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Multifunctional nanoparticles for head and neck squamous cell carcinoma targeted treatment and preparation method

A nanoparticle and targeted therapy technology, applied in the direction of general/multifunctional contrast agents, preparations for in vivo experiments, medical preparations with non-active ingredients, etc., can solve the problem that photosensitizers are difficult to penetrate tumor tissue, efficiency and accuracy Insufficient performance and other problems, to achieve effective biological tissue penetration, high resolution, and improve the effect of enrichment rate

Inactive Publication Date: 2020-10-16
NANJING STOMATOLOGICAL HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the efficiency and accuracy of these ligands are not yet sufficient for tumor targeting in clinical applications, such as photosensitizers having difficulty penetrating tumor tissue due to the lack of deep blood vessels in tumors.

Method used

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  • Multifunctional nanoparticles for head and neck squamous cell carcinoma targeted treatment and preparation method
  • Multifunctional nanoparticles for head and neck squamous cell carcinoma targeted treatment and preparation method
  • Multifunctional nanoparticles for head and neck squamous cell carcinoma targeted treatment and preparation method

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Experimental program
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Embodiment 1

[0021] The following parts are all parts by mass,

[0022] 17 parts of chlorin e6 (Sigma, 1g) were dissolved in dimethylsulfoxide, in 15 parts of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 15 parts of N-hydroxysulfosuccinimide was stirred at room temperature for 1 hour under the condition of catalyst, and reacted with 140 parts of polyethylene glycol (Sigma, 100g) at room temperature to generate Ce6-PEG; dimethyl sulfoxide, freeze-dried to obtain the Ce6-PEG product; then Ce6-PEG was dissolved in methanol, tirapazamine (Sigma, 1g) was dissolved in chloroform, after mixing, sonicated for 5 minutes, and rotary evaporated to obtain the product CPT; Utilize 10 parts of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride as a cross-linking agent, add the product CPT and 10 parts of anti- LDLR (Sigma, 1ml), stirred at room temperature for 2 hours, and then purified by centrifugation to obtain CPTA nanoparticles.

[0023] CPTA nanoparticle head and neck...

Embodiment 2

[0030] This embodiment is improved on the basis of the embodiments. Before sonication, adding methanol solution containing sulfuric acid to the mixture of Ce6-PEG and tirapazamine can significantly reduce the content of impurity groups.

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Abstract

The invention discloses a preparation method of multifunctional nanoparticles for head and neck squamous cell carcinoma targeted treatment. The preparation method comprises the following steps of combining carboxyl in a chlorin e6 structure with amino contained in polyethylene glycol, forming a shell structure in a freeze-drying manner, forming nanoparticles by combination with tirapazamine through self-assembly, and reacting the amino of the polyethylene glycol with anti-LDLR carboxyl to generate the final product. The defects in the prior art can be overcome, and the enrichment rate and thefluorescence imaging effect of a diagnosis and treatment reagent in the head and neck squamous cell carcinoma are improved.

Description

technical field [0001] The invention relates to the technical field of cancer photodiagnosis and treatment reagents, in particular to a multifunctional nanoparticle for targeted therapy of head and neck squamous cell carcinoma and a preparation method thereof. Background technique [0002] Clinical studies have shown that hypoxia is one of the typical characteristics of almost all solid tumors, and the hypoxic microenvironment in the tumor plays an important role in promoting treatment resistance, especially resistance to radiotherapy and chemotherapy, and tumor hypoxia is closely related to regional lymph node metastasis and patient prognosis relevant. The typical hypoxic microenvironment also exists in head and neck squamous cell carcinoma, and it is closely related to tumor clinical stage, pathological grade, lymph node metastasis and patient survival. Hypoxia can induce a series of changes in cytology, physiology and molecular biology, and then change the normal process...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/00A61K49/22A61K9/51A61K47/10A61K31/53A61P35/00
CPCA61K49/0002A61K49/0021A61K49/0054A61K49/0093A61K49/221A61K49/225A61K9/5146A61K31/53A61P35/00
Inventor 韩伟蔡宇宋传慧汤传超
Owner NANJING STOMATOLOGICAL HOSPITAL
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