A kind of triblock polymer, its preparation method and application

A technology of polymer, polymer glue

Active Publication Date: 2019-01-04
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Despite the above advantages, most of the micelles reported in the literature are non-covalently entrapped chemotherapy drugs. Under physiological conditions, these self-assembled micelles are easy to adsorb proteins and dissociate, resulting in decreased stability and drug leakage.

Method used

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  • A kind of triblock polymer, its preparation method and application
  • A kind of triblock polymer, its preparation method and application
  • A kind of triblock polymer, its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Embodiment 1: Preparation of polyethylene glycol-aminated polyglycidyl methacrylate-polydiisopropylaminoethyl methacrylate polymer

[0053] Take 1.0 g of polyethylene glycol 5000 macromolecular initiator modified by acid bromide and dissolve it in 1.44 ml N,N-dimethylacetamide, stir and mix well, add glycidyl methacrylate 0.525 ml, and initiate with the above macromolecular Equimolar cuprous chloride catalyst and pentamethyldiethylenetriamine were reacted at 40°C for 15 hours to obtain a methoxy-terminated polyethylene glycol-polyglycidyl methacrylate diblock copolymer.

[0054] Take 0.2 g of the above-prepared methoxy-terminated polyethylene glycol-polyglycidyl methacrylate diblock copolymer and dissolve it in 0.3 ml of N,N-dimethylacetamide, stir and mix, and then add formaldehyde 0.4 ml of diisopropylaminoethyl acrylate monomer, cuprous chloride catalyst and pentamethyldiethylenetriamine equimolar to the above two-block copolymer, reacted at 40°C for 48 hours. Vacuu...

Embodiment 2

[0056] Embodiment 2. Preparation of polymer micelles

[0057]Take 25 mg polyethylene glycol-aminated polyglycidyl methacrylate-polydiisopropylaminoethyl methacrylate triblock polymer (wherein the polymerization degree of polyethylene glycol is 113, and the aminated polymethylmethacrylate The degree of polymerization of glycidyl acrylate is 50, and the degree of polymerization of polydiisopropylaminoethyl methacrylate is 60) dissolved in 0.2ml N,N'-dimethylacetamide, and added dropwise under the condition of ultrasonic (200mW) into 1.8ml of deionized water, vortexed (1000rpm) for 1 minute, and dialyzed in deionized water for 24 hours with a dialysis bag with a molecular weight cut-off of 3500 Daltons to obtain polymer micelles.

Embodiment 3

[0058] Example 3. Preparation of chemically crosslinked polymer micelles

[0059] Get double-terminal carboxylated cisplatin (compound of formula 3) 16mg, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride 18mg and 1-hydroxybenzotriazole 9.6mg, dissolve In 0.2ml dimethyl sulfoxide. After the activation reaction at room temperature for 2 hours, it was added dropwise to the polymer micelles prepared in Example 2 under ultrasonic conditions (200 mW), and the reaction was continued at room temperature for 12 hours. Carboxylated cisplatin-crosslinked polymer micelles were obtained after dialysis with a dialysis bag with a molecular weight cut-off of 3500 Daltons in deionized water for 24 hours.

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Abstract

The invention discloses a tri-block polymer as shown in a formula I, a medicine-loading polymer micelle, a chemically crosslinked medicine-loading polymer micelle, and a preparation method and application of the tri-block polymer, wherein R1 is carboxyl, amino, cyan, sulfydryl, aldehyde group or C1-C3 alkyl; R2 is halogen; R3 is hydroxyl or aminated glycidol; x is an integer of 20 to 300; y is an integer of 10 to 100; z is an integer of 10 to 100. The chemotherapeutic medicine-loading chemical crosslinked polymer micelle provided by the invention not only can maintain the stability of the micelle in the blood circulation process, but also can be degraded in tumor or cancer cells so as to effectively release the chemotherapeutic medicine and fulfill the treatment aim.

Description

technical field [0001] The invention belongs to the technical field of medicine and chemical industry, and specifically relates to a triblock polymer, a polymer drug-loaded micelle, a chemically cross-linked polymer drug-loaded micelle, a preparation method and an application thereof. Background technique [0002] Chemotherapy is currently one of the main means of clinical treatment of malignant tumors. Polymer micelles can nanometerize insoluble chemotherapeutic drugs, improve drug solubility, increase drug bioavailability, and significantly reduce its toxic and side effects. It has been used in the treatment of metastasis and drug resistance. Sexual tumors have received extensive attention. Despite the above advantages, most of the micelles reported in the literature are loaded with chemotherapy drugs through non-covalent interactions. Under physiological conditions, these self-assembled micelles are easy to adsorb proteins and dissociate, resulting in decreased stability ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08F293/00C08F8/32C08G65/00C08J3/24A61K47/32A61K9/107A61K45/00A61K47/59A61P35/00A61P35/04
Inventor 于海军李亚平崔智睿冯兵刘建萍王当歌姚霞
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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