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Active targeting star polymer carrier with physiological environment response function and preparation method thereof

A star-shaped polymer and physiological environment technology, which can be applied in the direction of drug combination, anti-tumor drugs, etc., can solve the problems of inability to achieve targeted therapeutic properties of tumor therapy, carrier polymers that are not star-shaped polymers, and inability to achieve carrier stability, etc. , to achieve the effect of easy-to-obtain raw materials, low-cost raw materials, and mature and simple methods

Inactive Publication Date: 2016-05-18
SOUTHWEST JIAOTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] At present, Chinese patent applications 200910273157.0 and 201110004873.6 disclose the preparation of copolymers containing disulfide bonds, but do not involve the targeting of the carrier, and the carrier polymer is not a star polymer
According to the previous analysis, these polymer materials cannot achieve the stability of the carrier in the blood circulation, nor can it achieve the targeted therapeutic effect on tumor treatment.

Method used

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  • Active targeting star polymer carrier with physiological environment response function and preparation method thereof
  • Active targeting star polymer carrier with physiological environment response function and preparation method thereof
  • Active targeting star polymer carrier with physiological environment response function and preparation method thereof

Examples

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preparation example Construction

[0020] (1) Preparation of star-shaped polycaprolactone (synthetic route such as figure 1 shown): stannous chloride is used as the catalyst, and the polyol is the nucleus of the star structure. Usually, for 1 equivalent of pentaerythritol, put 70 equivalents of caprolactone and 1% of the total mass of stannous chloride to synthesize star-shaped polycaprolactone with a theoretical molecular weight of 8000. After evacuating for 3 hours, ring-opening polymerization was carried out at a temperature of 150 degrees, and the reaction was carried out for 6 hours. After the product is cooled, it is dissolved in dichloromethane, precipitated in a large amount of ice ethanol, filtered with suction, and the product is vacuum-dried to obtain four-arm polycaprolactone.

[0021] In the above preparation process, the molecule used as the core of the star structure can be a kind of polyhydric alcohol such as glycerol, pentaerythritol and dipentaerythritol, which respectively form three-arm, fo...

Embodiment 1

[0030]Take by weighing 0.17 gram of pentaerythritol, 10 gram of caprolactone and 0.1 gram of tin protochloride, place in a one-necked bottle, after vacuumizing for 3 hours, ring-opening polymerization under the condition of temperature 150 degrees, take out after 6 hours, treat that the product cools from melting to In solid state, add 5 mL of dichloromethane to dissolve, drop into 250 mL of ice ethanol for precipitation, filter with suction, and dry in vacuum to obtain four-arm polycaprolactone.

[0031] Weigh 2 grams of dithiodipropionic acid, add 20 grams of acetyl chloride, reflux reaction at a temperature of 65 degrees, stir magnetically for 4 hours, remove most of the organic solvent by rotary evaporation, precipitate with glacial ether, filter with suction, and dry in vacuum, namely have to.

[0032] Weigh 1 part of dithiodipropionic anhydride and 5.2 grams of the above-mentioned star-shaped polycaprolactone, add them to 70 mL of DMF, catalyst DMAP 0.3176 grams, triethy...

Embodiment 2

[0036] In this example, the pentaerythritol in Example 1 was replaced with dipentaerythritol, and the ratio of dipentaerythritol to caprolactone was 1:105. Other implementation methods in Example 1 were used to obtain a six-armed star-shaped copolymer.

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Abstract

The invention relates to an active targeting star polymer carrier with a physiological environment response function and a preparation method thereof. The carrier has the function of specific targeting to tumour cells and can be quickly degraded by responding to the reduction environment in the cells; the carrier is an amphiphilic star polymer; the hydrophilic segment is polyethylene glycol grafted with an active targeting ligand at the end; the hydrophobic segment is degradable absorbable star polycaprolactone; the hydrophilic segment and the hydrophobic segment are chemically connected through disulfide bonds with physiological environment response function to form the functionalized star segmented copolymer. The polymer can be used as a drug carrier, forms nanometer particles carrying drugs in water through self assembly, and can be used for targeting treatment of tumours.

Description

technical field [0001] The invention relates to a preparation method of an active targeting star-shaped polymer carrier with a physiological environment response function, and belongs to the technical field of drug controlled release. Background technique [0002] The side effects of anticancer drugs seriously hinder their clinical application. In order to solve this problem, researchers currently use nanoparticles as drug carriers, such as nanomicelles to carry drugs. The main basis for this application is that polymer micelles carry anticancer drugs through endocytosis of cells. Entering cells, bypassing P-glycoprotein, avoiding the outflow of drugs through extracellular secretion, so that drugs can be absorbed in large quantities by tumor cells with multi-drug resistance, improving the therapeutic effect and greatly reducing toxic and side effects. [0003] However, polymer micelles still face many challenges in the application of anticancer drugs. It is expected that th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G81/00C08G63/91C08G65/48A61K47/34A61P35/00
Inventor 周绍兵史春丽郭星王毅
Owner SOUTHWEST JIAOTONG UNIV
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