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Medicine co-carried compound, micelle and preparation method of micelle

A compound and co-loading technology, which can be used in drug combinations, pharmaceutical formulations, medical preparations with inactive ingredients, etc., can solve problems such as the inability to meet the needs of the market, achieve good tumor growth, good stability, and reduce toxic and side effects. Effect

Active Publication Date: 2015-07-22
中科应化(长春)科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, among the existing anticancer drugs, only a few such as Doxil are prepared by physically loading doxorubicin, and there are few studies on using other carriers to load doxorubicin by electrostatic interaction, which is far from satisfying market needs

Method used

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  • Medicine co-carried compound, micelle and preparation method of micelle
  • Medicine co-carried compound, micelle and preparation method of micelle
  • Medicine co-carried compound, micelle and preparation method of micelle

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Experimental program
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preparation example Construction

[0048] The present invention has no special limitation on the preparation method of the multi-arm copolymer having the structure of formula I, and the technical solution for preparing the multi-arm copolymer having the structure of formula I that is well known to those skilled in the art can be used. In the present invention, the preparation method of the multi-arm copolymer having the structure of formula I preferably comprises the following steps:

[0049] Mixing and reacting polyethyleneimine, amine-based polyethylene glycol derivatives, and amino acid N-carboxylic acid anhydride in the ring, and deprotecting to obtain a multi-arm copolymer;

[0050] The amino acid N-carboxyl ring acid anhydride is glutamic acid N-carboxyl ring acid anhydride or aspartic acid N-carboxyl ring acid anhydride;

[0051] The polyethyleneimine has the structure of formula II;

[0052]

[0053] m and n are degrees of polymerization; the number average molecular weight of the polyethyleneimine ...

Embodiment 1

[0084] Add 5.0 g of mPEG-NHS with a number average molecular weight of 2000 Da to the dry reaction flask, add 50 mL of anhydrous N,N-dimethylformamide to dissolve, add 1.5 g of polyethyleneimine with a molecular weight of 600 Da, and stir at room temperature for 24 h. Dialyze with deionized water for 72 hours in a 7000Da dialysis bag, change the water 6-8 times, and freeze-dry to obtain mPEG-PEI;

[0085] Weigh 2.6g of mPEG-PEI, use toluene to azeotropically remove water for 3h, vacuum dry, add 60mL of anhydrous N,N-dimethylformamide to dissolve, weigh 10.48g of glutamic acid NCA to another dry reaction safe Vacuum the bottle, add 60 mL of anhydrous DMF to dissolve with a syringe, quickly add mPEG-PEI to glutamic acid NCA, and react at room temperature for 72 hours. The product was settled with more than 10 times the volume of anhydrous ether, filtered, washed and dried to obtain a compound with a protective group.

[0086]Take 2 g of the compound with a protective group, dis...

Embodiment 2

[0089] Add 5.0 g of mPEG-NHS with a number average molecular weight of 5000 Da to the dry reaction flask, add 50 mL of anhydrous N,N-dimethylformamide to dissolve, add 0.6 g of polyethyleneimine with a molecular weight of 600 Da, and stir at room temperature for 24 h. Dialyze with deionized water for 72 hours in a 7000Da dialysis bag, change the water 6-8 times, and freeze-dry to obtain mPEG-PEI;

[0090] Weigh 2.8g of mPEG-PEI, use toluene to azeotropically remove water for 3h, vacuum dry, add 60mL of anhydrous N,N-dimethylformamide to dissolve, weigh 5.24g of glutamic acid NCA to another dry reaction safe Vacuum the bottle, add 30 mL of anhydrous DMF to dissolve with a syringe, quickly add mPEG-PEI to glutamic acid NCA, and react at room temperature for 72 hours. The product was settled with more than 10 times the volume of anhydrous ether, filtered, washed and dried to obtain a compound with a protective group.

[0091] Take 2 g of the compound with a protective group, dis...

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Abstract

The invention provides a medicine co-carried compound, micelle and a preparation method of micelle. The medicine co-carried compound is compounded by cis-platinum, adriamycin and a multi-arm copolymer, and the multi-arm copolymer has a structure of formula I (which is shown in the description). The medicine co-carried compound forms the micelle in an aqueous medium, a PEG block of the multi-arm copolymer is positioned on an external kernel of the micelle, a polyglutamic acid block or an aspartic acid block of the multi-arm copolymer is positioned on an internal kernel of the micelle, and the cis-platinum and the adriamycin are protected between the PEG block and the polyglutamic acid block or the aspartic acid block, so that the stability is good, and sudden release situation is avoided. Furthermore, the cis-platinum and a carboxyl of the multi-arm copolymer generate coordination, so that a cross linking function is achieved, and the stability of the micelle is improved; the adriamycin and the cis-platinum can quickly release and exert medicine functions around the tumor tissue or the tumor cell, so that the curative effect of the medicine is improved, and the toxic and side effects are reduced; based on experimental results, the medicine co-carried compound has an excellent tumor growth suppressing effect when being directly applied to treating rat melanoma lung metastatic cancer.

Description

technical field [0001] The invention relates to the field of macromolecular medicines, in particular to a medicine co-loading complex, micelles and a preparation method of micelles. Background technique [0002] Doxorubicin (DOX), also known as daunorubicin, is a common anthraquinone antibiotic mainly used in the treatment of malignant tumors. Doxorubicin has high toxicity and good solubility, and has become a drug for treating acute leukemia, breast cancer, lung cancer and other malignant tumors, and has been widely used clinically. However, due to the short biological half-life of doxorubicin and its non-specific distribution, its effective use is limited. In addition, the toxic side effects of doxorubicin (such as myocardial damage, inhibition of bone marrow growth, hair loss, etc.) limit its dose in the treatment of malignant tumors. [0003] In order to improve drug efficacy, polymer materials are often used as carriers for drug delivery. Micro- and nano-scale polyme...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K33/24A61K9/107A61K47/34A61P35/00A61P35/04A61K31/704
Inventor 田华雨徐彩娜陈学思王萍郭兆培焦自学
Owner 中科应化(长春)科技有限公司
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