专利摘要:
Compositions for topical use. The present invention relates to compositions suitable for the topical administration of cosmetic or pharmacological active ingredients. The present invention also relates to the use of said preparations in the treatment and/or non-therapeutic cosmetic care of the skin and/or hair; as well as its use in medicine, in particular, for the treatment and/or prevention of pathological conditions the skin and/or hair. (Machine-translation by Google Translate, not legally binding)
公开号:ES2596720A1
申请号:ES201531003
申请日:2015-07-10
公开日:2017-01-11
发明作者:Puig ANASTASI
申请人:Juvilis Cosmetics S L;Juvilis Cosmetics SL;
IPC主号:
专利说明:

Compositions for topical use
5 Field of the invention
The present invention is framed in the field of compositions for topically administering cosmetic or pharmacological active ingredients. The present invention also refers to the use of said compositions in non-cosmetic treatment.
10 therapeutic and! Or skin and hair care; as well as its use in medicine, in particular, for the treatment and / or prevention of pathological conditions of the skin and / or hair.
Background of the invention
15 Topical administration of cosmetic or therapeutic agents is a challenge in the field of cosmetic formulations! Pharmaceuticals
The skin is a barrier of the body that acts as a 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, granular stratum, spiny stratum and basal stratum, the stratum corneum constituting the surface of the skin and constituting the basal stratum
25 the deepest part of the epidermis. The dermis is under the epidermis and consists mainly of collagen.
The main function of the skin is the regulation of the entry of substances into the body. The stratum corneum provides the main barrier function in the permeability of the skin; measure
30 between 15 and 20 ... 1m thick and consists of 15 to 20 layers of compressed cells, densely grouped, and metabolically inactive, followed by several histologically distinguishable layers formed by clusters, wall to wall, of cells. On the other hand, the membranes of epidermal cells are so tightly bound that there is hardly any intercellular space through which to diffuse polar non-electrolytic molecules
35 or ions. The proteins and lipids of the stratum corneum form a complex interlocking structure, as if they were bricks and lipid mortar. The main lipids that are
found in the stratum corneum include cholesterol and fatty acids. Ceramides, inIn particular, ceramide 2 and ceramide 5, play a very important role in the organizationgeneral of the corneal stratum lipid matrix, and in the skin's barrier function. Theceramides are strongly grouped within the lipid layers due to the5 strength of hydrogen bonds between groups with opposite amide terminations.This fact indicates that there is a transversal organization in addition to the lateral organizationorthorhombic chain of ceramide molecules. The hydrogen bond provides theproperties of resistance, integrity and barrier to the lipid layers of the stratum corneum.This layer is very selective with the typology of molecules transportable through the skin;
10 Thus, only molecules with specific physical-chemical properties can pass through the skin significantly.
The assumptions regarding the absorption of substances in the skin are referred to diffusion through the lipid area of the stratum corneum. More recently, it has been reported that 15 hair follicles are involved in the percutaneous absorption process since they represent a weak point in the skin's shield.
Regarding this fact, topical administration through the hair follicle of active ingredients to the different layers of the skin, including the epidermis and dermis (US) has been described.
20 2005/0238606).
The nanoparticles have been widely studied as topical drug release systems, in particular, as a reservoir on the surface of the skin from which in a controlled manner the release over time of a drug can be achieved, however in such systems the nanoparticles do not penetrate beyond the surface layers of the skin barrier (Campbeli et al., J Control Release, 2012, 162, 201
207)
In other administration systems, it has been described that nanoparticles penetrate the
30 follicular hole. However, these nanoparticles remain in the follicle, but their penetration into the viable skin tissue has not been detected (Lademann et al., Skin Pharmaco / App / Skin Physio /., 1999, 12, 247-56].
There is a need to find topical administration systems for cosmetic and pharmacological active ingredients that are capable of penetrating the skin efficiently and allowing transfolicular absorption of nanoparticles.
Summary of the Invention
The first aspect of the present invention is related to a composition that
5 comprises: a) an oil with a 0o value of 15 to 18, an Op value of 2 to 5 and an OH value of 2 to 5; b) a surfactant selected from the group consisting of polyethylene glycol ethers of oleyl alcohol or stearyl alcohol with 10 to 22 units of ethylene oxide, sorbitan laurates, sorbitan oleates, polysorbates and mixtures thereof;
10 c) a nanoparticle selected from the group consisting of hydroxyapatite nanoparticles, tri-calcium phosphate nanoparticles, poly-lactic-coglycolic acid nanoparticles, hyaluronic acid nanoparticles and mixtures thereof; d) a cosmetically or pharmacologically active ingredient with 0o, Op and OH such that
.) 4 (00 19.5) '+ (op 10.1)' + (OH 13.0) ''; 9;
E) optionally, an absorption aid through the skin; and f) optionally water;
J112
where 0o, Op and OH are Hansen's solubility parameters expressed in · cm-3/2.
In a second aspect, the present invention refers to the use of a composition according to the first aspect, in which the active ingredient is a pharmaceutical active ingredient, to prepare a medicament.
In a third aspect, the present invention refers to the use of a composition according to the first aspect, in which the active ingredient is an ingredient
25 active pharmacological, in the preparation of a medicament for the treatment and / or prevention of a pathology of the skin and / or hair selected from a group consisting of microbial infections, fungal infections, and pathological hair loss.
In a fourth aspect, the present invention refers to the use of a composition according to the first aspect, in which the active ingredient is a cosmetic active ingredient, in the cosmetic treatment and / or non-therapeutic care, of the skin and / or hair.
Description of the invention
35 Determination of Hansen parameters Hansen solubility parameters were developed by Charles Hansen as a way to predict whether one material will dissolve in another. There are three Hansen parameters: -oo, which corresponds to the energy of the dispersion force between the molecules,
5 -óp, which corresponds to the energy of the intermolecular dipole force between the molecules, and -ÓH, which corresponds to the energy of the hydrogen bonds between the molecules.
These three parameters can be treated as coordinates to represent a point in a three-dimensional space, also known as the Hansen space. The more 10 next two molecules are in this three-dimensional space, the more likely they are to dissolve with each other.
The Hansen parameters of a compound can be determined following the binary solvent gradient method published by Machui et al. [Solar Energy Materia / s Solar Cells, 15 2012, 100, 13.8-146]. This method analyzes the solubility of any compound in a series of solvents with known Hansen parameters (as described for example in Hansen Solubility Parameters: A Users' Handbook. With an updated database at http://hansen-solubility.com /Contents/HSPiPDataSet.xls). The Hansen parameters of said compound are located in the center of a sphere in the Hansen space where the
20 radius R indicates the maximum difference in affinity tolerable for complete dissolution, as explained below. Good solvents remain inside the sphere and bad solvents remain outside the sphere.
