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WO2020162842A1 - Gel based formulation for the treatment of the dark circles under eyes - Google Patents

Gel based formulation for the treatment of the dark circles under eyes Download PDF

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Publication number
WO2020162842A1
WO2020162842A1 PCT/TR2019/050073 TR2019050073W WO2020162842A1 WO 2020162842 A1 WO2020162842 A1 WO 2020162842A1 TR 2019050073 W TR2019050073 W TR 2019050073W WO 2020162842 A1 WO2020162842 A1 WO 2020162842A1
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WO
WIPO (PCT)
Prior art keywords
gel based
based formulation
sln
formulation
vitamin
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.)
Ceased
Application number
PCT/TR2019/050073
Other languages
French (fr)
Inventor
Şeyda ATABAY
Original Assignee
Dr. Şeyda Atabay Sağlik Ve Kozmeti̇k Ürünleri̇ A.Ş.
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 Dr. Şeyda Atabay Sağlik Ve Kozmeti̇k Ürünleri̇ A.Ş. filed Critical Dr. Şeyda Atabay Sağlik Ve Kozmeti̇k Ürünleri̇ A.Ş.
Priority to EP19914573.1A priority Critical patent/EP3920883A4/en
Publication of WO2020162842A1 publication Critical patent/WO2020162842A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • 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
    • A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/00—Medicinal preparations containing organic active ingredients
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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/12—Ketones
    • A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • A—HUMAN NECESSITIES
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    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
    • A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline 
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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    • A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
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    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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    • 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
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    • 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
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    • A61K8/4973—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with oxygen as the only hetero atom
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Definitions

  • the present invention is related to a gel based formulation for the treatment of the dark circles under eyes.
  • the invention is particularly related to a nanotech, gel based cosmetic formulation which is effective in changing the view of the dark circles under eyes, includes Solid Lipid Nanoparticles (SLN) obtained from fats similar to fat structures in our body.
  • SBN Solid Lipid Nanoparticles
  • the reasons of the dark circles under eyes may be such that the skin in this region is thin and the blood passing through major veins close to the skin surface creates a bluish view, leakage occurs from the capillary veins due to loss of collagen and hyperpigmentation.
  • the hyperpigmentation is known as darkening of the skin color and generally occurs due to increasing melanin production in only one region of the skin.
  • the hyperpigmentation seen on the eye contour occurs due to various factors specific to this region. This pigmentation occurred as a result of abnormal pigmentation can have many reasons such as lack of sleep, excessive sleep, allergic reactions, continuous stress, improper product applications used, aging, long term computer usage, nutritional deficiency, hormonal changes and vitamin deficiency etc.
  • the region on the in the eye contour is sensitive against wrinkle and dryness due to rareness of sebaceous glands in the eye contour.
  • one of the problems on the eye contour is the eye bags which develop due to water retention. Generally fat accumulation in these regions is responsible from these eye bags.
  • Topical compositions prepared in gel or cream form consist of mainly dimethylmethoxy chromanyl palmitate active ingredient and a cosmetically acceptable carrier. It is stated that dimethylmethoxy chromanyl palmitate not only has features such as it bleaches the color of the skin and it is photo protective, but also it does not cause side effects in respect to the pigment decreasing other substances. Also other substances which bleach skin color, moisturizing agents and antioxidants etc. which are beneficial to the skin can be added to the formulation aimed for brightening supraorbital region.
  • US5643587 patent describes a component for a topical treatment, which comprises using a living yeast cell derivative in combination with a carrier appropriate for treating colorings on the supraorbital skin and eye bag formation.
  • Living yeast cell derivative is a very complex, biyologically active material with low molecular weight consisting of amino acids, monosaccharides, disaccharides and vitamins and minerals with trace quantities.
  • the yeast cell derivative used in this invention is produced from the living yeast cultures of Saccharomyces cerevisiae.
  • the circles under eyes are not a simple pigmentation problem which is melanocyte mediated, however it is stated that it is due to circulatory disorders, inflammation and environmental factors and this problems does not respond well to the well-known hypopigmentation or skin bleaching compositions. It is described that by promoting oxygen intake of the active substance made of a living yeast derivative and by fastening metabolic processes in human cells, for example by increasing collagen production, it provides an alternative solution to all these problems.
  • the formulation developed with the present invention comprises Solid Lipid Nanoparticles (SLN) which gains different functions, obtained with similar fats available in our body, gelling agents and herbal and non-herbal other cosmetic substances and vitamins.
