A kind of curcumin nano-micelle preparation and preparation method thereof

A technology of nano micelles and curcumin, applied in the field of medical applications, can solve the problems of poor oral absorption, low solubility, limited application, etc., and achieve the effects of increasing stability, good safety, and prolonging circulation time.

Inactive Publication Date: 2011-12-14
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, its solubility in water is extremely low, and it is rapidly metabolized in the body; its oral absorption is poor, and its oral bioavailability in rats is only 1%, which limits its clinical application

Method used

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  • A kind of curcumin nano-micelle preparation and preparation method thereof
  • A kind of curcumin nano-micelle preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Weigh 8.0 mg of curcumin, 80.0 mg of amphiphilic block copolymer methoxypolyethylene glycol-polylactic acid, stir and dissolve with an appropriate amount of dichloromethane, remove the organic solvent by rotary evaporation in a water bath at 30 ° C, and place in a vacuum oven After drying overnight, a dry and transparent drug film skeleton was obtained. Add 2.0ml of deionized water, ultrasonically disperse at room temperature for 15 minutes, combine with constant temperature oscillation at 37°C, and centrifuge at 10,000rpm for 20 minutes (to remove unencapsulated crystalline drug). Qing is a transparent curcumin micellar preparation.

[0034] In the micellar preparation, the encapsulation rate of curcumin was 87.5%, the drug loading capacity was 8.05%, and it was stored at 4° C. for 24 hours without precipitation of the drug. Take the micellar preparation and dilute it in an appropriate amount, drop it on the copper grid, carry out negative staining with 2% phosphotungs...

Embodiment 2

[0036] Weigh 4.8mg of curcumin, 80.0mg of amphiphilic block copolymer methoxypolyethylene glycol-polylactic acid, stir and dissolve with an appropriate amount of methanol, remove the organic solvent by rotary evaporation in a water bath at 40°C, and dry in a vacuum oven overnight Finally, to obtain a dry and transparent drug film skeleton, add 13.95ml of deionized water, ultrasonically disperse at room temperature for 20 minutes, and combine with constant temperature oscillation at 37°C, centrifuge at 10000rpm for 20 minutes (to remove unencapsulated crystalline drug), the supernatant is ready It is a transparent curcumin micellar preparation. The encapsulation rate of curcumin in the micellar preparation was 82.4%, and the drug loading capacity was 6.82%. It was stored at 4°C for 24 hours, and no drug precipitated out.

Embodiment 3

[0038] Weigh 1.6mg of curcumin, 80.0mg of amphiphilic block copolymer methoxypolyethylene glycol-polylactic acid, stir and dissolve with an appropriate amount of acetone, remove the organic solvent by rotary evaporation in a water bath at 60°C, and dry in a vacuum oven overnight Finally, to obtain a dry and transparent drug film skeleton, add 9ml of deionized water, ultrasonically disperse at room temperature for 15 minutes, and combine with constant temperature oscillation at 37°C, centrifuge at 10000rpm for 25 minutes (to remove unencapsulated crystalline drug), the supernatant is Clear curcumin micellar formulation.

[0039] Add 4% (w / v) mannitol and freeze-dry to prepare a freeze-dried preparation. Take an appropriate amount of freeze-dried agent and redissolve it with physiological saline, take an appropriate amount of the solution, drop it on the copper grid, use 2% (w / v) phosphotungstic acid solution for negative staining, and observe it under the transmission electron ...

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Abstract

The invention relates to a curcumin nano micelle preparation and a preparation method thereof. The preparation consists of curcumin and amphiphilic block copolymer. The preparation method comprises the following steps of: jointly dissolving the curcumin and the amphiphilic block copolymer in an organic solvent, performing rotary evaporation to remove the organic solvent, performing vacuum drying on the obtained a medicine-containing film, sanding overnight, removing residual organic solvent, adding an aqueous phase, combining ultrasonic dispersion and 35-38 DEG C thermostatic oscillation to obtain a micelle solution, centrifuging at a high speed, and taking supernate, namely the curcumin nano micelle preparation. The curcumin nano micelle preparation is prepared by an improved film dispersion method, the solubility of the curcumin in water is improved, the loading rate of the preparation can reach 8 percent, the micelle particle size is less than 100nm, and the curcumin nano micelle preparation has the advantages of stable structure, small particle size, low toxicity, high safety, long in-vivo circulation time, simple storage and the like.

Description

technical field [0001] The invention relates to a curcumin nano-micelle preparation and a preparation method thereof, belonging to the technical field of medical applications. Background technique [0002] Curcumin (curcumin, Cur) is a phenolic compound extracted from the rhizomes of turmeric, curcuma, and turmeric, etc., plants of the genus Zingiberaceae (curcuma L.). Pharmacological experiments have shown that curcumin has anti-inflammatory, anti-cancer In addition to its anti-oxidation effect, it also has inhibitory effects on the production, proliferation and metastasis of lung cancer, colon cancer, gastric cancer, liver cancer, breast cancer and other cells. The research on the treatment of various cancers using Cur abroad is in the clinical trial stage. However, its solubility in water is extremely low, and it is rapidly metabolized in the body; its oral absorption is poor, and its oral bioavailability in rats is only 1%, which limits its clinical application. Therefo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/12A61K47/34A61P35/00A61P35/02
Inventor 翟光喜赵丽艳曹丰亮
Owner SHANDONG UNIV
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