In a first step the solubility of the compound is determined in a reduced number of
25 pure solvents, in order to identify at least one good solvent and one bad solvent for the compound. The solvents used in this first stage are, for example, toluene, propylene carbonate, 2-propanol, acetonitrile, hexane and dimethylsulfoxide (DMSO), isopropyl myristate, dicaprilyl ether, water, tetrahydrofuran, glycerol, diethylene glycol, can also be used. dimethyl formamide and 1,4-dioxane. The determination is
30 by stirring the compound under study (approximately 70 mg) with approximately 5 ml of each of the solvents mentioned above for 30 minutes at 800 rpm. Next, the sample is examined visually and the solvent is classified as a "good solvent" if a clear solution or a suspension that does not form sediments is obtained after standing for 1 hour. Otherwise the solvent is classified
35 as a "bad solvent". Next, binary mixtures of solvents are used, which comprise a good solvent and a bad solvent in a volume ratio of 3: 1, 2: 3
and 1: 3, or if more values are necessary to improve the accuracy of the binary solvent mixture method, the mixtures may comprise a good solvent and a bad solvent in a volume ratio of 17:86, 29:71, 43 : 57, 57:43, 71: 29 and 86:14, although other volume ratios can also be used.
The Hansen parameters of a binary solvent mixture correspond to the sum of the volume contributions of each solvent. For example, the Hansen parameters of a mixture containing 29% by volume of a good solvent A, represented by the Hansen parameters ÓOA, ÓPA and ÓHA. And 71% by volume of a bad solvent B represented
1st by Hansen parameters Ó08, ÓP8 and ÓH8. it would be calculated as follows: Óome ~ Cla = 0.29 · oOA + 0.71 · or08 Ópme ~ cla = 0.29 · oPA + 0.71 · oP8 ÓHme ~ cla = 0.29 · ÓHA + 0.71 · ('5H8
15 Table 1 shows the Hansen parameter values of some pure solvents.
Table 1. Hansen parameters of solubility of some pure solvents.
Solvent OrderopOh
Toluene 181.42
Propylene Carbonate twenty184, 1
2-Propanol 15.860116.4
Acetonitrile 15.3186.1
Hexane 14.9OROR
Isopropyl Myristate 16.22.43.7
Ether Dicaprilil 16.12.22
Water 15.51642.3
Tetrahydrofuran 16.85.78
Glycerol 17.411, 327.2
Diethylene glycol 16.61219
Dimethyl formamide 17.413.711, 3
1,4-Dioxane 17.51.89
Next, the solubility of the compound under study in said binary mixtures of solvents is evaluated, assigning a score of 1 to 6 to each sample, as detailed (the assessment is carried out visually observing the result of the mixture of the
composed with the solvent (s) in a glass test tube or other suitable container of a transparent material and with the help of a millimeter paper bottom, with the following parameters):
1 = completely dissolved (no aggregates) and no turbidity (clear solution);
2 = completely dissolved (no aggregates) and turbidity (you can see the graph paper
background);
3 = completely dissolved (without aggregates) and strong turbidity (you cannot see the role of
background graphic);
4 = Not completely dissolved (small aggregates) and strong turbidity (cannot be seen
the background graphic paper);
5 = Not completely dissolved (small aggregates) and turbidity (you can see the paper
background graphic);
6 = Do not touch (large aggregates) and without turbidity (clear solution).
The solution refers to the loss of integrity of the compound and to be visibly less massive. Turbidity refers to the degree of transparency, the limits being a clear solution and the ability to see through an unclear solution.
In the case of particles, such as nanoparticles representing component c) of the composition of the present invention, "solubility" is determined as the sedimentation rate or lack thereof. The sedimentation rate is the time for the nanoparticles studied to settle in the solvent (in particular in the binary mixtures of solvents defined above) and quantified by the relative sedimentation time (RST) using the following formula:
RST = t, (pp -p,) / ~ where ts is the settling time (expressed in seconds), pp is the density of particles (expressed in g / mi), Ps is the density of the solvent (in particular of the binary solvent mixture; expressed in g / mi) and '1 is the viscosity of the solvent (in particular of the binary solvent mixture; expressed in mpa · s). The assignment of the score from 1 to 6 from the RST values is carried out by assigning the score 6 to the shortest times of all the solvents studied for the same particle (in particular of all the binary mixtures of solvents studied), while the longest and most stable dispersions obtained lower values when applying the following equation:
Score = n - ((n-1) 'RSTlMaxRST)
where n is the value of the maximum study score (for example 6), RST is the relative settling time and MaxRST is the maximum value of the relative settling time obtained in the study (that is, for the same particle in all the solvents, in particular in the binary mixtures of solvents tested). Punctuation value
5 obtained is rounded to the unit.
The solvents of the binary mixtures are represented in the Hansen space according to their Hansen parameters, and the Hansen parameters of the particular compound are then calculated by adjusting a solubility sphere in which all the good mixtures of solvents are found within it (i.e., those with scores of 1-3) and all bad solvent mixtures are found outside of it (i.e., those with scores of 4-6). An algorithm adjusts a sphere in 3D Hansen space (Bo, op Y ot-t) minimizing the number of so-called erroneous solvents, which includes a) good solvents that are outside the sphere and b) bad solvents inside the sphere . It is established that if there are different spheres without erroneous solvents, the sphere with the smallest radius is selected. If there are different spheres with the same number of erroneous solvents, the sphere with the smallest error distance (distance from a bad solvent inside the sphere or distance from a good solvent outside the sphere) is selected. This adjustment is made by evaluating the data.
20 using the following adjustment quality formula:
DATAFIT = (A, A, ... A ,,) 1 / n, where n is the number of solvents, and A, = e- (error distance), where the error distance is the distance between the wrong solvent and the
25 edge of the dial.
Ai will be equal 1.0 when there is a good solvent inside the sphere, and when there is a bad solvent outside the sphere.
30 The coordinates of the center of the sphere correspond, therefore, to the Hansen óo, op Yót-t parameters of the molecule under study.
Compositions of the invention
Component a) of the composition, according to the first aspect of the present invention is an oil having a Bo value of 15 to 18, a Bp value of 2 to 5 and an or tt value of 2 to 5. Preferably , the oil has an OD value of 15.5 to 16.5. Preferably, the oil has an op value of 2 to 3. Preferably, the oil has an OH value of 2 to 4. More preferably, the oil has an 15.5 to 16.5, an op value of 2 to 3 and an OH value of
2 to 45
The term "oil" is used in the present invention to designate any liquid organic substance at 20 ° C, which has a water solubility of less than 0.05 gIl, preferably less than 0.01 gIl, more preferably less than 0.001 gIl, even more preferably less than 0.0001 gIl. The oil includes petroleum derivatives, or oils of
10 animal, plant or synthetic origin, whose Hansen parameter values are as defined above.
