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Biodegradable unimolecular multi-support-arm polymer as well as preparation method f and application thereof

A polymer and single-molecule technology, applied in the field of medicine, can solve problems such as poor water solubility and stability, limited effective treatment of tumors, and large toxic and side effects

Active Publication Date: 2013-06-26
SHENZHEN INST OF ADVANCED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chemotherapy is a common method to treat cancer, but traditional chemotherapy drugs have poor water solubility and stability, and have high toxic and side effects, which limit the effective treatment of tumors.

Method used

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  • Biodegradable unimolecular multi-support-arm polymer as well as preparation method f and application thereof
  • Biodegradable unimolecular multi-support-arm polymer as well as preparation method f and application thereof
  • Biodegradable unimolecular multi-support-arm polymer as well as preparation method f and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0061] Please refer to image 3 and Figure 5 , the preparation method of the above-mentioned biodegradable single-molecule multi-arm polymer, comprising the following steps:

[0062] Step S110, adding diethylenetriaminepentaacetic anhydride and 4-dimethylaminopyridine into dimethylformamide containing hyperbranched polyester-polycaprolactone, reacting for 12h to 24h, settling with ether, vacuum After drying, hyperbranched polyester-polycaprolactone-diethylenetriaminepentaacetic acid is obtained.

[0063] The molar ratio of the hydroxyl unit of hyperbranched polyester-polycaprolactone, diethylenetriaminepentaacetic anhydride and 4-dimethylaminopyridine is 1:10-20:0.2.

[0064] Hyperbranched polyester-polycaprolactone is prepared by the following steps:

[0065] Under vacuum conditions, react hyperbranched polyester, caprolactone and stannous octoate at a temperature of 125°C to 135°C for 8h to 12h, and then settle with cold ether to obtain hyperbranched polyester-polycaprol...

Embodiment 1

[0115] 400mg H40, 1500mg caprolactone and 1.5mg stannous octoate (Sn(Oct) 2 ) into a completely dry silanized polymerization tube with a magnetic stirring bar. The polymerization tube was purged with nitrogen three times before use, then sealed under vacuum, and stirred in an oil bath at 135°C for 8 h. Then dissolve the reacted mixture in chloroform, then quickly add a sufficient amount of cold ether for precipitation, collect the filter residue after filtration, dry the filter residue at room temperature and vacuum for two days to obtain H40-PCL (the hydroxyl group of H40 and the mole of PCL The ratio is 1:15).

[0116] Add 492.91mg of DTPA and 2mg of 4-dimethylaminopyridine (DMAP) into dimethylformamide (DMF) containing 200mg of H40-PCL. After 12 hours of reaction, settle with ether to obtain H40-PCL-DTPA.

[0117] Add 34.29 mg 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDC) and 10.32 mg N-hydroxysuccinimide (NHS) to DMF containing 100 mg H40-PCL-DTPA , after activatio...

Embodiment 2

[0121] 200mg H40, 1000mg caprolactone and 1mg stannous octoate (Sn(Oct) 2 ) into a completely dry silanized polymerization tube with a magnetic stirring bar, the polymerization tube was purged with nitrogen three times before use, then sealed under vacuum, and stirred in an oil bath at 125 °C for 12 h. Then dissolve the reacted mixture in chloroform, then quickly add a sufficient amount of cold ether for precipitation, collect the filter residue after filtration, dry the filter residue at room temperature and vacuum for two days to obtain H40-PCL (the hydroxyl group of H40 and the mole of PCL The ratio is 1:20).

[0122] Add 328.6mg of DTPA and 2mg of 4-dimethylaminopyridine (DMAP) into dimethylformamide (DMF) containing 200mg of H40-PCL. After 24 hours of reaction, settle with ether to obtain H40-PCL-DTPA.

[0123] Add 27.5 mg 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (EDC) and 8.26 mg N-hydroxysuccinimide (NHS) to DMF containing 100 mg H40-PCL-DTPA, After activation fo...

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Abstract

The invention discloses a biodegradable unimolecular multi-support-arm polymer. The polymer comprises a hydrophobic core, a hydrophobic core shell layer and a hydrophilic outer shell layer, wherein the hydrophobic core is hyperbranched polyester, the hydrophobic core shell layer is polycaprolactone, and the hydrophilic outer shell layer is polyethylene glycol. The biodegradable unimolecular multi-support-arm polymer is applied to diagnostic integration nanometer medicine carrying polymer as a carrier, gadolinium and cisplatin can be wrapped into a molecular carrier hydrophobic section, and the water solubility of the cisplatin can be improved on the basis of the strong hydrophilcity of polyethylene glycol, so that the immunogenicity is reduced, and the circulation time of the gadolinium and cisplatin in the blood can be prolonged. Compared with the conventional magnetic resonance imaging (MRI) contrast medium and conventional chemotherapeutics, the diagnostic integration nanometer medicine carrying polymer can circulate in the blood for a long time, has small toxic or side effects and can wrap the gadolinium and the cisplatin at the same time, so that diagonistic integration is realized. The invention further discloses a preparation method and application of the biodegradable unimolecular multi-support arm polymer.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a biodegradable single-molecule multi-arm polymer and its preparation method and application. Background technique [0002] Cancer is a general term for a large class of malignant tumors, which seriously endanger human life and health. Therefore, accurate diagnosis and effective treatment of cancer have become an urgent need. [0003] The development of nanotechnology has provided new means for the treatment of cancer. Nanoparticles have the advantages of quantum size effect, large specific surface area, and easy surface modification, and have many advantages in the application of drug delivery. Nanocarriers can target the release of anticancer drugs to the lesion and increase the local drug concentration at the lesion, which can not only significantly improve the curative effect, but also reduce the damage of anticancer drugs to normal tissues. [0004] Magnetic resonance ima...

Claims

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Application Information

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IPC IPC(8): C08G81/00C08G63/91C08G65/48A61K47/48A61K33/24A61K9/19A61K49/00A61P35/00
Inventor 蔡林涛邓吉喆魏伟李明星王亚楠马轶凡
Owner SHENZHEN INST OF ADVANCED TECH
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