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Biodegradable polymer vesicles and preparation and application thereof

A technology for degrading polymers, polymers

Inactive Publication Date: 2010-08-04
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the past few years, in order to improve the bioavailability of proteins, people have developed polymer nanoparticles, liposomes and hydrogel systems as carriers to encapsulate protein drugs, but the protein encapsulation efficiency is low and protein is easy to The problem of sex change (C. Kirby, Nature Biotechnology 1984, 2, 979)

Method used

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  • Biodegradable polymer vesicles and preparation and application thereof
  • Biodegradable polymer vesicles and preparation and application thereof
  • Biodegradable polymer vesicles and preparation and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0040] Embodiment one, RAFT method synthesizes triblock polymer PEG 5 -PCL 18 -PDEA 1

[0041] Under the protection of nitrogen, add macromolecular RAFT reagent PEG to a 10 ml Schlenk vacuum-sealed bottle 5 -PCL 18 - CPADN (0.5mg, 0.022mmol), add DEA monomer (0.028g, 0.15mmol) and AIBN (0.7mg, 4.3μmol) at a conversion rate of 70%, and then add 3.5ml of 1,4-dioxane. After the reaction bottle was ventilated with nitrogen for 30 minutes, the reaction bottle was placed in a preset 70° C. oil bath, and the reaction was sealed for 24 hours. After the reaction was finished, after the reaction flask was cooled, excess ether precipitated, and then the sample was filtered, vacuum-dried, and vacuum-dried for 48 hours to obtain a tri-block copolymer with a yield of 57%. The NMR results showed that the molecular weight of its PDEA was 1100, whose structure is marked as PEG 5 -PCL 18 -PDEA 1 .

Embodiment 2

[0042] Embodiment two, RAFT method synthesizes triblock polymer PEG 5 -PCL 18 -PDEA 4

[0043] Under the protection of nitrogen, add macromolecular RAFT reagent PEG to a 10 ml Schlenk vacuum-sealed bottle 5 -PCL 18 - CPADN (0.4mg, 0.017mmol), add DEA monomer (0.162g, 0.87mmol) and AIBN (0.6mg, 3.4μmol) at a conversion rate of 70%, and then add 3.5ml of 1,4-dioxane. After the reaction bottle was ventilated with nitrogen for 30 minutes, the reaction bottle was placed in a preset 70° C. oil bath, and the reaction was sealed for 24 hours. After the reaction was finished, after the reaction flask was cooled, excess n-hexane precipitated, then the sample was filtered, vacuum-dried, and vacuum-dried for 48 hours to obtain a tri-block copolymer with a yield of 65%. The NMR results showed that the molecular weight of PDEA was 4100, whose structure is marked as PEG 5 -PCL 18 -PDEA 4 .

Embodiment 3

[0044] Embodiment three, RAFT synthesis triblock polymer PEG 5 -PCL 18 -PAA 3

[0045] Under the protection of nitrogen, add macromolecular RAFT reagent PEG to a 10 ml Schlenk vacuum-sealed bottle 5 -PCL 18 - CPADN (0.5 mg, 0.022 mmol), add acrylic acid monomer (0.022 g, 0.3 mmol) and AIBN (0.7 mg, 4.3 μmol), then add 3 ml of 1,4-dioxane. After the reaction bottle was ventilated with nitrogen for 30 minutes, the reaction bottle was placed in a preset 70° C. oil bath, and the reaction was sealed for 24 hours. After the reaction was finished, after the reaction bottle was cooled, excess n-hexane precipitated, and then the sample was filtered, vacuum-dried, and vacuum-dried for 48 hours to obtain a tri-block copolymer with a yield of 86%. The NMR results showed that the molecular weight of PAA was 2700, whose structure is marked as PEG 5 -PCL 18 -PAA 3 .

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Abstract

The invention relates to a medicament carrier and a preparation method thereof, in particular to a medicament delivery system comprising biodegradable polymer vesicles with asymmetric membranes. The invention discloses the biodegradable polymer vesicles and preparation and application thereof. The biodegradable polymer vesicles are prepared from A-B-C type block polymer, wherein a block A is polyethylene glycol (PEG) distributed on outer surfaces of the vesicles; a block B is hydrophobic biodegradable polymer to form the nucleuses of the vesicles; and a block C is polyelectrolyte distributed on inner walls of the vesicular membranes and used for efficiently loading medicaments with opposite electric charge. The biodegradable polymer vesicles are formed in aqueous solution directly, can efficiently load protein and polypeptide medicaments, nucleic acid medicaments and micro-molecular medicaments, and are expected to be applied to the protein therapy and the combination therapy of cancers.

Description

technical field [0001] The invention relates to a drug carrier and a preparation method thereof, in particular to a drug release system of a biodegradable polymer vesicle containing an asymmetric membrane. Background technique [0002] A multi-block ABC type polymer, A and C are hydrophilic blocks, B is a hydrophobic block, such polymers can form vesicles with an asymmetric membrane structure, that is, inside and outside the vesicle membrane The chemistry of the surface is different (F.T.Liu, J.Am.Chem.Soc.2003, 125, 15059; A.Wittemann, Langmuir 2007, 23, 2224; S.Yu, J.Am.Chem.Soc.2009, 131, 10557). For example, Meier et al. studied the polymer PEO with different anionic hydrophilic blocks 45 -PDMS 17 -PMOXA 341 In the vesicles formed by self-assembly, PEO with a shorter hydrophilic block and PMOXA with a longer hydrophilic block are distributed on the inner and outer surfaces of the vesicle, respectively (R. Stoenescu, Chem. Commun. 2002, 3016). [0003] In the above t...

Claims

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Application Information

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IPC IPC(8): C08F293/00A61K47/34
Inventor 刘桂景李少科孟凤华钟志远
Owner SUZHOU UNIV
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