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Application of nanometer drug-loading system in preparation of medicines for curing refractory thyroid cancer

A nano-drug-loading, thyroid cancer technology, applied in the biological field, can solve the problems of high side effects, poor prognosis and high cost of treatment methods

Inactive Publication Date: 2018-08-03
JILIN 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 solve the disadvantages of the existing refractory thyroid cancer treatment methods, such as poor prognosis, high cost, and high side effects, and to provide an application of a nano drug-loading system in the preparation of drugs for the treatment of refractory thyroid cancer

Method used

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  • Application of nanometer drug-loading system in preparation of medicines for curing refractory thyroid cancer
  • Application of nanometer drug-loading system in preparation of medicines for curing refractory thyroid cancer
  • Application of nanometer drug-loading system in preparation of medicines for curing refractory thyroid cancer

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preparation example Construction

[0037] According to the present invention, the preparation method of the nano drug system, the method comprises:

[0038] Step 1: preparing ROS-responsive hyperbranched polymers;

[0039] Step 2: Dissolving the ROS-responsive hyperbranched polymer obtained in Step 1 in a solvent, then adding photosensitizers and chemotherapeutic drugs, stirring, and mixing uniformly to obtain a mixed solution;

[0040] Step 3: Under the condition of vigorous stirring, drop the mixed solution of Step 2 into the water phase, and self-assemble into nanoparticles. After the addition, adjust the rotation speed and continue to stir slowly for 2 hours to obtain a nano drug system.

[0041] According to the present invention, described step one is specifically:

[0042] 1) Acetone and cysteine ​​salt are synthesized into diamine thioketal monomer through carbonyl addition reaction at normal temperature; the reaction time is preferably 12h; the acetone and cysteine ​​salt The mass ratio is preferably...

Embodiment 1

[0048] 15.6 g of acetone and 11.36 g of cysteine ​​salt were reacted for 12 hours at room temperature, and the obtained crude product was purified to obtain the diaminothiocarboxone monomer;

[0049]Take 0.5g mPEG and 0.45g phosphorus oxychloride to react at room temperature for 2h, the solvent is chloroform, add 1g diaminothiocarboxone monomer and 1.26g TEA to the above solution, and react overnight at room temperature to obtain a ROS responsive hyperbranched structure. H NMR spectrum as figure 1 as shown, figure 1 Among them, a, b, c, and d represent different chemical bonds, and the peak area of ​​the hydrogen spectrum represents the number of chemical bonds. From the figure, we can conclude that the detected substance is consistent with the ROS-responsive hyperbranched structure.

[0050] Weigh 10 mg of ROS-responsive hyperbranched polymer material into a sterile 5 mL EP tube with an electronic balance, add 1 mL of DMSO, and vortex until completely dissolved; take a 10 mL...

Embodiment 2

[0055] Embodiment 2 Preparation of drug-loaded nanosystems containing fluorescent dyes DiI and / or DiD

[0056] Weigh 10 mg of the ROS-responsive hyperbranched polymer material prepared in Example 1 with an electronic balance into a sterile 5mLEP tube, add 1mL DMSO, and vortex until completely dissolved; take a 10mL round-bottomed flask, add magnetons, and dissolve the above solution Transfer to a round-bottomed flask and add in three groups respectively. The first group was added with 2 mg Sfb, 2 mg Ce6 and 5 μg DiD dye (100 μL 20 mg / mL Sfb, 100 μL 20 mg / mL Ce6 DMSO solution, 1 μL 5 mg / mL DiD DMSO solution); The second group added 2mg Sfb, 2mg Ce6 and 5μg DiI dye (100μL 20mg / mL Sfb, 100μL 20mg / mL Ce6 DMSO solution, 1μL 5mg / mL DiI DMSO solution); the third group added 2mg Sfb, 2mg Ce6, 5μg DiD dye and 5 μg of DiI dye (100 μL of 20 mg / mL Sfb, 100 μL of 20 mg / mL Ce6DMSO solution, 1 μL of 5 mg / mL DiD DMSO solution, 1 μL of 5 mg / mL DiI DSMO solution); the three groups were stirred ...

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Abstract

The invention provides application of a nanometer drug-loading system in the preparation of medicines for curing refractory thyroid cancer, and belongs to the field of biotechnology. The nanometer drug-loading system comprises an ROS responsive hyperbranched macromolecule, a photosensitizer and a chemotherapy drug, wherein the structural formula of the hyperbranched macromolecule is shown as a formula I; the photosensitizer is chlorines e6; and the chemotherapy drug is Sorafenib. The nanometer drug-loading system can be enriched in tumor tissue, the ROS level inside the tumor tissue further can be increased under the laser radiation of 660 nm, a nano-carrier inside the tumor tissue is disintegrated, and the chemotherapy drug is quickly released, so that the cure of a tumor is synergistically interacted, simultaneously the using amount of the chemotherapy drug is reduced, and toxic and side effects of the chemotherapy drug are alleviated.

Description

technical field [0001] The invention belongs to the field of biotechnology, and in particular relates to the application of a nano drug loading system in the preparation of drugs for treating refractory thyroid cancer. Background technique [0002] Thyroid cancer is the most common malignant tumor of the endocrine system. In recent years, the incidence of thyroid cancer has been increasing year by year worldwide. In the United States, the incidence of thyroid cancer has increased at an average annual rate of 6.4% in the past 10 years, while the prevalence of thyroid cancer in my country has risen to the third place among female malignant tumors. Patients with differentiated thyroid cancer have a long disease-free survival and a good prognosis after surgery, but recurrence or distant metastasis after surgery cannot be avoided in some patients. According to statistics, about 20% of patients with thyroid cancer have postoperative recurrence or cervical lymph node metastasis wi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/34A61K31/44A61K41/00A61P35/00
CPCA61K9/5146A61K31/44A61K41/0071A61P35/00A61K2300/00
Inventor 孟宪瑛孙旭王瑶琪魏佳张强李勇逄仁柱杨帅李锐王培松
Owner JILIN UNIV
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