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pH-response tumor targeted cancer resistant medicine carrier and preparation method thereof

An anti-cancer drug and tumor-targeting technology, applied in the field of medicinal chemistry, can solve the problems of only 19.2% high and low drug loading rate, and achieve the effects of reducing drug resistance, easy operation, and high grafting rate

Active Publication Date: 2019-12-06
TAIYUAN UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

For example, Chen Qiuchi and others modified polyaspartic acid to obtain a targeting carrier capable of loading doxorubicin. However, the hydrophobic segment of this study used histidine, and the grafting rate reached only 17%, and the drug loading rate reached only 17%. 19.2%, low drug loading rate
Hima Bindu Ruttala et al. used aspartic acid, tyrosine and ethylene glycol to form a three-block copolymer carrier with pH response and redox effect, and loaded lonidamine and docetaxel at the same time, but still There is a problem of low drug loading rate, the highest is only 25%

Method used

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  • pH-response tumor targeted cancer resistant medicine carrier and preparation method thereof
  • pH-response tumor targeted cancer resistant medicine carrier and preparation method thereof
  • pH-response tumor targeted cancer resistant medicine carrier and preparation method thereof

Examples

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Embodiment 1

[0032] This example provides a pH-responsive and tumor-targeting dual-drug anticancer drug carrier and its preparation method. The preparation process is shown in the attached figure 1 As shown, the specific steps are as follows:

[0033] (1) Preparation of polyaspartic acid-tyrosine graft (PT): Weigh 0.36 g of tyrosine and add it into 20 mL of water for ultrasonic dispersion for 20 min, and another 0.8 g of polyaspartic acid is dissolved In 20 mL of water, add 0.192 g of carbodiimide (EDC) and 0.115 g of N-hydroxysuccinimide (NHS) and stir for 40 min, then add the previously reserved tyrosine aqueous dispersion, and stir for 24 h , filtered to remove unreacted tyrosine, the filtrate was dialyzed for three days with a 2000 Da dialysis bag, dried at 50 °C and ground to obtain PT powder;

[0034] (2) Preparation of ethylenediamine-polyaspartic acid-tyrosine (EPT): 80 mg of PT powder prepared in step (1) was dissolved in 30 mL of water, and 19.2 mg of EDC and 14 mg of NHS were a...

Embodiment 2

[0048] This example provides a pH-responsive and tumor-targeting dual-drug anticancer drug carrier and a preparation method thereof, and the specific steps are as follows:

[0049] (1) Preparation of polyaspartic acid-tyrosine graft (PT): Weigh 0.108 g of tyrosine and add it into 20 mL of water for ultrasonic dispersion for 20 min, and take another 0.8 g of polyaspartic acid to dissolve In 50 mL of water, add 0.038 g of carbodiimide (EDC) and 0.023 g of N-hydroxysuccinimide (NHS) and stir for 40 min, then add the prepared tyrosine aqueous dispersion, and stir for 24 h , filtered to remove unreacted tyrosine, the filtrate was dialyzed for three days with a 2000 Da dialysis bag, dried at 50 °C and ground to obtain PT powder;

[0050] (2) Preparation of ethylenediamine-polyaspartic acid-tyrosine (EPT): Dissolve 80 mg of PT powder prepared in step (1) in water, add 3.8 mg of EDC and 2.8 mg of NHS and stir to react for 40 min, add a drop of ethylenediamine (EDA) dropwise, stir for...

Embodiment 3

[0055] This example provides a pH-responsive and tumor-targeting dual-drug anticancer drug carrier and a preparation method thereof, and the specific steps are as follows:

[0056] (1) Preparation of polyaspartic acid-tyrosine graft (PT): Weigh 0.18 g of tyrosine and add it to 20 mL of water for ultrasonic dispersion for 20 min, and another 0.8 g of polyaspartic acid is dissolved In 20 mL of water, add 0.038 g of carbodiimide (EDC) and 0.023 g of N-hydroxysuccinimide (NHS) and stir for 40 min, then add the prepared tyrosine aqueous dispersion, and stir for 24 h , filtered to remove unreacted tyrosine, the filtrate was dialyzed for three days with a 2000 Da dialysis bag, dried at 50 °C and ground to obtain PT powder;

[0057] (2) Preparation of ethylenediamine-polyaspartic acid-tyrosine (EPT): Dissolve 80 mg of PT powder prepared in step (1) in water, add 3.8 mg of EDC and 2.8 mg of NHS and stir to react for 40 min, add a drop of ethylenediamine (EDA) dropwise, stir for 24 h, ...

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Abstract

The invention discloses a pH-response tumor targeted cancer resistant medicine carrier and a preparation method thereof. Polyaspartate (PASP) is used as a raw material, through an amidation reaction,tyrosine (Tyr) is grafted to a polyaspartate side chain, a polyaspartate-tyrosine grafted substance having amphipathicity is formed, and the grafted substance can be self-assembled in a water phase toform a nanometer micelle; and based on the nanometer micelle, through the amidation reaction, ethylenediamine is grafted to a polyaspartate side chain, the ethylenediamine is used as a bridge, hyaluronic acid (HA) is grafted to be used as a target ligand, and target action on cancer cells is given to the micelle. Curcumin is used as a hydrophobic medicine model, doxorubicin hydrochloride is usedas a hydrophilic medicine model, simultaneous loading on two medicines is realized, and besides, the medicine loading rate is high. The medicine carrier has the following advantages that the medicinecarrier can load two kinds of medicines simultaneously, is high in the medicine loading rate, has obvious pH response, has targeting properties on the cancer cells, and is good in biocompatibility, low in cost and simple and convenient to operate.

Description

technical field [0001] The invention relates to a pH-responsive and tumor-targeted anticancer drug carrier and a preparation method thereof, belonging to the field of medicinal chemistry. Background technique [0002] Cancer has always been one of the most frightening diseases that people fear, and since the side effects of drugs during chemotherapy can cause great damage to the human body, improving the specificity of drugs to cancer cells has become crucial. The pH value of the surrounding environment of cancer cells is lower than that of normal tissue cells, and there are overexpressed specific receptors on the surface of cancer cells, such as CD44 receptors specific to HA, which are not found in normal tissue cells. Drug resistance of cancer cells is also one of the most troublesome characteristics of people. [0003] Drug carriers have been widely studied in anticancer drugs since they were discovered. It can use its own pH sensitivity and targeting to reduce the toxic...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/34A61K47/36A61K31/704A61K31/12A61P35/00
CPCA61K9/1075A61K31/12A61K31/704A61K47/34A61K47/36A61P35/00A61K2300/00
Inventor 郭睿劼张杰李天杨侯文娟张耀东晏泓王慧芳牛宝龙
Owner TAIYUAN UNIV OF TECH
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