Ginsenoside Rg3 liposome and preparation method thereof

A technology of ginsenosides and liposomes, applied in the field of medicine

Inactive Publication Date: 2013-12-04
JILIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, there is no relevant patent on making ginsenoside Rg3 into liposomes or proliposomes

Method used

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  • Ginsenoside Rg3 liposome and preparation method thereof
  • Ginsenoside Rg3 liposome and preparation method thereof
  • Ginsenoside Rg3 liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044]Weigh 0.5g ginsenoside Rg3, 7.5g egg yolk lecithin, and dissolve 1.25g cholesterol in 50ml n-butanol, place the solution in a pear-shaped bottle, evaporate under reduced pressure above the rotary evaporation to remove n-butanol, and make the phospholipids in the bottle A uniform film was formed on the wall, and the organic solvent was completely volatilized and removed by vacuum drying for 24 hours. 10ml of 10mM pH6.5 phosphate buffer solution was added to fully hydrate at the phospholipid phase transition temperature to obtain a ginsenoside Rg3 liposome suspension. The obtained liposome suspension was homogenized for 3 cycles through a high-pressure homogenizer, and then granulated through a 100nm polycarbonate membrane under high pressure through an extruder, and the encapsulation efficiency of the finally gained liposomes was 87.3%, the average particle size is 131nm.

Embodiment 2

[0046] Weigh 0.5g ginsenoside Rg3, 5g soybean lecithin, and dissolve 1.25g cholesterol in 50ml ethanol, and slowly inject the phospholipid ethanol solution into 20mL of 20mM pH6.5 phosphate buffer solution shaken in a constant temperature water bath at 50 degrees Celsius with a micro-syringe to obtain Ginsenoside Rg3 liposome suspension, the obtained liposome suspension is homogenized through a high-pressure homogenizer for 3 cycles, and then granulated through a 100nm polycarbonate membrane under high pressure by an extruder, An ultrafiltration membrane with a molecular weight cut-off of 5000 was selected, and ethanol was removed by ultrafiltration and concentration. The encapsulation efficiency of the finally obtained liposome was 81.2%, and the average particle size was 136nm.

Embodiment 3

[0048] Weigh 0.5g ginsenoside Rg3, 7.5g egg yolk lecithin, and dissolve 1.25g cholesterol in 50ml ethanol, slowly inject the phospholipid ethanol solution into 20mL of 10mM pH6.5 phosphate buffer solution shaken in a constant temperature water bath at 50 degrees Celsius with a micro-syringe, To obtain the ginsenoside Rg3 liposome suspension, the obtained liposome suspension was homogenized by a high-pressure homogenizer for 3 cycles, and then passed through a 100nm polycarbonate membrane for 2 times under high pressure by an extruder , select the ultrafiltration membrane with molecular weight cut off 5000, remove ethanol with the mode of ultrafiltration concentration, finally gained liposome encapsulation rate is 81.2%, and average particle diameter is 105nm.

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Abstract

The invention provides ginsenoside Rg3 liposome and a preparation method thereof, a drug is encapsulated by using the manner of liposome and proliposome, the obtained liposome has a high encapsulation rate and a stable property, and can significantly improve the absorbable degree and bioavailability of the ginsenoside Rg3, meanwhile enhance the targeting property thereof to a tumor tissue, and improve drug efficacy. At the same time, the obtained liposome can be dosed in a plurality of manners such as oral taking, injection, inhalation by lung, and the like, and can improve the application scope of drugs and the compliance of patients.

Description

technical field [0001] The invention relates to the technical field of medicine, and in particular provides a ginsenoside Rg3 liposome, a preparation method thereof, and an application as a medicine and a health care product. Background technique [0002] Ginsenoside Rg3 is a tetracyclic triterpene saponin present in the natural medicine Panax ginseng with the molecular formula C 42 h 72 o 13 , The relative molecular weight is 784. Ginsenoside Rg3 has the effect of inhibiting tumor growth, mainly acts on the G2 / M phase of the cell proliferation cycle, induces tumor cell apoptosis, selectively inhibits tumor cell adhesion and infiltration, resists tumor metastasis, and inhibits tumor angiogenesis. Regulate the body's immune function and so on. [0003] But ginsenoside Rg3 human body pharmacokinetic research finds, plasma concentration is very low after oral administration, and the maximum blood drug concentration value recorded after oral administration of 3.2mg / kg is onl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/704A61K47/28A61P35/00A61P35/04A61P37/02
Inventor 滕利荣于欢孟庆繁逯家辉程瑛琨王贞佐李玉环杨爽
Owner JILIN UNIV
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