Non-limiting examples of oils having a 00 value of 15 to 18, an op value of 2 to 5 and an OH value of 2 to 6 are; Isopropyl myristate, dicaprilyl ether, squalane, oleyl erucate,
15 Oleyl oleate, isopropyl palmitate, acai oil, sweet almond oil, soy glycerides, avocado oil and shea butter, whose Hansen parameters are listed in Table 2.
Table 2. Hansen solubility parameters of some oils.
Oil Isopropyl myristate Dicaprilyl ether Squalane Oily erucato Olello oleate Isopropyl palmitate Acai oil Sweet almond oil Soy glycerides Avocado oil Shea butter ORD 16.2 16.1 15.8 16.0 16.0 16.2 16 16 16 16 16op 2.4 2.2 2.1 2.2 2.3 2.3 3 3 3 3 3OH 3.7 2.0 2.2 2.3 2.4 3.8 3 3 2 2 3
In a preferred embodiment, the oil is selected from the group consisting of isopropyl myristate, dicaprilyl ether, squalane, avocado oil and mixtures thereof.
Preferably, the oil (component a)) is present in an amount of 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 with 10 to 22 units of ethylene oxide, sorbitan laurates, oleates of sorbitan, polysorbates and mixtures thereof.
The 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 units of ethylene oxide. Non-limiting examples of oleic alcohol polyethylene glycol ethers with 10 to 22 ethylene oxide units are
15 Oleth-10, Oleth-11, Oleth-12, Oleth-15, Oleth-16 and Oleth-20.
Stearyl alcohol polyethylene glycol ethers are known as Steareth followed by the number of ethylene oxide units, for example Steareth-10 is stearyl alcohol polyethylene glycol ether comprising 10 units of ethylene oxide.
20 Non-limiting examples of stearyl alcohol polyethylene glycol ethers with 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 means sorbitan monolaurate, sorbitan dilaurates, sorbitan trilaurate and mixtures thereof.
Sorbitan oleates means sorbitan monooleate, sorbitan dioleates, sorbitan trioleate, and mixtures thereof.
30 Polysorbates are sorbitan esters with fatty acids such as lauric acid, palmitic acid, stearic acid and oleic acid. The number that follows the polysorbate part is related to the type of fatty acid associated with the polyoxyethylene sorbitan part of the molecule. Monolaurate is indicated at 20, monopalmitate is indicated at 40, monostearate at 60 and monooleate at 80. Non-limiting examples
35 of polysorbates are polysorbate-20, polysorbate-21, polysorbate-40, polysorbate-60, polysorbate-61, polysorbate-65, polysorbate-80, polysorbate-81 and polysorbate-85.
In a preferred embodiment, the surfactant is selected from the group consisting of Oleth10, Oleth-11, Oleth-12, Oleth-15, Oleth-16, Oleth-20, sorbitan monooleate, sorbitan trioleate, polysorbate-20, polysorbate- 21, polysorbate-40, polysorbate-60, polysorbate-61,
5 polysorbate-65, polysorbate-80, polysorbate-81, polysorbate-85 and mixtures thereof; pluspreferably the surfactant is selected from the group consisting of Oleth-10,sorbitan monooleate, polysorbate 80 and mixtures thereof.
Preferably, the surfactant (component b)) is present in an amount of 0.25% to 10 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, tri-calcium phosphate nanoparticles, poly-Ictic acid-co nanoparticles
Glycolic (PLGA), hyaluronic acid nanoparticles and mixtures thereof.
In the context of the present invention, "nanoparticle" means a particle, preferably a spherical particle, with a diameter of 1 nm to 1000 nm, preferably 1 nm to 500 nm, even more preferably 1 nm to 400 nm, even more preferably
From 10 nm to 350 nm, even more preferably from 50 nm to 300 nm, and more preferably from 100 nm to 250 nm.
Preferably, the nanoparticles (component c)) are present in an amount of 0.5% to 2% by weight with respect to the total weight of the composition.
Preferably, when the nanoparticle is a PLGA nanoparticle, the surfactant (component b)) is selected from the group consisting of Oleth-10, Oleth-11, Oleth-12, Oleth-15, Oleth-16 and Oleth-20; preferably from the group consisting of Oleth-10, Oleth-12 and mixture thereof; more preferably, the surfactant is Oleth-10.
Preferably, when the nanoparticle is a hydroxyapatite nanoparticle, the surfactant (component b)) is selected from the group consisting of sorbitan monooleate, sorbitan trioleate, sorbitan monolaurate and mixtures thereof.
Preferably, when the nanoparticle is a tricalcium phosphate nanoparticle, the surfactant (component b)) is selected from the group consisting of polysorbate-20, polysorbate-21, polysorbate-40, polysorbate-60, polysorbate-61, polysorbate-65 , polysorbate-BO,
polysorbate-B1, polysorbate-B5 and mixture thereof; preferably, the surfactant is polysorbate-BO.
5 Preferably, when the nanoparticle is a hyaluronic acid nanoparticle, thesurfactant (component b »is selected from the group consisting of polysorbate-20,polysorbate-21, polysorbate-40, polysorbate-60, polysorbate-61, polysorbate-65, polysorbate-BO,polysorbate-B1, polysorbate-B5 and mixture thereof; preferably, the surfactant is thepolysorbate-BO.
The component d) of the composition according to the first aspect of the present invention is a cosmetically or pharmacologically active ingredient with OD. op Y iHtal that
) 4 (OD 19.5) '+ (op 10.1)' + (OH 13.0) 'S 9
15 where Ó Y IH are Hansen's solubility parameters of ingredient 312
cosmetically or pharmacologically active expressed in J 112 · cm-. These parameters
Hansen can be determined as explained above.
A cosmetically active ingredient is a compound or mixture of compounds that exerts
20 a beneficial effect on the skin and / or hair, such as the improvement or maintenance of the cosmetic qualities of the skin and / or hair, for example the level of hydration, elasticity, firmness, brightness, tone and texture, among others.
A pharmacologically active ingredient is a compound or mixture of compounds that
25 prevents and / or treats a disease or disorder of the skin and / or hair, such as microbial infections, fungal infections, and / or pathological loss of hair, among others_
In a preferred embodiment, the cosmetically active ingredient is selected from the group
30 consisting of antioxidants, moisturizers, skin conditioning agents, antistatic agents, softening agents, soothing agents, emollient agents, astringent agents, anti-seborrheic agents, anti-dandruff agents, tonics, bleaching agents, cleansing agents, keratolytic agents, lipid agents, agents with tensor effect, anti-wrinkle agents, repairing agents, regenerating agents, firming agents,
35 energizing agents, bulking agents, anti-dark agents, anti-bag agents, pore-minimizing agents, protective agents and mixtures thereof;
or the pharmacologically active ingredient is selected from the group consisting of antimicrobial agents, anti-inflammatory agents, fungicides, agents that prevent hair loss.
