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Amphiphilic micelle of carrier with anti-tumor and anti-metastasis activity

An anti-metastasis and anti-tumor technology, applied in the direction of anti-tumor drugs, organic active ingredients, medical preparations of non-active ingredients, etc., can solve the problems of clinical use restrictions, achieve good biocompatibility and degradability, enhance The effect of anti-tumor effect

Inactive Publication Date: 2016-03-23
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the existence of some toxic and side effects, the clinical application is greatly limited.

Method used

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  • Amphiphilic micelle of carrier with anti-tumor and anti-metastasis activity
  • Amphiphilic micelle of carrier with anti-tumor and anti-metastasis activity
  • Amphiphilic micelle of carrier with anti-tumor and anti-metastasis activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031]Synthesis of embodiment 1 connecting fragment (6-aminocaproic acid ethyl ester)

[0032] Add 30ml of absolute ethanol to a 100ml three-neck flask, cool in an ice bath to below -10°C, slowly add 5ml of thionyl chloride dropwise, and keep the temperature below 0°C. After dropping, stir for 10 minutes, add 4.37g of 6-aminocaproic acid, heat up to about 70°C and reflux for 8 hours. Excess thionyl chloride and ethanol were distilled off under reduced pressure, and the residue was solidified. Recrystallized with methanol:petroleum ether (V:V=5:1) to obtain a white solid, namely ethyl 6-aminocaproate.

Embodiment 2

[0033] Example 2 Hydrazination of Linked Fragments

[0034] Accurately weigh 195.7mg of ethyl 6-aminocaproate in a 50ml round-bottomed flask, dissolve in a small amount of ethanol, then add 80μl of hydrazine hydrate, heat up to 70°C, reflux for 8 hours in the dark, monitor by TLC (developing agent dichloro Methane:methanol=1:1), after the reaction was complete, the crude product was obtained by rotary evaporation. The pure product was separated by silica gel column.

Embodiment 3

[0035] Embodiment 3 linking fragments-the synthesis of doxorubicin

[0036] Accurately weigh 94.8 mg of hydrazide in a 50 ml round bottom flask, dissolve it in a small amount of ethanol, then add 271.8 mg of doxorubicin dehydrochloride and a small amount of trifluoroacetic acid. The reaction was carried out in the dark for 24 hours at room temperature, and the product was obtained by rotary evaporation.

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Abstract

The invention relates to amphiphilic micelle of a carrier with anti-tumor and anti-metastasis activity. According to the micelle, a hydrophilic polysaccharide material with the anti-metastasis activity and a hydrophobic chemotherapy drug with anti-tumor activity are coupled, and micelle nanoparticles are formed in a water medium through self-assembling. The nanoparticles can effectively convey the anti-tumor drug to tumors through the EPR effect, the heparin component in the carrier can restrain metastasis of tumor cells, and a better tumor treatment effect is shown.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an amphiphilic carrier with anti-tumor and anti-transfer activities and a preparation method thereof. Background technique [0002] Malignant tumors are one of the most threatening diseases to human health in the world today. Although surgery, chemotherapy, and radiotherapy can control some cancer conditions, the survival rate of patients is still very low. Statistics show that within 5 years after surgical resection, 50% of patients with rectal cancer have liver metastasis, 60%-70% of patients with liver cancer have metastasis within 5 years after radical resection, and 60% of patients with cervical cancer have metastases. Pelvic metastases, 60%-70% of ovarian cancer patients also have multiple metastases. Clinical data over the past half a century shows that about 80% of tumor patients are mainly caused by local recurrence and distant metastasis. For more than a hundr...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/48A61K31/704A61P35/04
CPCA61K9/1075A61K31/704
Inventor 何勤梅凌张志荣
Owner SICHUAN UNIV
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