  • SPN Solid Lipid Nanoparticles
  • the formulation of the present invention not only provides a decrease in the dark circles on the eye contour, but also decreases the effect of sun beams by means of the nanoparticles included within itself, shows sun protective feature, also besides having an effect against aging around the eye contour, it provides moisturizing, firming around the eye contour and decreases swelling and helps eliminating line view. Due to selected raw materials have antimicrobial activity and the ratio of protective material usage within the formulation is low, possible harmful effects of the product used by the consumer are minimized. The other deficiencies around the eye contour are also decreased by targeting the dark circles under eyes.
  • the nanotech, gel based formulation developed for solving the relevant problems in terms of the region under eyes has the advantages of being appropriately used in any skin types with its features such as its being multi-functional, has a low side effect potential and it is oil free.
  • the aim of the present invention is to prepare a gel based formulation which comprises Solid Lipid Nanoparticles (SLN) for the treatment of the dark circles under eyes.
  • SPN Solid Lipid Nanoparticles
  • Another aim of the present invention is to provide a multi-functional formulation with the effect of SLN’s and natural herbal substances included within the formulation.
  • Another aim of the present invention is to minimize the possible side effects aroused out of using a low amount protective material.
  • Another aim of the invention is to have a formulation which does not give an oily sense, has a hydrophilic gel based structure.
  • the cosmetic products are all preparations or substances prepared for applying on various external regions of the human body such as epiderma, nails, hairs, hair, lips and external genital organs etc., teeth and mouth mucosa, which only aim for cleaning these regions, give fresh odor, change view and/or restore body odors and/or protect or keep in a good state. For this reason are the products which must be designed in a safe and risk-free manner.
  • Thyrosinase enzyme is inactivated
  • An ideal bleaching substance shall have pharmacologically appropriate features, shall show its effect within 2 - 3 month period, shall have less probability of showing side effect, and shall remove undesired skin spots permanently.
  • the combinations of these substances are used in most of these formulations. Particularly, decreasing the side effect, increasing the efficiency by selecting low concentrations of the substances which show efficiency in different mechanisms is aimed.
  • the skin peeling products such as tricholoracetic acid is used for eliminating the skin surfaces which comprise melanine by means of the peeling effect.
  • acidic peelings are appropriate for using in other regions, they may not be recommended for the eyelids. Due to the thin skin on the eyelids, it can cause harmful results on the eyes.
  • Carbomers which are widely used in the pharmaceutical and cosmetic industries are synthetic, high molecular weighted acrylic acid polymers which comprise carboxylic acid in a ratio of 56 - 68 %. It is a white, low characteristic scented, hygroscopic and acidic powder. It dissolves in the water, alcohol and glycerin. It is recorded in the literature that carbomers particularly Carbopol® 934 and 940 types are used for preparing gel formulations. Gelling mechanism is based on the neutralization of the carboxylic acid content within the structure of the acrylic acid. The neutralization of the carbomers is provided by substances such as; sodium hydroxide, potassium hydroxide, sodium bicarbonate, borax, amino acids, diethanolamine or triethanolamine. The neutralization process increases the viscosity of the polymer by moving carboxylate groups from each other. The viscosity of the carbomers decreases in the presence of various ions. Optimum gel viscosity and transparency is realized at approximately pH 7.
  • Aloe Vera Gel It is obtained from the leaves of the Aloe Vera plant. It comprises; aloin, mannose, glucose, sterols, amino acids (tryptophan and phenylalanine) and cinnamic acid esters. It has an anti-inflammatory effect due to the sterols and amino acid carried, and has an UVA filtering feature due to the cinnamic acid esters. This effect causes the Aloe Vera gel to have a delaying role in aging due to UV beams and free radicals. In addition to this, it has treating, skin moisturizing and softening effects.
  • gels are prepared by means of carbomers and Aloe Vera gel.
  • Solid Lipid Nanoparticles are produced by replacing fluid oil included within the emulsion with the solid lipid in both room and body temperature.
  • SLN’s are the colloidal systems wherein biodegradable and biocompatible solid lipids between 50 - 1000 nm are stabilized with surface active agents.
  • Lipid nanoparticles are alternative carrier systems to the liposome and emulsions for cosmetic and topical applications.
