EP3319583A1 - Compositions destinées à une utilisation topique - Google Patents

Compositions destinées à une utilisation topique

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Publication number
EP3319583A1
EP3319583A1 EP16736189.8A EP16736189A EP3319583A1 EP 3319583 A1 EP3319583 A1 EP 3319583A1 EP 16736189 A EP16736189 A EP 16736189A EP 3319583 A1 EP3319583 A1 EP 3319583A1
Authority
EP
European Patent Office
Prior art keywords
agents
skin
group
composition according
composition
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
EP16736189.8A
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German (de)
English (en)
Inventor
Anastasi PUIG
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
LABORATORIOS ASDERCO, S.L.
Original Assignee
Juvilis Cosmetics SL
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Juvilis Cosmetics SL filed Critical Juvilis Cosmetics SL
Publication of EP3319583A1 publication Critical patent/EP3319583A1/fr
Pending legal-status Critical Current

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A61Q19/08—Anti-ageing preparations
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/44—Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/0241—Containing particulates characterized by their shape and/or structure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/19—Cosmetics or similar toiletry preparations characterised by the composition containing inorganic ingredients
    • A61K8/24—Phosphorous; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/31—Hydrocarbons
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • A61K8/347—Phenols
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37—Esters of carboxylic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/39—Derivatives containing from 2 to 10 oxyalkylene groups
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/494—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom
    • A61K8/4953—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with more than one nitrogen as the only hetero atom containing pyrimidine ring derivatives, e.g. minoxidil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4993—Derivatives containing from 2 to 10 oxyalkylene groups
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/60—Sugars; Derivatives thereof
    • A61K8/602—Glycosides, e.g. rutin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67—Vitamins
    • A61K8/673—Vitamin B group
    • A61K8/675—Vitamin B3 or vitamin B3 active, e.g. nicotinamide, nicotinic acid, nicotinyl aldehyde
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/67—Vitamins
    • A61K8/676—Ascorbic acid, i.e. vitamin C
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73—Polysaccharides
    • A61K8/735—Mucopolysaccharides, e.g. hyaluronic acid; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/85—Polyesters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/86—Polyethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/92—Oils, fats or waxes; Derivatives thereof, e.g. hydrogenation products thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9771—Ginkgophyta, e.g. Ginkgoaceae [Ginkgo family]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9789—Magnoliopsida [dicotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/96—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution
    • A61K8/97—Cosmetics or similar toiletry preparations characterised by the composition containing materials, or derivatives thereof of undetermined constitution from algae, fungi, lichens or plants; from derivatives thereof
    • A61K8/9783—Angiosperms [Magnoliophyta]
    • A61K8/9794—Liliopsida [monocotyledons]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q5/00—Preparations for care of the hair
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q7/00—Preparations for affecting hair growth
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/41—Particular ingredients further characterized by their size
    • A61K2800/412—Microsized, i.e. having sizes between 0.1 and 100 microns

Definitions

  • the present invention is comprised in the field of compositions for topical delivery of cosmetic or pharmacological active ingredients .
  • the present invention also relates to the use of said compositions in the non-therapeutic cosmetic treatment and/or care of skin and/or hair; as well as their use in medicine, in particular, for the treatment and/or prevention of skin and/or hair pathological conditions.
  • Topical delivery of cosmetic or therapeutic agents is a challenge in the field of cosmetic/pharmaceutical formulations.
  • the skin is a body barrier which serves as protective shield against the environment.
  • Mammalian skin consists of two main layers, the epidermis and the dermis.
  • the epidermis is formed by the stratum corneum, the stratum granulosum, the stratum spinosum and the stratum basale, with the stratum corneum being at the surface of the skin and the stratum basale being the deepest portion of the epidermis.
  • the dermis is beneath the epidermis and is primarily made up of collagen.
  • the primary function of the skin is to regulate the entry of substances into the body.
  • the stratum corneum provides the main permeability barrier function of the skin.
  • the stratum corneum is 15-20 ⁇ thick and is made up of 15-20 layers of flattened, densely packed, metabolically inactive cells, which are followed by several histologically distinguishable layers of closely packed cells.
  • the epidermal cell membranes are so closely joined that there is hardly any intercellular space through which polar non-electrolyte molecules and ions can diffuse.
  • the proteins and lipids of the stratum corneum form a complex crosslinking structure, resembling bricks and lipid mortar.
  • the main lipids found in the stratum corneum include cholesterol and fatty acids.
  • Ceramides in particular ceramide 2 and ceramide 5, play an important role in the stratum corneum' s overall lipid matrix organization and skin barrier function. Ceramides are tightly packed in lipid layers due to the strong hydrogen bonds between opposing amide head groups. This indicates a transverse organization in addition to the lateral orthorhombic chain organization of ceramide molecules. This hydrogen bond is responsible for the strength, integrity and barrier properties of the lipid layers in the stratum corneum. This layer is very selective with respect to the type of molecules that can be transported through the skin; therefore, only molecules with specific physicochemical properties can cross the skin in a significant manner.
  • Nanoparticles have been extensively studied as topical drug release systems, in particular, as skin surface reservoir from which controlled drug release over time may be achieved, however in said systems the nanoparticles do not permeate beyond the superficial layers of the skin barrier [Campbell et al., J Control Release, 2012, 162, 201-207] .