When mixtures of cosmetically or pharmacologically active ingredients are used, the Hansen parameters of the mixture correspond to the sum of the contributions by weight of each of the compounds.
10 An antioxidant is a compound that inhibits reactions caused by oxygen, thus preventing oxidation reactions. These compounds also prevent the thinning of the compositions. Non-limiting examples of antioxidants having suitable oo, op, and OH values are CameJ / ia sinensis leaf extract, trans-resveratrol, alpha-lipoic acid, nordihydroguaiartic acid, caffeine, Aloe vera, ascorbyl palmitate, alpha-arbutin,
15 arbutin, extract of Echinacea pupurea, niacinamide and astaxanthin.
A moisturizer is a compound that increases the water content of the skin and helps keep it soft and smooth. Non-limiting examples of moisturizers having suitable 150, 15p and Y15H values are Echinacea pupurea extract, niacinamide and pyroglutamic acid.
20 A skin conditioning agent is a compound that keeps the skin in good condition. Non-limiting examples of skin conditioning agents having suitable Io, Ip and ÓH values are Echinacea pupurea extract, Camellia sinensis leaf extract, salicylic acid, biotin, Helichrysum arenarium flower extract, Chamomilla flower extract
25 recutita, Ginkgo biloba leaf extract, Aloe vera, caprililo glycol, Ranunculus ficaria extract, Centella asiatica extract, Aesculus hippocastanum seed extract, ethyl nicotinate, glycyretinic acid, alpha-arbutin, arbutin, bark extract Enables chlorantha, astaxanthin, flower extract of Spilanthes acmella and benzyl nicotinate.
30 An antistatic agent is a compound that reduces static electricity, neutralizing the electrical charge on a surface. Non-limiting examples of antistatic agents having suitable values of 60, OP and OH are niacin, acrylate copolymer and benzyl nicotinate.
35 A softening agent is a compound that decreases the roughness of the skin or its irregularities, thus achieving a smooth skin surface. Non-limiting examples of softening agents having suitable 60, 15p and 15H values are niacin, Spirulina maxima extract, niacinamide and Centella asiatica extract.
A soothing agent is a compound that helps relieve discomfort in the skin or scalp. Non-limiting examples of soothing agents having suitable 150, 15p and 15H values are methyl nicotinate, Centella asiatica extract and Echinacea pupurea extract.
An emollient agent is a compound that softens the skin. Non-limiting examples of emollient agents having suitable 150, 15p and 15H values are CameJ / ia sinensis leaf extract, Panax ginseng root extract, glyceryl stearate, and caprilyl glycol.
An astringent agent is a compound that contracts the skin. A non-limiting example of an astringent agent having suitable 150, 15p and 15H values is the leaf extract of
CameJ / ia sinensis.
An antiseborrhoeic agent is a compound that helps control sebum production. Non-limiting examples of antiseborrhoeic agents having oo values, 15p Y15H suitable are biotin and Enantia eh / orantha bark extract.
An anti-dandruff agent is a compound that helps control dandruff. A non-limiting example of an anti-dandruff agent having suitable ID, Ip Y IH values is salicylic acid.
A tonic is a compound that produces a feeling of well-being in the skin and hair. Non-limiting examples of tonics that have ID, Ip and IHadacuados values are Echinacea pupurea extract, Camellia sinensis leaf extract, Panax ginseng root extract, methyl nicotinate and Centella asiatiea extract.
A bleaching agent is a compound that lightens skin tone or corrects imperfections in skin pigmentation by decreasing the concentration of melanin. Non-limiting examples of bleaching agents having suitable ID, Ip and IH values are glabridin, alpha-arbutin yarbutin.
A cleaning agent is a compound that helps keep the surface of the body (skin and / or hair) clean. Non-limiting examples of cleaning agents having suitable 15o • op and Ó values are Centella asiatica and alpha-lipoic acid.
5 A keratolytic agent is a compound that helps remove dead cells from thehorny layer A non-limiting example of a keratolytic agent that has values oo, op YÓHSuitable is salicylic acid.
A lipid agent is a compound that replenishes the lipids of the hair or upper layers of the skin. A non-limiting example of a lipid agent having suitable 15o, oP and ÓH values is ceramide C (6).
A tensor effect agent is a compound that tightens the skin. A non-limiting example of an agent with tensor effect having suitable 15o, op and Oh values is the 15 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 50, OP and OH values are ascorbyl palmitate and niacinamide.
20 A repairing agent is a compound that helps the body restore alterations produced in the skin such as scars. Non-limiting examples of repair agents having suitable 15o, oP and ÓH values are Centella asiatica extract and Echinacea purpurea extract.
25 A regenerating agent is a compound that helps the skin in its self-regeneration through mechanisms such as cell stimulation. A non-limiting example of a regenerating agent that has suitable o, o and Y H values is Centella asiatica extract.
A firming agent is a compound that provides firmness to the skin. Non-limiting examples
of reaffirming agents that have suitable oO, op YÓH values are biotin and niacinamide.
An energizing agent is a compound that brings combined luminosity and astringency to the skin. Non-limiting examples of energizing agents having suitable oo, Óp and ÓH values are trans-resveratrol, Panax ginseng root extract, and Camellia sinensis leaf extract.
An agent that provides volume is a compound that stimulates skin adipocytes. A non-limiting example of an agent that provides volume that has 15o values, or p and OH, is Centella asiatica extract.
An anti-dark agent is a compound that reduces pigmented areas under the eyes. Non-limiting examples of antiojera agents having suitable 15o, I p and ÓH values are caffeine, Camellia sinensis leaf extract and Gingko biloba leaf extract.
An anti-bag agent is a compound that reduces swelling, usually in the area around the eye. Non-limiting examples of antibolous agents having suitable o, op and Ó values are; Caffeine, Aesculus hippocasstanum seed extract and Chamomilla recutita flower extract.
A pore minimizing agent is a compound that helps clean pores and reduce their appearance. A non-limiting example of a pore minimizing agent that has 150, I p YÓH values is Rannuculus ficaria extract.
A protective agent is a compound that protects the skin against external agents. Non-limiting examples of protective agents having suitable And D, Op and IH values are trans-resveratrol, Centella asiatica extract and niacinamide.
An antimicrobial agent is a compound that helps control the growth of microorganisms in the skin. Non-limiting examples of antimicrobial agents having suitable ID, Ip and IH values are Camellia sinensis leaf extract, ferulic acid, resorcinol hexyl, Enantia chlorantha bark extract and Sphilanthes acmella flower extract.
A fungicide is a compound that helps control the growth of fungus on the skin. A non-limiting example of a fungicide that has oo values, Ip Y IH is pyraclostrobin.
