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

A technology of nanocapsules and quercetin, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, microcapsules, etc., can solve the problems of low solubility, limited application, instability, etc., and achieve improved solubility , Improve the solubility or dispersion degree, and the effect of high encapsulation efficiency

Inactive Publication Date: 2015-07-08
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 144 mg of polyethylene glycol monostearate The acid ester consumption is 288mg, and the distilled water consumption is 528mg. Mix all components in a certain proportion, and undergo the following heating and cooling process at a speed of 4°C / min under electromagnetic stirring: room temperature——85°C——60°C——85°C——60°C——85°C——72 °C, when the system temperature reaches 72 °C, add 2 mL of distilled water at 0 °C to induce irreversible shock of the mixed components and destroy the stable system. Stirring was continued for 5 minutes at room temperature to obtain a stable colloidal solution of lipid nanocapsules.

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

Embodiment 2

[0037] Weigh 5 mg of quercetin, 20 mg of folic acid lipid material, 10 mg of lecithin, 20.5 mg of sodium chloride, 288 mg of medium-chain triglycerides, 576 mg of polyethylene glycol monostearate, and 576 mg of distilled water is 328 mg. Mix all components in a certain proportion, and undergo the following heating and cooling process at a speed of 4°C / min under electromagnetic stirring: room temperature——85°C——60°C——85°C——60°C——85°C——72 °C, when the system temperature reaches 72 °C, add 5 mL of 0 °C distilled water to induce irreversible shock of the mixed components and destroy the stable system. Stirring was continued for 5 minutes at room temperature to obtain a stable colloidal solution of lipid nanocapsules.

Embodiment 3

[0039] Take quercetin 10mg, folic acid lipid material 30mg, lecithin 5mg, the consumption of sodium chloride is 15mg, the consumption of medium chain triglyceride is 216mg, the consumption of polyethylene glycol monostearate is 576mg, the consumption of distilled water is 528 mg. Mix all components in a certain proportion, and undergo the following heating and cooling process at a speed of 4°C / min under electromagnetic stirring: room temperature-85°C-60°C-85°C-60°C-85°C-72°C, when the system temperature reaches At 72°C, add 3mL of 0°C distilled water to induce irreversible shock of the mixed components and destroy the stable system. Stirring was continued for 5 minutes at room temperature to obtain a stable colloidal solution of lipid nanocapsules.

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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, which has various pharmacological activities, such as anti-tumor, anti-oxidation, anti-inflammatory, anti-allergic, etc., and has little toxic and side effects. At present, studies on the pharmacological effects of quercetin on healthy volunteers and patients have been reported. 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. Therefore urgently need to seek a kind of new preparation, to improve the solubility of quercetin in water. [0003] Folate receptor is a glycosylated phosphatidylinositol-linked membrane glycoprotein with a molec...

Claims

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Application Information

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