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Active targeting polymer nanoparticle magnetic resonance contrast agent and preparation method thereof

A magnetic resonance contrast agent, active targeting technology, applied in pharmaceutical formulations, preparations for in vivo tests, etc., can solve the problem of tumor targeting efficiency to be improved, and achieve the effects of increasing strength, improving curative effect, and reducing toxic and side effects

Inactive Publication Date: 2010-12-15
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In our previous patent application (CN101612407A), we invented a passive targeting magnetic resonance contrast agent, which achieves passive targeting of the liver by controlling the particle size of the nanoparticle magnetic resonance contrast agent, and has good passive targeting Efficiency, but compared with active targeting, its targeting efficiency for tumors needs to be improved. Therefore, we researched and invented this active targeting nanoparticle magnetic resonance contrast agent

Method used

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  • Active targeting polymer nanoparticle magnetic resonance contrast agent and preparation method thereof
  • Active targeting polymer nanoparticle magnetic resonance contrast agent and preparation method thereof
  • Active targeting polymer nanoparticle magnetic resonance contrast agent and preparation method thereof

Examples

Experimental program
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Embodiment 1

[0038] Synthesis of polylysine-polyethylene glycol-polylactic acid copolymer (PLA-PEG-PLL block copolymer)

[0039](1) Under an argon atmosphere, sequentially add 15g of THF (tetrahydrofuran), 1.5g of KHMDS (potassium hexamethyldisilazide), and 4g of EO (ethylene oxide) into the reaction flask, and place in an ice bath After reacting for 3 days, 3.5g of D, L-LA (D, L-lactide) was then added to the reaction flask. After 8 hours of reaction, 1 g of glacial acetic acid with a volume ratio of 1:6 was added dropwise to the reaction flask. Acetone mixed solution, stirred at room temperature for 30min, terminated and acidolyzed the product, and the product was dropped into 200g of anhydrous ether for precipitation and purification treatment to obtain H 2 N-PEG-b-PLA.

[0040] (2) take 4gH 2 Put N-PEG-b-PLA into a three-neck flask, add 20g DMF, pass in dry argon, stir, then add 1.2gLys(z)-NCA, react at room temperature for 30 hours, distill off the solvent under reduced pressure and...

Embodiment 2

[0043] Preparation method of active targeting polymer nanoparticle magnetic resonance contrast agent:

[0044] (1) Synthesis of diethylenetriaminepentaacetic acid (DTPA) cyclic anhydride

[0045] React 0.1 mol of diethylenetriaminepentaacetic acid with 0.5 mol of acetic anhydride in 0.7 mol of anhydrous pyridine at 65°C for 24 hours, then filter, wash the solid with anhydrous ether, and dry it in vacuo to obtain a white solid diethylene triamine Aminopentaacetic acid cyclic anhydride;

[0046] (2) Synthesis of diethylenetriaminepentaacetic acid-polylysine-polyethylene glycol-polylactic acid copolymer (PLA-PEG-PLL-g-DTPA)

[0047] 1. The synthesis of PLA-PEG-PLL block copolymer adopts the method synthesis (as embodiment 1) by patent publication number CN 101565497A;

[0048] ② Place the PLA-PEG-PLL block copolymer prepared in the above ① and the diethylenetriaminepentaacetic acid cyclic anhydride prepared in step (1) in a round-bottomed flask, feed nitrogen gas, and react at ...

Embodiment 3

[0056] Preparation of Actively Targeting Polymeric Nanoparticle Magnetic Resonance Contrast Agents:

[0057] (1) Synthesis of diethylenetriaminepentaacetic acid (DTPA) cyclic anhydride

[0058] React 0.1 mol of diethylenetriaminepentaacetic acid with 0.5 mol of acetic anhydride in 0.7 mol of anhydrous pyridine at 65°C for 24 hours, then filter, wash the solid with anhydrous ether, and dry it in vacuo to obtain a white solid diethylene triamine Aminopentaacetic acid cyclic anhydride;

[0059] (2) Synthesis of diethylenetriaminepentaacetic acid-polyethylene glycol-polylactic acid copolymer (PLA-PEG-DTPA)

[0060] 1. The synthesis of PLA-PEG-PLL block copolymer adopts the method synthesis (as embodiment 1) by patent publication number CN 101565497A;

[0061] ② Place the PLA-PEG-PLL block copolymer prepared in the above ① and the diethylenetriaminepentaacetic acid cyclic anhydride prepared in step (1) in a round-bottomed flask, feed nitrogen gas, and react at room temperature fo...

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Abstract

The invention discloses an active targeting polymer nanoparticle magnetic resonance contrast agent and a preparation method thereof. The magnetic resonance contrast agent is prepared by chelating nanoparticles of a diethylenetriamine pentaacetic acid-polylysine-polyethylene glycol-polylactic acid copolymer and gadolinium chloride (GdCl3) and connecting a plurality of amino groups of the polylysine and a targeting factor; the structural formula of the diethylenetriamine pentaacetic acid-polylysine-polyethylene glycol-polylactic acid copolymer is shown in the specification; and the targeting factor and chelating ions are connected to the amino groups of a polylysine segment of the copolymer. The magnetic resonance contrast agent of the invention has a remarkable development enhancing function and active targeting development has the characteristics of specificity, selectivity, remarkable biological effect and the like. Poly lactic acid-polyethylene glycol-phase-locked loop-g-diethylenetriaminepentaacetic acid-Ga (PLA-PEG-PLL-g-DTPA-Gd) nanoparticles are taken as carriers of DTPA-Gd and the local concentration of the contrast at a tumor position is increased and a diagnosis effect is enhanced through an active targeting function, toxic and side effects are reduced and the aim of active targeting development is fulfilled.

Description

technical field [0001] The present invention relates to an active targeting magnetic resonance contrast agent mediated by a targeting factor, in particular to a polymer targeting nanoparticle contrast agent capable of specifically actively targeting liver development in magnetic resonance imaging and a preparation method thereof . Background technique [0002] In clinical magnetic resonance imaging (Magnetic Resonance Imaging, MRI), the application of common contrast agents for dynamic enhancement can improve the accuracy of liver cancer diagnosis. Currently, the clinically used contrast agents are small molecule contrast agents, such as gadopentetate glutenium injection (trade name : Ma Genweixian), it is based on the blood vessel density in the nodule or mass, reflecting the blood supply characteristics of the lesion, not characteristic, and the early diagnosis of liver cancer has not achieved the desired effect. In our previous patent application (CN101612407A), we inven...

Claims

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Application Information

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IPC IPC(8): A61K49/12A61K49/14A61K49/16A61K103/34
Inventor 张娜陈智金鲁在君马春红于德新
Owner SHANDONG UNIV
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