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Cholesterol-low molecular weight heparin nano preparation for anti-tumor and anti-metastasis therapy and preparation method thereof

A low-molecular-weight heparin and cholesterol technology, which is applied in the field of nanomicelles encapsulating antitumor drugs and their preparation, can solve the problems of limited scope and efficiency of chemotherapy, high toxicity of chemotherapy drugs, leukocyte and thrombocytopenia, etc.

Inactive Publication Date: 2018-08-28
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the range and efficiency of chemotherapy is extremely limited
Due to the high toxicity of chemotherapy drugs, long-term use will cause serious adverse reactions such as irreversible cardiomyopathy, bone marrow suppression, leukopenia and thrombocytopenia

Method used

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  • Cholesterol-low molecular weight heparin nano preparation for anti-tumor and anti-metastasis therapy and preparation method thereof
  • Cholesterol-low molecular weight heparin nano preparation for anti-tumor and anti-metastasis therapy and preparation method thereof
  • Cholesterol-low molecular weight heparin nano preparation for anti-tumor and anti-metastasis therapy and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0026] 2.3g of cholesterol chloroformate (Chol, 5mmol) was dissolved in 50mL of anhydrous dichloromethane, and the above solution was slowly added dropwise to 6.7mL (100mmol) of ethylenediamine and 0.7mL (5mmol) of ) Triethylamine mixed solution, continue to react for 10h. After the reaction, the precipitate was removed by filtration, the filtrate was washed three times with deionized water, dried by adding anhydrous magnesium sulfate and filtered, and the filtrate was dried under reduced pressure overnight to obtain a white solid cholesterol-ethylenediamine whose connecting arm was ethylenediamine.

Embodiment 2

[0028] 2.3g of cholesterol chloroformate (Chol, 5mmol) was dissolved in 50mL of anhydrous dichloromethane, and the above solution was slowly added dropwise to 100mmol of cystamine dihydrochloride and 0.7mL (5mmol) In the mixed solution of triethylamine, the reaction was continued for 10 h. After the reaction, the precipitate was removed by filtration, the filtrate was washed three times with deionized water, dried by adding anhydrous magnesium sulfate and filtered, and the filtrate was dried under reduced pressure overnight to obtain a white solid cholesterol-cystamine whose linking arm was cystamine.

Embodiment 3

[0030] Accurately weigh 100 mg (0.25 mmol) of low molecular weight heparin with a molecular weight of 1000 into a round bottom flask, add 10 mL of formamide, heat in an oil bath at 50°C with magnetic stirring to dissolve, add 143.8 mg (0.8 mmol) of carbon dioxide after cooling to room temperature Imine hydrochloride (EDC) and 101.6mg (0.8mmol) 1-hydroxybenzotriazole (HOBT) were stirred for 15min, then cholesterol-ethylenediamine or cholesterol-cystamine or (0.05mmol) was added and stirred at room temperature for 24h. Transfer to a dialysis bag for dialysis in water for 48 hours, and the dialysis medium is DMF and distilled water in turn. Freeze-drying to obtain white loose solid powder is cholesterol-low molecular weight heparin graft copolymer, and the reaction steps are as follows: figure 2 . The degree of cholesterol substitution was determined to be 20.0% by ferric ammonium sulfate colorimetric method.

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Abstract

The invention relates to a cholesterol-low molecular weight heparin nano preparation loaded with anti-tumor drugs for anti-tumor and anti-metastasis therapy and a preparation method thereof. Specifically, the nano preparation is characterized in that cholesterol with excellent biocompatibility serves as a hydrophobic fragment and a hydrophobic drug reservoir for encapsulation of an anti-tumor drug, hydrophilic low molecular weight heparin with anti-metastasis activity serves as a shell so as to prepare the novel nano preparation for preventing postoperative recurrence, and therefore tumor cells can be killed, and meanwhile, the effect of inhibiting tumor cell metastasis can be achieved. The nano preparation has the advantages that the drug loading capacity is within 5-20wt%, the prepared nano preparation has an injectable property, administration is realized through tail intravenous injection, and therefore the anti-tumor effect of the drug can be improved, and meanwhile, the anti-metastasis activity of the low molecular weight heparin can be exerted.

Description

technical field [0001] The invention belongs to the technical field of medicines, and specifically relates to a nano-micelle with cholesterol as a hydrophobic inner core, low-molecular-weight heparin as a hydrophilic outer shell and anti-tumor drugs and a preparation method thereof. Background technique [0002] Tumor metastasis has become one of the important causes of death in cancer patients. Tumor cell metastasis is a complex multi-step cascade process, which generally includes the following consecutive steps: the initial primary tumor cells obtain genetic phenotype changes, acquire metastatic potential, detach from the tumor tissue, and pass through the vascular wall barrier. Finally, extravasation enters adjacent blood vessels, invades other tissues and organs with the help of blood circulation, and then forms new metastases in secondary tissues and organs. Blocking any of the above steps may inhibit tumor metastasis. At present, the use of novel nano-drug delivery s...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/36A61K47/28A61K31/727A61K31/704A61P35/00A61P35/04
CPCA61K9/0019A61K9/1075A61K31/704A61K31/727A61K47/28A61K47/36A61P35/00A61P35/04A61K2300/00
Inventor 慈天元柯学曹丁凌格李锦冯淑君
Owner CHINA PHARM UNIV
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