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Folic acid modified quercetin lipid nano-capsule preparation and preparation method thereof

A nano-capsule, quercetin technology, applied in the directions of non-active ingredients medical preparations, active ingredients-containing medical preparations, microcapsules, etc., can solve the problems of limited application, low solubility, instability, etc. , The effect of high drug loading and high encapsulation efficiency

Inactive Publication Date: 2013-09-25
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although quercetin has a variety of pharmacological activities, its clinical application is greatly limited due to its extremely low solubility in water and instability in physiological environments.

Method used

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  • Folic acid modified quercetin lipid nano-capsule preparation and preparation method thereof
  • Folic acid modified quercetin lipid nano-capsule preparation and preparation method thereof
  • Folic acid modified quercetin lipid nano-capsule preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Weigh 15 mg of quercetin, 10 mg of folic acid-polyethylene glycol-cholesterol hemisuccinate, 15 mg of lecithin, 17.5 mg of sodium chloride, 144 mg of medium-chain triglycerides, and polyethylene glycol monostearate. The amount of acid ester is 288mg, and the amount of distilled water is 528mg. Mix all the components in a certain proportion, and undergo the following temperature rise and fall process at a speed of 4°C / min under electromagnetic stirring: Room temperature——85°C——60°C——85°C——60°C——85°C——72 ℃, when the system temperature reaches 72℃, add 2mL of 0℃ distilled water to induce irreversible shock of the mixed components and destroy the stable system. Continue to stir for 5 min at room temperature to obtain a stable lipid nanocapsule colloid solution.

[0035] The folic acid-modified quercetin lipid nanocapsule preparation obtained in Example 1 has a drug concentration of 4.29 mg / mL in the colloidal solution, which is more than 400 times that of the crude drug, and ...

Embodiment 2

[0037] Weigh 5mg of quercetin, 20mg of folate lipid material, 10mg of lecithin, 20.5mg of sodium chloride, 288mg of medium-chain triglycerides, 576mg of polyethylene glycol monostearate, and distilled water It is 328mg. Mix all the components in a certain proportion, and undergo the following temperature rise and fall process at a speed of 4°C / min under electromagnetic stirring: Room temperature——85°C——60°C——85°C——60°C——85°C——72 ℃, when the system temperature reaches 72℃, add 5mL of 0℃ distilled water to induce irreversible shock of the mixed components and destroy the stable system. Continue to stir for 5 min at room temperature to obtain a stable lipid nanocapsule colloid solution.

Embodiment 3

[0039] Weigh 10 mg of quercetin, 30 mg of folate lipid material, 5 mg of lecithin, 15 mg of sodium chloride, 216 mg of medium-chain triglycerides, 576 mg of polyethylene glycol monostearate, and distilled water 528mg. Mix all the components in a certain proportion, and undergo the following temperature rise and fall process at a speed of 4℃ / min under electromagnetic stirring: room temperature -85℃-60℃-85℃-60℃-85℃-72℃, when the system temperature reaches At 72°C, add 3 mL of 0°C distilled water to induce irreversible shock of the mixed components and destroy the stable system. Continue to stir for 5 min at room temperature to obtain a stable lipid nanocapsule colloid solution.

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Abstract

The invention discloses a folic acid modified quercetin lipid nano-capsule preparation and a preparation method thereof. The preparation comprises the following components in parts by weight: 0.05-5 parts of quercetin, 15-60 parts of distilled water, 5-20 parts of medium chain triglyceride, 10-50 parts of polyethylene glycol monostearate, 0.05-5 parts of lecithin, folic-acid-polyethylene glycol-cholesteryl hemisuccinate and sodium chloride, wherein a folic acid lipid material accounts for 0.01-3 percent of the total weight of the preparation, and sodium chloride accounts for 1-3 percent of the total weight of the preparation. The grain size of the nano-capsule preparation is between 10 and 150nm, a used surfactant contains massive PEG (polyethylene glycol) chains, and the preparation in a body is prevented from being devoured by the reticuloendothelial system by virtue of the nano-grade grain size, a hydrophobic core and a hydrophilic shell; and the mode of intravenous injection plays roles in targeting, long circulating and the like, and is advantageous to clinical application of the preparation.

Description

Technical field [0001] The invention relates to a lipid nanocapsule preparation, in particular to a folic acid modified quercetin lipid nanocapsule preparation and a preparation method thereof. Background technique [0002] Quercetin (QT) is a natural flavonoid compound extracted from plants. It has a variety of pharmacological activities, such as anti-tumor, anti-oxidation, anti-inflammatory, anti-allergic, etc., and has low side effects. There have been reports on the pharmacological effects of quercetin on healthy volunteers and patients. Although quercetin has a variety of pharmacological activities, its extremely low solubility in water and its instability in physiological environments greatly limit its clinical application. Therefore, there is an urgent need to find a new formulation to improve the solubility of quercetin in water. [0003] Folate receptor is a glycosylated phosphatidylinositol-linked membrane glycoprotein with a molecular weight of 38-40kD. Studies have s...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K31/352A61K47/22A61K47/34A61P35/00
Inventor 翟光喜丁步云
Owner SHANDONG UNIV
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