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Quercetin skin lipidosome, lyophilized powder thereof and preparation method and application thereof

A technology of liposome and quercetin, applied in the field of medicine

Active Publication Date: 2013-05-01
SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The content of the inventions of the above-mentioned patents are all aimed at the route of intravenous injection, but the research and invention of quercetin topical skin preparations are not.

Method used

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  • Quercetin skin lipidosome, lyophilized powder thereof and preparation method and application thereof
  • Quercetin skin lipidosome, lyophilized powder thereof and preparation method and application thereof
  • Quercetin skin lipidosome, lyophilized powder thereof and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0073] Example 1: 100 mg of quercetin, 1 g of phospholipid, 0.05 mL of vitamin E and 200 mg of cholesterol were dissolved in 10 mL of ethanol, 200 mg of sodium cholate, 1 g of mannitol, and 500 mg of lactose were dissolved in 100 mL of purified water, and ethanol and Put the water phase into a constant temperature water bath at 55°C, pour the ethanol solution into the water phase while stirring magnetically, evaporate the ethanol, and continue stirring for 30 min. Filter the liposome solution through a microporous membrane (0.22 μm) for 3-5 The second time, pre-freeze at -80°C for 24 hours, put it into a vacuum freeze dryer for drying for 48 hours, and then obtain the liposome freeze-dried powder.

Embodiment 2

[0074] Example 2: 10 mg of quercetin, 1.2 g of phospholipids, 200 mg of DOTAP, 0.05 mL of vitamin E and 600 mg of cholesterol were dissolved in 10 mL of ethanol, 1 g of mannitol, 500 mg of lactose were mixed with lyoprotectant and 300 mg of sodium cholate, poloxamer Dissolve 100mg in 100mL of purified water, put the ethanol and the water phase into a 55°C constant temperature water bath, pour the ethanol solution into the water phase while stirring magnetically, evaporate the ethanol, and continue stirring for 30min. Filter with a filter membrane (0.22 μm) for 3-5 times, pre-freeze at -80°C for 24 hours, put it into a vacuum freeze dryer for drying for 48 hours to obtain the liposome freeze-dried powder.

Embodiment 3

[0075] Example 3: 50 mg of quercetin, 500 mg of phospholipid, 0.05 mg of sodium sulfite and 150 mg of cholesterol were dissolved in 100 mL of chloroform, 50 mg of sodium cholate, 50 mg of poloxamer, 500 mg of mannitol, and 300 mg of glucose were dissolved in 100 mL of purified water. , Pour the organic phase into a pear-shaped flask to remove the solvent by evaporating under reduced pressure, continue to reduce the pressure for 24h, then pour into the water phase and stir in a constant temperature water bath at 45°C, and continue stirring for 2h. Filter the liposome solution through a microporous membrane (0.22 μm) for 3-5 times, pre-freeze at -80° C. for 24 hours, put it into a vacuum freeze dryer for drying for 48 hours to obtain a liposome freeze-dried powder.

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Abstract

The invention discloses a quercetin skin lipidosome and lyophilized powder thereof, belongs to the technical field of medicines, and aims to solve the problems that the quercetin is poor in solubility and difficult to apply, improve the penetration amount and the penetration rate of quercetin into a corneum and enhance the retention of a medicine in an epidermis and a dermis so as to play the efficacy better. Every 100 mL of lipidosome solution is prepared from the following substances: 0.01-0.1g of quercetin, 0.1-1.2g of amphiphilic lipid, 0.025-0.6g of cholesterol, 0.05-3g of surfactant, 0.001-0.5g of antioxidant and the balance of aqueous medium. The quercetin skin lipidosome and the lyophilized powder thereof are external preparations for a skin, and are applicable to oxidation resistance, inflammation resistance, ultraviolet radiation damage resistance, skin cancer resistance, and resistance to edema, red spots, pigmentation, inflammation and immune suppression which are caused by ultraviolet radiation.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a quercetin flexible liposome for skin and a preparation method thereof. Background technique [0002] At present, with the increasing air pollution, the threat of excessive ultraviolet radiation to the organisms on the earth's surface is increasing day by day, and the skin damage caused by ultraviolet rays is also becoming more and more serious. When the ozone layer is reduced by 10%, the ultraviolet radiation reaching the ground will increase by 2%, and the incidence of skin diseases will increase by 25% to 32%. According to the "World Cancer report", 30% of the newly diagnosed cancers in the world each year are skin cancers, and 90% of the skin cancers are caused by ultraviolet radiation in the sun. Skin damage caused by ultraviolet rays is mainly related to UVA and UVB, among which UVB is the main cause of skin damage. [0003] Various pollutants such as ultraviolet rays lea...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/19A61K31/352A61P17/00A61P17/18A61P29/00A61P17/16A61P35/00A61P37/04
Inventor 史小军刘丹朱永原
Owner SHENZHEN GRADUATE SCHOOL TSINGHUA UNIV
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