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Preparation method of radionuclide 131I labeled functional polyphosphazene nanosphere

A technology of radionuclide and polyphosphazene, which is applied in the field of preparation of functional polyphosphazene nanospheres, can solve the problems of difficult radiotherapy, non-specificity, low accumulation of lesion sites, and short circulation time in the body, and achieve easy Separation of operation, good radiation stability, simple and easy preparation process

Active Publication Date: 2019-06-11
DONGHUA UNIV +1
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  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to the short circulation time of radionuclides in the body, non-specificity and low accumulation in the lesion site, it is difficult to achieve effective radiotherapy

Method used

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  • Preparation method of radionuclide 131I labeled functional polyphosphazene nanosphere
  • Preparation method of radionuclide 131I labeled functional polyphosphazene nanosphere
  • Preparation method of radionuclide 131I labeled functional polyphosphazene nanosphere

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Embodiment 1

[0048] (1) Dissolve 100 mg of hyperbranched polyethyleneimine (PEI) with a relative molecular weight of 25,000 g / mol in 20 mL of acetone, and quickly add 1 mL of triethylamine to the dissolved PEI solution under stirring conditions at 25-35 ° C. Stir vigorously for 1-10 min until well mixed. 50 mg of hexachlorocyclotriphosphazene (HCCP) was dissolved in 5 mL of acetone, and the solution of hexachlorocyclotriphosphazene dissolved in acetone was slowly added dropwise to the above PEI solution. Stir at room temperature for 2-3h. After the reaction, collect the precipitate by centrifugation at 3000rpm. After ultrasonically dispersing the precipitate in water for 15min-1h, wash it by centrifugation at 6000-8000rpm for 3 times to obtain highly cross-linked nanospheres PZS of PEI and HCCP.

[0049] (2) Take 50 mg of PZS nanospheres and ultrasonically disperse them in 20 mL of DMSO, take 10.52 mg of HPAO and dissolve them in 5 mL of DMSO, and add them dropwise into the above PZS solut...

Embodiment 2

[0054] Get the PZS nanosphere in embodiment 1 after diluting 100 times, observe material appearance by SEM, illustrate that PZS nanosphere has regular spherical structure, size distribution is uniform, and average particle diameter is 179.9nm ( figure 2 ). Then, the hydrated particle size and surface potential of PZS nanospheres and their modified materials were characterized by DLS. The results showed that the hydrated particle sizes of PZS nanospheres and PZS.NHAc-HPAO-PS were 426.1nm and 474.5nm ( image 3 ). The surface potential results show that the surface potential of PZS is 37.5mV, and the surface potential of PZS.NHAc-HPAO-PS is 11.9mV, so the toxicity of amino groups on the surface of PZS materials can be effectively avoided through surface modification, and the surface potential of the materials has dropped significantly. , improving the biocompatibility of the material ( Figure 4 ). Figure 5 (a) shows that: the prepared PZS polyphosphazene nanospheres are at...

Embodiment 3

[0056] Take (4) in Example 1 and the product obtained in step (3) in Comparative Example 1 to configure the mother solution with a concentration of 1 mg / mL with sterile physiological saline, and then serially dilute to 100, 50, 20, 10, 5, 2, 1 μg / mL of material. The cultured 4T1 cells were planted in a 96-well plate, and inoculated at a density of 10,000 cells / well, with a volume of 100 μL per well. After culturing overnight, wash with physiological saline for 3 times, then add the above-mentioned materials of each dilution gradient, and co-culture with the cells for 24 hours. Six parallel wells were made for each gradient, and normal saline was used as a blank control. After the culture, wash with 100 μL of normal saline for 3 times, then add 90 μL of serum-free medium and 10 μL of CCK-8 solution to each well, incubate at 37 °C for 2 h, and detect the absorbance at 450 nm with a microplate reader. The results of cell viability detected by CCK-8 method showed that PZS.NHAc-H...

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Abstract

The invention relates to a preparation method of a radionuclide 131I labeled functional polyphosphazene nanosphere. The preparation method comprises the following steps: preparing a nanosphere PZS; modifying the surface with 3-(4-hydroxyphenyl) propionic acid N-hydroxysuccinimide (HPAO) to form PZS-HPAO to; enabling the nanospheres to react with 1,3-propane sultone (1,3-PS) to obtain PZS-HPAO-PS;adding triethylamine and acetic anhydride into the solution, carrying out acetylation treatment on amino groups on the surface of PZS, and carrying out 131I marking to obtain the radionuclide 131I marked functional nanospheres. The radionuclide 131I labeled functional polyphosphazene nanosphere has good water dispersibility and biocompatibility, has a good single photon emission computed tomography (SPECT) imaging effect and a good radiotherapy effect, and has potential application value in the field of diagnosis and treatment integration.

Description

technical field [0001] The invention belongs to the field of SPECT imaging, in particular to a radionuclide 131 Preparation method of I-labeled functionalized polyphosphazene nanospheres. Background technique [0002] In the field of biomedicine, the integrated system of diagnosis and treatment can not only diagnose the disease in real time and accurately and carry out treatment simultaneously, but also monitor the curative effect and adjust the dosing regimen at any time during the treatment process, which is conducive to achieving the best therapeutic effect and reducing side effects. With the development of nanoscience and technology, the development of a new, efficient and multifunctional nanoplatform that integrates imaging and therapy has attracted widespread attention from scientific researchers. [0003] Due to the advantages of high sensitivity and low injection dose of radiotherapy, nuclear medicine treatment is more and more commonly used in the field of clinical...

Claims

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Application Information

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IPC IPC(8): A61K51/06A61P35/00A61K101/02
Inventor 沈明武朱蔚范钰史向阳赵晋华赵凌舟
Owner DONGHUA UNIV
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