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Nano-drug and synthesis method thereof

A synthesis method and nano-drug technology, applied in the direction of drug combination, medical formula, genetic material components, etc., can solve the problems of cell membrane instability, non-cancerous tissue cytotoxicity, etc., achieve good therapeutic effect, avoid normal tissue lesions, and prolong half-life Effect

Active Publication Date: 2018-12-18
HENAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, these strong cationic carriers often destabilize cell membranes and cause severe cytotoxicity to non-cancerous tissues due to the high positive charge on the particle surface

Method used

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preparation example Construction

[0040] The synthetic method of nano medicine, comprises the steps:

[0041] (1) Synthesis of DxDPA monomer

[0042] 2,2'-dipicolylamine reacted with α,α'-dichloro-p-xylene to obtain DxDPA monomer. Specifically, both 2,2'-dipicolylamine and α,α'-dichloro-p-xylene were dissolved in methyl chloride and reacted for 24-28 hours under inert gas conditions to obtain DxDPA monomer.

[0043] Optionally, the molar ratio of 2,2'-dipicolylamine to α,α'-dichloro-p-xylene is 1:(1.5-2.5).

[0044] The specific steps are as follows: 2,2'-dipicolylamine (DPA) (8mmol) and α,α'-dichloro-p-xylene (Dx) (16mmol) were dissolved in dichloromethane or chloroform, and then added Anhydrous K 2 CO 3 (40mmol) or anhydrous sodium sulfate to remove water. And stirred at room temperature and inert gas (nitrogen as an option) for 24 hours to obtain DxDPA monomer.

[0045]

[0046] Since the DxDPA monomer solution contains certain impurities such as reactants and organic solvents, the sample is extrac...

Embodiment 1

[0067] The synthetic method of nano medicine, comprises the steps:

[0068] (1) Synthesis of DxDPA monomer: 2,2'-dipicolylamine reacts with α,α'-dichloro-p-xylene to obtain DxDPA monomer.

[0069] (2) Synthesis of DxDPA-Cys polymer: react cystamine dihydrochloride and triethylamine to obtain cystamine, then add monomer to obtain DxDPA-Cys polymer.

[0070] (3) Synthesis of HA-SS-DPA polymer: react hyaluronic acid, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and N-hydroxysuccinimide Then add the mixed solution of triethylamine and DxDPA-Cys polymer and react to obtain HA-SS-DPA polymer.

[0071] (4) Synthesis of HA-SS-DPA(Zn) / siRNA nanomedicine: Dissolve HA-SS-DPA polymer in buffer solution and add chelating agent to react to obtain HA-SS-DPA(Zn), and HA-SS- DPA(Zn) is mixed with small fragments of interfering RNA and incubated under the condition of 55-65°C to obtain nano-medicine.

Embodiment 2

[0073] The synthetic method of nano medicine, comprises the steps:

[0074] (1) Synthesis of DxDPA monomer: 2,2'-dipicolylamine and α,α'-dichloro-p-xylene with a molar ratio of 1:1.5 or 1:2.5 or 1:2 are dissolved in chlorine DxDPA monomer was obtained by reacting in methane for 24h or 26h or 28h under the condition of inert gas.

[0075] (2) Synthesis of DxDPA-Cys polymer: First, dissolve cystamine dihydrochloride and triethylamine in dimethyl sulfoxide with a molar ratio of 1:2 or 1:4 or 1:3 in an inert gas Under the conditions of reaction for more than 1.5h to obtain the first mixed solution, then dissolve the DxDPA monomer in dimethyl sulfoxide and add it to the first mixed solution, and react at 55°C or 60°C or 65°C for 12h or 14h or DxDPA-Cys polymer was obtained in 16h; wherein, the molar ratio of cystamine dihydrochloride to DxDPA monomer was 1:0.2 or 1:0.3 or 1:0.4.

[0076] (3) Synthesis of HA-SS-DPA polymer: hyaluronic acid with a molar ratio of 1:4:4 or 1:5:5 or 1...

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Abstract

The invention provides a nano-drug and a synthesis method thereof and belongs to the technical field of drug synthesis. The synthesis method of the nano-drug comprises the following steps: (1) taking2,2'-bipyridinemethylamine and alpha,alpha'-dichloro para-xylene to react to obtain a monomer; (2) taking cystamine dihydrochloride and triethylamine to react to obtain cystamine, and then adding themonomer to obtain a first polymer; (3) taking hyaluronic acid, 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and N-hydroxysuccinimide to react, and then adding a mixed solution of the triethylamine and the first polymer; then reacting to obtain a second polymer; (4) after dissolving the second polymer into a buffering solution, adding a chelating agent containing Zn<+> and reactingto obtain a third polymer; mixing the third polymer and small fragment interfered RNA (Ribonucleic Acid) and incubating under the condition of 55 to 65 DEG C to obtain the nano-drug. The nano-drug obtained by the synthesis method has a better treatment effect on malignant glioblastoma multiforme.

Description

technical field [0001] The invention relates to the technical field of drug synthesis, in particular to a nano-medicine and a synthesis method thereof. Background technique [0002] RNA interference (RNAi), which uses small interfering RNAs to inhibit the activity of specific genes, is a new therapeutic option for treating cancer. However, the delivery of siRNA molecules remains one of the greatest challenges in the clinical and practical application of emerging technologies. To date, the most studied delivery systems for siRNAs in cancer therapeutic strategies include cationic polymers, cationic lipids, and cationic inorganic nanoparticles. These cationic materials are able to condense anionic siRNAs into nanoparticles through charge interactions and protect siRNAs from RNase enzymatic degradation after in vivo circulation. [0003] However, these strong cationic carriers often destabilize cell membranes and cause severe cytotoxicity to noncancerous tissues due to the hig...

Claims

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Application Information

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IPC IPC(8): A61K47/36A61K31/713A61K48/00A61P35/00C08B37/08
CPCA61K31/713A61K47/36A61P35/00C08B37/0072
Inventor 师冰洋杨志朋郑蒙阮卫民
Owner HENAN UNIVERSITY
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