Method for preparing biocompatible polymer nano-vesicle in pure water

A biocompatible, nanovesicle technology, used in pharmaceutical formulations, medical preparations with inactive ingredients, etc., can solve problems such as unfavorable large-scale production and time-consuming dialysis methods.

Inactive Publication Date: 2012-03-28
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But using dialysis is time-consuming

Method used

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  • Method for preparing biocompatible polymer nano-vesicle in pure water
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  • Method for preparing biocompatible polymer nano-vesicle in pure water

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] 1) Amphiphilic block copolymer PCL- b -The specific synthetic scheme of PMPC is as follows:

[0033] a) Ring-opening polymerization to generate macroinitiator PCL-Br

[0034] Add 60 mL of dried anhydrous toluene, 76.3 g of ε-caprolactone, 1.2 g of benzyl alcohol, and 18.8 uL of stannous octoate into a 500 mL round-bottomed flask, 110 O Stir the reaction in an anaerobic state in a C oil bath for 48 hours, then place it at room temperature to cool, continue to add 400 mL of dried toluene, 7.8 mL of dry triethylamine, and 6.8 mL of 2-bromoisobutyryl bromide into the round bottom flask, Stir and react in an ice-water bath for 48 hours, filter, extract, collect the organic phase, dry, filter, precipitate, filter with suction, and dry in vacuum to obtain the macromolecular initiator PCL-Br.

[0035] b) Synthesis of amphiphilic block copolymer PCL- by atom transfer radical polymerization b -PMPC

[0036] Add 1.0 g macroinitiator PCL-Br, 1.6 g monomer MPC, 44.6 mg catalyst ...

Embodiment 2

[0040] 1) Amphiphilic block copolymer PCL- b -The specific synthetic scheme of PMPC is as follows:

[0041] a) Ring-opening polymerization to generate macroinitiator PCL-Br

[0042] Add 60 mL of dried toluene, 76.3 g of ε-caprolactone, 1.2 g of benzyl alcohol, and 18.8 uL of stannous octoate into a 500 mL round-bottomed flask, 110 OStir the reaction in an anaerobic state in an oil bath for 48 hours, then cool at room temperature, and then add 400 mL of dried toluene, 7.8 mL of dry triethylamine, and 6.8 mL of 2-bromoisobutyryl bromide into the round bottom flask , stirred and reacted in an ice-water bath for 48 hours, filtered, extracted, collected the organic phase, dried, filtered, precipitated, suction filtered, and vacuum-dried to obtain the macromolecular initiator PCL-Br.

[0043] b) Synthesis of amphiphilic block copolymer PCL- by atom transfer radical polymerization b -PMPC

[0044] Add 1.0 g macroinitiator PCL-Br, 0.3 g monomer MPC, 44.6 mg catalyst ligand bipyrid...

Embodiment 3

[0048] 1) Amphiphilic block copolymer PCL- b -The specific synthetic scheme of PMPC is as follows:

[0049] a) Ring-opening polymerization to generate macroinitiator PCL-Br

[0050] Add 40 mL of dried toluene, 38.2 g of ε-caprolactone, 0.6 g of benzyl alcohol, and 9.4 uL of stannous octoate into a 250 mL round bottom flask, 110 O Stir the reaction in an anaerobic state in a C oil bath for 48 hours, then cool at room temperature, and then add 400 mL of dried toluene, 3.9 mL of dry triethylamine, and 3.4 mL of 2-bromoisobutyryl bromide into the round bottom flask , stirred and reacted in an ice-water bath for 48 hours, filtered, extracted, collected the organic phase, dried, filtered, precipitated, suction filtered, and vacuum-dried to obtain the macromolecular initiator PCL-Br.

[0051] b) Synthesis of amphiphilic block copolymer PCL- by atom transfer radical polymerization b -PMPC

[0052] Put 1.0 g macroinitiator PCL-Br, 0.8 g monomer MPC, 89.2 mg catalyst ligand bipyridi...

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Abstract

The invention belongs to the technical field of materials, in particular to a method for preparing a biocompatible polymer nano-vesicle in pure water, which comprises the following specific steps that: an amphiphilic block copolymer PCL-b-PMPC (polycaprolactone-b-1-palmitoyl-2-myristoyl-sn-glycero-3-phosphocholine) is obtained by a series of reactions (caprolactone is subjected to ring-opening polymerization to obtain PCL-OH (hydroxyl-terminated polycaprolactone), the terminal group modification is conducted to obtain PCL-Br (bromine-terminated polycaprolactone) in an esterification reaction, the PCL-Br initiates MPC (2-myristoyl-sn-glycero-3-phosphocholine) atom transfer radical polymerization), and is added with hot water for few minutes to form vesicles. In the invention, the biocompatible vesicles are directly prepared in water without any organic co-solvents and pH adjustment, even without stirring. The method is simpler and more convenient than the widely used solvent exchange method. A PCL membrane has certain hydrophobicity and can be completely degraded, and PMPC has hydrophilicity and good biocompatibility.

Description

technical field [0001] The invention belongs to the field of macromolecular nano biomedical materials, and in particular relates to a method for preparing biocompatible macromolecular nanovesicles in pure water. Background technique [0002] Polymer nanovesicles have attracted extensive attention in recent years due to their wide applications in drug sustained release, gene delivery, cell simulation, nanoreactors and other fields. Polymeric nanovesicles generally have a hydrophobic membrane that is 10-30 nm thick. The inner and outer surfaces of the membrane are hydrophilic polymer chains. The former can be loaded with hydrophobic molecules, while the hollow inner structure can contain hydrophilic molecules. Hydrophilic polymer chains on the membrane stabilize the nanoparticles. Therefore, it can simultaneously carry hydrophilic and hydrophobic substances, and thus has important applications in the field of biomedicine. More importantly, this block copolymer vesicle is m...

Claims

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Application Information

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IPC IPC(8): C08F293/00C08F220/36C08G63/08C08G63/78A61K47/30
Inventor 杜建忠肖杰
Owner TONGJI UNIV
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