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NO-loaded docetaxel nano-drug as well as preparation method and application thereof

A technology of docetaxel and nano-medicine, which is applied in the field of NO-loaded docetaxel nano-medicine and its preparation, which can solve the problems of poor water solubility, insufficient targeting, and easy drug resistance of docetaxel. Improved kinetic properties, high drug loading, and improved sensitivity

Active Publication Date: 2022-06-07
WEST ANHUI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Purpose of the invention: Based on the existing objective problems, the present invention provides a NO-loaded docetaxel nano-drug and its preparation method and application, so as to solve the problem of poor water solubility of docetaxel, insufficient targeting, and easy drug resistance Improve the effect of tumor treatment

Method used

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  • NO-loaded docetaxel nano-drug as well as preparation method and application thereof
  • NO-loaded docetaxel nano-drug as well as preparation method and application thereof
  • NO-loaded docetaxel nano-drug as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0029] Embodiment 1: Synthesis of isosorbide mononitrate docetaxel conjugate (ISMN-DTX), the process is as follows:

[0030] At room temperature, isosorbide mononitrate and succinic anhydride were placed in an eggplant-shaped flask, dissolved in dichloromethane, and then 4-dimethylaminopyridine (DMAP) was slowly added, and the reaction was stirred at room temperature. After the completion of the reaction monitored by TLC, 20 mL of water was added to the reaction solution, the mixture was extracted with ethyl acetate (20 mL×3), the organic layers were combined, washed with saturated sodium chloride solution, dried over anhydrous sodium sulfate, filtered, and concentrated under reduced pressure , and purified by silica gel column chromatography to obtain the intermediate.

[0031] At room temperature, put docetaxel and the intermediate in an eggplant-shaped flask, add 10 mL of dry N,N-dimethylformamide, and slowly add 1-ethyl-3-(3-dimethylpropylamine) under an ice bath Carbodii...

Embodiment 2

[0033] Example 2: Preparation of NO-loaded Docetaxel Nanomedicine and Determination of Particle Size

[0034] The NO-loaded docetaxel nanomedicines were prepared by solvent exchange method. First prepare a 4 mg / mL solution of ISMN-DTX in ethanol. 100 μL of the ISMN-DTX solution was then mixed with 40 μL of a 5% solution of vitamin E polyethylene glycol succinate (TPGS) in ethanol. Deionized water was added dropwise under ultrasonic conditions, and the final concentration was controlled to be 0.4 mg / mL. Thereafter, dialysis was performed against deionized water (Spectra / Pore, MWCO 1000). The particle size and appearance of the NO-loaded docetaxel nanomedicine were observed by dynamic light scattering and transmission electron microscopy. The results showed that the prepared nanomedicine could be formed into monodisperse nanoparticles with a hydrated particle size of 164.5 nm and a particle size distribution index of 0.195. Electron microscopy results show that the nanomedici...

Embodiment 3

[0035] Example 3: Evaluation of the stability of NO-loaded docetaxel nanomedicines

[0036] In order to study the storage stability of NO-loaded docetaxel nanomedicines, the size of the prepared nanomedicines was measured on day 0, day 3, day 6 and day 9 by monitoring NO-loaded docetaxel nanomedicines by DLS, respectively. distributed. The results showed that the particle size and particle size distribution index of the NO-loaded docetaxel nanomedicine did not change significantly during the detection period, indicating that it has good stability. figure 2 shown.

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Abstract

The invention discloses a nitric oxide (NO) loaded docetaxel nano-drug as well as a preparation method and application thereof, the nano-drug is formed by self-assembly of a NO donor docetaxel conjugate, and the NO donor docetaxel conjugate is a conjugate formed by connection of a NO donor and docetaxel through a chemical bond. The NO-loaded docetaxel nano-drug disclosed by the invention is good in stability and capable of controlling the release of NO and enhancing the cytotoxicity of docetaxel.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a NO-loaded docetaxel nanomedicine and a preparation method and application thereof. Background technique [0002] Cancer is one of the major diseases that endanger human health, and it is difficult to cure. At present, the main treatment methods for cancer include surgery, chemotherapy, immunotherapy and radiotherapy. Among them, chemotherapy is the main treatment method and an indispensable adjuvant treatment method. Docetaxel is currently the most representative anticancer chemotherapy drug. However, docetaxel is poorly water-soluble, and requires co-solvent in clinical use, which reduces the therapeutic effect and also causes side effects. In addition, docetaxel also lacks targeting, and can kill normal cells in addition to tumor cells. More importantly, long-term use can lead to multidrug resistance. [0003] At present, the self-assembly of amphiphilic small mo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/55
CPCA61K47/55A61K31/34A61K31/337A61K47/22A61P35/00Y02P20/55
Inventor 高雷雷王芳侯婷婷耿春叶刘东韩邦兴陈艳君李芳
Owner WEST ANHUI UNIV
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