrobial activity of other components in the composition, even though they themselves generally do not have antimicrobial activity.

[0094] All features that are preferred with respect to the composition of the first aspect of the present invention are equally preferred in this use of the polyhydroxy compound according to the present invention. The polyhydroxy compound is preferably selected from glycerol, panthenol, sucrose and combinations thereof.

[0095] The present invention will now be illustrated by means of the following non - limiting examples.

[0096] Examples

[0097] The following materials were used in the following examples: glycerol (Merck cat. No. G9012), panthenol (Sigma cat. No. 76200), sucrose (Sigma cat. No. S8501), fructose (Sigma cat. No. F0127), FOS (Tata NQ cat. No. FOSSENCE TMPowder P95), THPE (Sigma-Aldrich cat. No. 122262), phytosphingosine (Evonik), lauric acid (Lobachemie cat. No. 0435100500), palmitoleic acid (Chemscene cat. No. CS-0105451), sphingosine (Sigma cat. No. S9666), dihydrosphingosine (Sigma cat. No. D6783) and palmitoleic acid (Sigma cat. No. P9417).

[0098] The antimicrobial activity of a composition comprising one or more components selected from polyhydroxy compounds (glycerol or panthenol), THPE and antimicrobial lipids (phytosphingosine) is determined using the following assay:

[0099] · By adding 200 mL of sterile Difco TM M9 Minimal Salts, 5x (containing disodium hydrogen phosphate, potassium dihydrogen phosphate, sodium chloride and ammonium chloride) to 750 mL of sterile purified water, adjusting the final volume to 1 L, and adding 20 mL of filter-sterilized 20% glucose solution and 2 mL of sterile 1.0 M MgSO4 solution under sterile conditions to prepare M9 Minimal Medium.

[0100] · Inoculate Staphylococcus epidermidis ATCC 12228 (Chromachemie) into 10 ml of M9 Minimal Medium + 10% Tryptic Soy Broth (TSB) medium, and

[0101] (a) without addition

[0102] (b) 1% by weight glycerol

[0103] (c) 1% by weight panthenol

[0104] (d) 1% by weight glycerol + 1% by weight panthenol

[0105] · Incubate at 37 °C for 72 hours under shaking conditions

[0106] · After 72 hours, collect the supernatant from the above fermentation broth by centrifugation and pass it through a 0.22 μm filter (filtered to remove residual bacteria from the culture supernatant). During incubation, Staphylococcus epidermidis can utilize glycerol and / or panthenol to produce metabolites that can inhibit the growth of pathogens.

[0107] · Inoculate Staphylococcus aureus ATCC 6538 (Chromachemie) in a culture medium together with the culture supernatant (collected as shown above) and the following additions:

[0108] (1) No addition

[0109] (2) 1% by weight of THPE

[0110] (3) 2% by weight of THPE

[0111] (4) 0.0004% by weight of phytosphingosine

[0112] (5) 1% by weight of THPE + 0.0004% by weight of phytosphingosine

[0113] ● Incubate without shaking at 37 °C for 16 hours

[0114] ● After 16 hours, measure the absorbance at 600 nm (the absorbance value represents bacterial growth - the higher the absorbance value, the more bacterial growth).

[0115] An X in a cell in the following table indicates the presence of a specific component in the amount shown above.

[0116] The results are shown in the following table:

[0117] Table 1

[0118]

[0119] Table 2

[0120] [[ID=4[1]]

[0121] Table 3

[0122]

[0123] Table 4[[ID=4[9]]

[0124]

[0125]

[0126] Table 5

[0127]

[0128] Table 6

[0129]

[0130] The data in Tables 1 to 6 above show that the composition according to the present invention provides synergistic antimicrobial activity.

[0131] Furthermore, except for using sucrose (2% by weight) instead of glycerol / panthenol as the polyhydroxy compound, the above experiment was repeated in exactly the same manner. The data was also analyzed in the same way, and the results are summarized in Tables 7 and 8 below:

[0132] Table 7

[0133]

[0134]

[0135] Table 8

[0136]

[0137] The data in Tables 7 and 8 above indicate that when the polyhydroxy compound is sucrose, the synergistic effect is reproducible.

[0138] Furthermore, except for using fructose (2% by weight) as the polyhydroxy compound, the above experiment was repeated in exactly the same manner. The data was also analyzed in the same way, and the results are summarized in Tables 9 and 10 below:

[0139] Table 9

[0140]

[0141] Table 10

[0142]

[0143] The data in Tables 9 and 10 above indicate that when the polyhydroxy compound is fructose, the synergistic effect is reproducible.

[0144] Furthermore, except for using fructooligosaccharide (2% by weight) as the polyhydroxy compound, the above experiment was repeated in exactly the same manner. The data was also analyzed in the same way, and the results are summarized in Tables 11 and 12 below:

[0145] Table 11

[0146]

[0147] Table 12

[0148]

[0149] The data in Tables 11 and 12 above indicate that when the polyhydroxy compound is fructooligosaccharide, the synergistic effect is reproducible.