  • nanoparticles have been reported to permeate into the follicular orifice. It has also been reported that depending on their size, nanoparticles which have permeated into the follicular orifice may penetrate the follicular epithelium [Vogt et al., J. Invest. Dermatol., 2006, 126, 1316-1322] .
  • the first aspect of the present invention relates to a composition
  • a composition comprising:
  • a surfactant selected from the group consisting of polyethylene glycol ethers of oleyl alcohol or stearyl alcohol having from 10 to 22 ethylene oxide units, sorbitan laurates, sorbitan oleates, polysorbates and mixtures thereof;
  • a nanoparticle selected from the group consisting of hydroxyapatite nanoparticles, tricalcium phosphate nanoparticles, poly ( lactic—cio-glycolic aci
  • the present invention relates to the use of a composition according to the first aspect, wherein the active ingredient is a pharmaceutical active ingredient, for preparing a medicinal product.
  • the present invention relates to the use of a composition according to the first aspect, wherein the active ingredient is a pharmacological active ingredient, in the preparation of a medicinal product for the treatment and/or prevention of a skin and/or hair pathology selected from the group consisting of microbial infections, fungal infections and pathological hair loss.
  • the present invention relates to the use of a composition according to the first aspect, wherein the active ingredient is a cosmetic active ingredient, in the non- therapeutic cosmetic treatment and/or care of skin and/or hair.
  • the present invention relates to a composition according to the first aspect for use as a medicinal product .
  • the present invention relates to a composition according to the first aspect for use in the treatment and/or prevention of a skin and/or hair pathological condition selected from the group consisting of microbial infections, fungal infections and pathological hair loss.
  • the present invention relates to a method for the treatment and/or prevention of a skin and/or hair pathological condition selected from the group consisting of microbial infections, fungal infections and pathological hair loss in a patient affected or susceptible of being affected by said pathological conditions comprising the topical application of a composition according to the first aspect .
  • the present invention relates to a method for the non-therapeutic cosmetic treatment and/or care of skin and/or hair selected from the group consisting of treatment and/or prevention of aging and/or photoaging, treatment and/or prevention of wrinkles comprising the topical application to skin and/or hair of a composition according to the first aspect.
  • Hansen solubility parameters were developed by Charles Hansen as a way of predicting if one material will dissolve in another one . There are three Hansen parameters :
  • the Hansen parameters of a compound can be determined following the binary solvent gradient method published by Machui et al. [Solar Energy Materials Solar Cells, 2012, 100, 13.8- 146] . Said method analyzes the solubility of a target compound in a series of solvents with known Hansen parameters (as described for example in Hansen Solubility Parameters: A Users' Handbook. Updated database at http : //hansen- solubility.com/Contents/HSPiPDataSet.xls) . The Hansen parameters of said compound are at the centre of a sphere in the Hansen space where the radius R indicates the maximum difference in tolerable affinity for complete dissolution, as explained below. Good solvents are inside the sphere and bad ones are outside the sphere .
  • a first step the solubility of the compound in a reduced number of pure solvents is determined in order to identify at least one good solvent and at least one bad solvent for the compound.
  • the solvents used in this first step are, for example, toluene, propylene carbonate, 2-propanol, acetonitrile, hexane and dimethylsulfoxide (DMS0) , wherein isopropyl myristate, dicaprylyl ether, water, tetrahydrofuran, glycerol, diethylene glycol, dimethyl formamide and 1,4-dioxane may also be used.
  • the determination is made by shaking the target compound (about 70 mg) with about 5 ml of each of the aforementioned solvents for 30 min at 800 rpm. Then the sample is examined by human eye and the solvent is classified as a "good solvent” if a clear solution or a suspension that does not form sediments when left standing for 1 hour is obtained.
  • binary mixtures of solvents comprising one good solvent and one bad solvent in a volume ratio of 3:1, 2:3 and 1:3, or if more values are needed for improving the accuracy of the method consisting of binary mixtures of solvents, the mixtures can comprise one good solvent and one bad solvent in a volume ratio of 17:86, 29:71 43:57, 57:43, 71:29 and 86:14; but other volume ratios can also be used .
  • the Hansen parameters of a binary mixture of solvents correspond to the sum of the volume contributions of each solvent.
  • the Hansen parameters of a mixture containing 29% by volume of a good solvent A with Hansen parameters ⁇ 0 ⁇ , ⁇ ⁇ and ⁇ ⁇ and 71% by volume of a bad solvent B with Hansen parameters ⁇ 0 ⁇ , ⁇ ⁇ and 5HB would be calculated as follows :
  • Table 1 shows the values of Hansen parameters of some pure solvents .
  • Dissolution refers to the loss of compound integrity and to the compound being visibly less massive. Turbidity relates to the degree of transparency, the limits being a clear solution and the capacity to see through an unclear solution.
  • sedimentation rate il the time for the studied nanoparticles to settle in the solvent (in particular in the binary mixtures of solvents defined above) and is quantified by means of relative sedimentation time (RST) using the following formula:
  • t s is the sedimentatilon time (expressed in seconds)
  • p p is particle density (expressed in g/ml)
  • p s is solvent density (particularly of the binary mixture of solvents; expressed in g/ml)
  • ⁇ is solvent viscosity (particularly of the binary mixture of solvents; expressed in mPa-s) .
