US20050037079A1 - Temperature sensitive state-changing hydrogel composition and method for preparation - Google Patents

Temperature sensitive state-changing hydrogel composition and method for preparation Download PDF

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Publication number
US20050037079A1
US20050037079A1 US10/719,935 US71993503A US2005037079A1 US 20050037079 A1 US20050037079 A1 US 20050037079A1 US 71993503 A US71993503 A US 71993503A US 2005037079 A1 US2005037079 A1 US 2005037079A1
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Prior art keywords
hydrogel
state
skin
hydrogel composition
changing
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US10/719,935
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English (en)
Inventor
Taewon Son
Hyun Oh Yoo
Changmo Sung
Paul Kim
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UGENIC Inc
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UGENIC Inc
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Assigned to UGENIC, INC. reassignment UGENIC, INC. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: SON, TAEWON, YOO, HYUN OH, KIM, PAUL, SUNG, CHANGMO
Publication of US20050037079A1 publication Critical patent/US20050037079A1/en
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04—Dispersions; Emulsions
    • A61K8/042—Gels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/02—Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/0208—Tissues; Wipes; Patches
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34—Alcohols
    • A61K8/345—Alcohols containing more than one hydroxy group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73—Polysaccharides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00—Cosmetics or similar toiletry preparations
    • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73—Polysaccharides
    • A61K8/736—Chitin; Chitosan; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/06—Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7007—Drug-containing films, membranes or sheets
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q19/00—Preparations for care of the skin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/20—Chemical, physico-chemical or functional or structural properties of the composition as a whole
    • A61K2800/24—Thermal properties
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/54—Polymers characterized by specific structures/properties
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00—Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/40—Chemical, physico-chemical or functional or structural properties of particular ingredients
    • A61K2800/59—Mixtures
    • A61K2800/594—Mixtures of polymers

