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Compound of co-carried cis-platinum and adriamycin, micelle and preparation method of micelle

A doxorubicin and compound technology, applied in the field of polymer drugs, can solve the problems of large differences in hydrophilicity, hydrophobicity, charge properties and molecular weight, and cannot meet the needs of the market, avoiding rapid release, improving curative effect, and good stability. Effect

Inactive Publication Date: 2013-04-24
CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the large differences in the hydrophilicity and hydrophobicity, charge properties, and molecular weight of different drug molecules, among the existing anticancer drugs on the market, there are few polymer drug-loading systems that co-load two drugs, especially co-loaded cisplatin. The drug-loading system with doxorubicin is far from meeting the needs of the market

Method used

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  • Compound of co-carried cis-platinum and adriamycin, micelle and preparation method of micelle
  • Compound of co-carried cis-platinum and adriamycin, micelle and preparation method of micelle
  • Compound of co-carried cis-platinum and adriamycin, micelle and preparation method of micelle

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preparation example Construction

[0062] The present invention also provides a method for preparing micelles co-loading cisplatin and doxorubicin, comprising the following steps:

[0063] reacting doxorubicin, cisplatin and a block copolymer with a structure of formula (I) or formula (II) in an aqueous medium to obtain micelles co-loading cisplatin and doxorubicin;

[0064] In the present invention, doxorubicin, cisplatin and block copolymers having the structure of formula (I) or formula (II) are used as raw materials, and the order of addition of doxorubicin, cisplatin and block copolymers in the present invention has no With special restrictions, doxorubicin can be reacted with block copolymer first, and then cisplatin can be added for reaction; cisplatin can also be reacted with block copolymer first, and then doxorubicin can be added for reaction; Platinum is added to the reaction with the block copolymer. The reaction process is preferably carried out under dark conditions. The electrostatic complex ti...

Embodiment 1

[0083] Add 2.4454g of polyethylene glycol monomethyl ether having a structure of formula (III) with a number average molecular weight of 5000 to the dry reaction bottle, and remove water by azeotroping with 60mL of anhydrous toluene at 130°C for 3 hours, then pump it to dryness under reduced pressure The remaining toluene; the obtained solid was dissolved in 25 mL of dry N,N-dimethylformamide to obtain the first solution; 6.4460 g of γ-benzyl-L-glutamate-N-carboxylic acid anhydride was dissolved in In 40mL of dry N,N-dimethylformamide, the second solution was obtained; in a nitrogen atmosphere, the first solution was mixed with the second solution, and stirred and reacted for 72h at room temperature under nitrogen protection conditions; The N,N-dimethylformamide was dried under pressure, and then the obtained solid was dissolved in dichloromethane, then settled with diethyl ether, filtered with suction, and dried to obtain a compound with a protective group.

[0084] Take 6.63...

Embodiment 2

[0087] Add 1.6251g of polyethylene glycol with a number average molecular weight of 4000 having the structure of formula (V) into the dry reaction bottle, and remove water by azeotroping with 50mL of anhydrous toluene at 130°C for 3 hours, then vacuum the remaining toluene to dryness ; The obtained solid was dissolved in 15 mL of dry N,N-dimethylformamide to obtain a first solution; 4.2790 g of γ-benzyl-L-glutamate-N-carboxylic acid anhydride was dissolved in 30 mL of dry In N,N-dimethylformamide, the second solution was obtained; in a nitrogen atmosphere, the first solution was mixed with the second solution, and stirred and reacted for 72 hours at room temperature under nitrogen protection conditions; after the reaction, vacuum pumping to dryness N,N-dimethylformamide, and then the obtained solid was dissolved in dichloromethane, then settled with diethyl ether, filtered with suction, and dried to obtain an intermediate product.

[0088] Take 4.4241 g of the prepared interme...

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Abstract

The invention provides a compound of co-carried cis-platinum and adriamycin, micelle and a preparation method of the micelle. The compound is compounded by cis-platinum, adriamycin and a segmented copolymer, wherein the cis-platinum and the segmented copolymer are compounded through coordination; the adriamycin and the segmented copolymer are compounded through electrostatic interaction; and the segmented copolymer has the structure of formula (I) or formula (II). The compound micelle of the co-carried cis-platinum and adriamycin comprises the compound of the co-carried cis-platinum and adriamycin and an aquosity medium. The preparation of the compound micelle comprises the step of reacting the adriamycin, the cis-platinum and the segmented copolymer having the structure of formula (I) or formula (II) in the aquosity medium so as to obtain the micelle of the co-carried cis-platinum and the adriamycin. The compound micelle can stably carry the cis-platinum and the adriamycin under physiological conditions, and the release of the compound micelle has pH value sensitivity.

Description

technical field [0001] The invention relates to the field of macromolecule drugs, in particular to a compound, micelles and micelles co-loading cisplatin and doxorubicin and a preparation method of the micelles. Background technique [0002] Due to the drug resistance of tumors, traditional single-drug chemotherapy has poor curative effect on tumors, and tumor cells are not sensitive to traditional single drugs. In recent years, combination chemotherapy has gradually become the mainstream of tumor chemotherapy. Combination chemotherapy refers to the combined application of two or more non-crossover and synergistic drugs in the treatment of tumor diseases, with the purpose of increasing curative effect, reducing toxic and side effects, reducing drug resistance or delaying the emergence of drug resistance, and maximizing drug resistance. potency. [0003] The combined chemotherapy regimen should follow the following principles: 1. Various drugs in the combined chemotherapy r...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/34A61K33/24A61K31/704A61K9/107A61P35/00
Inventor 汤朝晖李明强林坚宋万通吕世贤陈学思
Owner CHANGCHUN INST OF APPLIED CHEMISTRY - CHINESE ACAD OF SCI
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