Self-assembled targeting drug carrier nanoparticle and preparation method thereof

A nano-drug carrier and nano-particle technology, which is applied in drug combinations, pharmaceutical formulations, anti-tumor drugs, etc., can solve the problems of large adverse reactions, poor selectivity of anti-cancer drugs, and treatment of toxic reactions, and achieve improved stability and water solubility , prolong circulation half-life, reduce toxic and side effects

Inactive Publication Date: 2016-08-24
BEIJING FORESTRY UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] Cancer has become a major disease that endangers human health. One of the important methods to treat cancer is chemical drug therapy. However, many anticancer drugs have defects such as insoluble in water and poor stability.
In addition, the poor selectivity of anticancer drugs, large adverse reactions, and drug resistance of tumors have greatly affected the efficacy of tumor treatment, and severe toxic reactions often even force treatment to be discontinued.

Method used

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  • Self-assembled targeting drug carrier nanoparticle and preparation method thereof
  • Self-assembled targeting drug carrier nanoparticle and preparation method thereof
  • Self-assembled targeting drug carrier nanoparticle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Synthesis of eight-armed polyethylene glycol (10 KDa)-dihydroartemisinin conjugate: Continuously inject N into a 50ml dry three-neck flask 2 ; at N 2 Under the protection of 0.28g dihydroartemisinin, 1.25g eight-arm carboxypolyethylene glycol (Mw 10,000) was dissolved in 15ml dichloromethane, then added 0.19g EDC, 0.12g DMAP, stirred and dissolved at 0 °C, Stir the reaction for 1 hour, then stir the reaction at room temperature for 24 hours; after the reaction is completed, remove the solvent by rotary evaporation, precipitate with 100ml glacial ether, and filter to obtain the crude product of eight-armed polyethylene glycol-dihydroartemisinin conjugate; use 20ml DMF / IPA (1:4 (v / v)) recrystallization, filter out insoluble matter, precipitate the product with 100ml ether, filter, and vacuum-dry the product to obtain an eight-arm polyethylene glycol-dihydroartemisinin conjugate with a purity of more than 95%. ;

[0026] Synthesis of transferrin-eight-arm polyethylene gl...

Embodiment 2

[0029] Synthesis of eight-armed polyethylene glycol (20 KDa)-dihydroartemisinin conjugate: Continuously inject N into a 50ml dry three-neck flask 2 ; at N 2 Under the protection of 0.14g dihydroartemisinin, 1.25g eight-arm carboxypolyethylene glycol (Mw 20,000) was dissolved in 15ml tetrahydrofuran, then added 0.10g EDC, 0.06g DMAP, stirred to dissolve at 0 ° C, and stirred to react 1 hour, then stirred at room temperature for 24 hours; after the reaction was completed, the solvent was removed by rotary evaporation, 100ml of glacial ether was precipitated, and the crude product of the eight-armed polyethylene glycol-dihydroartemisinin conjugate was obtained after filtration; with 20ml DMF / IPA (1 : 4 (v / v)) recrystallization, filter out insoluble matter, the product is precipitated with 100ml ether, filters, and the product is vacuum-dried to obtain the eight-armed polyethylene glycol-dihydroartemisinin conjugate with a purity of more than 95%;

[0030] Synthesis of transferri...

Embodiment 3

[0033] Synthesis of eight-armed polyethylene glycol (40 KDa)-dihydroartemisinin conjugate: Continuously inject N into a 50ml dry three-neck flask 2 ; at N 2 Under the protection of 0.14g dihydroartemisinin, 2.50g eight-arm carboxypolyethylene glycol (Mw 40,000) was dissolved in 20ml 1,3-dioxane, then added 0.10g EDC, 0.06g DMAP, 0 ° Stir to dissolve at C, stir to react for 1 hour, then stir to react at room temperature for 24h; after the reaction is completed, the solvent is removed by rotary evaporation, 100ml of ice ether is precipitated, and the crude product of eight-armed polyethylene glycol-dihydroartemisinin conjugate is obtained after filtration; Recrystallize with 20ml DMF / IPA (1:4(v / v)), filter out the insoluble matter, precipitate the product with 100ml ether, filter, and dry the product in vacuum to obtain eight-armed polyethylene glycol-dihydro Artemisinin conjugates;

[0034]Synthesis of transferrin-8-arm polyethylene glycol (40 KDa)-dihydroartemisinin conjugat...

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Abstract

The invention discloses a method for preparing self-assembled targeting nano drug carrier particles, comprising: esterifying eight-armed carboxypolyethylene glycol with dihydroartemisinin to obtain eight-armed polyethylene glycol-dihydroartemisinin The eight-arm polyethylene glycol-dihydroartemisinin conjugate is activated by NHS; the activated conjugate is further chemically linked to the targeting molecule transferrin by using an amide bond; the eight-arm modified transferrin The polyethylene glycol-dihydroartemisinin conjugate removes impurities by dialysis, is filtered and freeze-dried; self-assembles to obtain transferrin-modified nano drug carrier particles. The nanoparticle has a double-layer structure, the outer layer is hydrophilic polyethylene glycol, and the inner layer is hydrophobic small molecule drug dihydroartemisinin. The advantages of the present invention: the use of eight-arm carboxypolyethylene glycol greatly increases the drug loading; the targeting effect of drugs on tumor cells and the pH-sensitive release in tumor cells can be realized; the targeted therapy reduces the toxic and side effects on normal tissues ; The preparation process is simple and easy to operate.

Description

technical field [0001] The invention relates to a method for preparing self-assembled targeting nano drug carrier particles. Background technique [0002] Cancer has become a major disease that endangers human health. One of the important methods to treat cancer is chemical drug therapy. However, many anticancer drugs have defects such as insoluble in water and poor stability. In addition, poor selectivity of anticancer drugs, large adverse reactions, and drug resistance of tumors have greatly affected the efficacy of tumor treatment, and severe toxic reactions often even force treatment to be discontinued. Therefore, how to solubilize insoluble anticancer drugs, improve the selectivity to cancer cells and reduce the adverse reactions of drugs is very important. [0003] At present, the use of hydrophilic polyethylene glycol to modify insoluble drugs can greatly improve the solubility and stability of drugs. Polyethylene glycol (PEG) is a water-soluble polyether with low m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K9/19A61K31/366A61K47/42A61P35/00
CPCA61K31/366
Inventor 雷建都刘刻峰何静
Owner BEIJING FORESTRY UNIVERSITY
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