Three-arm star hydrophilic copolymer, and synthesis method and application thereof

A technology of a hydrophilic copolymer and a synthesis method, applied in the field of biomedical materials, can solve the problems of difficulty in fully exerting drug efficacy, slow drug release rate, etc., and achieve the effects of low critical micelle concentration, improved efficacy, and mild reaction conditions.
CN104045837AInactive Publication Date: 2014-09-17XI AN JIAOTONG UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
XI AN JIAOTONG UNIV
Publication Date
2014-09-17
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a three-arm star hydrophilic copolymer, and a synthesis method and application thereof. The synthesis method comprises the following steps: initiating gamma-benzyl-L-glutamate-N-carboxy-alpha-amino acid anhydride ring-opening polymerization reaction by using a three-element primary amine inner core, and bonding small-molecule RAFT polymeric chain transfer agent to three terminated amino groups of the star polymer through a carbodiimide method, thus obtaining large-molecule RAFT chain transfer agent; and performing RAFT polymerization by using N-(3-dimethylaminopropyl) and N-hydroxymethyl acrylamide as monomers, finally reacting the hydroxyl group of the N-hydroxymethyl acrylamide component in the copolymer with isocyanated methyl-terminated polyethyleneglycol to realize connection to the polyethyleneglycol via a disulfide bond, and performing hydrazinolysis treatment to obtain the required three-arm star hydrophilic copolymer. According to the method, the molecular weight and chain length of each polymer component can be flexibly controlled, the reaction conditions are mild, and the raw materials are accessible; the synthesized polymer can improve the drug effect and reduce the toxic or side effect; and meanwhile, when loading amycin and gene-based drugs, the polymer realizes the synergic antitumor treatment effect.
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Description

technical field

[0001] The invention belongs to the field of biomedical materials, and in particular relates to a three-arm star-shaped hydrophilic copolymer and its synthesis method and application. Background technique

[0002] Chemotherapy based on cytotoxic drugs is one of the main strategies for the treatment of malignant tumors. However, cytotoxic drugs usually have high cytotoxicity, poor water solubility and no bioselectivity, and can kill tumor cells and normal cells at the same time, with serious side effects. Since the curative effect and side effects of chemotherapy are strongly positively correlated with the drug dose, it is difficult to improve the therapeutic effect by increasing the drug concentration. What's more serious is that almost all tumor cells will develop multidrug resistance during chemotherapy with cytotoxic drugs. These have become the main obstacles restricting the success of chemotherapy. Many studies in recent years have shown that the use ...

Claims

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