  • Assigning a score of 1 to 6 based on RST values is carried out by assigning the score of 6 to the shortest times among all the solvents studied for one and the same particle (particularly among all the studied binary mixtures of solvents) , whereas the most stable and long- lasting dispersions obtained lower values by applying the following equation:
  • n is the value of the maximum score of the study (for example, 6)
  • RST is the relative sedimentation time
  • axRST is the maximum value of the relative sedimentation time obtained in the study (i.e., for one and the same particle in all the solvents, particularly in the binary mixtures of tested solvents) .
  • the obtained score value is rounded off to the nearest unit.
  • the solvents of binary mixtures are represented in the Hansen space according to their Hansen parameters and the Hansen parameters of the specific compound are then calculated by fitting a solubility sphere so that all good solvent mixtures lie within it (i.e., those having scores of 1-3) and all bad solvent mixtures lie outside it (i.e., those having scores of 4- 6) .
  • An algorithm fits a sphere in the 3D Hanssen space ( ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ ) by minimizing the number of the so-called wrong solvents, including a) good solvents that are outside the sphere and b) bad solvents that are inside the sphere. By convention, if there are different spheres with no wrong solvents, the sphere with the smallest radius is selected.
  • the sphere with the smallest product of error distance (distance of a bad solvent inside the sphere or distance of a good solvent outside the sphere) is selected. This fitting is performed by evaluating the data using the following quali ty-of-fit function:
  • n is the number of solvents
  • a ⁇ e "(error dlstance » , wherein the error distance is the distance between the wrong solvent and the sphere boundary.
  • Ai will be 1.0 when there is a good solvent within the sphere and when there is a bad solvent outside the sphere.
  • the coordinates of the center of the sphere therefore correspond to the Hansen parameters ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ of the target molecule .
  • compositions of the invention are provided.
  • Component a) of the composition according to the first aspect of the present invention is an oil having a 5 D value from 15 to 18, a ⁇ ⁇ value from 2 to 5 and a ⁇ ⁇ value from 2 to 5.
  • the oil has a 5 D value from 15.5 to 16.5.
  • the oil has a ⁇ ⁇ value from 2 to 3.
  • the oil has a ⁇ ⁇ value from 2 to 4. More preferably, the oil has a ⁇ 0 value from 15.5 to 16.5, a ⁇ ⁇ value from 2 to 3 and a ⁇ ⁇ value from 2 to 4.
  • oil is used in the present invention to designate any organic substance which is liquid at 20°C and has a solubility in water of less than 0.05 g/1, preferably less than 0.01 g/1, more preferably less than 0.001 g/1, still more preferably less than 0.0001 g/1.
  • the oil includes petroleum products, animal, plant or synthetic oils, the Hansen parameter values of which are as defined above.
  • Non-limiting examples of oils having a ⁇ 0 value from 15 to 18, a ⁇ ⁇ value from 2 to 5 and a ⁇ ⁇ value from 2 to 5 are isopropyl myristate, dicaprylyl ether, squalane, oleyl erucate, oleyl oleate, isopropyl palmitate, acai oil, sweet almond oil, soybean glycerides, avocado oil and shea butter, the Hansen parameters of which are shown in Table 2.
  • the oil is selected from the group consisting of isopropyl myristate, dicaprylyl ether, squalane and mixtures thereof.
  • the oil (component a) ) is present in an amount from 60% to 90% by weight with respect to the total weight of the composition, more preferably from 65% to 90% by weight with respect to the total weight of the composition.
  • Component b) of the composition according to the first aspect of the present invention is a surfactant selected from the group consisting of polyethylene glycol ethers of oleyl alcohol or stearyl alcohol having from 10 to 22 ethylene oxide units, sorbitan laurates, sorbitan oleates, polysorbates and mixtures thereof.
  • Polyethylene glycol ethers of oleyl alcohol are known as
  • Oleth followed by the number of ethylene oxide units, for example, Oleth-10 is the polyethylene glycol ether of oleyl alcohol comprising 10 ethylene oxide units.
  • Non-limiting examples of polyethylene glycol ethers of oleyl alcohol having from 10 to 22 ethylene oxide units are Oleth-10, Oleth-11, Oleth-12, Oleth-15, Oleth-16 and Oleth-20.
  • Polyethylene glycol ethers of stearyl alcohol are known as Steareth followed by the number of ethylene oxide units, for example, Steareth-10 is the polyethylene glycol ether of stearyl alcohol comprising 10 ethylene oxide units.
  • Non-limiting examples of polyethylene glycol ethers of stearyl alcohol having from 10 to 22 ethylene oxide units are Steareth-10, Steareth-11, Steareth-12, Steareth-13, Steareth-14, Steareth-15, Steareth-16, Steareth-20 and Steareth-21.
  • Sorbitan laurates are understood as sorbitan monolaurate, sorbitan dilaurates, sorbitan trilaurate and mixtures thereof.
  • Sorbitan oleates are understood as sorbitan monooleate, sorbitan dioleates, sorbitan trioleate and mixtures thereof.
  • Polysorbates are understood as fatty acid esters of sorbitan such as lauric acid, palmitic acid, stearic acid and oleic acid.
  • the number following the polysorbate part refers to the type of fatty acid associated with the polyoxyethylene sorbitan part of the molecule.
  • Monolaurate is indicated by numbers in the 20s
  • monopalmitate is indicated by numbers in the 40s
  • monostearate by numbers in the 60s and monooleate by numbers in the 80s.
  • Non-limiting examples of polysorbates are polysorbate-20 , polysorbate-21 , polysorbate-40 , polysorbate-60 , polysorbate- 61 , polysorbate- 65 , polysorbate-80 , polysorbate-81 and polysorbate-85.
