Three-arm hyperbranched star amphiphilic polylactic acid-poly 2-methacryloyloxyethyl phosphorylcholine block polymer and preparation method thereof

A technology of methacryloyloxyethylphosphorylcholine and block polymer, applied in three-arm hyperbranched star-shaped amphiphilic polylactic acid-poly 2-methacryloyloxyethylphosphorylcholine In the field of alkali block polymers and its 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 mild conditions and maintaining stability

Inactive Publication Date: 2011-12-28
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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  • Three-arm hyperbranched star amphiphilic polylactic acid-poly 2-methacryloyloxyethyl phosphorylcholine block polymer and preparation method thereof
  • Three-arm hyperbranched star amphiphilic polylactic acid-poly 2-methacryloyloxyethyl phosphorylcholine block polymer and preparation method thereof
  • Three-arm hyperbranched star amphiphilic polylactic acid-poly 2-methacryloyloxyethyl phosphorylcholine block polymer and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] 1. Synthesis of three-arm hyperbranched star-shaped SPLA-b-PMPC polymer by click chemistry: add 0.01 g of three-arm 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 turns from re...

Embodiment 2

[0046] 1. Synthesis of three-arm hyperbranched star-shaped SPLA-b-PMPC polymer by click chemistry: Add 500 g of three-arm polylactic acid to the sealed tube, then add 100 g of alkyne-containing PMPC, 500 mg 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 ...

Embodiment 3

[0055] 1. Synthesis of three-arm hyperbranched star-shaped SPLA-b-PMPC polymer by click chemistry: add 0.26 g of three-arm polylactic acid to the sealed tube, then add 0.6 g of alkyne-containing PMPC, 34 mg 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 concentrati...

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Abstract

The invention relates to a tribrachia hyperbranched star-shaped amphiphilic polylactic acid-poly2-methyl acryloyloxy ethyl phosphorlcholine block polymer and a preparation method thereof. The preparation method comprises the following steps: adding polylactic acid containing a nitrine group into a reactor, adding PMPC (poly(2-methacryloyloxyethylphosphorylcholine)) containing an alkyl group, 2,2-bipyridine and cuprous bromide, stirring, and adding absolute methanol and dimethylformamide for dissolution; putting a reaction liquid into a thermos cup containing liquid nitrogen for freezing, vacuumizing, introducing noble gas, and simultaneously unfreezing in warm water; and putting the reactor into the thermos cup containing liquid nitrogen for freezing, vacuumizing, and finally reacting for1 hour-2 days at the temperature of 0-200 DEG C so as to obtain a product. According to the polymer prepared by the method in the invention, a nano-size medicament transmission system can be obtainedthrough self-assembly; the hydrophobic core of the polymer can be used as a medicament carrier for incorporating a hydrophobic medicament, the hydrophilic shell of the polymer takes the effect of prolonging in-vivo cycle time while maintaining the stability of micelle.

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 a three-arm hyperbranched star-shaped amphiphile 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 amphiphilic diblock po...

Claims

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Application Information

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Patent Type & Authority Applications(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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