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Black phosphorus microvesicle pharmaceutical carrier capable of realizing local fixedpoint radiotherapy for tumors and preparation method of black phosphorus microvesicle pharmaceutical carrier

A radiation therapy and radiopharmaceutical technology, applied in the field of black phosphorus microbubble drug carrier and its preparation, can solve the problems of difficult fixed-point enrichment therapy, low dose of radiopharmaceuticals, poor loading, etc., to achieve easy access to lesions and increase enrichment , technical solutions and technical effects with clear results

Inactive Publication Date: 2019-03-29
PEKING UNIV SHENZHEN HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The former uses radiation controlled by the precision of the instrument to perform three-dimensional directional and quantitative local irradiation therapy on the lesion. The difficulty of implementation lies in how to accurately irradiate the tumor lesion area and avoid radiation damage to normal tissues, that is, the former treatment method is likely to cause Radiation damage to normal tissue adjacent to the lesion
The latter is generally composed of micro-nanoparticles. Due to the poor drug loadability of micro-nanoparticles, it is difficult for the radiopharmaceuticals that can be carried to enrich the lesion through the blood circulation. Secondly, the dose of radiopharmaceuticals reaching the lesion is too low and quickly will be cleared, so it is difficult to achieve local targeted enrichment treatment

Method used

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  • Black phosphorus microvesicle pharmaceutical carrier capable of realizing local fixedpoint radiotherapy for tumors and preparation method of black phosphorus microvesicle pharmaceutical carrier

Examples

Experimental program
Comparison scheme
Effect test

specific Embodiment approach 1

[0024] Drug loading step, put through FMoc-NH-PEG12-CH 2 CH 2 COOH-modified black phosphorus aqueous solution injected into medical 99m TcN-NOET ampoule and mix evenly, and then draw out the uniformly dispersed mixed solution, wherein the black phosphorus in the black phosphorus aqueous solution is single-layer and / or few-layer nano black phosphorus flakes, and the particle size is between 500 nanometers and 5 microns between;

[0025] In the microbubble film forming step, inject the mixed solution formed in the drug loading step into the SonoVue microbubble preparation ampoule and fill it with SF 6 Gas, using ultrasonic oscillation and mechanical stirring and shearing successively to vibrate and stir and shear until foaming, and a gray-black dispersed emulsion is obtained. The microbubble concentration in the dispersed emulsion is about 3.0×10 9 pieces / ml. The particle size of the microbubbles in the emulsion is between 2 microns and 5 microns, and the microbubbles are co...

specific Embodiment approach 2

[0026] In the drug loading step, the aqueous solution of black phosphorus modified by fluorescent covalent injection is injected into the medical 99m TcN-NOET ampoule and mix evenly, then draw out the uniformly dispersed mixed solution, wherein the black phosphorus in the black phosphorus aqueous solution is single-layer and / or few-layer nano black phosphorus flakes, the particle size is between 200 nanometers and 4 microns between;

[0027] In the microbubble film-forming step, the mixed solution formed in the drug loading step is injected into the ampoule prepared by mixing phospholipid microbubbles, filled with perfluoropropane gas, and successively adopts ultrasonic oscillation and mechanical stirring and shearing to vibrate and stir until Bubbles, to obtain a gray-black dispersion emulsion, the microbubble concentration in the dispersion emulsion is about 3.2 × 10 9 pieces / ml. The diameter of the microbubbles in the emulsion is between 2 microns and 4 microns, and the i...

specific Embodiment approach 3

[0028] In the drug loading step, the black phosphorus aqueous solution modified by polydopamine is injected into the medical 99m TcN-NOET ampoule and mix evenly, then draw out the uniformly dispersed mixed solution, wherein the black phosphorus in the black phosphorus aqueous solution is single-layer and / or few-layer nano black phosphorus flakes, the particle size is between 200 nanometers and 5 microns between;

[0029] In the microbubble film forming step, inject the mixed solution formed in the drug loading step into the SonoVue microbubble preparation ampoule and fill it with SF 6Gas, using ultrasonic oscillation and mechanical stirring and shearing successively to vibrate and stir and shear until foaming, and a gray-black dispersed emulsion is obtained. The microbubble concentration in the dispersed emulsion is about 3.3×10 9 pieces / ml. The particle size of the microbubbles in the emulsion is between 2 microns and 5 microns, and the microbubbles are coated with SF 6 ga...

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Abstract

The application belongs to the technical field of anticancer drugs, and particularly relates to a black phosphorus microvesicle pharmaceutical carrier capable of realizing local fixedpoint radiotherapy for tumors and a preparation method of the black phosphorus microvesicle pharmaceutical carrier. The black phosphorus microvesicle pharmaceutical carrier capable of realizing local fixedpoint radiotherapy for tumors comprises lipid microvesicles and a black phosphorus carrier wrapped with the lipid microvesicles, radioactivity medicines and inert gas, wherein the radioactivity medicines are enriched on the black phosphorus carrier; and the black phosphorus carrier is monolayer and / or several-layer nanometer black phosphorus sheets. The preparation method comprises the step of loading the medicines and the step of microvesicle filming. The black phosphorus microvesicle pharmaceutical carrier capable of realizing local fixedpoint radiotherapy for tumors, provided by the application, has the technical advantages of being safe, reliable, easy in reaching focus of diseases, high in the dosage of effective medicines, capable of realizing local fixedpoint enrichment treatment and the like.

Description

technical field [0001] The application belongs to the technical field of anticancer drugs, and in particular relates to a black phosphorus microbubble drug carrier capable of realizing local tumor radiotherapy and a preparation method thereof. Background technique [0002] At present, there are two main types of radiotherapy technologies for tumors. One is the precise treatment of radiation instruments led by the "Speed ​​Edge Knife" that has been developed in clinical practice, and the other is the use of micro-nano-level radioactivity that is still being tried in preclinical research. The tracer carrier is loaded with radiopharmaceuticals for targeted treatment of malignant tumor lesions. [0003] Both have application flaws. The former uses radiation controlled by the precision of the instrument to perform three-dimensional directional and quantitative local irradiation therapy on the lesion. The difficulty of implementation lies in how to precisely irradiate the tumor l...

Claims

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Application Information

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IPC IPC(8): A61K51/02A61K51/06A61K51/12A61P35/00A61K103/10
CPCA61K51/02A61K51/06A61K51/1234A61P35/00
Inventor 郑婷婷陈芸贾红梅陈珂珂张雪彭佼裴涛姚瑶
Owner PEKING UNIV SHENZHEN HOSPITAL