  • the surfactant is selected from the group consisting of Oleth-10, Oleth-11, Oleth-12, Oleth-15, Oleth-16, Oleth-20, sorbitan monooleate, sorbitan trioleate, polysorbate-20, polysorbate-21 , polysorbate-40, polysorbate-60, polysorbate- 61 , polysorbate-65, polysorbate-80, polysorbate-81, polysorbate-85 and mixtures thereof, more preferably the surfactant is selected from the group consisting of Oleth-10, sorbitan monooleate, polysorbate-80 and mixtures thereof.
  • the surfactant (component b) ) is present in an amount from 0.25% to 2% by weight with respect to the total weight of the composition.
  • Component c) of the composition according to the first aspect of the present invention is a nanoparticle selected from the group consisting of hydroxyapatite nanoparticles , tricalcium phosphate nanoparticles, poly ( lactic-co-glycolic acid) (PLGA) nanoparticles, hyaluronic acid nanoparticles and mixtures thereof.
  • a nanoparticle selected from the group consisting of hydroxyapatite nanoparticles , tricalcium phosphate nanoparticles, poly ( lactic-co-glycolic acid) (PLGA) nanoparticles, hyaluronic acid nanoparticles and mixtures thereof.
  • nanoparticle is understood as a particle, preferably a spherical particle, with a diameter ranging from 1 nm to 1000 nm, preferably from 1 nm to 500 nm, even more preferably from 1 nm to 400 nm, still more preferably from 10 nm to 350 nm, still more preferably from 50 nm to 300 nm, and most preferably from 100 nm to 250 nm.
  • the diameter of the particle is taken to be that of a sphere of equivalent volume .
  • the nanoparticles (component c) ) are present in an amount from 0.5% to 2% by weight with respect to the total weight of the composition.
  • the surfactant (component b) ) is selected from the group consisting of Oleth-10, Oleth-11, 01eth-12, 01eth-15, 01eth-16 and Oleth-20; preferably from the group consisting of Oleth-10, 01eth-12 and mixtures thereof; more preferably the surfactant is Oleth-10.
  • the surfactant (component b) ) is selected from the group consisting of sorbitan monooleate, sorbitan trioleate, sorbitan monolaurate and mixtures thereof.
  • the surfactant (component b) ) is selected from the group consisting of polysorbate-20 , polysorbate-21 , polysorbate- 40, polysorbate-60 , polysorbate- 61, polysorbate-65 , polysorbate- 80, polysorbate-81 , polysorbate-85 and mixtures thereof; preferably the surfactant is polysorbate-80.
  • the surfactant (component b) ) is selected from the group consisting of polysorbate-20 , polysorbate-21, polysorbate- 40, polysorbate-60, polysorbate- 61, polysorbate-65, polysorbate- 80, polysorbate—81 , polysorbate—85 and mixtures thereof; preferably the surfactant is polysorbates—80.
  • Component d) of the composition according to the first aispect of the present invention is a cosmetically or pharmacologically active ingredient with ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ such that
  • a cosmetically active ingredient is a compound or mixture of compounds that exerts a beneficial effect on the skin and/or hair such as improving or maintaining the cosmetic qu!alities of the skin and/or hair, for example the level of hydration, elasticity, firmness, gloss, tone and texture, among others.
  • a pharmacologically active ingredient is a compound or mixture of compounds that prevents and/or treats a disease or disorder of the skin and/or hair, such as microbial infections, fungal infections, and/or pathological hair loss, among others.
  • the cosmetically active ingredient is selected from the group consisting of antioxidants, moisturizers, skin conditioning agents, antistatic agents, smoothing agents, soothing agents, emollient agents, astringent agents, antiseborrheic agents, antidandruff agents, tonics, bleaching agents, cleansing agents, keratolytic agents, refatting agents, lifting agents, antli—wrinkle agents, repairing agents, regenerating agents, firming agents, energizing agents, volumizing agents, anti-dark circle agents, anti-puffiness agents, pore minimizing agents, protective agents and mixtures thereof; or the pharmacologically active ingredient is selected from the group consisting of antimicrobial agents, antiinflammatory agents, fungicides and hair loss preventers.
  • the Hansen parameters of the mixture correspond to the sum of the weight contributions of each compound .
  • An antioxidant is a compound which inhibits reactions promoted by oxygen, thus avoiding oxidation reactions. These compounds also avoid rancidity of the compositions.
  • Non-limiting examples of antioxidants having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are Camellia sinensis leaf extract, trans-resveratrol, alpha lipoic acid, nordihydroguaiaretic acid, caffeine, Aloe vera, ascorbyl palmitate, alpha-arbutin, arbutin, Echinacea purpurea extract, niacinamide and astaxanthine .
  • a moisturizer is a compound that increases the water content of the skin and helps to keep it soft and smooth.
  • Non- limiting examples of moisturizers having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are Echinacea purpurea extract, niacinamide and pyroglutamic acid.
  • a skin conditioning agent is a compound that maintains the skin in good condition.
  • skin conditioning agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are Echinacea purpurea extract, Camellia sinensis leaf extract, salicylic acid, biotin, Helichrysum arenarium flower extract, Chamomilla recutita flower extract, Ginkgo biloba leaf extract, Aloe vera, caprylyl glycol, Ranunculus ficaria extract, Centella asiatica extract, Aesculus hippocastanum seed extract, ethyl nicotinate, glycyrrhetinic acid, alpha-arbutin, arbutin, Enantia chlorantha bark extract, astaxanthin, Spilanthes acmella flower extract and benzyl nicotinate.