[0150] Further, except for using lauric acid (0.00025% by weight) instead of phytosphingosine as the antimicrobial lipid in combination with glycerol (Table 13) or fructose (Table 14) or sucrose (Table 15) or fructooligosaccharide (Table 16); and THPE, the above experiment was repeated in exactly the same manner. The data was also analyzed in the same way, and the results are summarized in Tables 13 to 16 below:

[0151] Table 13

[0152]

[0153] Table 14

[0154]

[0155] Table 15

[0156]

[0157] Table 16

[0158]

[0159] The data in Tables 13 to 16 above shows that when the antimicrobial lipid is lauric acid, the synergistic effect is reproducible. The data in these tables also shows that when the antimicrobial lipid and THPE are present in the ratio range according to the present invention (1:10000 to 1:10) (here 1:8000), a synergistic effect can be obtained.

[0160] Further, the above experiment was repeated for glycerol as the polyhydroxy compound, phytosphingosine as the antimicrobial lipid, and THPE, where phytosphingosine and THPE were used in the ratios shown in Tables 17 to 22 below.

[0161] Table 17

[0162]

[0163] Phytosphingosine:THPE = 1:1

[0164] Table 18

[0165]

[0166] Phytosphingosine:THPE = 1:5

[0167] Table 19

[0168]

[0169] Phytosphingosine:THPE = 1:2500

[0170] Table 20

[0171]

[0172] Phytosphingosine: THPE = 1:5000

[0173] Table 21

[0174]

[0175] Phytosphingosine: THPE = 1:25,000

[0176] Table 22

[0177]

[0178] Phytosphingosine: THPE = 1:50,000

[0179] The data in Tables 17 to 22 above show that a synergistic effect can only be obtained when the antimicrobial lipid and THPE are present in the ratios according to the present invention.

Claims

1. A topical composition comprising: 0.01% to 25% by weight of a polyhydroxy compound selected from sugars, polyols, or combinations thereof, wherein the sugar is selected from monosaccharides, disaccharides, polysaccharides, or combinations thereof, and wherein the polyol is selected from glycerol, panthenol, or combinations thereof; From 0.0001% to 5% by weight of an antimicrobial lipid, wherein the antimicrobial lipid is selected from fatty acids, sphingolipids or combinations thereof comprising a straight-chain C 10-24 saturated or unsaturated aliphatic chain, wherein the aliphatic chain is optionally substituted with one or more hydroxyl groups; and 0.01% to 10% by weight of tetrahydroxypropyl ethylenediamine (THPE), wherein the antimicrobial lipid and THPE are present in a weight ratio of 1:10000 to 1:

10.

2. The topical composition according to claim 1, wherein the polyhydroxy compound is selected from glycerol, panthenol, sucrose, fructose, fructooligosaccharide, or combinations thereof.

3. The topical composition according to claim 1, wherein the antimicrobial lipid is selected from lauric acid, hexadecenoic acid, sphingosine, dihydrosphingosine, phytosphingosine, 6-hydroxysphingosine, palmitoleic acid, and combinations thereof.

4. The topical composition according to claim 1, wherein the antimicrobial lipid is selected from lauric acid, phytosphingosine, or combinations thereof.

5. The topical composition according to claim 3, wherein the antimicrobial lipid is phytosphingosine.

6. The topical composition according to any one of claims 1-5, wherein the composition comprises 0.1% to 10% by weight of the polyhydroxy compound.

7. The topical composition according to any one of claims 1-5, wherein the composition comprises 0.3% to 3% by weight of the polyhydroxy compound.

8. The topical composition according to any one of claims 1-5, wherein the composition comprises 0.0005% to 1% by weight of the antimicrobial lipid.

9. The topical composition according to any one of claims 1-5, wherein the composition comprises 0.001% to 0.1% by weight of the antimicrobial lipid.

10. The topical composition according to any one of claims 1-5, wherein the composition comprises 0.05% to 5% by weight of THPE.

11. The topical composition according to any one of claims 1-5, wherein the composition comprises 0.1% to 2% by weight of THPE.

12. The topical composition according to any one of claims 1-5, wherein the polyhydroxy compound and THPE are present in a weight ratio in the range of 1:20 to 20:

1.

13. The topical composition according to any one of claims 1-5, wherein the composition is a lotion, cream, deodorant, hand sanitizer, or body spray.

14. A non-therapeutic method of disinfecting a surface, comprising the step of applying the topical composition according to any one of claims 1 to 13 to the surface.

15. The non-therapeutic method according to claim 14, wherein the surface is skin or hair.

16. The non-therapeutic method according to claim 14, wherein the surface is selected from the inner walls of the oral cavity, the tongue, and the teeth.

17. The non-therapeutic method according to any one of claims 14 to 16, wherein at least a portion of the topical composition is removed by rinsing the surface with water after being applied to the surface.

18. The non-therapeutic use of the topical composition according to any one of claims 1 to 13 for disinfecting the skin, hair or oral cavity.

19. The non-therapeutic use of a polyhydroxy compound selected from sugars, polyols or combinations thereof as an antimicrobial activity promoter in a composition comprising a combination of an antimicrobial lipid and tetra-hydroxypropyl ethylenediamine (THPE).

20. The use according to claim 19, wherein the polyhydroxy compound is selected from glycerol, panthenol, sucrose and combinations thereof.

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