  • SLN creates a thin layer on the skin by means of its small fragment size and it causes a significant increase in the skin moisture due to its water retention capacity. Therefore active component penetration and efficiency also increases. It is a very appropriate carried for the substances with chemical stability problem due to its structure. It allows for formulating hydrophilic or hydrophobic many valuable but instable substances used in the cosmetic industry with this characteristic.
  • UV protective substances used in the sun protective products cause side effects, so that new systems are required.
  • SLN also provides an advantageous solution for this problem too. It is explored that SLN acts as a sun protective substance due to its crystal structure and it creates a pigment effect due to its white color. It is started to be used in the formulations of sun preparations due to its reflective and distributive effect of sun beams. It is explored that it provides a more effective protection compared to other carrier systems due to its fragmented structure. Therefore it is possible to prepare more effective and safer formulations without changing sun protection factor by decreasing concentrations of sun beam filtering substances which can cause serious side effects.
  • Green tea and caffeine with procirculatory effect which are rich in tannin and flavonoids are added to the formulation wherein UV protection is provided by means of the gel based SLN.
  • Arnica, K vitamin, P vitamin and Oligopeptide 34 are added due to their synergistic effects.
  • Oligopeptide-34 is a small protein molecule consisting of 13 amino acids sequenced together in order to create a very effective and active molecule which targets melanine formation. Oligopeptide-34 decreases melanine synthesis and thyrosinase activity in melanocytes and decreases transfer of melanosomes to new keratinocyte cells. In researches which compares Oligopeptit-34 with vitamin C and Arbutine, Oligopeptit-34 is found superior; vitamin C and Arbutine decreases pigmentation ratio respectively in an amount of 27 and 40 %, Oligopeptide-34 decrease pigmentation ratio by 47 %.
  • Green tea comprised flavonol, flavonoid and phenolic acid. Most of the polyphenols included in the green tea consists of flavonols known as“catechin”. Green tea is an anti-inflammatory and protective plant against UVB due to these active ingredients. As a polyphenolic component included within the green tea, it is determined that (-)- epigallocatechin-3-gallate determined prevents UVB based immunosuppression on the skin. It is shown that when this component is applied with a 2 % ratio in a hydrophilic ointment recorded in USP24, it has a protective activity against UVA.
  • Caffeine is a natural structured xanthine derivative. FDA (Food and Drug Administration) keeps the caffeine in the list of Generally Accepted Safe Substances (GRAS) as a multi-functional nutritional substance. Caffeine is increasingly used in the cosmetic preparations due to its high biological activity and its ability of easy penetration from the skin barriers. It prevents drying of the skin and it softens the skin. Therefore it corrects dry and worn skin view. Also caffeine has a strong antioxidant characteristic. It protects the cell against UV beams and it slows down the photo-aging period of the skin. Caffeine is applied topically and shows its effect by increasing capillary blood flow rate of the skin.
  • Vitamin K2 is found in animal products, whereas Menaquinones has an artificial source. A lot of studies indicate that longchain menaquinones have a longer haliime, which makes them more bioavailable. Vitamin K2 can cure skin disease related to skin pigmentation, such as melanin and shows advantageous effects against bruising or dark circles under the eyes
  • P vitamin is an herbal flavonoid. It serves as an antioxidant, skin refreshing and restorative component. It is embodied in some herbal components such as the quercetin, St. John's worth and Ginkgo biloba.
  • Arnica extract is obtained from the flowers of the Arnica Montana plant.
  • Arnica Montana flowers comprise sesquiterpene lactons, phenol carbonic acid, flavonoids, cumarins and essential oil.
  • Helenaline which is a sesquiterpene lacton is the major restorative component in Arnica Montana together with the flavoids, it helps to smooth and regenerate the skin after being subjected to stress.
  • the antiseptic, antibacterial and anti-inflammatory characteristics of Arnica are somewhat beneficial for the individuals with inflammatory skin deficiencies. At the same time it also stimulates the formation of granular tissues and therefore it facilitates the treatment period.
  • Arnica can be used for wounds, sun burn, minor burns and superficial phlebitis because it provides recovery.
  • the triterpene obtained from the flowers of Arnica Montana is one of the strongest among melanine biosynthesis inhibitors known in the culture cells and it is 50 fold stronger than 4-methoxyphenol used as an anti-pigmentation agent.
  • a microbial protective agent a chelating agent and if required a fragrance can be added to the formulation of the present invention.
