DOX-P micelle with anti-tumor drug resistance and preparation method thereof

Abstract

The invention discloses poloxamer-adriamycin conjugate (DOX-P) micelle with anti-tumor drug resistance and a preparation method of the DOX-P micelle. The synthetic process of the DOX-P comprises the steps of firstly, reacting poloxamer with succinic anhydride to obtain high-molecular polymer of which the tail end contains carboxyl; and then, directly bonding the carboxyl at the tail end of the polymer with primaquine group in the adriamycin in an amido bond mode. The DOX-P has the capability of forming the micelle; and compared with the adriamycin bulk drug, the adriamycin subjected to covalent binding in the DOX-P micelle has the advantages that the anti-tumor activity of the adriamycin is maintained, the drug resistance of the tumor is overcome, and the stability of the adriamycin is better than that of poloxamer micelle.

Description

【Technical field】

[0001] The invention belongs to the field of pharmaceutical preparations, and relates to a DOX-P micelle with antitumor drug resistance and a preparation method thereof. 【Background technique】

[0002] In tumor chemotherapy, it is found that more than 90% of chemotherapy drugs will be absorbed by normal tissues, with severe side effects, and tumor cells will develop drug resistance to most chemotherapy drugs.

[0003] Doxorubicin is an anthracycline antibiotic with broad-spectrum antitumor effects and is clinically used to treat leukemia, lymphoma and solid tumors. However, its application is limited due to its strong cardiotoxicity and tumor cell resistance to it.

[0004] Polymer-drug conjugates are a very effective way to increase drug water solubility and drug loading. It connects small molecule drugs to macromolecular carriers to make polymer prodrugs, especially nanoscale polymeric particles. Its small size effect and surface and interface effects h...

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