Definitions

  • FIG. 1 shows the viscosity of the Hydrogel composition measured at various temperatures.
  • FIG. 2 shows that the hydrogel is formed by two gel type Polymers. Part (a) shows that physical bond of the branched polymer and electrical bond of the electrolyte gel polymer exists together. Part (b) shows the fluid state of the polymers where electrical bond of the electrolyte gel polymer exists but the physical bond of the branched gel polymer does not exist.
  • FIG. 3 shows the skin care hydrogel sheet that was produced using invented hydrogel composition.
  • Part (a) is the base that is made out of rayon textile and part (b) is the invented Hydrogel.
  • This invention is about the temperature sensitive state-changing Hydrogel composition and the method for its preparation.
  • it is the Hydrogel composition and its method of production of the gel that transforms into state-changing condition by temperature difference which can be applied efficiently to skin as beauty care.
  • the state-changing Hydrogel composition means a material Hydrogel, which contains great quantity of water, changes its form into state of fluid at a certain temperature.
  • Hydrogel has been used in many areas of skin-care such as cosmetic products, and dermal treatment. Hydrogel is used as a base frame because it is suitable for the controlled release of drugs (N. A. Pappas Ed., “Hydrogels in Medicine and Pharmacy, Vol.11; Polymers’, CRC Press, Inc., 1987.). This means that Hydrogel is used as a base frame with hormones such as progesterone, and then slowly releases and controls the quantity of the hormones into the body.
  • hormones such as progesterone
  • Transdermal delivery of drugs is a technique that transfers hormones such as Progesterone, Progestin, Estrogen, and Testosterone into the body through the skin.
  • hormones such as Progesterone, Progestin, Estrogen, and Testosterone
  • This high level medicating system slowly releases adjusted quantity of medicine into body through transdermal from hydrogel which is attached on the skin.
  • Verner U.S. Pat. No. 5,064,654 also introduces the composition of adhesive hydrogel for transdermal delivery of drugs.
  • Rolf U.S. Pat. Nos. 6,361,790 and 6,406,712 introduced a patch and dressing method of skin application using hydrogel.
  • hydrogel When hydrogel is in the gel state, it takes relatively long time for the medicine to penetrate into skin, and the drug could only be delivered to the limited area where the hydrogel directly contacts the skin.
  • hydrogel is used in this skin care system to increase effectiveness, and it is produced in sheet and patch forms to effectively apply to the skin.
  • hydrogel is used, there are limitations when hydrogel is in the form of gel. This limitation causes delay in speed and the quantity of the drug delivery.
  • This invention is to provide the temperature sensitive state-changing hydrogel which delivers beauty substance into the skin evenly and rapidly.
  • the hydrogel composition changes its state into liquid which can flow due to body temperature after skin contact.
  • this invention is to provide the production method of temperature sensitive state-changing hydrogel that distributes beauty substance onto skin evenly and rapidly.
  • Temperature sensitive hydrogel composition consists of Branched Gel Polymer 1-10 wt %, Electrolyte Gel Polymer 0.5-5 wt %, Skin-friendly Enhancements 0.5-5 wt %, Natural Bio Material 1-10 wt %, Aliphatic Polyol 3-30 wt %, Functional Additive 1-10 wt % and water 30-93 wt % and transforms to the state of fluid at the temperature of 10 ⁇ 50° C.
  • Temperature Sensitive State-changing Hydrogel has two steps for its production.
  • the first step (Preparation of Gel solution): At room temperature, mix Aliphatic polyol 3-30 wt % with Branched gel polymer 1-10 wt % (extracted from group of Galactomannan, Glucomannan, Guagum, Locastgum and Plutonic), Electrolyte gel polymer 0.5-5 wt % (extracted from group of Aga, Algin, Carrageenan, Xantan and Gelan), Functional Additive 1-10 wt % (extracted from group of Chitosan derivative, Proteoglucan, Elastin, Collagen and Hyaluronic acid), and 30-93 wt % water. Then increase the temperature to 45 ⁇ 95° C.
  • the second step While maintaining the temperature at 45 ⁇ 95° C., sequentially add Natural Bio Material 1-10 wt % (extracted from Aloe, Green Tea, Ginseng, Wood Vinegar, Pine Needles, Gingko Leaf, Mulberry Leaf (Silkworm)), Skin-friendly Enhancements 0.5-5 wt % (Extracted from Metilparavin, Propilpaprvin, Kojic acid, ⁇ -Hydroxy Acid and Retinol), and cool it down to room temperature.
  • Natural Bio Material 1-10 wt % extracted from Aloe, Green Tea, Ginseng, Wood Vinegar, Pine Needles, Gingko Leaf, Mulberry Leaf (Silkworm)
  • Skin-friendly Enhancements 0.5-5 wt % (Extracted from Metilparavin, Propilpaprvin, Kojic acid, ⁇ -Hydroxy Acid and Retinol), and cool it down to room temperature.
  • temperature sensitive state-changing hydrogel composition transforms from gel to liquid state at an ideal temperature of 30-40° C., generally 10-50° C. Because it enhances the acceptance level between hydrogel and skin, it delivers beauty substance or medicine evenly and rapidly.
  • This invention is to construct ideal and effective method of hydrogel that can be used in short time beauty treatment, and then produce suitable temperature sensitive state-changing hydrogel composition.
  • This temperature sensitive state-changing hydrogel composition optimizes acceptance level between hydrogel composition and skin when gel transforms into liquid state after a skincare substance contained hydrogel sheet or patch is applied to skin.
  • hydrogel composition contains natural acceptance level enhancements, contented amount of cosmetic can be delivered into transdermal.
  • this invented Hydrogel when used in beauty care in a form of hydrogel sheet or patch, the body temperature will change the hydrogel state to liquid so that it becomes a flowable composition. This hydrogel will automatically adhere and penetrate into the skin and increase the acceptance level greatly.
  • this invented hydrogel composition includes gel substances that are comprised of tree type and electrolyte polymers together with acceptance level enhancer and natural bio materials to increase the acceptance level with the skin. Also, Polyhydric Alcohol and a functional substance will be added to give the liquid state hydrogel more flux.
  • Hydrogel composition consists of Branched Gel Polymer 1-10 wt %, Electrolyte Gel Polymer 0.5-5 wt %, Skin-friendly Enhancements 0.5-5 wt %, Natural Bio Material 1-10 wt %, Aliphatic Polyol 3-30 wt %, Functional Additive 1-10 wt % and water 30-93 wt %.