  • An antistatic agent is a compound that reduces static electricity by neutralizing electrical charge on a surface.
  • Non- limiting examples of antistatic agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are niacin, acrylate copolymer and benzyl nicotinate.
  • a smoothing agent is a compound that decreases skin roughness or irregularities, thus achieving an even skin surface.
  • Non-limiting examples of smoothing agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are niacin, Spirulina maxima extract, niacinamide and Centella asiatica extract.
  • a soothing agent is a compound that helps alleviate discomfort of the skin or of the scalp.
  • Non-limiting examples of soothing agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are methyl nicotinate, Centella asiatica extract and Echinacea purpurea extract .
  • An emollient agent is a compound that softens the skin.
  • emollient agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are Camellia sinensis leaf extract, Panax ginseng root extract, glyceryl stearate and caprylyl glycol.
  • An astringent agent is a compound that contracts the skin.
  • a non-limiting example of an astringent agent having suitable 5 D , ⁇ ⁇ and ⁇ ⁇ values is Camellia sinensis leaf extract.
  • An antiseborrheic agent is a compound that helps control sebum production.
  • Non-limiting examples of antiseborrheic agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are biotin and Enantia chlorantha bark extract.
  • An antidandruff agent is a compound that helps control dandruff.
  • a non-limiting example of an antidandruff agent having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values is salicylic acid.
  • a tonic is a compound that produces a feeling of well-being on skin and hair.
  • Non-limiting examples of tonics having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are Echinacea purpurea extract, Camellia sinensis leaf extract, Panax ginseng root extract, methyl nicotinate and Centella asiatica extract.
  • a bleaching agent is a compound that lightens skin tone or corrects imperfections in the skin' s pigmentation by lessening the concentration of melanin.
  • Non-limiting examples of bleaching agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are glabridin, alpha- arbutin and arbutin.
  • a cleansing agent is a compound that helps to keep the body surface (skin and/or hair) clean.
  • cleansing agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are Centella asiatica extract and alpha lipoic acid.
  • a keratolytic agent is a compound that helps to eliminate the dead cells of the stratum corneum.
  • a non-limiting example of a keratolytic agent having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values is salicylic acid.
  • a refatting agent is a compound that replenishes the lipids of the hair or of the top layers of the skin.
  • a non-limiting example of a refatting agent having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values is C ( 6) -ceramide .
  • a lifting agent is a compound that that lifts the skin.
  • a non-limiting example of a lifting agent having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values is acrylate copolymer.
  • An anti-wrinkle agent is a compound that can reduce fine lines on the skin.
  • Non-limiting examples of anti-wrinkle agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are ascorbyl palmitate and niacinamide .
  • a repairing agent is a compound that helps the body to restore skin alterations, such as scars.
  • Non-limiting examples of repairing agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are Centella asiatica extract and Echinacea purpurea extract.
  • a regenerating agent is a compound that helps in skin self- generation by means of mechanisms such as cell stimulation.
  • a non-limiting example of a regenerating agent having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values is Centella asiatica extract.
  • a firming agent is a compound that provides firmness to the skin.
  • Non-limiting examples of firming agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are biotin and niacinamide.
  • An energizing agent is a compound that provides in a combined manner brightness and astringency to the skin.
  • Non- limiting examples of energizing agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are trans-resveratrol , Panax ginseng root extract, Camellia sinensis leaf extract.
  • a volumizing agent is a compound that stimulates skin adipocytes.
  • a non-limiting example of a volumizing agent having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values is Centella asiatica extract.
  • An anti-dark circle agent is a compound that reduces pigmented areas under the eyes.
  • Non-limiting examples of anti- dark circle agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are caffeine, Camellia sinensis leaf extract and Gingko biloba leaf extract .
  • An anti-puffiness agent is a compound that reduces swelling, generally in the area around the eye.
  • Non-limiting examples of anti-puffiness agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are caffeine, Aesculus hippocastanum seed extract and Chamomilla recutita flower extract.
  • a pore minimizing agent is a compound that helps to clean out pores and make them look smaller.
  • a non-limiting example of a pore minimizing agent having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values is Ranunculus ficaria extract.
  • a protective agent is a compound that protects the skin against external agents.
  • protective agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are trans-resveratrol, Centella asiatica extract and niacinamide.
  • An antimicrobial agent is a compound that helps to control the growth of microorganisms on the skin.
  • Non-limiting examples of antimicrobial agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are Camellia sinensis leaf extract, ferulic acid, hexyl resorcinol, Enantia chlorantha bark extract and Spilanthes acmella flower extract .
  • a fungicide is a compound that helps to control the growth of fungi on the skin.
  • a non-limiting example of a fungicide having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values is pyraclostrobin .
  • An anti-inflammatory agent is a compound that reduces inflammation.
  • a non-limiting example of an anti -inflammatory agent having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values is glabridin.
  • a hair loss preventer is a compound that stimulates hair growth and prevents hair loss.
  • a non-limiting example of a hair loss preventer having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values is finasteride .
