Double-arm hyperbranched starlike amphiphilic polylactic acid-poly2-methacryloyloxy ethyl phosphorylcholine block polymer and preparation method thereof

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, maintaining stability, and small critical aggregation concentration

Inactive Publication Date: 2013-04-24
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] There are few studies on the preparation of hyperbranched star-shaped amphiphilic block polymers

Method used

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  • Double-arm hyperbranched starlike amphiphilic polylactic acid-poly2-methacryloyloxy ethyl phosphorylcholine block polymer and preparation method thereof
  • Double-arm hyperbranched starlike amphiphilic polylactic acid-poly2-methacryloyloxy ethyl phosphorylcholine block polymer and preparation method thereof
  • Double-arm hyperbranched starlike amphiphilic polylactic acid-poly2-methacryloyloxy ethyl phosphorylcholine block polymer and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] 1. Synthesis of two-armed hyperbranched star-shaped SPLA-b-PMPC polymer by click chemistry: add 0.01 g of two-armed polylactic acid to the sealed tube, then add 0.05 g of alkyne-containing PMPC, 0.3 g of 2,2-bipyridine mg, cuprous bromide 0.1mg and a small stirrer, connect the sealed tube to the vacuum line, evacuate the nitrogen for three times; inject 4ml of anhydrous methanol that has been protected by nitrogen into the sealed tube with a syringe replaced by argon, And 3ml DMF; the substance in the sealed tube dissolves quickly, and the solution is reddish brown; put the sealed tube into a thermos cup filled with liquid nitrogen to freeze for 0.5min, then vacuumize for 0.5min, then pass nitrogen gas, and warm water to thaw at the same time, repeat 3 times; seal the tube and freeze it for 0.5 min, then evacuate it for 0.5 min, burn the sealed tube with an alcohol blowtorch, and finally transfer it to an oil bath, and react for 2 days at 0°C; , the system turned from r...

Embodiment 2

[0047] 1. Synthesis of two-arm hyperbranched star-shaped SPLA-b-PMPC polymer by click chemistry: Add 500g of two-arm polylactic acid to the sealed tube, then add 100g of alkyne-containing PMPC, 500mg of 2,2-bipyridine, bromide Connect the sealed tube to the vacuum line with 250 mg of cuprous metal and a small stirring bar, and evacuate the nitrogen for three times; inject 4 ml of anhydrous methanol that has been protected by nitrogen gas, and 3 ml of DMF into the sealed tube with a syringe replaced by argon; The substance in the tube dissolves quickly, and the solution turns reddish brown; put the sealed tube into a thermos cup filled with liquid nitrogen and freeze it for 100 minutes, then vacuumize it for 150 minutes, then pass nitrogen gas, and thaw with warm water at the same time, repeat this 3 times; seal the tube and freeze again 100min, then evacuated for 150min, burned the sealed tube with an alcohol blowtorch, finally transferred to an oil bath, and reacted at 200°C f...

Embodiment 3

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

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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 combining ring-opening polymerization, atom transfer radical polymerization and click chemistry, in particular to two-arm hyperbranched star-shaped amphiphilic block polymers The invention relates to a permanent polylactic acid-poly 2-methacryloyloxyethyl phosphorylcholine block polymer and a preparation method thereof. Background technique [0002] Amphiphilic diblock polymers can self-assemble into micelles in aqueous environment, the hydrophobic core can be used as drug carrier, and the hydrophilic shell can stabilize the micelles. Compared with linear amphiphilic two-block polymers, star-shaped amphiphilic two-block polymers have smaller critical aggregation concentration and solution viscosity, and thus have good in vivo stability and longer blood circulation time. Due to its unique structure and properties, star-shaped amphiphili...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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