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A preparation method of alpha-tos-loaded dendrimer-wrapped gold nanoparticles

A technology of dendritic macromolecules and nano-gold particles, which can be used in medical preparations with non-active ingredients, pharmaceutical formulations, inorganic non-active ingredients, etc., and can solve the problem of large dosage of drugs.

Inactive Publication Date: 2014-10-15
DONGHUA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

To achieve this kind of drug treatment, not only the dosage of drugs is large, but also has a certain degree of blindness

Method used

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  • A preparation method of alpha-tos-loaded dendrimer-wrapped gold nanoparticles
  • A preparation method of alpha-tos-loaded dendrimer-wrapped gold nanoparticles
  • A preparation method of alpha-tos-loaded dendrimer-wrapped gold nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0067] (1) Dissolve alpha-TOS with a dry weight of 11.94 mg in 5 mL of DMSO, and add EDC with a dry weight of 4.31 mg dissolved in 2 mL of DMSO solution dropwise while stirring. After stirring and reacting for 3 hours, add Add 30 mg dry weight of NH dissolved in 5 mL DMSO solution 2 -PEG-COOH, where TOS and NH 2 -The molar ratio of PEG-COOH is 1.5:1, the molar ratio of EDC to TOS is 1:1, react for 1d, dialyze the resulting solution with cellulose dialysis membrane MWCO=1000 in phosphate buffer solution and distilled water for 3d, freeze Drying treatment gives TOS-PEG-COOH.

[0068] (2) 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 dropwise while stirring. 34.36 mg dry weight of NH in 5 mL DMSO solution 2 -PEG-COOH, where FA and NH 2 -The molar ratio of PEG-COOH is 1.5:1, the molar ratio of EDC to TOS is 1:1, react for 1d, dialyze the resulting solution with cellulose dialysis membrane MWCO=1000...

Embodiment 2

[0076] Analyze the stability of the material with the ultraviolet-visible absorption spectrogram, take the functionalized dendrimer material prepared in Example 1 of 0.5mg / mL, the solvent is distilled water, place 4°C, 37°C, 50°C Under the condition of temperature and pH=5, 6, 7, 8, measure its UV-Vis absorption spectrum, it can be seen from the spectrum that its peak shape is consistent and good, without shifting phenomenon, see Figure 5 , indicating that the material is adaptable to different temperature and pH conditions, and has good stability and dispersibility.

Embodiment 3

[0078] Use cell morphology to analyze the drug activity of the prepared material, weigh 1.0mgTOS, dissolve in 7535.8μL of 0.5% ethanol to prepare a solution with an alpha-TOS concentration of 250μM; weigh 4mg of the material in Example 1, dissolve in 1112.7μL of Prepare a solution with an alpha-TOS concentration of 250 μM in PBS buffer; weigh 3.75 mg of the material in Comparative Example 1, dissolve it in 1051.3 μL of PBS buffer to prepare a solution with a concentration of 25 μM; plant U87MG cells in a 96-well plate, 10 4 After incubation for 24 hours, add 10 μL PBS, 0.5% ethanol, alpha-TOS (250 μM), the material of Example 1 (25 μM, the concentration of alpha-TOS is 250 μM), and the material of Comparative Example 1 (25 μM, without containing alpha-TOS) and 90 μL medium, after incubation for 24 h, the material was discarded, and the cell image was taken by phase contrast microscope, the results showed that the free alpha-TOS and {(Au 0 )200 -G5.NHAc-FI-(PEG-TOS)-(PEG-FA)}...

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Abstract

The invention relates to a preparation method for alpha-TOS-loaded and dendrimer-wrapped gold nanoparticles. The method comprises the following steps: (1) adding EDC and an NH2-PEG-COOH solution into an alpha-TOS solution and reacting to obtain TOS-PEG-COOH; (2) adding the EDC and the NH2-PEG-COOH solution into folic acid and reacting to obtain FA-PEG-COOH; (3) adding a poly amidoamine dendrimer solution into an FI solution and reacting to obtain G5.NH2-FI; (4) adding the TOS-PEG-COOH and FA-PEG-COOH solution into the EDC for activation, adding into the G5.NH2-F1 water solution, and reacting to obtain a dendrimer solution; and (5) adding chloroauric acid, NaBH4, N(C2H5)3 and acetic anhydride into the above solution, and reacting to obtain the gold nanoparticles. The method is simple in preparation process, and is easy to implement.

Description

technical field [0001] The invention belongs to the field of preparation of dendrimers, in particular to a method for preparing alpha-TOS-loaded dendrimer-wrapped nano gold particles. Background technique [0002] alpha-tocopherol succinate (alpha-TOS), a vitamin E derivative, induces apoptosis in cancer cells, triggers massive apoptosis of cancer cells in various types of tumors, inhibits cell growth cycle, and disrupts tumor growth Essential autocrine signaling pathway. In its specific structure, the succinyl group triggers cancer cell apoptosis by inducing the generation of reactive oxygen species. In traditional drug therapy, due to the non-specificity of drugs, it is inevitable to cause damage to normal cells and tissues. Secondly, the drug toxicity is increased by increasing the dose of the drug, and the toxic side effects directly produced by the drug are used to destroy rapidly differentiated cells. To realize this type of drug treatment, not only the drug dosage ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/48A61K47/02A61K31/355A61K49/04A61P35/00
Inventor 史向阳朱静怡
Owner DONGHUA UNIV
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