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Nano-carriers and nano-preparations of anti-tumor drugs that can co-load anti-tumor drugs and nucleic acid drugs

An anti-tumor drug and nano-carrier technology, applied in the field of nano-formulations, can solve problems such as large viscosity and affect mitochondrial efficiency, and achieve the effects of reducing cytotoxicity, improving release, and overcoming tumor multidrug resistance.

Active Publication Date: 2020-05-12
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the environment of mitochondria is translucent colloidal cytoplasm, which contains a variety of organelles, proteins, polysaccharides, etc., and has a relatively high viscosity. Nanocarriers with surface-modified triphenylphosphine need to overcome many obstacles to reach mitochondria, which may cause Affects the efficiency of mitochondrial targeting

Method used

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  • Nano-carriers and nano-preparations of anti-tumor drugs that can co-load anti-tumor drugs and nucleic acid drugs
  • Nano-carriers and nano-preparations of anti-tumor drugs that can co-load anti-tumor drugs and nucleic acid drugs
  • Nano-carriers and nano-preparations of anti-tumor drugs that can co-load anti-tumor drugs and nucleic acid drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Embodiment 1: synthetic N, N, N-trimethylcystamine trifluoroacetate

[0065] 1) Weigh 200 mg of cystamine dihydrochloride (referred to as cystamine) and dissolve in 10 ml of methanol, and add 386 μl of triethylamine; dissolve 192.5 mg of di-tert-butyl dicarbonate (BOC anhydride) in 2 ml of methanol, gradually Add it dropwise to methanol solution of cystamine dihydrochloride, stir at room temperature for 30 minutes, and evaporate methanol to dryness by rotary evaporation. Continue to add 50ml of sodium dihydrogen phosphate solution (NaH 2 PO 4 , 1M), washed twice with ether to remove the product that both ends are connected to BOC anhydride, using NaOH (1M) to adjust the pH of the solution to 9, extracting with ethyl acetate to obtain the cystamine protected by BOC at one end, rotary steaming The ethyl acetate layer was dried to give a white product (designated cystamine-BOC).

[0066] 2) Weigh 50 mg of the above product, dissolve it in 1 ml of acetonitrile, add 64.6 ...

Embodiment 2

[0071] Embodiment 2: Synthetic N, N, N-trimethylcystamine iodide salt

[0072] (1) Dissolve 500 mg of cystamine dihydrochloride (referred to as cystamine) in 10 ml of methanol, and add 965 μl of triethylamine; react for 30 minutes, dissolve 223 mg of benzyl chloroformate (CBZ) in 2 ml of methanol, Add it dropwise to methanol solution of cystamine dihydrochloride, stir at room temperature, observe the reaction progress by thin-layer chromatography, and evaporate the methanol to dryness after the raw material point disappears. Continue to add hydrochloric acid solution (HCl, 1M), wash twice with ether to remove the product with CBZ anhydride attached to both ends, use NaOH (1M) to adjust the pH of the solution to 9, and extract with ethyl acetate to obtain CBZ protected at one end. Cystamine, and the ethyl acetate layer was evaporated to dryness by rotary evaporation to obtain a white product (referred to as cystamine-CBZ).

[0073] (2) Weigh cystamine-CBZ 39mg, add 64.6mg K 2...

Embodiment 3

[0075] Embodiment 3: synthetic N, N, N-trimethylcystamine chloride salt

[0076] In this example, 1 ml of saturated ethyl acetate (3M) hydrochloric acid was added to remove BOC, reacted at room temperature for 30 minutes, and the solvent was spin-dried, and the rest of the steps were the same as in Example 1 to prepare solid N,N,N-trimethylcystamine chloride Salt.

[0077] The result shows: carry out mass spectrometric characterization for N,N,N-trimethylcystamine iodonium salt-BOC and N,N,N-trimethylcystamine chloride salt in embodiment 3, such as Figure 3-4 shown. Molecular ion peak of N,N,N-trimethylcystamine iodide-BOC ([M+H] + ) is 295.17, and the molecular ion peak of N,N,N-trimethylcystamine chloride ([M+H] + ) is 195.10, which proves that N,N,N-trimethylcystamine chloride has been successfully synthesized.

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Abstract

The invention relates to a nanometer carrier capable of carrying an antitumor drug and a nucleic acid drug and an antitumor drug nanometer preparation. The nanometer carrier takes hydrophilic macromolecule as a framework material, and is formed by crosslinking the hydrophilic macromolecule and a polyamine compound, and a GSH stimulate respondence cationic compound modifies the surface of the nanometer carrier. The nanometer carrier can carry the antitumor drug and the nucleic acid drug, and the further synthesized nanometer preparation has double responsiveness in tumor cells, can respectively release the nucleic acid drug and the antitumor drug, and can obviously improve the anti-tumor effect of the drugs.

Description

technical field [0001] The invention relates to the field of nano-preparation, in particular to a nano-carrier capable of co-carrying anti-tumor drugs and nucleic acid drugs and a nano-preparation of anti-tumor drugs. Background technique [0002] In the clinical treatment of tumors, chemotherapy occupies a very important position, but its efficacy has been severely restricted by the toxic side effects of drugs in vivo and tumor drug resistance. Tumor multidrug resistance (MDR) refers to the phenomenon of cross-resistance of tumor cells to multiple structurally unrelated chemotherapeutic drugs. Studies have found that the MDR mechanism of tumor cells is very complex, and changes in the tumor microenvironment can cause abnormal cell apoptosis, which has also become an important factor in the occurrence and development of tumor drug resistance. It can be seen that the abnormality of tumor cell apoptosis pathway plays an important role in the development of tumor drug resistan...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/60A61K47/58A61K47/61A61K31/7088A61K47/18A61K47/32A61K47/36A61K31/704A61K38/14A61K31/4745A61K31/337A61P35/00B82Y5/00
CPCA61K31/337A61K31/4745A61K31/704A61K31/7088A61K38/14A61K47/18A61K47/32A61K47/36B82Y5/00A61K2300/00
Inventor 韩旻刘惠娜林梦婷郭宁宁郭望葳王田田皇甫铭一陈捷键高建青
Owner ZHEJIANG UNIV
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