  • Tween 80 is added to the heated water and mixed at 24000 rpm. Compritol weighted in a required amount is added to this mixture, and mixing process is continued by means of ultra sonox. After homogenization is obtained then obtained SLN is kept waiting during 1 night at +4 °C.
  • Oligopeptide, K vitamin, Citric acid monohydrate, Caffeine and P vitamin is dissolved in distilled water by mixing thoroughly in order to obtain a solvent.
  • Carbopol is added to the last obtained mixture and kept waiting during 1 night.
  • the formulation is formed as a transparent gel on the other day by adding triethanolamine in drops in a slow manner.
  • the formulation is kept in the refrigerator at +4-8 degrees by closing its cover.
  • the obtained mixture is applied locally to the eye contour.

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Abstract

The present invention is related to a gel based formulation for the treatment of the dark circles under eyes. The invention is particularly related to a, nanotech, gel based cosmetic formulation which is effective in changing the view of the dark circles under eyes, includes Solid Lipid Nanoparticles (SLN) obtained from fats similar to fat structures in our body.

Description

A GEL BASED FORMULATION FOR THE TREATMENT OF THE DARK CIRCLES
UNDER EYES
Technical Field
The present invention is related to a gel based formulation for the treatment of the dark circles under eyes.
The invention is particularly related to a nanotech, gel based cosmetic formulation which is effective in changing the view of the dark circles under eyes, includes Solid Lipid Nanoparticles (SLN) obtained from fats similar to fat structures in our body. State of the Art
The eyelids and the skin right under the eyes are the thinnest skin on the body and have a sensitive structure. In this sensitive region, due to environmental and genetic reasons, some problems are encountered such as bags under eyes and prolapse of the skin, formation of dark circles and wrinkles. These problems not only occur due to factors such as aging, stress, tiredness, obesity but also occur as a result of the environmental factors such as over temperature and extreme colds, UV radiation, micro organisms and being subject to chemical agents.
The reasons of the dark circles under eyes may be such that the skin in this region is thin and the blood passing through major veins close to the skin surface creates a bluish view, leakage occurs from the capillary veins due to loss of collagen and hyperpigmentation. The hyperpigmentation is known as darkening of the skin color and generally occurs due to increasing melanin production in only one region of the skin. The hyperpigmentation seen on the eye contour occurs due to various factors specific to this region. This pigmentation occurred as a result of abnormal pigmentation can have many reasons such as lack of sleep, excessive sleep, allergic reactions, continuous stress, improper product applications used, aging, long term computer usage, nutritional deficiency, hormonal changes and vitamin deficiency etc.
When it is compared to the rest of the face, the region on the in the eye contour is sensitive against wrinkle and dryness due to rareness of sebaceous glands in the eye contour. In addition to this, one of the problems on the eye contour is the eye bags which develop due to water retention. Generally fat accumulation in these regions is responsible from these eye bags.
A cosmetic care composition is disclosed for improving the view of particularly the periocular region in US10034825B2 patent. Topical compositions prepared in gel or cream form consist of mainly dimethylmethoxy chromanyl palmitate active ingredient and a cosmetically acceptable carrier. It is stated that dimethylmethoxy chromanyl palmitate not only has features such as it bleaches the color of the skin and it is photo protective, but also it does not cause side effects in respect to the pigment decreasing other substances. Also other substances which bleach skin color, moisturizing agents and antioxidants etc. which are beneficial to the skin can be added to the formulation aimed for brightening supraorbital region.
US5643587 patent describes a component for a topical treatment, which comprises using a living yeast cell derivative in combination with a carrier appropriate for treating colorings on the supraorbital skin and eye bag formation. Living yeast cell derivative is a very complex, biyologically active material with low molecular weight consisting of amino acids, monosaccharides, disaccharides and vitamins and minerals with trace quantities. The yeast cell derivative used in this invention is produced from the living yeast cultures of Saccharomyces cerevisiae. The circles under eyes are not a simple pigmentation problem which is melanocyte mediated, however it is stated that it is due to circulatory disorders, inflammation and environmental factors and this problems does not respond well to the well-known hypopigmentation or skin bleaching compositions. It is described that by promoting oxygen intake of the active substance made of a living yeast derivative and by fastening metabolic processes in human cells, for example by increasing collagen production, it provides an alternative solution to all these problems.