  • the present invention relates to a composition as defined herein, wherein the cosmetically or pharmacologically active ingredient is selected from the group consisting of Echinacea purpurea extract, niacin, Camellia sinensis leaf extract, Spirulina maxima extract, salicylic acid, ferulic acid, biotin, Helichrysum arenarium flower extract, acrylate copolymer, trans-resveratrol, Chamomilla recutita flower extract, niacinamide, alpha lipoic acid, hexyl resorcinol, nordihydroguaiaretic acid, Panax ginseng root extract, Ginkgo biloba leaf extract, pyraclostrobin, caffeine, C ( 6) -ceramide, glyceryl stearate, Aloe vera, ascorbyl palmitate, caprylyl glycol, Ranunculus flcarla extract, methyl nicotinate, Centella asiatica
  • the cosmetically or pharmacologically active ingredient has 5 D , ⁇ ⁇ and ⁇ ⁇ values such that
  • the active ingredient in the composition according to the present invention is a cosmetically active ingredient.
  • the active ingredient in the composition according to the present invention is a pharmacologically active ingredient.
  • the cosmetically or pharmacologically active ingredient (component d) ) is present in an amount from 2% to 15% by weight with respect to the total weight of the composition.
  • compositions of the present invention can optionally comprise a skin permeation enhancer, component e) .
  • said skin permeation enhancer is present in the compositions of the invention.
  • a skin permeation enhancer is a compound that facilitates the passage of molecules through the stratum corneum of the skin.
  • skin permeation enhancers are dimethyl isosorbide, transcutol (i.e., 2- (2- ethoxyethoxy) ethanol ) , propylene glycol, oleic acid, ethanol, dimethyl sulfoxide, dodecyl-N, N-dimethylaminoacetate, ethyl acetate, sodium dodecyl sulfate, d-limonene, 1, 3-diphenylurea, N-methyl-2-pyrrolidone , beta-cyclodextrin and azone® (i.e., N- dodecylcaprolactam) .
  • the skin permeation enhancer is selected from the group consisting of dimethyl isosorbide, transcutol (i.e., 2- (2-ethoxyethoxy) ethanol) and mixtures thereof
  • the skin permeation enhancer (component e) ) is present in an amount from 0.2% to 0.8% by weight with respect to the total weight of the composition.
  • compositions of the present invention can optionally comprise water, component f) .
  • water is present in the compositions of the invention.
  • the water (component f ) ) is present in an amount from 0.01% to 10% by weight with respect to the total weight of the composition.
  • composition of the present invention comprises:
  • an oil selected from the group consisting of isopropyl myristate, dicaprylyl ether, squalane and mixtures thereof;
  • a surfactant selected from the group consisting of Oleth—10, sorbitan monooleate, sorbitan trioleate, polysorbate— 80 and mixtures thereof;
  • a nanoparticle selected from the group consisting of hydroxyapatite nanoparticles, tricalcium phosphate nanoparticles, poly ( lactic—cio-glycolic acid) nanoparticles, hyaluronic acid nanoparticles and mixtures thereof;
  • e optionally a skin permeation enhancer selected from the group consisting of dimethyl isosorbide, transcutol (i.e., 2- (2- ethoxyethoxy) ethanol ) and mixtures thereof; and
  • composition of the present invention comprises :
  • a surfactant selected from the group consisting of Oleth—10, sorbitan monooleate, sorbitan trioleate, polysorbate—80 and mixtures thereof;
  • a nanoparticle selected from the group consisting of hydroxyapatite nanoparticles, tricalcium phosphate nanoparticles, poly ( lactic—co-glycolic acid) nanoparticles, hyaluronic acid nanoparticles and mixtures thereof;
  • composition of the present invention comprises :
  • a surfactant selected from the group consisting of Oleth—10, sorbitan monooleate, sorbitan trioleate, polysorbate—80 and mixtures thereof;
  • a nanoparticle selected from the group consisting of hydroxyapatite nanoparticles , tricalcium phosphate nanoparticles, poly ( lactic—co-glycolic acid) nanoparticles, hyaluronic acid nanoparticles and mixtures thereof;
  • e from 0.2% to 0.8% by weight with respect to the total weight of the composition of a skin permeation enhancer selected from the group consisting of dimethyl isosorbide, transcutol (i.e., 2— (2-ethoxyethoxy) ethanol ) and mixtures thereof; and
  • the cosmetically or pharmacologically active ingredient in said particular compositions is selected from the group consisting of Echinacea purpurea extract, niacin, Camellia sinensis leaf extract, Spirulina maxima extract, salicylic acid, ferulic acid, biotin, Helichrysum arenarium flower extract, acrylate copolymer, trans—resveratrol , Chamomilla recutita flower extract, niacinamide, alpha lipoic acid, hexyl resorcinol, nodihydroguaiaretic acid, Panax ginseng root extract, Ginkgo biloba leaf extract, pyraclostrobin, caffeine, pyroglutamic acid, C ( 6) -ceramide, glyceryl stearate, Aloe vera, ascorbyl palmitate, caprylyl glycol, Ranunculus ficaria extract, methyl nicotinate, Centella asiatica extract, Aesculus
  • the preparations of the present invention can also comprise additional ingredients.
  • Said additional ingredients have 5 D , ⁇ ⁇ and ⁇ ⁇ such that
  • Non—limiting examples of such additional ingredients are emulsion stabilizers, emulsifiers, humectants, gelling agents, viscosity controlling agents, perfumes and preservatives.
  • An emulsion stabilizer is a compound that helps in the emulsification process and improves emulsion stability and shelf—-life of the preparations.
