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Preparation method of radionuclide 131I-labeled folic acid targeted multifunctional dendrimer

A technology of dendrimers and radionuclides, applied in the field of preparation of multifunctional dendrimers, can solve the problems of limited biomedical applications, short blood circulation time, poor specific distribution, etc., and achieve the goal of increasing circulation time in the body Effect

Inactive Publication Date: 2015-07-08
DONGHUA UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

but due to the molecular 131 The short blood circulation time and poor specific distribution of I in the body limit its biomedical application as an effective diagnostic nuclide

Method used

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  • Preparation method of radionuclide 131I-labeled folic acid targeted multifunctional dendrimer
  • Preparation method of radionuclide 131I-labeled folic acid targeted multifunctional dendrimer
  • Preparation method of radionuclide 131I-labeled folic acid targeted multifunctional dendrimer

Examples

Experimental program
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Effect test

Embodiment 1

[0067] (1) Dissolve FA with a dry weight of 11.37 mg in 5 mL of DMSO, and add EDC with a dry weight of 4.94 mg dissolved in 2 mL of DMSO solution dropwise while stirring. After stirring for 3 hours, add A dry weight of 85.86 mg of NH dissolved in 5 mL of DMSO solution 2 -PEG-COOH (Mw=5000), wherein FA and NH 2 -The molar ratio of PEG-COOH is 1.5:1, the molar ratio of EDC and FA is 1:1, react for 1 day, and dialyze the resulting solution with cellulose dialysis membrane MWCO=1000 in phosphate buffer solution and distilled water for 3 days , freeze-dried to obtain FA-PEG-COOH.

[0068] (2) Dissolve the G5PAMAM dendrimer with a dry weight of 30mg with 5mL of DMSO, and add drop by drop the HPAO with a dry weight of 3.64mg dissolved in 2mL of DMSO solution while stirring, wherein the moles of HPAO and G5PAMAM dendrimer The ratio is 12:1, react for 1 day, dialyze the resulting solution with cellulose dialysis membrane MWCO=14000 in phosphate buffer solution and distilled water for...

Embodiment 2

[0073] The product obtained by thin layer chromatography 131 Stability analysis of I-G5.NHAc-HPAO-PEG-FA, see appendix image 3 . Mix 100 μL of radioactive markers with 1 mL of 0.9% normal saline and fetal calf serum, and then use thin-layer chromatography to test at 37 ° C 131 The radiochemical purity of I-G5.NHAc-HPAO-PEG-FA at 0h, 1h, 3h, 5h, 27h and 44h, the results showed that at different time points, 131 The radiochemical purity of I-G5.NHAc-HPAO-PEG-FA is above 80%, without a large amount of 131 I come off the carrier. Description of the product obtained 131 I-G5.NHAc-HPAO-PEG-FA has good stability.

Embodiment 3

[0075] The in vitro biocompatibility of the prepared folic acid-targeted multifunctional dendrimer carrier was tested by MTT test. Weighed 12.7 mg of the carrier material in Example 1 and dissolved it in 300 μL of PBS buffer to prepare G5.NHAc- The HPAO-PEG-FA solution with a concentration of 200 μM was diluted to a solution with a concentration of 100 μM, 50 μM, 10 μM, and 1 μM respectively. After incubating C6 cells with the above-mentioned materials at different concentrations (the respective final concentrations are 20 μM, 10 μM, 5 μM, 1 μM, and 0.1 μM) for 24 h, discard the materials, add 180 μL of medium and 20 μL of MTT, and incubate at 37 °C for 4 h , Pour off the culture medium, add 200 μL DMSO, shake on a shaker for 20 minutes, measure the result with a microplate reader, and get Figure 4 Shown data, the result shows that embodiment 1 is unlabeled within a certain concentration range 131 The carrier material of I has no obvious cytotoxicity and has good biocompatib...

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Abstract

The invention relates to a preparation method of a radionuclide 131I-labeled folic acid targeted multifunctional dendrimer. The preparation method comprises the following steps: (1) adding EDC and an NH2-PEG-COOH solution to folic acid for reacting so as to obtain FA-PEG-COOH; (2) adding HPAO to a dendrimer solution for reacting so as to obtain G5.NH2-HPAO; (3) adding EDC to the FA-PEG-COOH solution, activating, and adding to the G5.NH2-HPAO water solution for reacting so as to obtain dendrimer solution; and (4) adding N(C2H5)3 and acetic anhydride to the solution for reacting so as to obtain a functionalized dendrimer solution, and then adding Na131I for carrying out a labeling reaction so as to obtain the multifunctional dendrimer. The material prepared by the invention has excellent SPECT imaging and radioactive therapy functions, and the material has a potential application value in the field of forming a nano material integrating diagnosis and treatment.

Description

technical field [0001] The invention belongs to the field of preparation of functional dendritic macromolecular materials, in particular to a radionuclide 131 Preparation of I-labeled folate-targeted multifunctional dendrimers. Background technique [0002] Cancer is an abnormal lesion formed by the body under the action of various carcinogenic factors, the cells of local tissues lose the normal regulation of their growth at the gene level, resulting in abnormal clonal proliferation. In view of the local invasion and distant metastasis characteristics of malignant tumors, the treatment effect and cost of cancer are closely related to the period when the cancer is discovered. Early detection and early treatment are the most effective ways to reduce cancer mortality. With the development of nanoscience and technology, various nanosystems have begun to be applied to the early diagnosis and treatment of cancer, including iron oxide nanoparticles, quantum dots, carbon nanotubes...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K51/06A61P35/00A61K101/02
Inventor 史向阳朱静怡熊智娟赵晋华赵凌舟
Owner DONGHUA UNIV
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