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Sound-sensitive agent with aggregation-induced emission characteristics and preparation method thereof

A technology for aggregation-induced luminescence and sound sensitizers, applied to medical preparations containing active ingredients, preparations for in vivo tests, and pharmaceutical formulations, etc., can solve the problem of quenching of light/sound sensitizers, reduction of active oxygen generation, etc. problem, to achieve the effect of expanding the range

Active Publication Date: 2020-04-24
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In addition, another way to improve the efficacy of photo / sound sensitizers is to increase the load of photo / sound sensitizers, but the overload of organic molecules can easily lead to the quenching of photo / sound sensitizers, and the quenching effect caused by aggregation can also lead to active The reduction of oxygen generation has become the bottleneck problem faced by sound sensitizers

Method used

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  • Sound-sensitive agent with aggregation-induced emission characteristics and preparation method thereof
  • Sound-sensitive agent with aggregation-induced emission characteristics and preparation method thereof
  • Sound-sensitive agent with aggregation-induced emission characteristics and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The preparation of the sonosensitizer with AIE characteristic comprises the following steps:

[0040] 1) Add 0.2 mg of the prepared fluorophore molecule TTMN with aggregation-induced luminescent properties into the organic solvent tetrahydrofuran to dissolve it;

[0041] 2) Add 3 mg distearoylphosphatidylethanolamine-polyethylene glycol-2000 (PEG-DSPE) to the above solution 2000 ) and stir evenly to obtain 1mL mixed solution;

[0042] 3) Add 1 mL of the above mixed solution into 10 mL of pure water and stir at room temperature for 8 hours to volatilize the organic solvent in the water and self-assemble to form nanoparticles;

[0043] 4) After the obtained solution is ultrafiltered, the above-mentioned sound sensitizer with aggregation-induced luminescent properties is obtained, and its core-shell structure is as follows: figure 1 shown.

[0044] figure 2 Electron micrograph of the sound sensitizer with aggregation-induced luminescent properties prepared in this exa...

Embodiment 2

[0052] The preparation of the sonosensitizer with AIE characteristic comprises the following steps:

[0053] 1) Add 0.2 mg of the prepared fluorophore molecule MeTTMN with AIE characteristics into the organic solvent tetrahydrofuran to dissolve it;

[0054] 2) Add 3 mg distearoylphosphatidylethanolamine-polyethylene glycol-5000 (PEG-DSPE) to the above solution 5000 ) and stir evenly to obtain 1mL mixed solution;

[0055] 3) Add 1 mL of the above mixed solution into 10 mL of pure water and stir at room temperature for 8 hours to volatilize the organic solvent in the water and self-assemble to form nanoparticles;

[0056] 4) After the obtained solution is ultra-filtered, the above-mentioned sonosensitizer with aggregation-induced luminescent properties is obtained.

[0057] Using DPBF as a probe for singlet oxygen, the ability of the sonosensitizer with AIE characteristics described in 4) to degrade DPBF under ultrasonic irradiation was investigated. The ultrasonic conditions...

Embodiment 3

[0059] The preparation of the sonosensitizer with AIE characteristic comprises the following steps:

[0060] 1) Add 0.2 mg of the prepared fluorophore molecule MeOTTMN with AIE characteristics into the organic solvent DMSO to dissolve it;

[0061] 2) Add 3 mg distearoylphosphatidylethanolamine-polyethylene glycol-2000 (PEG-DSPE) to the above solution 2000 ) and stir evenly to obtain 1mL mixed solution;

[0062] 3) Add 1 mL of the above mixed solution into 10 mL of pure water and stir at room temperature for 8 hours to volatilize the organic solvent in the water and self-assemble to form nanoparticles;

[0063] 4) After the obtained solution is ultra-filtered, the above-mentioned sonosensitizer with aggregation-induced luminescent properties is obtained.

[0064] Using DPBF as a probe for singlet oxygen, the ability of the sonosensitizer with AIE characteristics described in 4) to degrade DPBF under ultrasonic irradiation was investigated. The ultrasonic conditions used are ...

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Abstract

The invention relates to a sound-sensitive agent with aggregation-induced emission characteristics and a preparation method thereof. The sound-sensitive agent has a core-shell structure: the inner core is fluorophore molecules with aggregation-induced emission characteristics, and the outer shell is a hydrophilic substance. The preparation method of the sound-sensitive agent comprises the following steps: 1) dissolving the fluorophore molecules with aggregation-induced emission characteristics in an organic solvent, then adding the hydrophilic substance, and uniformly mixing to obtain a mixedsolution; and 2) adding the mixed solution into water, stirring to form a core-shell structure, and separating to obtain the sound-sensitive agent with aggregation-induced emission characteristics. Compared with the prior art, the prepared sound-sensitive agent has no fluorescence quenching effect, so that more singlet oxygen can be generated in the sonodynamic therapy process to inhibit tumor growth; due to the characteristics of the AIE molecules, fluorescence navigation interventional therapy can be introduced; meanwhile, the AIE molecules are various in variety, so that the range of the sound-sensitive agent can be expanded.

Description

technical field [0001] The invention belongs to the technical field of functional materials and medicines, and relates to a sound sensitizer with aggregation-induced luminescent properties and a preparation method thereof. Background technique [0002] The high morbidity and mortality of malignant tumors have seriously threatened human life and health, so it is urgent to find an effective treatment method for malignant tumors. Currently, there are certain drawbacks in the clinically applied means of treating malignant tumors, such as surgical resection, radiotherapy, and chemotherapy. In recent years, photodynamic therapy, a minimally invasive treatment method, has entered people's field of vision, but light decays very quickly in tissues and cannot penetrate deep tissues, so the photosensitizers accumulated in deep tissues cannot be fully excited to generate enough reactive oxygen species. Kill tumor cells. [0003] Acoustodynamic therapy developed on the basis of photody...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K9/51A61K49/00A61P35/00
CPCA61K9/5138A61K9/5146A61K9/5169A61K41/0033A61K49/0021A61K49/0093A61P35/00
Inventor 张兵波曾维薇杨维涛徐琰
Owner TONGJI UNIV
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