Metal polymer, metal polymer nano-micelle as well as preparation method and application of metal polymer nano-micelle

A technology of metal polymers and nano micelles, which is applied in the direction of drug combination, pharmaceutical formulation, photodynamic therapy, etc., can solve the problems of poor biocompatibility, limited tumor tissue enrichment ability, low water solubility, etc., to achieve convenient preparation, Anti-tumor application prospect and good reproducible effect

Active Publication Date: 2020-11-17
SOUTHEAST UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The nanomicelle provided at the same time is a kind of metal-polymer nanomicelle with high biocompatibility, easy synthesis operation, good reproducibility and quality control, aiming to solve the problem of existing metal-based drugs with low water solubility and biophase Poor capacity, limited tumor tissue enrichment ability, etc.

Method used

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  • Metal polymer, metal polymer nano-micelle as well as preparation method and application of metal polymer nano-micelle
  • Metal polymer, metal polymer nano-micelle as well as preparation method and application of metal polymer nano-micelle
  • Metal polymer, metal polymer nano-micelle as well as preparation method and application of metal polymer nano-micelle

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Synthesis of polymer I-1:

[0035] The synthetic route is as follows:

[0036]

[0037] The specific process is:

[0038] (1) Synthesis of compound 1

[0039] Weigh 2-bromopyridin-5-ol (10.0g, 57.4mmol), p-toluenesulfonyl chloride (16.0g, 86.1mmol), Et 3 N (8 mL) was dissolved in DCM (200 mL) and stirred at room temperature for 2 h. After the reaction was completed, the solvent was removed, and purified by silica gel column chromatography (dichloromethane / methanol = 50 / 1 as the eluent) to obtain a white solid powder (13.0 g, 77.0%), namely Compound 1.

[0040] (2) Synthesis of compound 2

[0041] Weigh compound 1 (327.0mg, 1.0mmol), phenylboronic acid (183.0mg, 1.5mmol), Pd (PPh 3 ) 4 (34.6mg, 30.0μmol) was dissolved in the there-necked bottle that THF (10mL) was housed, N 2 protection, inject Na with a syringe 2 CO 3 Aqueous solution (2.0M, 1.5mL) was heated to reflux at 66°C for 12h. After the reaction was completed, the solvent was removed, extracted wit...

Embodiment 2

[0055] Preparation of polymer I-1 nanomicelles: Weigh 1 mg of polymer I-1, dissolve it in 0.2 mL of DMSO and sonicate for 10 min, take 5 mL of pure water into a 10 mL centrifuge tube, and dissolve the dissolved I-1 All of the DMSO solution was slowly injected into water, and after continuous ultrasonication for 10 minutes, it was added into a 5000KDa dialysis bag and dialyzed for 48 hours, during which the water was changed every 8 hours. After the dialysis is completed, the liquid remaining in the dialysis bag is taken out and freeze-dried to obtain the target nanomicelle, the average particle size of the nanomicelle is about 100nm. Electron microscope image of nanoparticles Figure 4 shown.

Embodiment 3

[0057] ABDA is a common singlet oxygen indicator, which has a characteristic fluorescence emission peak at 427nm when excited by 360nm light. When ABDA is oxidized by singlet oxygen, its fluorescence intensity at 427nm will be weakened, and the decline trend of fluorescence intensity has a certain linear relationship with the generation of singlet oxygen. The faster the fluorescence intensity decreases, the more singlet oxygen is produced.

[0058] Weigh ABDA solid and dissolve it in DMSO, and prepare 10.0mM ABDA mother liquor for subsequent use; prepare 2.0mM DMSO solution of nanomicelle I-1, mix it with the mother liquor of ABDA in equal volume and dilute with water, and prepare the final concentration of 50.0 μM of ABDA, a solution of micelles I-1 at a concentration of 10.0 μM. Mix the two solutions and place them in a cuvette, and use a laser (808nm, 0.5W·cm -2 ) irradiation, the irradiation time interval is 30s, and the fluorescence emission spectrum at its 375nm-550nm p...

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Abstract

The invention discloses a metal polymer, a metal polymer nano-micelle as well as a preparation method and application of the metal polymer nano-micelle. The metal polymer or pharmaceutically acceptable salt or solvate of the metal polymer is shown as a formula I or a formula II; alkynyl is introduced into metal iridium and ruthenium complexes and reacts with water-soluble monoazide polyethylene glycol through a click reaction to synthesize the metal polymer, and the metal polymer can be self-assembled into a nano-micelle with a core-shell structure in an aqueous solution. The preparation method is simple and convenient, the reproducibility is good, the quality is controllable, in addition, the nano-micelle can greatly improve the biocompatibility of metal drugs, can be applied to optical treatment, and has potential anti-tumor application prospects.

Description

technical field [0001] The invention belongs to the field of anti-tumor polymers, and in particular relates to a metal polymer, a metal polymer nano-micelle, a preparation method thereof, and an application thereof in treating tumor diseases. Background technique [0002] With the success of platinum-based anti-tumor drugs on the market worldwide, metal-based drugs have attracted more and more interest from researchers in the field of tumor treatment. At present, more than ten anti-tumor metal-based drugs have entered clinical research. However, metal-based drugs have problems such as low water solubility, poor biocompatibility, and limited ability to accumulate in tumor tissues. In addition, metal complexes have a short circulation time in the body and are easily removed from the body. [0003] Polymer nanomicelle is a new drug-loading system with clinical application prospects. In recent years, nanomicelles have achieved rapid development in anti-tumor research. At prese...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K41/00A61K47/10A61P35/00
CPCA61K9/1075A61K41/0057A61K41/0052A61K47/10A61P35/00A61K2300/00
Inventor 赵健吴昱颖韩天宇
Owner SOUTHEAST UNIV
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