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Quercetin nanoparticle and preparation method thereof

A nanoparticle, quercetin technology, applied in pharmaceutical formulations, medical preparations with inactive ingredients, medical preparations containing active ingredients, etc., can solve the problems of large particle size and limited solubility improvement, and achieve sustained release time. Long, simple ingredients, easy to expand the effect of production

Active Publication Date: 2015-12-02
INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Quercetin nanocrystals with very high drug loading, although there are also research reports, but their particle size is relatively large (nearly 400nm), and the solubility improvement is limited.

Method used

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  • Quercetin nanoparticle and preparation method thereof
  • Quercetin nanoparticle and preparation method thereof
  • Quercetin nanoparticle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Accurately weigh 20 mg of quercetin and 4 mg of TPGS, dissolve them in 0.5 mL of DMF, slowly add them dropwise to 10 mL of water under ultrasonic conditions at 10 °C, 13000 r min -1 Centrifuge for 20 min, discard the supernatant, add 5 mL of water to the precipitate, ultrasonically redissolve, and homogenize at 10°C and 2000 bar for 5 times. The result is as figure 1 (Left), the average particle size after preparation is 173.21nm, the PDI is 0.18, the potential is -19.02mV, the average particle size is 175.91nm after 10 days at 4°C, and the storage stability is good.

Embodiment 2

[0028] Accurately weigh 20mg of quercetin and 20mg of TPGS, dissolve in 0.5mL of DMF, slowly add dropwise to 10mL of water at 10°C and ultrasonic conditions, 13000r·min -1 Centrifuge for 20 min, discard the supernatant, add 5 mL of water to the precipitate, ultrasonically redissolve, and homogenize at 10°C and 2000 bar for 5 times. The result is as figure 1 (Right), the average particle size after preparation is 159.13nm, the PDI is 0.16, and the potential is -13.73mV.

Embodiment 3

[0030] Accurately weigh 20 mg of quercetin and 20 mg of TPGS, dissolve in 0.5 mL of DMF, slowly add dropwise to 10 mL of water under stirring at 10 °C, 13000 r min -1 Centrifuge for 20 min, discard the supernatant, add 5 mL of water to the precipitate, ultrasonically redissolve, and homogenize at 10°C and 2000 bar for 5 times. After preparation, the average particle diameter is 231.18nm, the PDI is 0.21, and the potential is -10.03mV.

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Abstract

The invention relates to a quercetin nanoparticle and a preparation method thereof. The quercetin nanoparticle is prepared by using one or two selected from the group consisting of a nanometer precipitation process and a high pressure homogenization process. According to the invention, quercetin is used as a bulk drug, TPGS (vitamin E polyethanediol succinate) is used as a main stabilizing agent, and a mass ratio of the bulk drug to the carrier stabilizing agent is 1: 20 to 10: 1. The prepared quercetin nanoparticle has a small particle size and a high drug loading rate, and when a drug-carrier ratio is 5: 1, the average particle size of the quercetin nanoparticle is 173.21 nm and the drug-loading rate is about 80%; moreover, the prepared quercetin nanoparticle has good stability, the drug exists in crystal form in the nanoparticle, and an obvious slow release effect in vitro is obtained. The quercetin nanoparticle with a high drug loading rate and a small particle size can be prepared by using TPGS, shows obvious slow release effect in vitro, overcomes the problem of poor water-solubility and has good application prospects.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a preparation method of quercetin nanoparticles with TPGS as a main auxiliary material and an investigation on its in vitro properties. Background technique [0002] Quercetin is a flavonoid compound present in many plants with the molecular formula C 12 h 10 o 7 , with a molecular weight of 302.23, has a wide range of pharmacological activities, such as anti-tumor, anti-oxidation, kidney protection, vasodilation and heart protection, etc. It has high medicinal value, but due to its poor water solubility, the measured saturated solubility in water is only (6.83 ±0.41)μg·mL -1 , Difficult to absorb when taken orally, unable to be administered by injection, etc. make the application limited. In recent years, some scholars have tried to prepare quercetin into different dosage forms, such as micelles, polymer nanoparticles, solid lipid nanoparticles, etc., with low drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/352A61K47/34A61P35/00A61P39/06A61P13/12A61P9/08A61P9/00
Inventor 王向涛邸静洪靖怡刘营营
Owner INST OF MEDICINAL PLANT DEV CHINESE ACADEMY OF MEDICAL SCI
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