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Preparation method of hepatoma carcinoma cell-targeted polyamido-amine dendrimer support

A technology of polyamidoamine dendrimers and macromolecular carriers, which is applied in the direction of non-active ingredient medical preparations, pharmaceutical formulations, antineoplastic drugs, etc., can solve the problems of complex synthesis methods and no related reports, and achieve simple preparation methods , good biocompatibility, and mild reaction conditions

Inactive Publication Date: 2012-01-04
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The synthesis method of this targeting material is relatively complicated, and it can only be used for the loading and delivery of anti-tumor drugs through layer-by-layer self-assembly, so there are still certain limitations in the use and promotion.
[0004] A search of domestic and foreign literature and patents on liver cancer cell targeting carriers shows that there is no relevant report on the functional modification of polyamidoamine dendrimers with lactobionic acid and as a targeting carrier for the diagnosis or treatment of liver cancer cells

Method used

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  • Preparation method of hepatoma carcinoma cell-targeted polyamido-amine dendrimer support
  • Preparation method of hepatoma carcinoma cell-targeted polyamido-amine dendrimer support
  • Preparation method of hepatoma carcinoma cell-targeted polyamido-amine dendrimer support

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] (1) FITC modification of polyamidoamine dendrimers with fluorescein isothiocyanate:

[0036] In the 5th generation polyamidoamine dendrimer G5.NH containing 20 mg of amino-terminated 2 10 mL of anhydrous dimethyl sulfoxide (DMSO) solution containing 1.5 mg FITC was added dropwise to 10 mL of DMSO solution containing 1.5 mg FITC, and stirred with strong magnetic force at room temperature for 24 hours, and then the reaction product was successively dissolved in PBS with a cellulose dialysis membrane with a molecular weight cut-off of 10,000. Dialyze in buffer solution 4L×3 and ultrapure water 4L×3 for 3 days, and finally freeze-dry to obtain the product G5.NH 2 -FI.

[0037] (2) Partial acetylation modification of polyamidoamine dendrimers:

[0038] G5.NH 2-FI was dissolved in 10 mL of DMSO solution, mixed well with 9.6 μL of triethylamine, 5 mL of DMSO solution containing 7.1 mg of acetic anhydride was added dropwise, reacted for 24 hours under strong magnetic stirrin...

Embodiment 2

[0043] Synthesize two kinds of materials G5-FI-Ac-La and G5-FI-Ac according to the method of embodiment 1 and comparative example 1, carry out medium-assisted laser desorption ionization time-of-flight mass spectrometry (MALDI-TOF MS) test, the result is as follows attached figure 2 shown. The results showed that the molecular weight of the compound G5-FI-Ac-La modified with lactobionic acid was significantly higher than that of the compound G5-FI-Ac without modified lactobionic acid. Through calculation, it was found that there were 4 lactobionic acid molecules on the surface of G5-FI-Ac-La. Although there is a certain difference between this test result and the NMR result, considering that the test result of MALDI-TOF MS cannot reflect the average molecular weight of the material, it can only give a broad range of molecular weight distribution, so this result can still be proved very well Lactobionic acid has been successfully modified on the surface of dendrimers, and G5...

Embodiment 3

[0045] The cytotoxicity of the two materials G5-FI-Ac-La and G5-FI-Ac synthesized in Example 1 and Comparative Example 1 was tested using human liver cancer cell HepG2 as a model cell. After the model cells were cultured for 24 hours in the culture solution containing G5-FI-Ac-La and G5-FI-Ac at different concentrations, the survival of the model cells was tested by the MTT method, and the results are shown in the appendix image 3 . The result analysis shows that when the concentration range is 0-2000nM, after HepG2 cells are treated with G5-FI-Ac-La and G5-FI-Ac for 24 hours, the survival rate of the cells tested by MTT method is still higher than 95%. The carrier material synthesized by the invention has good biocompatibility and has no in vitro cytotoxicity within a certain concentration range.

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Abstract

The invention relates to a preparation method of a hepatoma carcinoma cell-targeted polyamido-amine dendrimer support, which comprises the following steps of: (1) modifying a polyamido-amine dendrimer by using fluorescein isothiocyanate to obtain G5.NH2-FI; (2) partially acetylizing the G5.NH2-FI to obtain a product of G5-FI-Ac-NH2 in which an amino-group on the surface of the dendrimer is partially acetylized; (3) modifying the G5-FI-Ac-NH2 by using lactobionic acid to obtain G5-FI-Ac-La with functions of targeting a hepatoma carcinoma cell and tracing by fluorescent. The preparation method provided by the invention is simple and has moderate reaction conditions. Furthermore, a used polymer is an environmental-friendly high polymer material and has a prospect of being industrialized. Thefunctional dendrimer material prepared by the invention is good in biocompatibility and can combine a specific target with the hepatoma carcinoma cell, so that the support can be used in load and targeting delivery of medicines, genes or molecule diagnosing probes.

Description

technical field [0001] The invention belongs to the field of preparation of macromolecule targeting nanocarriers, in particular to a preparation method of polyamidoamine dendritic macromolecular carriers targeting liver cancer cells. Background technique [0002] Chemotherapy, as one of the important means of cancer treatment, has been highly concerned for a long time. However, many anti-tumor drugs have problems such as low clinical efficacy and high toxicity and side effects, which have become the bottleneck in cancer drug treatment. Especially in the treatment of liver cancer, due to the inability to control the concentration of antineoplastic drugs on the focus of the liver, it will cause unnecessary damage to the patient's normal tissues and organs, and even threaten the patient's life. In recent years, the development of a liver-targeting nanocarrier to achieve specific delivery of drugs to the lesion of the liver, improving the therapeutic effect and reducing the dam...

Claims

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Application Information

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IPC IPC(8): A61K47/34A61P35/00
Inventor 史向阳郭睿
Owner DONGHUA UNIV
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