Polymer-antitumor drug conjugate as well as preparation method and application thereof

A technology of anti-tumor drugs and polymers, applied in anti-tumor drugs, pharmaceutical formulations, drug combinations, etc., to achieve the effects of long blood circulation time, large drug accumulation, and broad market application prospects

Active Publication Date: 2019-05-17
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, despite great progress in research on polymers as drug carriers, only a few polymers have been used in in vivo and clinical studies, mainly due to the inherent toxicity and / or immunogenicity of polymers. sex

Method used

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  • Polymer-antitumor drug conjugate as well as preparation method and application thereof
  • Polymer-antitumor drug conjugate as well as preparation method and application thereof
  • Polymer-antitumor drug conjugate as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0046] Embodiment 1, synthetic pHPMA-DOX polymer drug conjugate

[0047] Synthetic steps such as figure 1 shown.

[0048] 1. Preparation of pHPMA-NHNHBoc

[0049] Add chain transfer agent CTA (7.0mg, 0.025mmol), monomer HPMA (1400.0mg, 9.8mmol), MA-Ala-NHNHBoc (140.0mg, 0.52mmol) into a 15mL small-mouth round bottom bottle in proportion, and replace the argon (repeat 3 times). Under ice bath, the solvent (H 2 O / CH 3 OH=1:4, 7.0 mL) was added into the round bottom bottle with a syringe, and continued to bubble with argon for 30 minutes. Then transfer the round-bottom bottle to 45°C for 17 hours in the dark. After quenching the reaction, drop the reaction solution into a mixed solution of acetone and ether (300mL, acetone / ether=1:1), collect the precipitate, and filter After vacuum drying, the crude product was purified by FPLC column, and the mobile phase containing the product part was collected. With deionized water as the medium, the collected mobile phase was placed i...

Embodiment 2

[0054] Embodiment 2, synthesis pOEGMA-DOX polymer drug conjugate

[0055] Synthetic steps such as figure 1 shown.

[0056] 1. Preparation of pPEG-NHNHBoc

[0057] The chain transfer agent CTA (9.2mg, 0.033mmol), the monomer OEGMA (2.05g, 4.1mmol), and MA-Ala-NHNHBoc (243.9mg, 0.9mmol) were added in proportion to the small-mouth round bottom bottle, and the argon gas was replaced. Under ice bath, the solvent (H 2 O / CH 3 OH=1:4, 10.4mL) into the round bottom bottle with a syringe, and continue to bubble with argon for half an hour. Then the round bottom bottle was transferred to 45° C. and protected from light for 17 hours. After quenching the reaction, the reaction solution was placed in a dialysis bag (MWCO 3500) and dialyzed for 1 day to remove excess solvent and unreacted small molecules. The crude product was purified by FPLC column, and the mobile phase containing the product was collected to remove Ionized water was used as the medium, and the collected mobile phase...

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Abstract

The invention provides a polymer shown as formula (I) in the description and a preparation method of the polymer. The prepared polymer has narrower polydispersity index. The invention further discloses a polymer-antitumor drug conjugate and a preparation method thereof. The prepared polymer-antitumor drug conjugate has longer blood circulation time and can obtain more drug accumulation at a tumorpart, so that a drug has better antitumor effect and has broad market application prospects.

Description

technical field [0001] The invention relates to a polymer-antitumor drug conjugate, a preparation method and application thereof. Background technique [0002] Polymer-drug conjugates as nanoscale drug delivery systems have become a hotspot in the field of targeted cancer chemotherapy research. Conjugation of low-molecular-weight anticancer drugs to biocompatible water-soluble polymers has become a general strategy to improve the anticancer efficacy of small-molecule drugs. This is because drug delivery systems based on polymer-drug conjugates have many unique structures and properties that can potentially improve the solubility and stability of drugs through enhanced permeability and retention (EPR) effects. The drug accumulates in the tumor and reduces its side effects. For example, the topoisomerase II inhibitor doxorubicin (DOX) induces transcription and replication of irreversible single- and double-strand DNA breaks, however due to its short plasma half-life and non-...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F220/28C08F220/60C08F220/58C08F8/32A61K47/58A61K31/704A61P35/00
Inventor 罗奎蔡豪戴幸杭龚启勇
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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