Preparation method of RGD targeting tree-shaped nanoparticle marker

A nanoparticle and marker technology, applied in the directions of drug delivery, radioactive physical shape, powder delivery, etc., can solve the problems of single imaging function, low specific targeting, unsustainable stability, etc. The effect of high product purity and short reaction time

Inactive Publication Date: 2017-05-24
GUANGZHOU GENERAL HOSPITAL OF GUANGZHOU MILITARY COMMAND
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Problems solved by technology

But at present, there are mainly three problems that need to be solved and improved for radioactive drug probes: first, the stability is difficult to sustain; second, the specific targeting is not high; third, imaging and treatment cannot At the same time
Furthermore, most of the currently synthesized targeted nanoparticles have only a single imaging function (such as 18 F. 99m Tc, Cy5.5, etc.), or just carry out tumor-targeted therapy by loading drugs (DOX, PTX, etc.), and there are few studies on nanoparticles with two functions at the same time.

Method used

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  • Preparation method of RGD targeting tree-shaped nanoparticle marker
  • Preparation method of RGD targeting tree-shaped nanoparticle marker
  • Preparation method of RGD targeting tree-shaped nanoparticle marker

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preparation example Construction

[0032] A preparation method for RGD targeting dendritic nanoparticles, comprising the steps of:

[0033] RGDyC and bifunctional PEG Mixed with solvent to generate NHS-PEG-RGDyC by click reaction , wherein the number n of ethylene glycol units in the bifunctional PEG is an integer between 40 and 120;

[0034] NHS-PEG-RGDyC and PAMAM nanoparticles are mixed, and the NHS-PEG-RGDyC is covalently connected with the amine groups on the PAMAM nanoparticles to obtain PAMAM-PEG-RGDyC.

[0035] The prepared PAMAM-PEG-RGDyC can be further loaded with drug molecules or markers.

[0036] As a further improvement of the above preparation method, the pH of the reaction between RGDyC and bifunctional PEG is 5-7. More preferably, the pH of the reaction between RGDyC and bifunctional PEG is 6.

[0037] As a further improvement of the above preparation method, the solution for the reaction of RGDyC and bifunctional PEG is NaAc-HAc solution.

[0038] As a further improvement of the above...

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Abstract

The invention discloses a preparation method of an RGD targeting tree-shaped nanoparticle marker. The method comprises the following steps: mixing RGDyC and bifunctional PEG in a solvent, and carrying out a click reaction to generate NHS-PEG-RGDyC; and mixing the NHS-PEG-RGDyC with a PAMAM nanoparticle to make the NHS-PEG-RGDyC react and covalently connect with the amino group of the PAMAM nanoparticle in order to obtain PAMAM-PEG-RGDyC. The method has the advantages of high efficiency of the reaction process, short reaction time, simplicity in operation, high marking rate and high product purity. The RGD targeting tree-shaped nanoparticle marker prepared through the method can be used as an SPECT molecular probe, and the method provides a new idea for synthesis of the clinic SPECT molecular probe. The RGD targeting tree-shaped nanoparticle marker prepared through the method also carries an effective amount of drug molecules, and can realize specific development and targeting therapy of tumors to make the therapy process of malignant tumors possibly in a visual state.

Description

technical field [0001] The invention relates to a preparation method of a radioactive marker, in particular to a preparation method of an RGD-targeted dendritic nanoparticle marker. Background technique [0002] In recent years, cancer has become a serious social problem and a health focus of public concern. The "2012 China Cancer Registration Annual Report" shows that in the past 20 years, cancer in my country has shown a trend of younger age and higher incidence and mortality in the "third line". The national cancer mortality rate is 1.8054 / 100,000, with 2.7 million deaths due to cancer every year. Including breast cancer, lung cancer, colon cancer, and thyroid cancer, the age of onset was lower than before. At present, new tumor molecular probes have become an important tool for the diagnosis and treatment of tumors. Targeted diagnosis and treatment mediated by various tumor molecular probes has become a hot spot in molecular imaging research. [0003] In previous stu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/06A61K51/12
CPCA61K51/06A61K51/1251
Inventor 张金赫王欣璐钟建秋尹吉林禹晖杨玉婷吴凡
Owner GUANGZHOU GENERAL HOSPITAL OF GUANGZHOU MILITARY COMMAND
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