  • hydrogel composition changes its state to liquid by body temperature when it is applied to the skin. It was also found that because of the above characteristics, substances included in hydrogel composition rapidly adhere and penetrate into skin.
  • Electrolyte Gel Polymers keeps the invented gel composition to stay in a gel state, and in some cases it keeps invented gel composition to stay in the gel state in room temperature (ideally between 0-30° C.).
  • the Branched Gel Polymers acts as a substance to change the state from solid to liquid form when the temperature increases 10-50° C. (ideally 30-40° C.).
  • FIG. 2 shows the formation of the two polymers. Part (a) shows that physical bond of the branched gel polymer and electrical bond of the electrolyte gel polymer exists together. Part (b) shows the liquid state of the polymers where electrical bond of the electrolyte gel polymer exists but the physical bond of the branched gel polymer does not exist.
  • the Branched gel polymers are water soluble Polysaccharide Polymers which are Galactomannan, Glucomannan, Guagum, Locastgum and Plutonic.
  • the Electrolyte gel polymers are Polysaccharide Polymers which are Aga, Algin, Carrageenan, Xantan and Gelan), Functional Additive 1-10 wt %(extracted from group of Chitosan derivative, Proteoglyucans, Elastin, Collagen and Hyaluronic acid.
  • the Branched gel polymers have 1-10 wt % and the Electrolyte gel polymers have 0.5-5 wt %. If the composition is not within this range, gel state will not form nor will it change to liquid state even with increase in temperature.
  • skin-friendly enhancer will improve the acceptability of the skin to help the drugs to rapidly penetrate into skin, these substance are but not limited to the Polysaccharides like Chitosan, Proteoglycans, Chitosan derivative, Elastin, Collagen, Hyaluronic Acid or other Proteins that can be water soluble.
  • the desired quantity of 0.5-5 wt % is based on the total weight of the composition.
  • biomaterials are also added to improve the acceptability of the skin. They are natural substances that are extracted from plant, animal or mineral which are as follows but not limited to extracted substance from aloe, green tea, ginseng, wood vinegar, pine needles, propolis, gingko leaves, and mulberry leaves (silkworm).
  • the desirable quantities are about 1-10 wt % based on total weight of the composition.
  • Aliphatic Polyols like Propylene glycol and glycerine are soluble in water liquid which facilitates hydrogel composition to adhere and penetrate into the skin.
  • the desirable quantities are about 3-30 wt % based on total weight. If the alcohol content is more than the desirable amount, formation of the gel state will be a problem. If it is less than the desirable amount, then the problem of stationary state as a gel will arise.
  • Functional additives listed below are the additives that can provide stability and functionality. They are propilparavin, Kojic acid, ⁇ -Hydroxy acid, imidazolidinylurea, twin80 and retinol. Desirable quantities are 1-10 wt % based on total weight of the composition. If the additive content are less than the desirable amount, stability will be decreased which would prohibit from long-term storage, and if it has more than the desirable amount, the problem of stationary state as a gel will arise.
  • Water is the main substance of the hydrogel composition that is based on total weight of the composition its quantity is about 30-93 wt %. Water content less than the amount will rose a problem of stationary state when the temperature rises, and more water will have a problem of not forming a gel.
  • Hydrogel composition comprised as above will have unique characteristics of staying in a gel state in temperature between 0-10° C., and changing to liquid state in 10-50° C. Also this invented hydrogel composition can remain as a gel state at 0-30° C. or at room temperature, and transform to liquid state in 20-40° C. depending upon different amount of substances in the composition. As it was stated above, this invented hydrogel composition is sensitive to temperature difference and has characteristic of changing its states so that skin care substances in the hydrogel composition can rapidly and evenly penetrate into skin when it is applied directly to the skin.
  • the Hydrogel composition can be produced by the following method. First, mix Branched gel polymer and electrolyte gel polymer into the Aliphatic Polyol and make the polymer solution, then mix the functional additive to the Aliphatic Polyol and make the functional solution. Combine the two polymer solution and the functional solution and produce the basic mixture solution.
  • Next step is to mix the basic mixture solution with the deionized water and heat the solution temperature to 45-95° C. While maintaining the temperature, add the acceptance enhancer and the natural biomaterials to the solution which will produce the liquid state Hydrogel composition.
  • the amount of added substance should be as mentioned before, and their benefits have also been mentioned earlier.
  • this invented hydrogel composition can be produced as a patch or sheet to be applied to skin.
  • gel type hydrogel can be produced by cooling liquid hydrogel composition made in sheet or patch form to a temperature in between 45-95° C.
  • FIG. 3 shows the beauty care hydrogel sheet by inserting rayon textile as a wick into hydrogel composition. Part (a) is the rayon textile and part (b) is the invented hydrogel composition.
  • FIG. 1 shows the viscosity of the above hydrogel composition measured at various temperatures. As it is shown in FIG. 1 , the hydrogel composition decreases its viscosity when the temperature increases and transforms to liquid state.
  • Hydrogel sheet can be produced by adding a rayon textile as a wick to this hydrogel composition at the temperature of 80° C. and then cooling it. This will be used to release beauty care ingredients to the skin.
  • hydrogel when hydrogel is applied to skin the coverage is 40-70%. However, due to the characteristic of the invented hydrogel which is temperature sensitive state-changing, it has 100% coverage and faster migration rate of ingredient. It is a product that increases epidermal absorption of hydrogel.
  • the invented hydrogel composition is not only very effective in skin care but also effective in skin treatment if rapid delivery of drug or skin-friendly material is required. Especially, the invented hydrogel can be used very effectively in skin care transdermal cosmetic delivery.

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