Purpose of naringenin, naringenin nanoliposome and preparation method and application thereof

A nano-liposome and naringenin technology applied in the field of medicine to achieve high encapsulation efficiency, reduced drug dosage, and uniform average particle size

Active Publication Date: 2017-12-05
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The above dosage forms have improved the solubility and oral bioavailabi...

Method used

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  • Purpose of naringenin, naringenin nanoliposome and preparation method and application thereof
  • Purpose of naringenin, naringenin nanoliposome and preparation method and application thereof
  • Purpose of naringenin, naringenin nanoliposome and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0042] Embodiment 1, the preparation of naringenin nano liposome

[0043] Accurately weigh 0.0126g of naringenin, 0.1127g of soybean lecithin, and 0.0124g of cholesterol, add 2mL of chloroform and 1mL of methanol, fully dissolve, and remove the solvent by rotary evaporation under reduced pressure in a water bath at 37°C until a uniform layer is formed on the wall of the eggplant-shaped bottle. lipid film. Add 3mL of 0.01mol / L phosphate buffer (pH=7.4) for hydration at 40°C for 30min, then sonicate at 80W in a 40°C water bath for 30min to obtain a naringenin nanoliposome suspension. Ultrasound for 15 minutes (80% of full amplitude) in an ice bath to obtain light blue opalescent naringenin nanoliposomes of the present invention.

Embodiment 2

[0044] Embodiment 2, the preparation of naringenin nano liposome

[0045]Accurately weigh 0.0056g of naringenin, 0.0617g of soybean lecithin, and 0.0143g of cholesterol, add 1mL of chloroform and 2mL of methanol to fully dissolve, and remove the solvent by rotary evaporation under reduced pressure in a water bath at 37°C until a uniform layer is formed on the wall of the eggplant-shaped bottle. lipid film. Add 3mL of 0.01mol / L phosphate buffer (pH=7.4) to hydrate at 40°C for 30min, then ultrasonicate in a 50W, 40°C water bath for 30min to obtain a naringenin nanoliposome suspension. Ultrasound for 15 minutes (50% of full amplitude) under an ice bath to obtain light blue opalescent naringenin nanoliposomes of the present invention.

Embodiment 3

[0046] Embodiment 3, the preparation of naringenin nano liposome

[0047] Accurately weigh 0.0096g of naringenin, 0.0629g of soybean lecithin, and 0.0146g of cholesterol, add 2mL of chloroform and 1mL of methanol, fully dissolve, and remove the solvent by rotary evaporation under reduced pressure in a water bath at 40°C until a uniform layer is formed on the wall of the eggplant-shaped bottle. lipid film. Add 3mL of 0.01mol / L phosphate buffer (pH=7.4) for hydration at 40°C for 25min, then sonicate at 80W in a 30°C water bath for 25min to obtain a naringenin nanoliposome suspension. Ultrasound for 20 minutes (50% of full amplitude) in an ice bath to obtain light blue opalescent naringenin nanoliposomes of the present invention.

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Abstract

The invention discloses purpose of naringenin, naringenin nanoliposome and a preparation method and application thereof. The naringenin is applied in the preparation of drugs for treating non-alcoholic fatty liver. The naringenin nanoliposome comprises naringenin and nanoliposome. The nanoliposome comprises phosphatide and cholesterol. The mass ratio of naringenin to phosphatide to cholesterol is 1:4-9:1-2. The preparation method comprises the following steps: 1) dissolving naringenin, phosphatide and cholesterol in a solvent, mixing, and removing the solvent to obtain a mixture; 2) hydrating the mixture obtained in the step 1) by the use of an aqueous medium to obtain a naringenin nanoliposome crude suspension; and 3) successively carrying out water-bath ultrasonic treatment and probe ultrasonic treatment on the naringenin nanoliposome crude suspension obtained in the step 2), so as to obtain the naringenin nanoliposome. The naringenin nanoliposome can raise oral bioavailability of naringenin and enhance the control effect of naringenin on non-alcoholic fatty liver.

Description

technical field [0001] The invention relates to the use of naringenin, naringenin nano-liposome and its preparation method and application, belonging to the technical field of medicine. Background technique [0002] Nonalcoholic fatty liver disease (NAFLD) is a genetic-environment-metabolic stress-related disease, characterized by hepatic steatosis and excessive fat accumulation as the main pathological features, but without a history of excessive alcohol consumption sign. In recent years, with the improvement of living standards in my country and changes in lifestyle and dietary structure, the prevalence of this liver disease, which was relatively common in Western countries, has been increasing year by year in China, so it has attracted more and more attention. The pathogenesis of NAFLD mainly includes "one hit" mainly including insulin resistance and "second hit" mainly including oxidative stress, massive death of liver cells and fibrosis. At present, there is no clear ...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61K9/127A61K47/24A61K47/28A61P1/16
CPCA61K9/127A61K31/352A61K47/24A61K47/28
Inventor 祁荣陈聪
Owner PEKING UNIV
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