  • emulsion stabilizers having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are carbomer, polyacrylate crosspolymer—6 and hydroxypropyl methyl cellulose .
  • An emulsifier is a compound that promotes the formation of intimate mixtures of non-miscible liquids by altering the interfacial tension.
  • emulsifiers having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are glyceryl stearate, polysorbate- 20, octadecenedioic acid and PEG-60 almond glycerides.
  • a humectant is a compound that holds and retains moisture.
  • Non-limiting examples of humectants having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are Camellia sinensis leaf extract, pyroglutamic acid, C ( 6 ) -ceramide and Aloe vera.
  • a gelling agent is a compound that gives the consistency of a gel to the composition.
  • a non-limiting example of a gelling agent having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values is carbomer.
  • a viscosity controlling agent is a compound that increases or decreases the viscosity of the composition.
  • Non-limiting examples of viscosity controlling agents having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are carbomer, polyacrylate crosspolymer-6, hydroxypropyl methyl cellulose and disodium EDTA.
  • a perfume is a compound used for perfuming the compositions.
  • perfumes having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are Citrus aurantium flower extract, phenylpropanol and ethyl nicotinate.
  • a preservative is a compound that stops or minimizes deterioration caused by the presence of different types of microorganisms.
  • Non-limiting examples of preservatives having suitable ⁇ 0 , ⁇ ⁇ and ⁇ ⁇ values are methylpropanediol , caprylyl glycol and phenylpropanol .
  • the preparations of the present invention can also comprise cyclopentasiloxane and/or cyclohexasiloxane , preferably in an amount from 5% to 15% by weight with respect to the total weight of the composition.
  • ingredients used in cosmetic/pharmacological preparations and known in the art can also be present, preferably in an amount less than 15% by weight with respect to the total weight of the composition.
  • composition of the present invention comprises:
  • a surfactant selected from the group consisting of polyethylene glycol ethers of oleyl alcohol or stearyl alcohol having from 10 to 22 ethylene oxide units, sorbitan laurates, sorbitan oleates, polysorbates and mixtures thereof;
  • a nanoparticle selected from the group consisting of hydroxyapatite nanoparticles , tricalcium phosphate nanoparticles, poly ( lactic—cD—glycolic acid) nanoparticles, hyaluronic acid nanoparticles and mixtures thereof;
  • compositions of the present invention have been designed for topical delivery of cosmetically or pharmacologically active ingredients. Therefore, the compositions of the present invention are in the form of topical compositions .
  • the composition of the present invention is provided in the form of a cream, an emulsion, a lotion, an ointment, a gel, a foam, a paste, a balm, a milk, a serum or a solution.
  • treatment refers to the delivery of a composition according to the invention to alleviate or eliminate a disease or disorder or reduce or eliminate one or more symptoms associated with this disease or disorder.
  • treatment when accompanied by the description "non-therapeutic cosmetic”, refers to the application of the composition of the invention to the skin and/or hair in particular for the purpose of improving the cosmetic qualities of the skin and/or hair such as, and not being limited to, their level of hydration, elasticity, firmness, wrinkles, gloss, tone or texture, among others.
  • the term "care” refers to the maintenance of the qualities of the skin and/or hair. These qualities are subject to improvement and maintenance through a cosmetic treatment and/or care of the skin and/or hair both in healthy subjects as well as in those having diseases and/or disorders of the skin and/or hair .
  • prevention refers to the ability of a composition of the invention to prevent, delay or hinder the onset or development of a disease or disorder before its onset.
  • the preparations of the present invention can comprise as a pharmacologically active ingredient the active ingredient defined as component d) .
  • the present invention relates to a composition as defined above, wherein the active ingredient is a pharmacologically active ingredient, for preparing a medicinal product.
  • the invention also relates to a composition according to the first aspect, wherein the active ingredient is a pharmacologically active ingredient, for use in medicine.
  • the present invention relates to the use of a composition according to the first aspect, wherein the active ingredient is a pharmacologically active ingredient, in the preparation of a medicinal product for the treatment and/or prevention of a skin and/or hair pathological condition selected from the group consisting of microbial infections (such as acne, for example), fungal infections (such as seborrheic dermatitis, for example) and pathological hair loss.
  • microbial infections such as acne, for example
  • fungal infections such as seborrheic dermatitis, for example
  • pathological hair loss selected from the group consisting of microbial infections (such as acne, for example), fungal infections (such as seborrheic dermatitis, for example) and pathological hair loss.
  • the invention also relates to a composition according to the first aspect, wherein the active ingredient is a pharmacologically active ingredient, for use in the treatment and/or prevention of a skin and/or hair pathological condition selected from the group consisting of microbial infections, fungal infections and pathological hair loss.
  • the active ingredient is a pharmacologically active ingredient, for use in the treatment and/or prevention of a skin and/or hair pathological condition selected from the group consisting of microbial infections, fungal infections and pathological hair loss.
  • the invention also relates to a method for the treatment and/or prevention of a skin and/or hair pathological condition selected from the group consisting of microbial infections, fungal infections and pathological hair loss, which comprises delivering to a patient needing such treatment and/or prevention a therapeutically effective amount of a composition according to the first aspect, wherein the active ingredient is a pharmacologically active ingredient.