Although there are studies made in respect to the abovementioned problems for the supraorbital region and there are many products, the activities of these products for providing required effects are very limited. The products within the market in order to eliminate the dark circles under eyes as one of the major problems encountered in respect to the skin around the eye contour are the products designed for creating color changes such as foundation creams or designed over one mechanism. Generally the supraorbital products within cosmetic drug market are in emulsion and cream form. Available gel based formulations do not comprise nanoparticles. Together with the present invention a gel based nanotech formulation is developed which has improved features compared to the formulations included within he prior art. The formulation developed with the present invention comprises Solid Lipid Nanoparticles (SLN) which gains different functions, obtained with similar fats available in our body, gelling agents and herbal and non-herbal other cosmetic substances and vitamins. The formulation of the present invention not only provides a decrease in the dark circles on the eye contour, but also decreases the effect of sun beams by means of the nanoparticles included within itself, shows sun protective feature, also besides having an effect against aging around the eye contour, it provides moisturizing, firming around the eye contour and decreases swelling and helps eliminating line view. Due to selected raw materials have antimicrobial activity and the ratio of protective material usage within the formulation is low, possible harmful effects of the product used by the consumer are minimized. The other deficiencies around the eye contour are also decreased by targeting the dark circles under eyes. Compared to the formulations of the present state of the art, the nanotech, gel based formulation developed for solving the relevant problems in terms of the region under eyes has the advantages of being appropriately used in any skin types with its features such as its being multi-functional, has a low side effect potential and it is oil free.
Aims of the Invention
The aim of the present invention is to prepare a gel based formulation which comprises Solid Lipid Nanoparticles (SLN) for the treatment of the dark circles under eyes.
Another aim of the present invention is to provide a multi-functional formulation with the effect of SLN’s and natural herbal substances included within the formulation.
Another aim of the present invention is to minimize the possible side effects aroused out of using a low amount protective material.
Another aim of the invention is to have a formulation which does not give an oily sense, has a hydrophilic gel based structure.
Detailed Description of the Invention
When the underlying reason of the dark circles under eyes which is one of the major problems around the eye contour is determined, due to the nature of the condition and efficiency of the treatment, it is possible to reverse the darkening which occurs previously. A hydrophilic, gel based, nanotech formulations which will eliminate the dark circles under eyes with a plurality of effects and will not give an oily feeling, are created together with the present invention.
There are different options for the treatment of the dark eye contour. The skin bleaching agents and tretinoine application with prescription are among these applications. However using these applications on sensitive eye contour may not be recommended at all times and they may be applied only with a prescription of a medical expert.
Another alternative to be applied except those products with prescription in order to bleach the color of the dark circles on the eye contour is the cosmetic products. The cosmetic products are all preparations or substances prepared for applying on various external regions of the human body such as epiderma, nails, hairs, hair, lips and external genital organs etc., teeth and mouth mucosa, which only aim for cleaning these regions, give fresh odor, change view and/or restore body odors and/or protect or keep in a good state. For this reason are the products which must be designed in a safe and risk-free manner.
The effect manner of the cosmetic preparations which bleach the skin color can be summarized as follows:
- Melanine stimulating cells (melanocytes) are destroyed,
Melanine biosynthesis is prevented,
Thyrosinase enzyme is inactivated,
The passage of Melanine granules to the stratum germinativum and stratum spinosum cells is prevented,
- Melanine pigment is bleached by oxidation or eliminated.
An ideal bleaching substance shall have pharmacologically appropriate features, shall show its effect within 2 - 3 month period, shall have less probability of showing side effect, and shall remove undesired skin spots permanently. In order to increase the effect by obtaining additional or synergistic effects, the combinations of these substances are used in most of these formulations. Particularly, decreasing the side effect, increasing the efficiency by selecting low concentrations of the substances which show efficiency in different mechanisms is aimed. The skin peeling products such as tricholoracetic acid is used for eliminating the skin surfaces which comprise melanine by means of the peeling effect. However although acidic peelings are appropriate for using in other regions, they may not be recommended for the eyelids. Due to the thin skin on the eyelids, it can cause harmful results on the eyes.
If no effect is observed during 6 months following the usage of the bleaching preparations, the application shall be terminated. As a result, in general there are many products in which the combinations of the components are used within the market. The researches in respect to the novel color bleaching substances in the cosmetic and pharmaceutical industries are increasingly continued. In parallel with this, the number of novel, more effective and safer components increase day by day. These preparations are generally prepared in the form of ointment, stearate cream and lotion. The effect of these preparations applied during predetermined time intervals is not seen immediately, the result is obtained after 3-6 weeks.