An anti-inflammatory agent is a compound that reduces inflammation. A non-limiting example of an anti-inflammatory agent that has adequate! 3o,! 3p and! 3H values is glabridin.
5 An agent that prevents hair loss is a compound that stimulates hair growth and / or prevents its loss. A non-limiting example of an agent that prevents hair loss that has adequate oo, op and ÓH values is finasteride.
Therefore, in a particular embodiment, the present invention refers to a
Composition as defined herein, wherein the cosmetically or pharmacologically active ingredient is selected from the group consisting of Echinacea pupurea extract, niacin, CameJlia sinensis leaf extract, Spirulina maxima extract, salicylic acid, ferulic acid , biotin, Helichrysum arenarium flower extract, acrylate copolymer, trans-resveratrol, Chamomilla reeutita flower extract,
15 niacinamide, alpha-lipoic acid, resorcinol hexyl, nordihydroguaiartic acid, Panax ginseng root extract, Ginkgo biloba leaf extract, pyraclostrobin, caffeine, pyroglutamic acid, ceramide C (6), glyceryl stearate, Aloe vera, palmitate ascorbyl, caprylic glycol, Rannueulus ficaria extract, methyl nicotinate, Centella asiatiea extract, Aeseu / us hippoeastanum seed extract, ethyl nicotinate, acid
20 glycyretin, alpha-arbutin, arbutin, bark extract of Enantia eh / orantha, astaxanthin, benzyl nicotinate, flower extract of Spilanthes aemeJla, finasteride, glabridin and mixtures thereof. Table 3 provides the oo, Ip and IH values of some cosmetically or pharmacologically active ingredients.
25 Table 3. Hansen parameters of solubility of some cosmetically or pharmacologically active ingredients.
Assets ~ D~ p~ H
Eehinaeea pupurea Extract 19.710.413.5
Niacin 19.9911, 4
CameJlia sinensis leaf extract 19.57.912.9
Spirulina maxima extract 1910fifteen
Salicylic acid 19.77.915.1
Ferulic acid 19.38.415.8
Biotin 18.712.912.2
Heliehrysum flower extract 20.811, 616
Arenarium Actives Trans-resveratrol Acrylate Copolymer Flm de Chamomilla recutita Niacinamide Alpha Lipoic Acid Resorcinol Hexylo Nordihydroguaiartic Acid Panax Root Extract Ginseng Ginkgo Biloba Leaf Extract Pyraclostrobin Caramoglycetic Acrylic Ceramide (6) Vera Ascorbyl palmitate Caprililglycol Ranuncu extract / us ficaria Methyl nicotinate Centella asiatica extract Semi-extract of Aesculus hippoeastanum semicotinate Ethyl nicotinate Glycyretinic acid Alpha-arbuti na Arbutin Bark extract of Entathin oxanthine Extant oxanthine extract By Spilanthes acmella Finasterida 00 17.8 20.6 20 19.8 18 18.2 18.5 18.7 16.9 20.1 19.5 19.6 16.7 16.5 17.6 16, 7 16.8 20 18.7 17.8 20 18.3 18.3 18.4 18.4 19.6 18.4 19.4 17.5 19 O, 7.5 7.5 11.6 15.4 7.1 5.4 5.2 5.4 11, 5 11, 4 10.1 15.2 8.4 8 14.1 6.8 5, 8 10 9 5.2 12 8.3 5.6 12.2 12.2 3.3 5.6 7.9 7.3 11OH 12.7 15.9 17.1 13.1 9.5 11, 6 15 10.2 14.9 7.4 13 16 10.3 11, 8 16.4 11, 8 13.9 20 6.2 9.1 20 5.4 6.6 20.6 20.6 8 6.2 4.5 6 15
I Assets
In a particular embodiment, the ingredient cosmetically or pharmacologically has values of i5o, i5p Yi5H such that
..) 4 (OD -19.5) 2 + (op 10.1) 2 + (OH 13.0) 2 "6,
5 where i5o, i5p Yi5H are the Hansen solubility parameters expressed in J1I2 · cm · 3I2.
In a preferred embodiment, the active ingredient in the composition according to the present invention is a cosmetically active ingredient.
In another preferred embodiment, the active ingredient in the composition according to the present invention is a pharmacologically active ingredient.
Preferably, the cosmetic or pharmacologically active ingredient (component d)) is present in an amount of 2% to 15% by weight with respect to the total weight of the composition.
The compositions of the present invention may optionally comprise an absorption aid through the skin (component e)). Preferably, said absorption aid through the skin is present in the compositions of the
20 invention.
An absorption aid through the skin is a compound that facilitates the passage of molecules through the corneal layer of the skin. Non-limiting examples of absorption aids through the skin are dimethyl isosorbide, transcutol (i.e. 2- (225 ethoxyethoxy) ethanol), propylene glycol, oleic acid, ethanol, dimethyl sulfoxide, dodecyl-N, N-dimethylaminoacetate, acetate ethyl, sodium dodecyl sulfate, d-limonene, 1,3-diphenylurea, Nmethyl-2-pyrrolidone, beta-cyclodextrin and Azone® (i.e., N-dodecylcaprolactam). Preferably, the absorption aid through the skin is selected from the group consisting of dimethyl isosorbide, transcutol (i.e. 2- (2-ethoxyethoxy) ethanol) and mixtures of
30 the same.
Preferably, the absorption aid through the skin (component e »ispresent in an amount of 0.2% to 0.8% by weight with respect to the total weight of thecomposition.
The compositions of the present invention may optionally comprise water(component f ". Preferably, water is present in the compositions of theinvention.
Preferably, water (component f "is present in an amount of 0.01% to 10% inweight with respect to the total weight of the composition.
In a particular embodiment, the composition of the present invention comprises:a) an oil selected from the group consisting of isopropyl myristate, ether ofdicaprilil, escualano avocado oil and mixtures thereof;b) a surfactant selected from the group consisting of Oleth-10, sorbitan monooleate,sorbitan trioleate, polysorbate-80 and mixtures thereof;c) a nanoparticle selected from the group consisting of nanoparticles ofhydroxyapatite, tricalcium phosphate nanoparticles, poly-Ictic acid-co nanoparticlesglycolic, hyaluronic acid nanoparticles and mixtures thereof;d) a cosmetically or pharmacologically active ingredient with i5o, i5p Yi5H such that
.J4 (OD -19.5) '+ (op -10.1)' + (OH -13.0) '"6;
e) optionally, an absorption aid through the skin selected from the group consisting of dimethyl isosorbide, transcutol (ie 2- (2-ethoxyethoxy) ethanol) and mixtures thereof; and f) optionally water; where i5o, i5p Yi5H are the Hansen solubility parameters expressed in J1I2 · cm · 312.
