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

A magnetic resonance contrast agent and active targeting technology, which is applied in the direction of pharmaceutical formulations and preparations for in vivo experiments, can solve the problems of tumor targeting efficiency that needs to be improved, and achieve the effect of increasing strength, good sensitivity, and improving curative effect

Inactive Publication Date: 2012-11-07
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

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Experimental program
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Effect test

Embodiment 1

[0036] Syntheses of polylysine-polyethylene glycol-polylactic acid copolymer (PLA-PEG-PLL block copolymer) (1) under argon atmosphere, the THF (tetrahydrofuran) of 15g, the KHMDS of 1.5g ( Potassium hexamethyldisilazide), 4g of EO (ethylene oxide) were added to the reaction flask, and reacted for 3 days under ice bath, and then 3.5g of D, L-LA (D, L-lactide ) into the reaction flask, after reacting for 8 hours, dropwise add 1 g of glacial acetic acid and acetone mixture with a volume ratio of 1:6 in the reaction flask, stir at room temperature for 30 min, terminate and acidolyze the product, and drop the product into 200 g of anhydrous diethyl ether Precipitation and purification treatment, H 2 N-PEG-b-PLA.

[0037] (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 use 20g Methyl chloride was dissolved, and then precip...

Embodiment 2

[0040] Preparation method of active targeting polymer nanoparticle magnetic resonance contrast agent:

[0041] (1) Synthesis of diethylenetriaminepentaacetic acid (DTPA) cyclic anhydride

[0042] 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;

[0043] (2) Synthesis of diethylenetriaminepentaacetic acid-polylysine-polyethylene glycol-polylactic acid copolymer (PLA-PEG-PLL-g-DTPA)

[0044] 1. The synthesis of PLA-PEG-PLL block copolymer adopts the method synthesis (as embodiment 1) by patent publication number CN 101565497A;

[0045] 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

[0053] Preparation of Actively Targeting Polymeric Nanoparticle Magnetic Resonance Contrast Agents:

[0054] (1) Synthesis of diethylenetriaminepentaacetic acid (DTPA) cyclic anhydride

[0055] 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;

[0056] (2) Synthesis of diethylenetriaminepentaacetic acid-polyethylene glycol-polylactic acid copolymer (PLA-PEG-DTPA)

[0057] 1. The synthesis of PLA-PEG-PLL block copolymer adopts the method synthesis (as embodiment 1) by patent publication number CN 101565497A;

[0058] 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 isenhanced 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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Patent Type & Authority Patents(China)
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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