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Core-shell nano drug particle, its preparation method and application

A nano-drug and particle technology, applied in pharmaceutical formulations, inactive medical preparations, etc., can solve problems such as killing tumor cells, and achieve the effect of simple preparation method and easy operation.

Active Publication Date: 2014-10-29
ZHUHAI INST OF ADVANCED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the complexity and diversity of molecular biological mechanisms involved in tumor formation, as well as the emergence of multidrug resistance of tumor cells, it is impossible to fundamentally kill tumor cells with only one chemotherapy drug.

Method used

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  • Core-shell nano drug particle, its preparation method and application
  • Core-shell nano drug particle, its preparation method and application

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Experimental program
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Effect test

Embodiment 1

[0039]The first drug is near-infrared photothermal conversion reagent indocyanine green (ICG), the second drug is chemotherapy drug doxorubicin (DOX), and the hydrophobic polymer is lactic acid-glycolic acid copolymer (PLGA). Lecithin is selected as the class molecule, and distearoylphosphatidylethanolamine-carboxypolyethylene glycol (DSPE-PEG-COOH) is selected as the amphiphilic macromolecular compound. PLGA and ICG adsorbed on it form a hydrophobic core, the phospholipid end of DSPE-PEG-COOH and the hydrophobic part of phospholipid are arranged on the surface of the hydrophobic inner core, DOX is adsorbed on the phospholipid end of DSPE-PEG-COOH and the phospholipid, forming shell.

[0040] The preparation method comprises the following steps:

[0041] PLGA is dissolved in acetone, the concentration of PLGA is 2mg / mL, ICG is dissolved in PLGA acetone solution, the concentration of ICG is 0.4mg / mL, take 1mL of PLGA acetone solution containing ICG and add it dropwise to 30mL ...

Embodiment 2

[0048] The preparation method comprises the following steps:

[0049] PLGA is dissolved in acetone, the concentration of PLGA is 5mg / mL, ICG is dissolved in PLGA acetone solution, the concentration of ICG is 0.2mg / mL, take 1mL of PLGA acetone solution containing ICG and add it dropwise to 30mL polyvinyl alcohol aqueous solution, using Ultrasonic cell disruptor ultrasonicated at a frequency of 20KHz and a power of 130W for 5 minutes; the precipitate was collected by centrifugation, and the obtained precipitate was washed three times with ultrapure water, and the ICG-PLGA nanoparticles (hydrophobic core) passing through the polycarbonate membrane with a pore size of 100nm were collected .

[0050] Dissolve 25 mg of soybean lecithin, DSPE-PEG-COOH, and cholesterol (mass ratio: 20:2:10) in a round bottom flask with 2 mL of chloroform, and perform rotary evaporation at 35-40°C to remove the organic solvent Chloroform, so that the above film-forming materials form a uniform film on...

Embodiment 3

[0052] The preparation method comprises the following steps:

[0053] PLGA is dissolved in acetone, the concentration of PLGA is 1mg / mL, ICG is dissolved in PLGA acetone solution, the concentration of ICG is 1mg / mL, take 1mL of PLGA acetone solution containing ICG and add it dropwise to 30mL polyvinyl alcohol aqueous solution, and use ultrasonic The cell disruptor was sonicated at a frequency of 20KHz and a power of 130W for 5min; the precipitate was collected by centrifugation, and the obtained precipitate was washed three times with ultrapure water, and the ICG-PLGA nanoparticles (hydrophobic core) passing through a polycarbonate membrane with a pore size of 100nm were collected.

[0054] Dissolve 25 mg of soybean lecithin, DSPE-PEG-COOH, and cholesterol (mass ratio: 20:2:10) in a round bottom flask with 2 mL of chloroform, and perform rotary evaporation at 35-40°C to remove the organic solvent Chloroform, so that the above film-forming materials form a uniform film on the b...

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Abstract

The invention discloses a core-shell drug nano-particle which comprises a hydrophobic inner core and a shell, wherein the inner core comprises a hydrophobic polymer and a first drug adsorbed on the hydrophobic polymer, the shell comprises a single layer of lipid molecules, an amphiphilic compound and a second drug, the hydrophobic inner core is wrapped by the single lipid layer formed by the single layer of lipid molecules, the single lipid layer has a hydrophobic part facing the hydrophobic inner core and a hydrophilic part facing the outside of the drug nano-particle, the amphiphilic compound has a lipid terminal and a hydrophilic terminal covalently cross-linked with the lipid terminal, the lipid terminal of the amphiphilic compound is inserted into the single lipid layer, the second drug is adsorbed to the lipid terminal of the amphiphilic compound and the single lipid layer. The drug nano-particle disclosed by the invention can achieve the effect of multi-stage release of the first and the second drugs and is prepared according to a two-step method.

Description

technical field [0001] The invention relates to the field of drug carriers, in particular to a core-shell type nanometer drug particle and its preparation method and application. Background technique [0002] Postoperative recurrence and metastasis of cancer are usually related to incomplete resection of tumor cells. After tumor resection, continuous administration of anti-tumor drugs in the lesion plays an active and effective role in preventing such recurrence and metastasis. However, due to the complexity and diversity of molecular biological mechanisms involved in tumor formation, as well as the multidrug resistance of tumor cells, it is impossible to kill tumor cells fundamentally with only one chemotherapy drug. In addition, according to the different growth cycles of tumor cells, the differential and sequential release of various chemotherapeutic drugs also plays an important role in killing tumor cells. Therefore, a variety of drugs with different mechanisms of acti...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/00
Inventor 蔡林涛郑明彬龚萍赵鹏飞岳彩霞郑翠芳
Owner ZHUHAI INST OF ADVANCED TECH
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