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Branched sugar-containing polymer-based nano particle as well as preparation method and application thereof

A polymer and compound technology, applied in the field of biomedicine, can solve the problem of lack of functionality of targeted tumor diagnosis, achieve long in vivo circulation time and targeting, high tumor signal enhancement degree, huge development potential and application Foreground effect

Active Publication Date: 2021-11-02
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The patent with application number 201610237966.6 discloses a hyperbranched N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer-DOX conjugate using RAFT polymerization, which has dual sensitive properties of pH sensitivity and enzyme sensitivity. As an intelligent drug delivery system, it can quickly release drugs in the tumor microenvironment, which has good anti-tumor effect and biological safety, but lacks certain targeting and tumor diagnosis functionality.

Method used

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  • Branched sugar-containing polymer-based nano particle as well as preparation method and application thereof
  • Branched sugar-containing polymer-based nano particle as well as preparation method and application thereof
  • Branched sugar-containing polymer-based nano particle as well as preparation method and application thereof

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Embodiment 1

[0092] Embodiment 1, synthetic branched sugar-containing polymer pGAEMA-PTX-DOTA-Gd

[0093] Synthetic steps such as figure 1 shown.

[0094] GAEMA (1.34g, 4.38mmol), MA-DOTA (803mg, 1.56mmol), MA-GFLG-PTX (648mg, 0.5mmol), PTEMA (31.8mg, 0.13mmol), MA-GFLG-CTA (68.9mg, 72μmol ) and MA-GFLGK-MA (61.5mg, 93.8μmol) were added to the polymerization bottle, and the polymerization bottle was placed under argon for protection. VAO44 (9.0mg, 28μmol) was dissolved in 15ml H 2 O / CH 3 OH:1 / 3 mixed solution, and added to the above-mentioned polymerization bottle, cooled in an ice bath, and bubbled with argon for 50 minutes. The polymerization bottle was heated in an oil bath at 46° C. for 20 h in the dark, and the reaction was quenched with liquid nitrogen. After the reaction solution was raised to room temperature, it was added dropwise into 300ml of acetone solution to obtain a pink precipitate. The crude product was further purified by SEC fractional distillation. It was dialyz...

Embodiment 2

[0096] Embodiment 2, preparation of nanoparticles of branched sugar-containing polymer pGAEMA-PTX-DOTA-Gd

[0097] Polymer branched sugar-containing polymer pGAEMA-PTX-DOTA-Gd (100 mg) was uniformly dispersed in 10 mL of chromatographically pure DMSO, and slowly added dropwise to vigorously stirred 10 mL of ultrapure water under ice cooling. After continuing to stir for 2 h, the mixed solution was dialyzed at 4° C. in the dark to remove DMSO. The solution after dialysis was freeze-dried to obtain drug-loaded nanoparticles branched sugar-containing polymer pGAEMA-PTX-DOTA-Gd NPs, which were stored at 4°C for future use.

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Abstract

The invention provides a preparation method and application of a branched sugar-containing polymer nanoparticle as shown in a formula I. The branched sugar-containing polymer prepared by the preparation method disclosed by the invention has good self-assembly performance and tumor microenvironment responsiveness. The nanoparticle formed by self-assembly of the branched sugar-containing polymer can significantly improve the pharmacological properties of a small-molecule contrast agent, so that the nanoparticle has a longer blood half-life period, more tumor site accumulation, a higher tumor signal enhancement degree, a longer enhancement duration and better tumor enhancement specificity. The branched sugar-containing polymer nanoparticle prepared by the invention can be rapidly taken in by cells, release drugs in a tumor microenvironment, has long in-vivo circulation time and targeting property, and can significantly improve in-vivo distribution of small molecular drugs, so that the drugs are effectively accumulated at tumor sites, tumor growth is significantly inhibited, and the nanoparticle has good biological safety, and has huge development potential and wide application prospects in the field of tumor diagnosis and treatment integrated medicines.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a branched sugar-containing polymer nanoparticle, a preparation method and application thereof. Background technique [0002] The design and preparation of multifunctional and stimuli-responsive polymer nano-drug delivery systems is currently a research hotspot in the field of tumor diagnosis and treatment. For example, introducing specific targeting groups and molecular imaging probes into the polymer structure can effectively improve the targeting of the delivery system and monitor its pharmacokinetic behavior in vivo. At the same time, many functional groups, such as disulfide bonds, hydrazone bonds, and phenylalanylleucylglycine (Gly-Phe-Leu-Gly, GFLG) short peptides, have also been widely used for the special physiological structure of tumor sites. Construction of polymeric drug delivery systems for tumor microenvironment responsiveness. Using stimuli-responsive poly...

Claims

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Application Information

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IPC IPC(8): C08F220/60C08F220/58C08F222/38C08F8/42C08F8/30A61K49/12A61K49/18B82Y5/00B82Y15/00B82Y25/00
CPCC08F220/603C08F8/42C08F8/30A61K49/1818B82Y5/00B82Y15/00B82Y25/00A61K49/124C08F220/58C08F220/606C08F222/385
Inventor 罗奎刘艳辉蔡豪向宇凡
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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