Two-arm hyperbranched star-shaped amphiphilic polylactic acid-poly 2-methacryloyloxyethyl phosphorylcholine block polymer and its preparation method

A technology of methacryloyloxyethylphosphorylcholine and block polymer, applied in two-arm hyperbranched star-shaped amphiphilic polylactic acid-poly2-methacryloyloxyethylphosphorylcholine In the field of alkali block polymers and their preparation, it can solve the problems of less research on hyperbranched star-shaped amphiphilic block polymers, and achieve the effects of prolonging the circulation time in the body, mild conditions, and small critical aggregation concentration

Inactive Publication Date: 2011-12-14
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] There are few studies on the preparation ...

Method used

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  • Two-arm hyperbranched star-shaped amphiphilic polylactic acid-poly 2-methacryloyloxyethyl phosphorylcholine block polymer and its preparation method
  • Two-arm hyperbranched star-shaped amphiphilic polylactic acid-poly 2-methacryloyloxyethyl phosphorylcholine block polymer and its preparation method
  • Two-arm hyperbranched star-shaped amphiphilic polylactic acid-poly 2-methacryloyloxyethyl phosphorylcholine block polymer and its preparation method

Examples

Experimental program
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Embodiment 1

[0037] 1. Click chemistry to synthesize two-arm hyperbranched star-shaped SPLA-b-PMPC polymer: add 0.01g two-arm polylactic acid to the sealed tube, then add 0.05g PMPC containing alkynyl groups, and 0.32,2-bipyridine mg, cuprous bromide 0.1mg and a small stirrer connect the sealing tube to the vacuum line, vacuum and pass nitrogen three times; inject 4ml of anhydrous methanol protected by nitrogen into the sealing tube with a syringe replaced by argon. And 3ml DMF; the material in the sealed tube dissolves quickly, and the solution is reddish brown; put the sealed tube into a thermos cup filled with liquid nitrogen and freeze for 0.5 min, then vacuum for 0.5 min, then pass nitrogen gas, and at the same time warm thaw, repeat the procedure 3 times; seal the tube and freeze for 0.5min, then vacuum for 0.5min, burn the sealed tube with an alcohol blowtorch, finally transfer to an oil bath, react at 0℃ for 2 days; after the reaction is completed, cut the sealed tube with a glass kn...

Embodiment 2

[0047] 1. Click chemistry to synthesize two-arm hyperbranched star-shaped SPLA-b-PMPC polymer: add 500g of two-arm polylactic acid to the sealed tube, then add 100g of PMPC containing alkynyl group, 500mg of 2,2-bipyridine, bromination Connect the sealing tube with cuprous 250mg and a small stirrer to the vacuum line, vacuum and pass nitrogen three times; inject 4ml of anhydrous methanol protected by nitrogen and 3ml DMF into the sealing tube with a syringe replaced with argon; The substance in the tube dissolves quickly, and the solution is reddish brown; put the sealed tube in a thermos cup filled with liquid nitrogen and freeze for 100 minutes, then vacuum for 150 minutes, then pass nitrogen gas, and at the same time warm thaw, repeat this 3 times; seal the tube and freeze again 100min, vacuum for another 150min, burn the sealed tube with an alcohol blowtorch, finally transfer to an oil bath, and react at 200°C for 1 hour; after the reaction is completed, cut the sealed tube ...

Embodiment 3

[0056] 1. Click chemistry method to synthesize two-arm hyperbranched star-shaped SPLA-b-PMPC polymer: add 0.26g of two-arm polylactic acid to the sealed tube, then add 0.6g of PMPC containing alkynyl group and 34mg of 2,2-bipyridine , 19mg cuprous bromide and a small stirrer connect the sealing tube to the vacuum line, vacuum and pass nitrogen three times; inject 4ml of anhydrous methanol protected by nitrogen and 3ml into the sealing tube with a syringe replaced with argon DMF; the substance in the sealed tube dissolves quickly, and the solution is reddish brown; put the sealed tube into a thermos cup containing liquid nitrogen and freeze for 10 minutes, then vacuumize for 15 minutes, then pour nitrogen through it, and at the same time warm thaw, repeat this 3 times; sealing Freeze the tube for another 10 minutes, then vacuum for 15 minutes, burn the sealed tube with an alcohol blowtorch, and finally transfer to an oil bath and react at 35°C for 12 hours; after the reaction is ...

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Abstract

The invention relates to a double-arm hyperbranched starlike amphiphilic polylactic acid-poly2-methacryloyloxy ethyl phosphorylcholine block polymer and a preparation method thereof. The preparation method comprises the following steps of: adding nitrine group-containing polylactic acid into a reactor; adding alkynyl-containing PMPC, 2,2-bipyridine and cuprous bromide to stir; adding absolute methanol and dimethylformamide to dissolve; placing the reactor into a heat-preserving cup accommodating liquid nitrogen to freeze; vacuumizing; introducing inert gas; unfreezing in warm water; placing the reactor into the heat-preserving cup accommodating the liquid nitrogen to freeze again; vacuumizing again; and reacting at the temperature of between 0 and 200 DEG C for 1 hour to 2 days to obtain a product. The block polymer prepared by the method is self-assembled to obtain a nano-sized medicine transmission system, wherein the hydrophobic core can serve as a medicine carrier to wrap and loada hydrophobic medicine; and the hydrophilic shell has the effects of maintaining stability of micelle and prolonging time of body circulation.

Description

Technical field [0001] The invention relates to a technique for synthesizing two-arm hyperbranched star-shaped amphiphilic block polymers by a combination of ring-opening polymerization, atom transfer radical polymerization and click chemistry, in particular to two-arm hyperbranched star-shaped amphiphilic block polymers Polylactic acid-poly-2-methacryloxyethyl phosphorylcholine block polymer and its preparation method. Background technique [0002] The amphiphilic diblock polymer can self-assemble to form micelles in an aqueous environment. Its hydrophobic core can be used as a drug carrier, and the hydrophilic shell can stabilize the micelles. Compared with linear amphiphilic diblock polymers, star amphiphilic two-stage polymers have a smaller critical aggregation concentration and solution viscosity, so they have good in vivo stability and longer blood circulation time. It is precisely because of its unique structure and performance that in recent years, star-shaped amphiphil...

Claims

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Application Information

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IPC IPC(8): C08G81/02C08G63/08C08F120/36
Inventor 亓洪昭马桂秋何立刚龙丽霞柳朝永盛京原续波
Owner TIANJIN UNIV
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