In another particular embodiment, the composition of the present invention comprises: a) from 65% to 90% by weight with respect to the total weight of the composition of an oil selected from the group consisting of isopropyl myristate, dicaprilyl ether, squalane oil of avocado and mixtures thereof; b) from 0.25% to 2% by weight with respect to the total weight of the composition of a surfactant selected from the group consisting of Oleth-10, sorbitan monooleate, sorbitan trioleate, polysorbate-80 and mixtures thereof; c) from 0.5% to 2% by weight with respect to the total weight of the composition of a nanoparticle selected from the group consisting of hydroxyapatite nanoparticles, tricalcium phosphate nanoparticles, poly-Ictic-co-glycolic acid nanoparticles, nanoparticles of hyaluronic acid and mixtures thereof;
5 d) from 2% to 15% by weight with respect to the total weight of the composition of a cosmetically or pharmacologically active ingredient with oo, op YÓH such that
.J4 (oo -19.5) '+ (Op -10.1) 2 + (OH -13.0)': 5 9; e) from 0.2% to 0.8% by weight with respect to the total weight of the composition of a skin absorption aid selected from the group consisting of dimethyl isosorbide,
10 transcutol (ie 2- (2-ethoxyethoxy) ethanol) and mixtures thereof; and f) from 0.01% to 10% by weight with respect to the total weight of the water composition; where ÓO, Ó YÓH are the Hansen solubility parameters expressed in J1I2 · cm · 3I2.
In another particular embodiment, the composition of the present invention comprises:
15 a) from 65% to 90% by weight with respect to the total weight of the composition of an oil selected from the group consisting of isopropyl myristate, dicaprilyl ether, squalane avocado oil and mixtures thereof; b) from 0.25% to 2% by weight with respect to the total weight of the composition of a surfactant selected from the group consisting of Oleth-10, sorbitan monooleate, trioleate
20 sorbitan, polysorbate-BO and mixtures thereof; c) from 0.5% to 2% by weight with respect to the total weight of the composition of a nanoparticle selected from the group consisting of hydroxyapatite nanoparticles, tricalcium phosphate nanoparticles, poly-Ictic-co-glycolic acid nanoparticles, nanoparticles of hyaluronic acid and mixtures thereof;
D) 2% to 15% by weight with respect to the total weight of the composition of a cosmetically or pharmacologically active ingredient with OO, Óp and ÓH such that .J4 (Oo 19.5) 2 + (Op 10.1) 2 + (OH 13.0) ': 5 6;
e) from 0.2% to 0.8% by weight with respect to the total weight of the composition of a skin absorption aid selected from the group consisting of dimethyl isosorbide,
Transcutol (ie 2- (2-ethoxyethoxy) ethanol), and mixtures thereof; and f) from 0.01% to 10% by weight with respect to the total weight of the water composition; where ÓO, Óp and ÓH are the Hansen solubility parameters expressed in J2cm3I2.
Preferably, the cosmetically or pharmacologically active ingredient in said specific compositions is selected from a group consisting of Echinacea pupurea extract, niacin, Camellia sinensis leaf extract, Spiru / ina maxima extract, salicylic acid, ferulic acid, biotin, Heliehrysum arenarium flower extract, acrylate copolymer, trans-resveratrol, Chamomilla reeutita flower extract, niacinamide, alfalipoic acid, resorcinol hexyl, nordihydroguaaric acid, Panax ginseng root extract, Ginkgo biloba leaf extract, pyraclostrobin, pyraclostrobin , pyroglutamic acid, ceramide C (6), glyceryl stearate, Aloe vera, ascorbyl palmitate, eaprililglieol, Ranuneulus fiearia extract, methyl nicotinate, Centella Asiatiea extract, Aeseulus hippoeastanum seed extract, ethyl nicotinate, gretic acid , alpha-arbutin, arbutin, Enanta eh / orantha bark extract, astaxanthin, nicotinat or of benzyl, flower extract of Spilanthes aemella, finasteride, glabridin and mixtures thereof.
The preparations of the present invention may also comprise additional ingredients. Such additional ingredients have 50, 5p YOH such that
) 4 (8D 19.5) 2 + (8p 10.1) 2 + (8 "13.0) 2 ,; 9
where iD, ip YÓH are the Hansen solubility parameters expressed in JlI2 · cm · 3I2.
Non-limiting examples of such additional ingredients are emulsion stabilizing agents, emulsifiers, humectants, gelling agents, viscosity controlling agents, perfumes and preservatives.
An emulsion stabilizing agent is a compound that helps in the emulsification process and improves the stability of the emulsion and the shelf life of the preparations. Non-limiting examples of emulsion stabilizing agents having suitable 50, 5p and 5H values are carbomer, crosslinked polyacrylate-6 polymer 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. Non-limiting examples of emulsifiers having suitable o, o, and OH values are glyceryl stearate, polysorbate-20, octadecenedioic acid and PEG-60 almond glycerides.
A humectant is a compound that contains and retains moisture. Non-limiting examples of humectants having suitable ID, Ip YÓH values are Camellia sinensis leaf extract, pyroglutamic acid, ceramide C (6) and A / oe vera.
A gelling agent is a compound that gives gel consistency to the composition. A non-limiting example of a gelling agent having suitable OD, op and OH values is the carbomer.
5 A viscosity control agent is a compound that increases or decreases viscosityof the composition. Non-limiting examples of viscosity control agents havingValues iD, ip Y iH are carbomer, crosslinked polyacrylate-6 polymer,hydroxypropyl methyl cellulose and disodium EDTA.
A perfume is a compound used to perfume the compositions. Non-limiting examples of perfumes having suitable ID, I p Y IH values are Citrus aurantium flower extract, phenylpropanol and ethyl nicotinate.
A preservative is a compound that stops or minimizes the deterioration caused by the presence of different types of microorganisms. Non-limiting examples of preservatives having OD values, IP YOH are methylpropanediol, caprylic glycol and phenylpropanol.
The preparations of the present invention may also comprise cyclopentasiloxane and / or cyclohexasiloxane. Preferably in an amount of 5% to 15% by weight with respect to the total weight of the composition.
Other ingredients used in cosmetic preparations! Pharmacological and known in the art may also be present, preferably in an amount of less than 15% by weight with respect to the total weight of the composition.
