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A kind of magnetic compound and its preparation method and application

A composite, magnetic technology, applied in the direction of magnetic objects, magnetic materials, drug combinations, etc., to achieve the effect of low cytotoxicity

Inactive Publication Date: 2011-12-07
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, not suitable as a carrier for nucleic acids / drugs

Method used

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  • A kind of magnetic compound and its preparation method and application
  • A kind of magnetic compound and its preparation method and application
  • A kind of magnetic compound and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Example 1: CH 3 SO 3 - Preparation of PEG-OH

[0043] Dissolve 3.8mL of methanesulfonyl chloride in 50mL of tetrahydrofuran, and then slowly drop it into 200mL of tetrahydrofuran dissolved in 10g of PEG (average molecular weight: 200) and 7mL of triethylamine. After 3 hours, the dropwise addition is completed and stirred at room temperature overnight. Filter the reaction solution, remove the solvent by rotary evaporation of the filtrate, and obtain CH through silica gel column separation. 3 SO 3 -PEG-OH.

Embodiment 2

[0044] Embodiment 2: Preparation of N3-PEG-OH

[0045] 2.8g CH 3 SO 3 -PEG-OH (average molecular weight 200) and 1 g of sodium azide were dissolved in 25 mL of water, and the reaction solution was reacted at 80° C. for 24 hours. After the reaction, cool to room temperature, distill off the solvent water under reduced pressure, add 100mL of dichloromethane, dry the organic phase with anhydrous sodium sulfate overnight, filter, remove the solvent by rotary evaporation, and separate through a silica gel column to obtain N 3 -PEG-OH.

Embodiment 3

[0046] Example 3: NH 2 - Preparation of PEG-OH

[0047] 1g N 3 -PEG-OH (average molecular weight 200) was placed in a reaction flask, 0.13 g of water was added, and 1.3 g of triphenylphosphine was dissolved in 35 mL of tetrahydrofuran, added to the reaction flask, and stirred at room temperature for 10 hours. After the reaction is over, filter, remove the solvent by rotary evaporation, and obtain NH through silica gel column separation. 2 -PEG-OH.

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Abstract

The invention belongs to the field of medicament and pharmaceutics, and relates to a magnetic compound. Specifically, the magnetic compound has a nuclear-casing structure, which means that an external layer is a segmented copolymer of chemical bond gathered basic amino acids or derivatives thereof, and a nuclear is metal oxide particles. A first block of the segmented copolymer is polyethylene glycol, and a second block is polyacrylic acid monoglyceride or polymethacrylic acid monoglyceride, wherein the second block is combined with surfaces of Fe3O4 particles. The invention also relates to apreparation method and a purpose of the magnetic compound. The magnetic compound of the invention not only has low toxicity, but also can permeate a cell membrane or even a karyotheca to enter a nucleus, or even pass through a blood cerebral barrier (BBB), so the magnetic compound can be used as a conveying carrier of various nucleic acids / medicaments.

Description

technical field [0001] The invention belongs to the field of medicine and pharmaceutics, and relates to a magnetic complex, specifically, the magnetic complex has a core-shell structure, that is, the outer layer is a block copolymer of chemically bonded polybasic amino acids or derivatives thereof, The inner core is metal oxide particles. The present invention also relates to the preparation method and application of the magnetic compound. Background technique [0002] The cell membrane is the barrier between the internal and external environment of the cell. Intracellular components need to be excreted through secretion and exocytosis, while extracellular components need to be transported into the cell through receptors and ion channels. It is precisely because of the selective permeability of the cell membrane to substances that it is difficult for macromolecular drugs to pass through the biomembrane to reach the lesion area. For example, cerebrovascular diseases often re...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/34A61K47/02A61K48/00A61K31/519A61K31/675A61P35/00
CPCA61K47/48A61K49/1854H01F1/0054A61K49/1857A61P35/00A61K47/50
Inventor 刘克良张权王晨宏贾启燕冯思良孟庆斌李思成
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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