The cosmetic formulation aimed to be prepared with the present invention comprises the following components which are described in detail in the following:
Carbomers (Acrylic acid polymers)
Carbomers which are widely used in the pharmaceutical and cosmetic industries are synthetic, high molecular weighted acrylic acid polymers which comprise carboxylic acid in a ratio of 56 - 68 %. It is a white, low characteristic scented, hygroscopic and acidic powder. It dissolves in the water, alcohol and glycerin. It is recorded in the literature that carbomers particularly Carbopol® 934 and 940 types are used for preparing gel formulations. Gelling mechanism is based on the neutralization of the carboxylic acid content within the structure of the acrylic acid. The neutralization of the carbomers is provided by substances such as; sodium hydroxide, potassium hydroxide, sodium bicarbonate, borax, amino acids, diethanolamine or triethanolamine. The neutralization process increases the viscosity of the polymer by moving carboxylate groups from each other. The viscosity of the carbomers decreases in the presence of various ions. Optimum gel viscosity and transparency is realized at approximately pH 7.
Aloe Vera Gel It is obtained from the leaves of the Aloe Vera plant. It comprises; aloin, mannose, glucose, sterols, amino acids (tryptophan and phenylalanine) and cinnamic acid esters. It has an anti-inflammatory effect due to the sterols and amino acid carried, and has an UVA filtering feature due to the cinnamic acid esters. This effect causes the Aloe Vera gel to have a delaying role in aging due to UV beams and free radicals. In addition to this, it has treating, skin moisturizing and softening effects.
In the formulation of the present invention gels are prepared by means of carbomers and Aloe Vera gel.
Solid Lipid Nanoparticles (SLN)
Solid Lipid Nanoparticles (SLN) are produced by replacing fluid oil included within the emulsion with the solid lipid in both room and body temperature. SLN’s are the colloidal systems wherein biodegradable and biocompatible solid lipids between 50 - 1000 nm are stabilized with surface active agents.
Lipid nanoparticles are alternative carrier systems to the liposome and emulsions for cosmetic and topical applications. SLN creates a thin layer on the skin by means of its small fragment size and it causes a significant increase in the skin moisture due to its water retention capacity. Therefore active component penetration and efficiency also increases. It is a very appropriate carried for the substances with chemical stability problem due to its structure. It allows for formulating hydrophilic or hydrophobic many valuable but instable substances used in the cosmetic industry with this characteristic.
UV protective substances used in the sun protective products cause side effects, so that new systems are required. SLN also provides an advantageous solution for this problem too. It is explored that SLN acts as a sun protective substance due to its crystal structure and it creates a pigment effect due to its white color. It is started to be used in the formulations of sun preparations due to its reflective and distributive effect of sun beams. It is explored that it provides a more effective protection compared to other carrier systems due to its fragmented structure. Therefore it is possible to prepare more effective and safer formulations without changing sun protection factor by decreasing concentrations of sun beam filtering substances which can cause serious side effects.
Other components Green tea and caffeine with procirculatory effect which are rich in tannin and flavonoids are added to the formulation wherein UV protection is provided by means of the gel based SLN. In addition to these, Arnica, K vitamin, P vitamin and Oligopeptide 34 are added due to their synergistic effects.
Oligopeptit-34
Oligopeptide-34 is a small protein molecule consisting of 13 amino acids sequenced together in order to create a very effective and active molecule which targets melanine formation. Oligopeptide-34 decreases melanine synthesis and thyrosinase activity in melanocytes and decreases transfer of melanosomes to new keratinocyte cells. In researches which compares Oligopeptit-34 with vitamin C and Arbutine, Oligopeptit-34 is found superior; vitamin C and Arbutine decreases pigmentation ratio respectively in an amount of 27 and 40 %, Oligopeptide-34 decrease pigmentation ratio by 47 %.
