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Tumor targeting polyamino acid graft copolymer and preparation method thereof

A tumor-targeting graft copolymer technology, which is applied in the field of polyamino acid graft copolymer and its preparation, can solve problems such as difficulty in universal promotion, differences in surface receptor expression, and expression levels. , to achieve the effects of increasing accumulation, increasing the probability of success, good controllability and universality

Active Publication Date: 2015-10-28
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, for different types of tumors, the expression of its surface receptors is significantly different; even for the same tumor, its expression level is different in different patients or even in different stages of the same patient
This makes the treatment results of the current "actively targeted" nano anti-tumor drugs vary widely, and it is difficult to obtain universal promotion.

Method used

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  • Tumor targeting polyamino acid graft copolymer and preparation method thereof
  • Tumor targeting polyamino acid graft copolymer and preparation method thereof
  • Tumor targeting polyamino acid graft copolymer and preparation method thereof

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preparation example Construction

[0072] The present invention also provides a method for preparing a polyamino acid graft copolymer with tumor targeting, comprising the following steps:

[0073] The polyamino acid grafted polyethylene glycol raw material is reacted with the targeting polypeptide in water to obtain a polyamino acid graft copolymer with tumor targeting;

[0074] The targeting polypeptide is a polypeptide targeting the blood coagulation reaction generated spontaneously by tumor tissue or under external stimulation; the polyamino acid grafted polyethylene glycol raw material has a structure of formula IV; the polyamino acid grafted with tumor targeting Branch copolymer has formula I structure;

[0075]

[0076] Among them, R 1 It is a peptide desulfhydryl group that targets the blood coagulation reaction generated spontaneously by tumor tissue or by external stimuli;

[0077] R 2 One or more selected from fluorescent dye dehydrogenation groups, bioactive molecule dehydrogenation groups, and...

Embodiment 1

[0104] Example 1 Preparation of poly-L-glutamic acid (PLG)

[0105] Dissolve 36.8 g (140.0 mmol) of γ-benzyl-L-glutamate-N-endocarboxylic anhydride monomer (BLG-NCA) in 270 mL of anhydrous N,N-dimethylformamide (DMF) After stirring and dissolving, 1.0 mL (1.0 mmol / L DMF solution) of n-hexylamine (n-HA) was added, sealed, and stirred and reacted for 72 h at a temperature of 25° C. Afterwards, 2.0 g (20.0 mmol) of acetic anhydride was added to the above reaction system, and the reaction was continued for 6 h. After the reaction was finished, the obtained reaction solution was settled into 2.0L of diethyl ether, filtered and washed with diethyl ether successively, and vacuum-dried at room temperature for 24h to obtain the intermediate product poly(γ-benzyl-L-glutamate) ( PBLG).

[0106] 10.0 g of the above-prepared poly(γ-benzyl-L-glutamate) was dissolved in 100 mL of dichloroacetic acid, and under stirring conditions, 30 mL of hydrogen bromide / glacial acetic acid solution with...

Embodiment 2

[0108] Example 2 Preparation of poly-L-glutamic acid grafted polyethylene glycol raw material (PLG-g-PEG)

[0109] In the dry reaction flask, add 1.7g (13.2mmol glutamic acid unit) of poly(L-glutamic acid) (prepared in Example 1), 2.8g (63.6mmol ethylene glycol unit) of polyethylene glycol mono Methyl ether (5000Da) and 0.7g (15.9mmol ethylene glycol unit) of maleimide-based polyethylene glycol (5000Da) were added to dissolve in 150mL of DMF. Afterwards, 178mg (1.4mmol) of N,N-diisopropylcarbodiimide (DIC) and 196mg (1.6mmol) of 4-dimethylaminopyridine (DMAP) were added, at a temperature of 25°C Seal the reaction, and after 48 hours, settle the obtained reaction solution with 1.0 L of ether, redissolve the obtained solid in DMF, dialyze with deionized water for 3 days, and freeze-dry to obtain poly-L-glutamic acid grafted polyethylene Glycol feedstock.

[0110]With deuterated water as a solvent, the above-mentioned poly-L-glutamic acid grafted polyethylene glycol raw materia...

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Abstract

The invention provides a tumor targeting polyamino acid graft copolymer and a preparation method thereof. The copolymer adopts a structure shown in formula I, wherein R1 is a blood coagulation reaction polypeptide group without sulfhydryl, and the polypeptide group is spontaneously generated by targeting tumor tissues or generated under the external stimulation; R2 is selected from one or more of a fluorochrome dehydrogenation group, a bioactive molecule dehydrogenation group and a C6-C30 alcohol dehydrogenation group which does not contain heteroatoms or at least contains one heteroatom; R3 is selected from phenyl, R'-CO-, linear alkyl of C2-C10 or branched alkyl of C3-C10; R4 is selected from acetyl, propionyl or cholesterol acyl; L is selected from methene or ethylene. The targeting scheme of the copolymer provided by the invention is higher in controllability and universality, and the promotion to clinical application is facilitated.

Description

technical field [0001] The invention relates to the technical field of antitumor drugs, in particular to a polyamino acid graft copolymer with tumor targeting and a preparation method thereof. Background technique [0002] The rapid development of nanotechnology has given birth to the birth of nano anti-tumor drugs. The so-called nano anti-tumor drug refers to a new dosage form prepared by loading anti-tumor drugs with nano-carriers that meet the safety requirements in the body, which can solve the solubility, stability and toxicity of many anti-tumor drugs currently in use. side effects etc. Due to the above-mentioned significant advantages, in the past two decades, a large number of nano-anti-tumor drugs have entered clinical trials or entered the market through approval, and nano-medicines have become more and more widely accepted by the public. [0003] The usual preparation method of nano-anti-tumor drugs is: using biodegradable and biocompatible polymer materials to ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G81/00A61K47/42A61K47/34A61K47/48A61P35/00
Inventor 汤朝晖宋万通于海洋张大为张瑜陈学思
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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