In a preferred embodiment, the composition of the present invention comprises:a) from 65% to 90% by weight with respect to the total weight of the composition, of an oil thatIt has an OD value of 16 to 118, an OP value of 2 to 5, and an OR value of 2 to 5;b) from 0.25% to 2% by weight with respect to the total weight of the composition of a surfactant
30 selected from the group consisting of polyethylene glycol ethers of oleyl alcohol or stearyl alcohol having 10 to 22 units of ethylene oxide, sorbitan laurates, sorbitan oleates, polysorbates and mixtures thereof; c) from 0.5% to 2% by weight with respect to the total weight of the composition, of a nanoparticle selected from the group consisting of hydroxyapatite nanoparticles,
35 tricalcium phosphate nanoparticles, poly-Ictic-co-glycolic acid nanoparticles, hyaluronic acid nanoparticles and mixtures thereof; d) from 2% to 15% by weight with respect to the total weight of the composition of a cosmetically or pharmacologically active ingredient with Ó, OP YÓH such that
..j4 (lio -19.5) '+ (lip -10.1)' + (lin -13.0) '~ 9;
e) from 0.2% to 0.8% by weight with respect to the total weight of the composition of a
5 absorption aid through the skin; Yf) from 0.01% to 10% by weight with respect to the total weight of the water composition;where ÓD, op YÓH are the Hansen solubility parameters expressed in J1I2 · cm · 3a.
The compositions of the present invention have been designed for the topical administration of cosmetically or pharmacologically active ingredients. Therefore, the compositions of the present invention are topically shaped compositions.
In a preferred embodiment, 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.
Uses of the compositions of the invention
The term "treatment", as used in the context of this invention, when not
20 accompanied by the qualifications "cosmetic, non-therapeutic", refers to the administration 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.
The term "treatment", when accompanied by the qualifications "cosmetic, non-therapeutic", refers to the application of the composition of the invention on the skin and / or hair, in particular, with the aim of improving cosmetic qualities of the skin and / or hair, such as, and not limited to these, its level of hydration, elasticity, firmness, wrinkles, shine, 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 and in those with diseases and / or disorders of the skin and / or hair.
The term "prevention", as used in this invention, refers to the ability
of a composition of the invention to prevent, delay, or prevent the onset or development of a disease or disorder before its appearance.
5 The preparations of the present invention may comprise as an ingredientpharmacologically active, the active ingredient defined as component d).
Therefore, in a second aspect, the present invention refers to the use of a composition as defined above, in which the active ingredient is a pharmacologically active ingredient, to prepare a medicament.
The invention also refers to a composition according to the first aspect, in which the active ingredient is a pharmacologically active ingredient, for use in medicine.
In a third aspect, the present invention refers to the use of a composition according to the first aspect, in which the active ingredient is a pharmacologically active ingredient, in the manufacture of a medicament for the treatment and / or prevention of a condition pathology of the skin and / or hair, selected from the group that
20 consists of microbial infections (such as acne), fungal infections (such as seborrheic dermatitis) and pathological hair loss.
The invention also refers to a composition according to the first aspect, in which the active ingredient is a pharmacologically active ingredient, for use in the
25 treatment and / or prevention of a pathological condition of the skin and / or hair selected from the group consisting of microbial infections, fungal infections and pathological hair loss.
The invention also refers to a method for the treatment and / or prevention of a
30 pathological condition of the skin and / or hair selected from the group consisting of microbial infections, fungal infections and pathological hair loss, which comprises administration to a patient in need of such treatment and / or prevention of a therapeutically effective amount of a composition according to the first aspect in which the active ingredient is a pharmacologically active ingredient.
In a fourth aspect, the present invention refers to the use of a composition according to the first aspect, in which the active ingredient is a cosmetic active ingredient, in non-therapeutic cosmetic treatment and / or skin care and / or hair, preferably, in which the non-therapeutic cosmetic treatment and / or skin care and / or
5 hair is selected from the group consisting of the treatment and / or prevention of aging and / or photoaging and the treatment and / or prevention of wrinkles.
In the context of the present invention, the term "aging" refers to changes experienced by the skin with age (chrono-aging) or through exposure to the sun (photo-aging), or to extreme cold or weather conditions. wind, chemical contaminants or pollutants, and includes all external changes visible and / or noticeable through touch, as non-limiting examples, the development of discontinuities in the skin such as wrinkles, fine lines, expression lines, stretch marks, wrinkles, irregularities or roughness, increased pore size, loss of hydration, loss of elasticity, loss of firmness, loss of softness, loss of ability to recover from deformations, loss of resilience, sagging skin such as sunken cheeks, the appearance of bags under the eyes, or the appearance of a double chin, among others, changes in the color of the skin, such as marks, redness, bags or the appearance of hyperpigmented areas such as age spots 20 or freckles among others, abnormal differentiation, hyperkeratinization, elastosis, keratosis, hair loss, orange peel, loss of the structure of COlagen and other histological changes of the corneal layer, the dermis, epidermis, the vascular system (for example the appearance of spider veins or telangiectasias) or tissues close to the skin, among others. The term "photoaging" groups the set of processes caused by prolonged exposure of the skin to ultraviolet radiation that results in premature aging of the skin and has the same physical characteristics as aging, as non-limiting examples, sagging, sinking, color changes
or irregularities in pigmentation 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.
The compositions of the invention can be applied to the area of the skin and / or hair 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. Examples of preferable skin areas for treatment are the face, including the forehead, chin, nose, cheeks and area
around the eyes, such as the eyelids, the area under the eyes, the area between the eyes, the area around the eyes at the opposite end of the area between the eyes (usually where crow's feet appear), the neck and The cleavage
5 Preparation of the compositions
The compositions of the present invention can be prepared by any suitable method known in the field of topical pharmacological formulations, where the following are involved, by way of non-limiting example; premix, heat, cool,
10 homogenize, mix, retrovaporate, filter, centrifuge, apply vacuum pressure, dry.
In a particular embodiment the method of preparation comprises heating the fatty phase, or one or more of the oils, which have a 50 value from 15 to 18, a 5p value from 2 to 5 and a 5H value from 2 to 5, that is , component a) of the composition of the present invention, in a
15 fuser (reactor) up to 70 ° C with constant stirring with blades until complete homogenization. If the composition comprises optional water (component f) of the composition of the present invention), then said optional water is added to the reactor at room temperature and heated to 60 ° C with constant stirring with 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 10 to 22 units of ethylene oxide, sorbitan laurates, sorbitan oleates, polysorbates, is premixed in another reactor that is, component b) of the composition of the present invention, with one or more of the
25 nanoparticles selected from the group consisting of hydroxyapatite nanoparticles, tricalcium phosphate nanoparticles, poly-Ictic-co-glycolic acid nanoparticles, hyaluronic acid nanoparticles, that is, component e) of the composition of the present invention, optionally the absorption aid through the skin, that is, the optional component d) of the composition of the present invention, and one or more
30 of the cosmetically or pharmacologically active ingredients with 0 0, 5p and OH such that
J 4 (OD 19.5) '+ (op 10.1)' + (OH 13.0) ': 5 9,
that is, component d) of the composition of the present invention.
The previously prepared fat phase (component a) is then cooled to 40 ° C and
Optionally water) and the premix of components b) -d) and optionally e) is added to said fatty phase with constant stirring with blades until complete homogenization.
