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Antitumor application of chlorambucil-polydopamine prodrug nanoparticles

A technology of chlorambucil and nanoparticles, applied in the field of biomedicine

Inactive Publication Date: 2018-12-18
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to provide an anti-tumor application based on chlorambucil-polydopamine prodrug nanoparticles in order to overcome the above-mentioned defects in the prior art, specifically mild photothermal therapy-chemotherapy combined with traceless treatment of tumors method to solve the problem of high-intensity and high-dose near-infrared light irradiation in the prior art to induce excessive temperature at the tumor site, severe scars, skin burns and damage to surrounding normal tissues at the tumor site, as well as tumor recurrence and Difficulties in clinical application such as metastasis

Method used

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  • Antitumor application of chlorambucil-polydopamine prodrug nanoparticles

Examples

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Effect test

Embodiment 1

[0074] Example 1 Preparation of chlorambucil-dopamine conjugate molecule

[0075] Step 1, 1000 mg of 3,4-dihydroxyphenylpropionic acid was dissolved in 20 mL of anhydrous acetone, and 383 μL of phosphorus trichloride was slowly added dropwise to the above reaction flask, and the reaction was carried out in an ice-water bath at 0°C for 6 After hours, the water pump was rotovaped. The crude product was dissolved in a mixture of water and ether, extracted with a separating funnel, the organic layer was extracted three times with water, concentrated and dried to obtain a white powder 2,2-dimethyl-1,3-benzodioxolane ene-5-propionic acid. Yield 60%.

[0076] Step 2, 222mg of 2,2-dimethyl-1,3-benzodioxol-5-propionic acid, 247.2mg of dicyclohexylcarbodiimide, 146.4mg of 4-dimethylamino Pyridine was dissolved in 5 mL of anhydrous dichloromethane, and after 4 hours of reaction at room temperature, 180 mg of the dichloromethane solution of 2-hydroxyethyl disulfide was added dropwise t...

Embodiment 2

[0082] Example 2 Preparation of redox-responsive chlorambucil-polydopamine prodrug nanoparticles

[0083] Add 410mg of tris, 20mL of distilled water to a 50mL round bottom flask, stir at 30°C for 30 minutes, dissolve 12.5mg of dopamine hydrochloride and 53.7mg of chlorambucil-dopamine conjugate molecules in 1mL of distilled water, And quickly injected into the above solution, the reaction time is 24 hours, and the nanoparticle solution is black. Distilled water dialysis (dialysis bag molecular weight cut-off 3500) for two days, 1000mL distilled water × 8. Freeze dry for 48 hours. The yield is 10% to 30%.

[0084] The dynamic light scattering pattern of the chlorambucil-polydopamine prodrug nanoparticles that the present embodiment makes is as follows Figure 4 shown.

Embodiment 3

[0085] Example 3 Preparation of redox-responsive chlorambucil-polydopamine prodrug nanoparticles

[0086] The steps of this example are the same as those in Example 2, except that the masses of dopamine hydrochloride and chlorambucil-dopamine conjugate molecules are 12.5 mg and 17.4 mg, respectively. The yield of this embodiment is 30%~40%.

[0087] The dynamic light scattering pattern of the chlorambucil-polydopamine prodrug nanoparticles that the present embodiment makes is as follows Figure 5 shown.

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Abstract

The invention relates to antitumor application of chlorambucil-polydopamine prodrug nanoparticles, and concretely relates to a mild photothermal therapy-chemotherapy combined tumor alete treatment technology based on the chlorambucil-polydopamine prodrug nanoparticles. The nanoparticles can realize spatiotemporal manipulation in an antitumor effect in order to achieve accurately-positioned tumor ablation, and passive targeting action of the prodrug nanoparticles on tumor parts can be achieved by the enhanced permeation and retention(EPR) effect; the mild photothermal effect can enhance the expansion of tumor blood vessels and the permeability of cell membrane effectively promote the accumulation and penetration of the nanoparticles in tumors and the endocytosis of tumor cells; and photothermal therapy can induce the antitumor immunity in order to improve the effect of chemotherapy, so synergistic antitumor effects are generated in the photothermotherapy-chemotherapy combined therapy. The application provides a new way for precise cancer treatment, and has a potential clinical application prospect.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to the antitumor application of a chlorambucil-polydopamine prodrug nanoparticle. Background technique [0002] Cancer is a major disease that seriously threatens human survival and social development. Although photothermal therapy and photothermal therapy-chemotherapy synergistic therapy have achieved complete ablation of solid tumors, they are usually achieved under high-intensity and high-dose near-infrared light irradiation at temperatures above 50 °C, so tumor sites often Severe scarring, as well as burning of the skin, and even damage to the surrounding normal tissue. To make matters worse, residual tumor cells at the treatment site are often not completely eradicated, leading to tumor recurrence and metastasis. These defects hinder the clinical application of photothermal therapy and its combined photothermal therapy-chemotherapy, and it is still very challenging to ach...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K31/196A61K49/22A61K49/00A61K47/69A61P35/00A61P35/04C07C319/22C07C323/12C08G73/06
CPCA61K41/0052A61K47/55A61K47/59A61K47/6935A61K49/00A61K49/0017A61K49/221A61P35/00A61P35/04A61K31/196C07C319/22C07D317/46C08G73/0672A61K2300/00
Inventor 杜畅董常明张蓉
Owner SHANGHAI JIAO TONG UNIV
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