ROS-responsive nanoparticle and application thereof in precise tumor treatment mediated by acoustic dynamic

A nanoparticle and reaction system technology, which is applied in the direction of antineoplastic drugs, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as toxicity, and achieve the effect of improving the therapeutic effect

Active Publication Date: 2019-10-22
XI AN JIAOTONG UNIV
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Problems solved by technology

[0005] At present, nano anti-tumor drugs mainly load the drug inside the nanocarrier. When the drug-loaded nanoparticles enter the tumor tissue and accumulate, the drug is released in the tumor tissue through a sustained release effect. However, the drug-loaded n

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  • ROS-responsive nanoparticle and application thereof in precise tumor treatment mediated by acoustic dynamic
  • ROS-responsive nanoparticle and application thereof in precise tumor treatment mediated by acoustic dynamic
  • ROS-responsive nanoparticle and application thereof in precise tumor treatment mediated by acoustic dynamic

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Embodiment Construction

[0051] The present invention will be described in further detail below through the accompanying drawings and embodiments. The examples are used to help understand the present invention, and should not be regarded as limiting the protection scope of the present invention.

[0052] (1) Preparation of PTX-TL-PEG 1K -NH 2

[0053] Dissolve 1.0mmol TL in 4mL anhydrous DMF, then dissolve 2mmol TEA, 6mmol TC and 2mmol DMAP in 5mL anhydrous DMF, then mix the TL solution with the TEA-TC-DMAP solution, and stir at room temperature for 30min to obtain a reaction system A: Dissolve 0.5mmoL PTX in 2mL of anhydrous DMF and add it dropwise to reaction system A, stir at room temperature for 24h, and then extract the compound obtained by deionized water into deionized water, dichloromethane extraction, saturated physiological Wash with brine, NaSO 4 Drying, purification by silica gel chromatography (dichloromethane / methanol, V:V, 20:1-10:1), and freeze-drying gave the reactant PTX-TL.

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Abstract

The invention discloses an ROS-responsive nanoparticle and application thereof in precise tumor treatment mediated by acoustic dynamic. An ROS sensitive molecule TL is utilized to be connected with anantitumor drug PTX and a hydrophilic fragment NH2-PEG1K-NH2 to obtain an amphipathic ROS sensitive fragment PTX-TL-PEG1K-NH2, and then an ultrasonic emulsification method is utilized to obtain the ROS-responsive nanoparticle loaded with a sensitizer IR780; the prepared nanoparticle can generate ROS under the action of external ultrasound to not only kill tumor cells, but also make the nanoparticle release the PTX to kill the tumor cells, thereby forming a cascading amplification synergistic effect during tumor treatment by the acoustic dynamic to achieve precise tumor treatment.

Description

technical field [0001] The invention relates to a drug preparation for treating tumors with a synergistic effect of sonodynamic cascade amplification, in particular to a method for preparing reactive oxygen species (ROS) responsive mixed nanoparticles. Background technique [0002] At present, chemotherapy is still the main treatment for cancer. Improving the targeting of drugs and reducing the side effects of drugs are the key to improving the effect of chemotherapy. In recent years, nanotechnology has brought new ideas and conceptual changes to tumor treatment. Nanocarriers can provide a means for targeted drug delivery and specific effects on tumor cells. Due to the small size effect, surface effect, volume effect and quantum effect of nanoparticles, it provides the basis for the diagnosis and treatment of tumors. The high permeability and high retention effect (EPR) caused by the unsound microvascular and lymphatic return system of tumor tissue makes nanomaterials with...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K41/00A61K31/337A61P35/00
CPCA61K31/337A61K41/0033A61K47/6935A61P35/00A61K2300/00
Inventor 万明习吴鹏英乔晓阳
Owner XI AN JIAOTONG UNIV
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