ExamplesExample 1
Composition for a day lotion:
Ingredient Squalane Avocado oil Polysorbate-BO Nanoparticles of Tricalcium Phosphate Echinacea pupurea extract Trans-resveratrol Ascorbyl palmitate Caffeine Citrus aurantium flower extract 2- (2-ethoxyethoxy) ethan 01) Water Cyclopentasiloxane Methylpropanyl glycol (1) ) Crosslinked polyacrylate-6 polymer % by weight 40 25 0.5 1 3 2 2 1 0.3 0.4 7.3 13.5 2 2
Example 2
Composition for a night cream:
Ingredient Squalane Sorbitan monooleate Hydroxyapatite nanoparticles Chamomilla flower extract recutita Centella asiatica extract Echinacea pupurea extract Alpha-arbutin Citrus aurantium flower extract 2- (2-ethoxyethoxy jetan 01 j % by weight 79.5 1 2 3 2 2 2 0.4 0.8
Ingredient Water Methylpropanediol, caprylic glycol, phenylpropanol (preservative) Crosslinked polyacrylate-6 polymer % by weight 3.3 2 2
Example 3Composition for a serum:
Ingredient Squalane Avocado oil Polysorbate-80 Tricocal Phosphate Nanoparticles Spilanthes acmella Aloe vera flower extract Spirulina maxima extract Panax ginseng root extract Niacinamide Ascorbyl palmitate Citrus aurantium flower extract 2- (2-ethoxy) Water Cyclopentasiloxane Methylpropanediol, caprilyl glycol, phenylpropanol (preservative) Cross-linked polyacrylate-6 polymer % by weight 55 15 0.5 1 3 2 2 0.5 0.2 2 0.3 0.4 6.02 8.08 2 2
权利要求:
Claims (12)
[1]
1. A composition comprising: a) an oil having an O value of 15 to 18, an op value of 2 to 5 and an OH value of 2 to 5; b) a surfactant selected from the group consisting of polyethylene glycol ethers of oleyl alcohol or stearyl alcohol having 10 to 22 units of ethylene oxide, sorbitan laurates, sorbitan oleates, polysorbates and mixtures thereof; c) a nanoparticle selected from a group consisting of hydroxyapatite nanoparticles, tricalcium phosphate nanoparticles, polylactic-co-glycolic acid nanoparticles, hyaluronic acid nanoparticles and mixtures thereof
d) a cosmetically or pharmacologically active ingredient with oo, op YÓH such that
../4(OD 19.5) 2 + (Op 10.1) 2 + (OH 13.0) 2: 5 9;
e) optionally, an absorption aid through the skin; Y
f) optionally water;
J 112 312
where óo, op YÓH are Hansen's solubility parameters expressed in · cm-.
[2]
2. A composition according to claim 1, wherein the oil is selected from the group consisting of isopropyl myristate, dicaprilyl ether, squalane avocado oil and mixtures thereof.
[3]
3. A composition according to any of the preceding claims, wherein the surfactant is selected from the group consisting of Oleth-10, Oleth-11, Oleth-12, Oleth-15, Oleth-16, Oleth-20, sorbitan monooleate, trioleate , polysorbate-20, polysorbate-21, polysorbate-40, polysorbate-60, polysorbate-61, polysorbate-65, polysorbate-80, polysorbate-81, polysorbate-85 and mixtures thereof.
[4]
Four. A composition according to any of the preceding claims, wherein the nanoparticles have a size between 100 nm and 250 nm.
[5]
5. A composition according to any of the preceding claims, wherein the absorption aid through the skin is present and is selected from the group consisting of dimethyl isosorbide, transcutol and mixtures thereof.
[6]
6. A composition according to any of the preceding claims, wherein the composition comprises: a) from 65% to 90% by weight with respect to the total weight of the composition of an oil having an O value of 16 to 18, an op value of 2 to 5, and an OH value of 2 to 5;
5 b) from 0.25% to 2% by weight with respect to the total weight of the composition of a surfactant selected from the group consisting of polyethylene glycol ethers of oleyl alcohol or stearyl alcohol having 10 to 22 units of ethylene oxide , sorbitan laurates, sorbitan oleates, polysorbates and mixtures thereof;
10 c) from 0.5% to 2% by weight with respect to the total weight of the composition of a nanoparticle selected from the group consisting of hydroxyapatite nanoparticles, tricalcium phosphate nanoparticles, polylactic-co-glycolic acid nanoparticles, nanoparticles of hyaluronic acid and mixtures thereof;
d) from 2% to 15% by weight with respect to the total weight of the composition of a cosmetically or pharmacologically active ingredient with Ó, OP YÓH such that, / 4 (00 -19.5) '+ (op -10, 1) '+ (OH -13.0)' "9; e) from 0.2% to 0.8% by weight with respect to the total weight of the composition of a skin absorption absorber; and f) from 0.01% to 1.0% by weight with respect to the total weight of the water composition; 20 where iD, ip and iH are the Hansen solubility parameters expressed in J2cm3I2.
[7]
7. A composition according to any of the preceding claims, which 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.
[8]
8. A composition according to any of the preceding claims, wherein the cosmetically active ingredient is selected from the group consisting of antioxidants, moisturizers, skin conditioning agents, antistatic agents, softening agents, soothing agents, emollient agents, astringent agents, 30 anti-seborrheic agents, anti-dandruff agents, tonics, bleaching agents, cleaning agents, keratolytic agents, lipid agents, tensing agents, anti-wrinkle agents, repairing agents, regenerating agents, firming agents, energizing agents, volume-contributing agents, anti-dark agents, agents anti-bags, pore minimizing agents, protective agents and mixtures thereof; or in what ingredient
Pharmacologically active is selected from the group consisting of agents
antimicrobials, anti-inflammatory agents, fungicides and agents that stimulate hair growth and / or prevent hair loss.
[9]
9. A composition according to any of the preceding claims, wherein the active ingredient is a pharmacologically active ingredient.
[10]
10. A composition according to any of the preceding claims, wherein the active ingredient is a cosmetically active ingredient.
11. Use of a composition according to claim 9 to prepare a medicament.
[12]
12. Use of a composition according to claim 9 in the manufacture of a medicament for the treatment and / or prevention of a pathological condition of the skin and / or hair selected from the group consisting of microbial infections, fungal infections, and
15 pathological hair loss.
[13]
13. Use of a composition according to claim 10 for non-therapeutic cosmetic treatment and / or skin and / or hair care.
Use according to claim 13, wherein the non-therapeutic cosmetic treatment and / or skin and / or hair care is selected from the group consisting of the treatment and / or prevention of aging and / or photoaging, the treatment and / or wrinkle prevention.
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同族专利:
公开号 | 公开日
WO2017009206A1|2017-01-19|
ES2596720B1|2018-01-29|
EP3319583A1|2018-05-16|
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