Green Tea
Green tea comprised flavonol, flavonoid and phenolic acid. Most of the polyphenols included in the green tea consists of flavonols known as“catechin”. Green tea is an anti-inflammatory and protective plant against UVB due to these active ingredients. As a polyphenolic component included within the green tea, it is determined that (-)- epigallocatechin-3-gallate determined prevents UVB based immunosuppression on the skin. It is shown that when this component is applied with a 2 % ratio in a hydrophilic ointment recorded in USP24, it has a protective activity against UVA. In vivo topical studies made show that it suppressed both chemo and photo carcinogenesis; prevented oxidative stress induced by UV and decreased matrix metalloproteins. It is stated that it decreases erythema on human skin, immunosuppression and DNA damage.
Caffeine
Caffeine is a natural structured xanthine derivative. FDA (Food and Drug Administration) keeps the caffeine in the list of Generally Accepted Safe Substances (GRAS) as a multi-functional nutritional substance. Caffeine is increasingly used in the cosmetic preparations due to its high biological activity and its ability of easy penetration from the skin barriers. It prevents drying of the skin and it softens the skin. Therefore it corrects dry and worn skin view. Also caffeine has a strong antioxidant characteristic. It protects the cell against UV beams and it slows down the photo-aging period of the skin. Caffeine is applied topically and shows its effect by increasing capillary blood flow rate of the skin.
K2 vitamin
Vitamin K2 is found in animal products, whereas Menaquinones has an artificial source. A lot of studies indicate that longchain menaquinones have a longer haliime, which makes them more bioavailable. Vitamin K2 can cure skin disease related to skin pigmentation, such as melanin and shows advantageous effects against bruising or dark circles under the eyes
P vitamin
P vitamin (quercetin) is an herbal flavonoid. It serves as an antioxidant, skin refreshing and restorative component. It is embodied in some herbal components such as the quercetin, St. John's worth and Ginkgo biloba.
Arnica extract
Arnica extract is obtained from the flowers of the Arnica Montana plant. Arnica Montana flowers comprise sesquiterpene lactons, phenol carbonic acid, flavonoids, cumarins and essential oil. Helenaline which is a sesquiterpene lacton is the major restorative component in Arnica Montana together with the flavoids, it helps to smooth and regenerate the skin after being subjected to stress. The antiseptic, antibacterial and anti-inflammatory characteristics of Arnica are somewhat beneficial for the individuals with inflammatory skin deficiencies. At the same time it also stimulates the formation of granular tissues and therefore it facilitates the treatment period. Arnica can be used for wounds, sun burn, minor burns and superficial phlebitis because it provides recovery. According to the researches made during late years, the triterpene obtained from the flowers of Arnica Montana is one of the strongest among melanine biosynthesis inhibitors known in the culture cells and it is 50 fold stronger than 4-methoxyphenol used as an anti-pigmentation agent.
Also, a microbial protective agent, a chelating agent and if required a fragrance can be added to the formulation of the present invention.
The components included within the formulation and their percentages are given in the following table:
Figure imgf000010_0001
Preparation of the formulation: 1. Carbopol prepared in 1 % amount is kept waiting during 1 night at +40 °C, after Carbopol molecules are provided to swell totally on the other day, it is neutralized by means of 1 -3 drops of triethylamine.
2. Tween 80 is added to the heated water and mixed at 24000 rpm. Compritol weighted in a required amount is added to this mixture, and mixing process is continued by means of ultra sonox. After homogenization is obtained then obtained SLN is kept waiting during 1 night at +4 °C.
3. Oligopeptide, K vitamin, Citric acid monohydrate, Caffeine and P vitamin is dissolved in distilled water by mixing thoroughly in order to obtain a solvent.
4. Arnica extract, SLN, green tea and Aloe Vera are added to this solvent under continuous stirring.
5. EDTA caprylyl glycol and phenoxyethanol is added on the obtained mixture.
6. Carbopol is added to the last obtained mixture and kept waiting during 1 night.
7. The formulation is formed as a transparent gel on the other day by adding triethanolamine in drops in a slow manner.
8. Finally lemon grass lead oil and basil oil are added as an essence.
9. The formulation is kept in the refrigerator at +4-8 degrees by closing its cover.
The obtained mixture is applied locally to the eye contour.
Instruction in respect to the application of the formulation
When thee obtained gel based eye contour cream is applied twice a day in the morning and in the evening in an amount of two lentils, it is expected that there will be a color balance on the eye contour, decrease in dark circles, gathering moisture, fading in wrinkles within 7 days.