  • the present invention relates to the use of a composition according to the first aspect, wherein the active ingredient is a cosmetic active ingredient, in the non- therapeutic cosmetic treatment and/or care of skin and/or hair, preferably, wherein the non-therapeutic cosmetic treatment and/or care of skin and/or hair is selected from the group consisting of treatment and/or prevention of aging and/or photoaging and treatment and/or prevention of wrinkles.
  • the term "aging" refers to the changes experienced by the skin with age ( chronoaging) or through exposure to the sun (photoaging) or to extreme environmental climatic conditions of cold or wind, chemical contaminants or pollutants, and includes all the external changes that are visible and/or perceptible through touch, such as, by way of non-limiting examples, the development of discontinuities on the skin such as wrinkles, fine lines, expression lines, stretch marks, furrows, irregularities or roughness, increase in pore size, loss of hydration, loss of elasticity, loss of firmness, loss of smoothness, loss of the capacity to recover from deformations, loss of resilience, sagging of the skin such as sagging cheeks, the appearance of bags under the eyes or the appearance of a double chin, among others, changes to the color of the skin such as marks, reddening, bags or the appearance of hyperpigmented areas such as age spots or freckles, among others, anomalous differentiation, hyperkeratinization, elastosis, keratosis, hair loss
  • photoaging groups together the set of processes caused by prolonged exposure of the skin to ultraviolet radiation which result in the premature aging of the skin, and it presents the same physical characteristics as aging, such as, by way of non-limiting examples, flaccidity, sagging, color changes or pigmentation irregularities and abnormal and/or excessive keratinization .
  • the sum of several environmental factors such as exposure to tobacco smoke, exposure to pollution and climatic conditions such as cold and/or wind also contribute to skin aging.
  • compositions of the inventions can be applied to the skin and/or hair area to be treated one or more times a day, such as 1 or 2, or 1, 2, or 3, or 1, 2, 3 or 4 times a day, preferably 1 or 2 times a day.
  • preferred skin areas to be treated are the face including the forehead, chin, nose, cheeks and the area around the eyes such as eyelids, area under the eyes, area between the eyes, area around the eyes on the opposite end of the area between the eyes (normally where crow' s feet appear), the neck and the neckline.
  • compositions of the present invention can be prepared any suitable method known in the field of topical pharmacological formulations, in which, by way of non—limiting example, the following steps are performed: premixing, heating, cooling, homogenizing, mixing, back evaporating, filtering, centrifuging, applying vacuum pressure, drying.
  • the preparation method comprises heating the fatty phase, or one or more of the oils, having a 5 D value from 15 to 18, a ⁇ value from 2 to 5 and a ⁇ ⁇ value from 2 to 5, i.e., component a) of the composition of the present invention, to 70°C in a reactor with constan
  • the composition comprises water (component f) , which is optional in the composition of the present invention) , said optional water is then added to the reactor at room temperature and heated to 60°C with constant stirring using blades until complete homogenization .
  • One or more of the surfactants selected from the group consisting of polyethylene glycol ethers of oleyl alcohol or stearyl alcohol having from 10 to 22 ethylene oxide units, sorbitan laurates, sorbitan oleates, polysorbates , i.e., component b) of the composition of the present invention is premixed in another reactor with one or more of the nanoparticles selected from the group consisting of hydroxyapatite nanoparticles, tricalcium phosphate nanoparticles, poly ( lactic—cio-glycolic acid) nanoparticles, hyaluronic acid nanoparticles, i.e., component c) of the composition of the present invention, optionally the skin permeation enhancer, i.e., optional component d) of the composition of the present invention, and one or more of the cosmetically or pharmacologically active ingredients with 5 D , ⁇ ⁇ and ⁇ ⁇ such that
  • the previously prepared fatty phase (component a) and optionally water) is then cooled to 40°C and the premixture consisting of components b) -d) and optionally e) is added to said fatty phase with constant stirring using blades until complete homogenization .
  • composition for a day lotion Composition for a day lotion
  • composition for a night cream Composition for a night cream:
  • composition for a serum Composition for a serum:

Abstract

La présente invention concerne des compositions adaptées à l'administration topique d'ingrédients actifs cosmétiques ou pharmacologiques. La présente invention concerne également l'utilisation desdites préparations dans le traitement cosmétique non-thérapeutique et/ou les soins de la peau et/ou des cheveux ; ainsi que leur utilisation en médecine, en particulier, pour le traitement et/ou la prévention de conditions pathologiques de la peau et/ou des cheveux.
EP16736189.8A 2015-07-10 2016-07-08 Compositions destinées à une utilisation topique Pending EP3319583A1 (fr)

Applications Claiming Priority (2)

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ES201531003A ES2596720B1 (es) 2015-07-10 2015-07-10 Composiciones para uso tópico
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JP2019131549A (ja) * 2018-02-01 2019-08-08 株式会社コーセー 組成物
EP3989921A1 (fr) 2019-06-28 2022-05-04 The Procter & Gamble Company Compositions anti-inflammatoires synergiques
US11701316B2 (en) 2020-12-18 2023-07-18 The Procter & Gamble Company Synergistic anti-inflammatory compositions
WO2024081033A1 (fr) * 2022-10-12 2024-04-18 The Procter & Gamble Company Composition cosmétique comprenant un polymère réticulé de polyacrylate-6 et un tensioactif non ionique à hlb élevé
CN116650347B (zh) * 2023-06-20 2023-12-01 康柏利科技（苏州）有限公司 一种含粉红微藻和千日菊精粹的抗皱精油面膜及其制备方法

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