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Polyglycol block modified polyhexanolactone and its preparing method

A kind of polyethylene glycol, polycaprolactone technology, applied in the field of polycaprolactone

Inactive Publication Date: 2003-06-25
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, PEG / PCL block copolymers only have the above two two- and three-block structures, and the copolymerization reaction of mono- or dihydroxyl-terminated PEG and caprolactone is used, but there is no information about BAB-type three-block copolymers. See the report

Method used

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  • Polyglycol block modified polyhexanolactone and its preparing method
  • Polyglycol block modified polyhexanolactone and its preparing method
  • Polyglycol block modified polyhexanolactone and its preparing method

Examples

Experimental program
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Effect test

Embodiment 1

[0027] Add 10g of bishydroxy end group PCL with a relative molecular weight of 2000 and 10-20mL of ethyl acetate into a round-bottomed flask, heat to dissolve and then cool down to 40°C. The feed ratio (molar ratio) of toluene diisocyanate / PCL is 2-2.2 Add toluene diisocyanate and 3-5 mL of ethyl acetate, slowly raise the temperature to 70-90°C and react for 2-5 hours, then add PEG with a relative molecular weight of 2000 and ethyl acetate 10 which are equimolar or slightly excess to the remaining isocyanate groups ~20mL, continue to react for 2~5h, then add the resulting block copolymer solution to 10~30 parts of ether at 4~10°C for precipitation, centrifugal separation or vacuum filtration to obtain polyethylene glycol block modified Polycaprolactone amphiphilic triblock copolymer. The particle size distribution of the micelles (the concentration of the block copolymer is 0.5%) formed by self-assembly of this polyethylene glycol block-modified polycaprolactone in water is as...

Embodiment 2

[0029]The device and operation are the same as in Example 1. Add 10 g of bishydroxy PCL with a relative molecular weight of 4000 and 10-20 mL of ethyl acetate into a round-bottomed flask, heat and dissolve, then cool down to 40 ° C, and use toluene diisocyanate / PCL as 2-2.2 Feed ratio (molar ratio) Add 3-5mL of toluene diisocyanate and ethyl acetate, slowly raise the temperature to 70-90°C and react for 2-5h, then add polystyrene with a relative molecular weight of 2000 that is equimolar or slightly excess with the remaining isocyanate groups. Ethylene glycol monomethyl ether and ethyl acetate 10 ~ 20mL, continue to react for 2 ~ 5h, then add the resulting block copolymer solution to 10 ~ 30 parts of 4 ~ 10 ℃ ether for precipitation, centrifugal separation or decompression Suction filtration obtains poly(ethylene glycol) block modified polycaprolactone amphiphilic tri-block copolymer.

Embodiment 3

[0031] The device and operation are the same as in Example 1. Add 10 g of dihydroxy PCL with a relative molecular weight of 2000 and 10 to 20 mL of ethyl acetate into a round bottom flask, heat to dissolve and then cool down to 40 ° C. Feeding ratio (molar ratio) Add 3-5mL of toluene diisocyanate and ethyl acetate, slowly raise the temperature to 70-90°C and react for 2-5h, and then add hydroxy End group ethylene oxide and propylene oxide block copolymer and ethyl acetate 10-20mL, continue to react for 2-5h, then add the resulting block copolymer solution to 10-30 parts of ether at 4-10°C The polycaprolactone amphiphilic three-block copolymer of poly(ethylene glycol) block modification is obtained by precipitation in medium, centrifugation or suction filtration under reduced pressure.

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Abstract

The present invention discloses a kind of amphiphilic BAB-type block copolymer with polyglycol blocks at two ends and polyhexanolactone section in the middle part and its preparation process and application. It is prepared with diisocyanate as cross-linking agent polyglycol or other single- or double-hydroxy derivative and polycaprolactone glycol as material. The copolymer can self-assemble in water into nanometer particle or micelle with shell of hydrophobic polydexanolactone section and shell of hydrophilic polyglycol. It has excellent coating capacity to hydrophobic medicine and thus may be used in preparing water soluble nanometer particle or micelle of hydrophobic medicine.

Description

technical field [0001] The present invention relates to a polycaprolactone modified by polyethylene glycol block, that is, a BAB type amphiphilic tri-block copolymer with polyethylene glycol blocks at both ends and a polycaprolactone segment in the middle and its preparation Methods and uses. Background technique [0002] Polycaprolactone (PCL) has excellent drug permeability and is an ideal hydrophobic drug carrier. The microspheres prepared from it have been used for the controlled release of vaccines, cytostatic agents and insulin. However, the shortcomings of PCL microspheres themselves limit their application in the field of biomedicine. First, PCL has strong crystallinity and slow biodegradation rate; The drug is delivered to the target tissue; the third is that the microsphere has a hydrophobic surface, which makes it easy to be adsorbed by proteins and recognized and captured by macrophages of the reticuloendothelial system. Therefore, it is...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34C08G81/00
Inventor 邓联东董岸杰
Owner TIANJIN UNIV
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