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PEG type elaioplast nanometer particle

A nanoparticle and liposome technology, applied in the field of drug carriers, can solve the problem of low biological activity

Inactive Publication Date: 2010-07-21
HUNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The purpose of the present invention is to provide a PEGylated liposome nanoparticle with an amino active molecule on the surface that is easily modified to solve the problem of low biological activity of the bioaffinity molecules attached to the surface of the liposome

Method used

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  • PEG type elaioplast nanometer particle
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  • PEG type elaioplast nanometer particle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Weigh 0.8g of p-nitrophenyl chloroformate (pNPC) and dissolve it in 10ml of anhydrous acetonitrile solvent, weigh 2.0g of PEG2000 and dissolve it in 30ml of acetonitrile solvent, quickly add 2.0g of pNPC solution to activate Molecular sieves and 1ml of anhydrous triethylamine solution were used to add the PEG2000 solution to the pNPC solution drop by drop with a constant pressure and low pressure funnel in a closed system. The flow rate was controlled at 0.5 drops / second, and stirred at room temperature for 14 hours. . Filter out the precipitate, add 400ml of anhydrous ether to the filtrate, place it in a refrigerator at 4°C for recrystallization overnight, filter the crystals with suction, wash with a small amount of ether, dissolve in acetonitrile, and recrystallize once to obtain the product PEG-(pNP) 2 , the solvent and moisture were removed under vacuum (NMR characterization results are shown in Figure 5), compared with the NMR characterization of the raw material ...

Embodiment 2

[0031] Weigh 0.6g of p-nitrophenyl chloroformate (pNPC) and dissolve it in 10ml of anhydrous acetonitrile solvent, weigh 2.0g of PEG2000 and dissolve it in 30ml of acetonitrile solvent, quickly add 2.0g of pNPC solution to activate Molecular sieves and 1ml of anhydrous triethylamine solution were used to add the PEG2000 solution to the pNPC solution drop by drop with a constant pressure and low pressure funnel in a closed system. The flow rate was controlled at 0.5 drops / second, and stirred at room temperature for 12 hours. . Filter out the precipitate, add 400ml of anhydrous ether to the filtrate, place it in a refrigerator at 4°C for recrystallization overnight, filter the crystals with suction, wash with a small amount of ether, dissolve in acetonitrile, and recrystallize once to obtain the product PEG-(pNP) 2 , remove the solvent and water under vacuum. Characterized by NMR. Weigh 1.0gPEG-(pNP) 2Dissolve in 20ml of chloroform, add 60mg of DPPE solution under nitrogen pr...

Embodiment 3

[0033] Weigh 1.2g of p-nitrophenyl chloroformate (pNPC) and dissolve it in 10ml of anhydrous acetonitrile solvent, weigh 2.0g of PEG2000 and dissolve it in 30ml of acetonitrile solvent, quickly add 2.0g of pNPC solution to activate Molecular sieves and 1ml of anhydrous triethylamine solution were used to add the PEG2000 solution to the pNPC solution drop by drop with a constant pressure and low pressure funnel in a closed system. The flow rate was controlled at 0.5 drops / second, and stirred at room temperature for 13 hours. Filter out the precipitate, add 400ml of anhydrous diethyl ether to the filtrate, place it in a refrigerator at 4°C for recrystallization overnight, filter the crystals with suction, wash with diethyl ether, dissolve in acetonitrile, and recrystallize once again to obtain the product PEG-(pNP) 2 , remove the solvent and water under vacuum. Characterized by NMR. Weigh 1.2g of synthesized PEG-(pNP) 2 Dissolve in 20ml of chloroform, add 50mg of DPPE solution...

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Abstract

A PEG coated liposome nanoparticle features that in its surficial PEG layer, some of terminals are modified by p-nitrophenyl carbonate (pNPC). Its preparing process includes such steps as activating the both terminals of PEG by p-nitrophenyl chloroformate for synthesizing DPPE-PEG-pNP, proportionally dissolving soybean phosphatide, cholesterol, DPPE-PEG and DPPE-PEG-pNP in organic solvent, preparing liposome nanoparticles by ultrasonic film method, and stirring for 4-5 hr for linking active moleculae.

Description

technical field [0001] The invention belongs to a drug carrier, in particular to a PEGylated liposome nanoparticle. Background technique [0002] Liposome has been used as a drug carrier for nearly two decades and has been widely used as a drug carrier. At home and abroad, a lot of research has been done on the use of liposomes as drug targeting carriers. At present, liposomes are used as drug targeting carriers, mainly by connecting biological affinity molecules to liposomes through some physical or chemical methods. surface, so as to achieve the purpose of targeting. After years of research, the research on the use of PEGylated liposomes as targeting carriers has made some progress in both experiments and clinics. However, at present, when connecting bioaffinity molecules on the surface of liposomes, it is mainly through the reaction of the carboxyl group at one end of PEG with the amino group of the active molecule. The biological activity of the molecule is greatly re...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/34A61K47/48C08G65/48A61K47/28A61K47/60A61K47/69
Inventor 王柯敏胡建兵何晓晓谭蔚泓李惠敏龚萍张寿春
Owner HUNAN UNIV