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Quercetin nano-micelle preparation and preparation method thereof

A nano-micelle and quercetin technology, which is applied in the direction of anti-toxic agents, anti-inflammatory agents, and pharmaceutical formulations, can solve unclear problems and achieve high drug loading, increased solubility and biological activity, and high encapsulation efficiency Effect

Inactive Publication Date: 2011-03-02
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, it can be expected that using P123 and TPGS together as the carrier of quercetin can increase the solubility and biological activity of quercetin in water, but there is no relevant report in the prior art, whether it can have the expected effect is not clear, therefore, it is necessary to verify its effect and screen out the preparation process suitable for large-scale production

Method used

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  • Quercetin nano-micelle preparation and preparation method thereof
  • Quercetin nano-micelle preparation and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0022] Embodiment 1: Preparation of quercetin nano-micelle preparation

[0023] Accurately weigh 24.0 mg of quercetin, 43.6 mg of non-ionic surfactant Pluronic P123, and 27.2 mg of TPGS, stir and dissolve with an appropriate amount of ethanol, remove the organic solvent by rotary evaporation in a water bath at 25°C, and dry in a vacuum oven overnight. To obtain a dry and transparent drug film skeleton, add 4 mL of deionized water, stir at a constant speed of 1,000 rpm for 5 hours at room temperature, and filter through a microporous membrane to obtain a transparent quercetin micelle solution. The photo of the micellar preparation is as figure 1 As shown, the average particle size is 18.43nm, and the dispersion coefficient is 0.294. The IC of quercetin micelles for MCF-7 cell line was determined by MTT method 50 1.64μg·mL -1 , while the IC of the API DMSO solution 50 16.46μg·mL -1 , indicating that the preparation of the drug into a micellar preparation significantly increa...

Embodiment 2

[0024] Embodiment 2: Preparation of quercetin nano-micelle preparation

[0025] Accurately weigh 24.0mg of quercetin, 23.0mg of non-ionic surfactant Pluronic P123, stir and dissolve with an appropriate amount of ethanol, remove the organic solvent by rotary evaporation in a water bath at 40°C, and dry in a vacuum oven overnight to obtain dry and transparent Add 4 mL of deionized water to the drug film skeleton, stir at 40°C and 1,500 rpm for 5 hours at a constant speed, and filter through a microporous membrane to obtain a transparent quercetin micelle solution. The micellar preparation contains quercetin 5.7mg·ml -1 , average particle size 29.04nm, dispersion coefficient 0.347. The freeze-dried powder was obtained by adding 4% mannitol and freeze-dried. The particle size of the micelle solution obtained after the obtained powder was stored in the refrigerator for 3 months was all less than 40nm, indicating that the freeze-dried preparation was stable in properties.

Embodiment 3

[0026] Embodiment 3: Preparation of quercetin nano-micelle preparation

[0027] Accurately weigh 36.0mg of quercetin, 250.0mg of non-ionic surfactant Pluronic P123, stir and dissolve with an appropriate amount of ethanol, remove the organic solvent by rotary evaporation in a water bath at 60°C, and dry in a vacuum oven overnight to obtain dry and transparent Add 6 mL of deionized water to the drug film skeleton, stir at 50° C. and 700 rpm for 5 hours at a constant speed, and filter through a microporous membrane to obtain a quercetin nano-micelle solution. The micellar preparation contains quercetin 5.8mg·ml -1 , average particle size 25.20nm, dispersion coefficient 0.243. Adding 4% mannitol to freeze-dry, the average particle size of the micelle solution obtained by hydration of the obtained powder is 30.3nm, and no drug is precipitated out, indicating that the freeze-drying process has no significant impact on the preparation.

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Abstract

The invention discloses a quercetin nano-micelle preparation which is made from the following components in parts by weight: 20-40 parts of quercetin as a bulk drug and 220-330 parts of a pluronic surfactant as a drug carrier. A preparation method comprises the following steps: mixing the quercetin with the pluronic surfactant and dissolving in an organic solvent until being fully dissolved, and carrying out rotary evaporation at 15-60 DEG C for removing the organic solvent to obtain a drug-containing film; and drying the film in vacuum, adding a water phase for hydrating at 15-60 DEG C to obtain micelle solution, and filtering with a millipore filter to obtain the quercetin nano-micelle preparation. The obtained nano-micelle preparation has small nano-grade particle size of 20-60nm, a hydrophobic core and a hydrophilic shell, thus ensuring that the preparation has small possibility of being swallowed by a reticuloendothelial system in body, achieving effects such as targeting, long circulating and the like, and being beneficial to clinical application.

Description

technical field [0001] The invention relates to a quercetin nano-micelle preparation and a preparation method thereof. Background technique [0002] Quercetin (Quercetin, QT) belongs to the flavonols extracted from plants. It has a multi-hydroxy structure and is widely found in fruits and vegetables. It has anti-inflammatory, anti-oxidant, neuroprotective and other effects. And other cancer cells have inhibitory effect, and its pharmacological effect is obvious. However, quercetin is almost insoluble in water, and the solubility in water is only 0.166 μg·ml -1 ~7.7μg·ml -1 , fat solubility is also poor, and oral bioavailability is low, which greatly limits its absorption and utilization in the body. Therefore, improving the solubility of quercetin in water and the absorption and utilization in the body are problems to be solved urgently in the application of this medicine. [0003] Polymer micelles are a self-assembled structure formed by block copolymers containing hydr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/34A61K31/352A61P25/00A61P29/00A61P35/00A61P35/02A61P39/06A61K47/10
Inventor 翟光喜赵丽艳
Owner SHANDONG UNIV
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