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Liver-targeting intelligent nano-micelle prodrug system and preparation thereof

A nanomicelle, liver-targeting technology, applied in the field of biomedicine, can solve the problems of reducing the phagocytosis of nanoparticles by cells, difficult to reach the therapeutic dose of drugs, slow drug release, etc., to improve clinical efficacy and bioavailability, overcome the The effect is not ideal and the effect of reducing toxic and side effects

Inactive Publication Date: 2009-11-11
EAST CHINA NORMAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Firstly, the drug and the drug carrier are connected by an amide bond that degrades very slowly, and the drug release is slow, and it is difficult for the drug to reach a therapeutic dose within a specified time; secondly, the hydrophilic polymer shell (PEG) reduces the phagocytosis of the nanoparticle by cells

Method used

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  • Liver-targeting intelligent nano-micelle prodrug system and preparation thereof
  • Liver-targeting intelligent nano-micelle prodrug system and preparation thereof
  • Liver-targeting intelligent nano-micelle prodrug system and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] The first step: 0.1834g (0.0054mmol) galactose polyethylene glycol active ester (Gal-PEG-NHS) (molecular weight is 35000Da), 0.3773g50% PEI aqueous solution (molecular weight is 1800Da, 0.1048mmol) is dissolved in 10mlDMF respectively middle. Under the ice-salt bath condition, the Gal-PEG-NHS solution was added dropwise to the PEI solution, and reacted under the ice-salt bath condition for 12 hours, and then reacted at room temperature for 72 hours. The obtained product was dialyzed in triple distilled water for 96 hours with a 7000 Da dialysis bag, and the obtained dialysate was freeze-dried for 72 hours to obtain a white flocculent product (Gal-PEG-PEI). Take a small amount of this product and dissolve it in heavy water. The NMR characterization results See attached image 3 .

[0032] The second step: take 0.2733g of Gal-PEG-PEI, dissolve it in 100ml round bottom flask with 20ml triple distilled water, and add 50 times excess succinate-4-(nitrogen maleimidomethyl)c...

Embodiment 2

[0038] With embodiment 1 method, the molecular weight of fixing PEI is 1800Da, adopts the galactose polyethylene glycol active ester (Gal-PEG-NHS) that molecular weight is 25000Da to carry out experiment

Embodiment 3

[0040] With embodiment 1 method, the molecular weight of fixed PEI is 1800Da, adopts the galactose polyethylene glycol active ester (Gal-PEG-NHS) that molecular weight is 10000Da to carry out experiment

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Abstract

The invention relates to a liver-targeting intelligent nano-micelle prodrug system based on polyethylene imine, and provides a method for preparing a macromolecular prodrug. The low-toxicity polyethylene imine modified by polyethylene glycol with a liver-targeting group (T) at the remote end is used as a carrier (T-PEG-PEI), adriamycin (ADR) is used as a treatment medicament, and the carrier is connected with the adriamycin through a lysosome degradable covalent bond to form a prodrug (T-PEG-PEI-ADR). The T-PEG-PEI-ADR prodrug is self-assembled into micelles with grain diameter being 10 to 500 nanometers in water solution. The micelle prodrug system can circulate with long effect in blood, strengthen the phagocytosis of liver cancer cells on polymer nano-micelle, selectively deliver the treatment medicament to the liver tumor part, directionally kill the liver tumor cells, reduce the toxic and side effects of the adriamycin on treating the liver caner, and improve the clinical efficacy and bioavailability of the prior liver cancer treatment medicament.

Description

technical field [0001] The invention relates to a liver-targeted intelligent nano-micelle prodrug system based on polyethyleneimine, and provides a method for preparing the nanoscale self-assembled macromolecular prodrug, which belongs to the technical field of biomedicine. Background technique [0002] Liver cancer is one of the most common malignant tumors. Due to the lack of characteristic signs, early liver cancer often manifests as dull pain in the liver area, poor appetite, abdominal distension, fatigue, etc., which are similar to the symptoms of most digestive tract diseases. It is difficult to diagnose early and accurately with current detection methods. The liver has been severely damaged, so the selection and efficacy of clinical treatment options are greatly restricted. At present, surgical resection is the first choice for the treatment of liver cancer, but it is easy to relapse after operation, mainly due to residual cancer. Postoperative adjuvant chemotherapy...

Claims

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Application Information

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IPC IPC(8): A61K48/00A61K31/704A61K9/00A61K47/34A61P35/00A61P1/16
Inventor 余家会公彦宝罗淑芳刘顺英
Owner EAST CHINA NORMAL UNIV
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