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Hypoxia response lipidosome drug carrier as well as preparation method and application thereof

A technology of liposomes and drugs, which is applied in the field of pharmacy, can solve the problems of no reports of hypoxia-responsive liposome drug carriers, etc., and achieve the effects of improving anti-tumor effects, easy scale-up production, and simple preparation methods

Active Publication Date: 2017-05-24
北京华诺泰生物医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, at this stage, hypoxia-responsive drug carriers are mainly limited to those formed by nitroaromatic functionalized polymers, and there are no reports of hypoxia-responsive liposome drug carriers.

Method used

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  • Hypoxia response lipidosome drug carrier as well as preparation method and application thereof
  • Hypoxia response lipidosome drug carrier as well as preparation method and application thereof
  • Hypoxia response lipidosome drug carrier as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] The hypoxia response molecule selected for this implementation is a 2-nitroimidazole derivative, and its preparation method is as follows:

[0044]

[0045] Take 60 mg of 2-nitroimidazole and 70 mg of 1,12-dibromododecane and add them into 5 mL of dimethylformamide (DMF) to dissolve fully, then add K 2 CO 3 80 mg, stirred at 50°C for 24 hours; add 5 mL of deionized water to the reaction solution, then add 5 mL of ethyl acetate for extraction, repeat the extraction 3 times, combine the extraction solution, then add 2 mL of deionized water to the extraction solution for shaking, then let it stand for separation layer, remove the lower aqueous solution, repeat 3 times, and remove the ethyl acetate by vacuum rotary evaporation to obtain 2-nitroimidazole derivatives, that is, linear hypoxia responsive molecules HR (hypoxia responsive elements), its hydrogen nuclear magnetic resonance spectrum (1H NMR) Such as figure 1 shown.

Embodiment 2-1

[0047] Preparation of liposomal drug carrier with hypoxia response effect:

[0048] Dipalmitoylphosphatidylcholine (DPPC), high-purity cholesterol (HP-CHOL), dimyristoylphosphatidylcholine (DMPC), methoxy-polyethylene glycol-distearoylphosphatidylethanolamine ( DSPE-MPEG2K), hydrophobic aromatic nitro compound derivatives (HR) are dissolved in methanol and chloroform mixed solution (volume ratio 1:4) according to the mass ratio (total 20mg) of 70:20:3:3:16, minus Press rotary steaming to form a film, and use 10mL deionized water to ultrasonically hydrate at 50°C to obtain blank hypoxia-responsive liposome HR-LPs; the preparation method of control blank liposome LPs is the same as HR-LPs, and the liposome components DPPC, HP-CHOL, DMPC, and DSPE-MPEG2K are also mass ratio 70:20:3:3 (total 20mg), without adding hypoxia response molecules, vacuum rotary steaming to form a film, 10mL deionized water 50 ℃ ultrasonic hydration , to get blank liposome LPs.

Embodiment 2-2

[0050] Preparation of liposomal drug carrier with hypoxia response effect:

[0051] Dipalmitoylphosphatidylcholine (DPPC), high-purity cholesterol (HP-CHOL), dimyristoylphosphatidylcholine (DMPC), methoxy-polyethylene glycol-distearoylphosphatidylethanolamine ( DSPE-MPEG2K), hydrophobic aromatic nitro compound derivatives (HR) were dissolved in methanol and chloroform mixed solution (volume ratio 1:3) according to the mass ratio of 70:18:3:3:12 (total 20mg), and the rest The procedure was the same as that in Example 2-1, and blank hypoxia-responsive liposome HR-LPs were prepared.

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Abstract

The invention discloses a hypoxia response lipidosome drug carrier. The hypoxia response lipidosome drug carrier is prepared from phospholipid, cholesterol and hypoxia response molecules, wherein the mass ratio of the cholesterol to the phospholipid ranges from 1:10 to 1:2, and the mass ratio of the hypoxia response molecules to the phospholipid ranges from 1:10 to 1:4; the phospholipid is a mixture of dipalmitoyl phosphatidylcholine, dimyristoyl phosphatidylcholine and methoxy-polyethylene glycol-distearoyl phosphoethanolamine; the hypoxia response molecules are derivatives of a hydrophobic aromatic nitro compound and are located between bimolecular layers of the phospholipid. The hypoxia response lipidosome drug carrier disclosed by the invention is used for loading an antitumor drug, and has a remarkable effect in application to drugs for treating tumors or other hypoxia-related diseases.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a liposome drug carrier with hypoxia response effect, and a preparation method and application of the drug carrier. Background technique [0002] Small-molecule chemotherapeutic drugs in tumor treatment have no tissue selectivity, and it is difficult to achieve high drug concentration at the tumor lesion site. When used in large doses, the therapeutic effect is poor and the side effects are strong. Loading small molecule chemotherapeutic drugs into nano-drug carriers such as liposomes can significantly reduce side effects, but traditional liposome drug carriers cannot significantly improve the therapeutic effect of anti-cancer drugs. Therefore, using novel controlled-release materials to improve Liposome drug carrier can release drug specifically at the tumor site and improve the curative effect, which is an urgent research content. [0003] Hypoxia is one of the basic characteristics of...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/24A61K47/18A61K47/22A61K45/00A61P35/00
Inventor 陈忠平李怡刘益飞陈秋萍赵越曹明翔朱俐
Owner 北京华诺泰生物医药科技有限公司
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