Claims

1. A gel based formulation for the treatment of the dark circles under eyes, characterized in that; it comprises SLN, green tea flower extract, Aloe Vera extract, Carbopol 974, oligopeptide-34, Arnica Montana flower extract, K2 vitamin, Compritol 888, Caffeine powder, quercetin dihydrate, caprylyl glycol, phenoxyethanol, triethanolamine, EDTA, basil oil and lemon grass leaf oil.
2. A gel based formulation according to claim 1 , characterized in comprising the following by weight in the whole formulation;
(a) about 84 - 87 % distilled water
(b) about 1 - 5 % green tea flower extract
(c) about 1 - 5 % Aloe Vera extract
(d) about 1 - 3 % SLN
(e) about 1 - 3 % Carbopol 974
(f) about 0,1 - 0,5 % oligopeptide - 34
(g) about 0,5 - 1 ,5 % Arnica Montana flower extract
(h) about 0,1 - 1 % K2 vitamin
(i) about 0,08 - 0,5 % compritol 888
(j) about 0,08 - 0,5 % caffeine powder
(k) about 0,01 - 0,1 % quercetin dihydrate
(I) about 0,01 - 0,1 % caprylyl glycol, phenoxyethanol
(m)about 0,01 - 0,1 % triethanolamine
(n) about 0,01 - 0,1 % EDTA
(o) about 0,01 - 0,5 % basil oil
(p) about 0,01 -0,5% lemon grass leaf oil.
3. A gel based formulation according to claim 1 , characterized in comprising; a microbial protective between 0,01 - 0,1 % ratio.
4. A gel based formulation according to claim 1 , characterized in comprising; a further chelating agent between 0,01 - 0,1 % ratio.
5. A gel based formulation according to claim 1 , characterized in comprising; a further fragrance agent between 0,01 - 0,08 % ratio.
6. A gel based formulation production method according to claim 1 , characterized in that, it comprises the following process steps; (a) Preparing Carbopol and keep it waiting during 1 night,
(b) Preparing SLN and keep it waiting during 1 night at +4 °C,
(c) Dissolving Oligopeptide, K vitamin, Caffeine and P vitamin in a distilled water by mixing thoroughly in order to obtain a solvent,
(d) Adding arnica extract, SLN, green tea and Aloe Vera to this solvent under continuous stirring,
(e) adding EDTA caprylyl glycol and phenoxyethanol on the obtained mixture,
(f) adding Carbopol to the last obtained mixture and keep it waiting during 1 night,
(g) bringing the formulation as a transparent gel on the other day by adding triethanolamine in drops in a slow manner,
(h) finally adding lemon grass lead oil and basil oil as an essence,
(i) covering the lid of the formulation and keeping it in the refrigerator at +4-8 degrees.
PCT/TR2019/050073 2019-02-05 2019-02-06 Gel based formulation for the treatment of the dark circles under eyes Ceased WO2020162842A1 (en)

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Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120045405A1 (en) * 2010-08-18 2012-02-23 Gilman Miles E Under eye cream
WO2016139602A1 (en) * 2015-03-05 2016-09-09 Lubrizol Advanced Materials, Inc. Ferment extract of eupenicillium crustaceum and cosmetic use thereof

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2397889B1 (en) * 2011-03-25 2014-02-07 Lipotec, S.A. MODULATING PEPTIDES OF PGC-1 Alpha.

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20120045405A1 (en) * 2010-08-18 2012-02-23 Gilman Miles E Under eye cream
WO2016139602A1 (en) * 2015-03-05 2016-09-09 Lubrizol Advanced Materials, Inc. Ferment extract of eupenicillium crustaceum and cosmetic use thereof

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
"Everything Eyes: Professional Techniques* Essential Tools* Gorgeous Makeup Looks", 2014, CHRONICLE BOOKS, US, ISBN: 1-4521-1961-9, article BOBBI BROWN : "What to look for in Eye Cream", pages: 24 - 28, XP009530070 *
See also references of EP3920883A4 *
SREEKUMAR PILLAI,SURABHI SINGH,CHRISTIAN ORESAJO // DONALD L. BISSETT,JOHN E. OBLONG,LAURA J. GOODMAN: "Solid Lipid Nanoparticles // Vitamine K.", COSMETIC DERMATOLOGY: PRODUCTS AND PROCEDURES, 30 November 2015 (2015-11-30), Chichester, West Sussex ; Hoboken, NJ, pages 69, 343, XP009530071, ISBN: 978-1-118-65558-0, DOI: 10.1002/9781118655566 *

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