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Preparing method and application of ginsenoside-multi-component jointly-loading targeting nanometer system

A ginsenoside, multi-component technology, which is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, pharmaceutical formulas, etc., can solve the problem of less distribution, low stability and poor biocompatibility of pharmaceutical active ingredients. and other problems to achieve the effect of improving bioavailability, small side effects and low cost

Active Publication Date: 2016-06-29
CHENGDU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to provide a preparation method of ginsenoside multi-component co-loaded targeting nano system, which can solve the defects of poor biocompatibility, low stability, and less distribution of drug active ingredients in tumor tissue cells in the prior art. It can achieve the effect of high water solubility, good absorption, high stability, active targeting, and active ingredients can gather in tumor tissues

Method used

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  • Preparing method and application of ginsenoside-multi-component jointly-loading targeting nanometer system
  • Preparing method and application of ginsenoside-multi-component jointly-loading targeting nanometer system
  • Preparing method and application of ginsenoside-multi-component jointly-loading targeting nanometer system

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Embodiment 1

[0034] 5 mg of egg yolk lecithin, 5 mg of cholesterol and 2.5 mg of PEG-DPPC material were dissolved in 2 mL of absolute ethanol, slowly added dropwise to 20 mL of water at 60°C, and stirred continuously for 5 min to obtain an aqueous lipid solution. Dissolve 15mg PLGA material, 10mg ginsenoside Rg3, 5mg ginsenoside Rh2 and 5mg ginsenoside Rb1 in acetonitrile, ultrasonically treat for 1min and slowly drop into the above lipid aqueous solution, ultrasonically treat under ice bath for 20min, continue stirring for 30min, and use rotating The residual organic solvent was removed by an evaporator under reduced pressure, 0.1uM of accounting aptamer AS1411 was added, and the stirring was continued for 30min. The unloaded drug was removed through a 0.45μm filter, and then sterilized through a 0.2μm filter to obtain uniform pan-opalescence. The nano solution is prepared into a lipid nanoparticle solution containing three ginsenoside components.

Embodiment 2

[0036] 5 mg of egg yolk lecithin, 5 mg of cholesterol and 2.5 mg of PEG-DSPE material were dissolved in 2 mL of absolute ethanol, slowly added dropwise to 20 mL of water at 60°C, and stirred continuously for 5 min to obtain an aqueous lipid solution. Dissolve 15mg PLGA material, 10mg ginsenoside Rg3, 5mg ginsenoside Rh2 and 5mg ginsenoside Rb1 in acetonitrile, ultrasonically treat for 1min, slowly drop into the above lipid aqueous solution, ultrasonically treat under ice bath for 20min, continue stirring for 30min, and use rotary The residual organic solvent was removed by the evaporator under reduced pressure, 0.1uM of accounting aptamer AS1411 was added, and the stirring was continued for 30min. The unloaded drug was removed through a 0.45μm filter, and then sterilized through a 0.2μm filter to obtain uniform pan-opalescence. The nano solution is prepared into a lipid nanoparticle solution containing three ginsenoside components.

Embodiment 3

[0038]5 mg of egg yolk lecithin, 5 mg of cholesterol and 2.5 mg of DSPE-PEG-COOH material were dissolved in 2 mL of absolute ethanol, slowly added dropwise to 20 mL of water at 60°C, and stirred continuously for 5 min to obtain an aqueous lipid solution. Dissolve 15mg PLGA material, 10mg ginsenoside Rg3, 5mg ginsenoside Rh2 and 5mg ginsenoside Rb1 in acetonitrile, ultrasonically treat for 1min and slowly drop into the above lipid aqueous solution, ultrasonically treat under ice bath for 20min, continue stirring for 30min, and use rotating The residual organic solvent was removed by an evaporator under reduced pressure, 0.1uM of accounting aptamer AS1411 was added, and the stirring was continued for 30min. The unloaded drug was removed through a 0.45μm filter, and then sterilized through a 0.2μm filter to obtain uniform pan-opalescence. The nano solution is prepared into a lipid nanoparticle solution containing three ginsenoside components.

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Abstract

The invention discloses a preparing method of a ginsenoside-multi-component jointly-loading targeting nanometer system.The preparing method includes the steps that after egg yolk lecithin, cholesterol and polyethylene glycol-dipalmitoyl phosphatidyl choline are dissolved, warm water is slowly and dropwise added for stirring, and a lipid water solution is obtained; the multi-component active ingredients containing ginsenoside Rg3, ginsenoside Rh2 and ginsenoside Rb1 and a copolymer of polylactic acid-hydroxyacetic acid are dissolved to be slowly and dropwise added into the lipid water solution to be stirred to be even, a solvent is removed, and lipidosome nanometer particles are obtained; aptamer is dissolved to be modified to the surfaces of the lipidosome nanometer particles, and an even and opalescence-flooding nanometer system solution is obtained by filtering and sterilizing.According to the preparing method, the anti-tumor effect of medicine is improved with the nanocrystallization technology, joint transmission of a multi-component tumor tissue can be achieved in the mode that the three ginsenoside ingredients are jointly loaded to the nanometer system, and therefore the problems that the metabolic behaviors and the tumor-cell entering capacity of different ingredients are different are solved.

Description

technical field [0001] The invention relates, in particular to a preparation method of a ginsenoside multi-component co-loaded targeting nanometer system. Background technique [0002] The active ingredients of traditional Chinese medicine have played an increasingly significant role in anti-tumor. At present, there are still some problems in the application of active ingredients of traditional Chinese medicine in anti-tumor. For example, most anti-cancer drugs have poor water solubility, difficult absorption, short half-life, low delivery efficiency, free Poor drug targeting, etc. The practical problems that need to be solved urgently for anti-tumor traditional Chinese medicine preparations are: on the premise of ensuring the safety of the preparations, improving the delivery of the active ingredients of traditional Chinese medicine and improving the tumor targeting of the active ingredients; rationally designing dosage forms for specific types of tumors, exploring and enri...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61K9/51A61K9/08A61K47/26A61K47/34A61P35/00
CPCA61K47/26A61K9/08A61K9/5146A61K31/704A61K2300/00
Inventor 邹亮章津铭李维胡一晨雨田符佳杨林郭晓恒赵江林赵钢
Owner CHENGDU UNIV
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