Cross-linked biologically degradable carrier polymer, micelle and vesicle, and preparation method and application of the cross-linked biologically degradable carrier polymer, micelle and vesicle

A technology of carrier polymers and polymers, applied in the field of biomedical materials, can solve the problems of poor stability of polymer micelles and vesicles, and achieve the effects of increasing difficulty, facilitating medical applications, and increasing costs

Active Publication Date: 2013-09-04
CHANGZHOU INST OF ENERGY STORAGE MATERIALS &DEVICES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to solve the problem of poor stability of existing polymer micelles and vesicles, and to provide cross-linked biodegradable carrier polymers, micelles, vesicles and their preparation methods and applications

Method used

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  • Cross-linked biologically degradable carrier polymer, micelle and vesicle, and preparation method and application of the cross-linked biologically degradable carrier polymer, micelle and vesicle
  • Cross-linked biologically degradable carrier polymer, micelle and vesicle, and preparation method and application of the cross-linked biologically degradable carrier polymer, micelle and vesicle
  • Cross-linked biologically degradable carrier polymer, micelle and vesicle, and preparation method and application of the cross-linked biologically degradable carrier polymer, micelle and vesicle

Examples

Experimental program
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Effect test

preparation example Construction

[0037] The preparation method of the cross-linked biodegradable carrier polymer, the specific steps are as follows:

[0038] (1) Firstly, the ring-opening polymerization of allyl glycidyl ether is initiated by the PEG protected by the end methoxy group, and the two-block polymer polyethylene glycol-polyallyl glycidyl ether is obtained;

[0039] (2) Use the two-block polymer obtained in step (1) to initiate ring-opening polymerization of ester monomers to prepare a three-block polymer polyethylene glycol-poly(side allyl substituted ethylene glycol)-polyester; The polyester is a polymer of L-lactide, D-lactide, racemic lactide, glycolide or ε-caprolactone, or a random copolymer of one or two of the above monomers thing;

[0040] (3) Addition reaction of the mercapto-containing monomer with the allyl group on the triblock polymer obtained in step (2) converts the double bond of the polymer side chain into a different functional group to obtain the A-B-C type triblock polymer. ...

Embodiment 1

[0079] Embodiment 1: the polymer PEG of preparation triblock 5000 -PEG / COOH -PCL 38000 :

[0080] Step 1: Under nitrogen protection, take PEG 5000 (PEG with a molecular weight of 5000) 2.0g (0.4mmol), add toluene to carry out azeotropic water removal, after 2 hours, add cerium hydroxide 74mg (0.44mmol) in the reaction vessel, stir and react at 60°C for 2 hours, then remove the solvent , add 0.95mL allyl glycidyl ether (AGE, 8.0mmol), react at 40°C for 24 hours, cool to room temperature, settle with 400mL ether, filter, and obtain 2g of solid powder after vacuum drying, the yield is 69%, the obtained product It is PEG-PAGE, and the molecular weight of the PAGE block measured by nuclear magnetic resonance method is 1700;

[0081] The second step: Take 0.2g (0.03mmol) of the above PEG-PAGE and dissolve it in 20mL of THF. After stirring and dissolving, add 0.01mL of catalyst Zn[N(SiMe 3 ) 2 ] 2 and 1.2mL (0.01mmol) of ε-caprolactone, after stirring at room temperature for ...

Embodiment 2

[0083] Example 2: Preparation of triblock polymers of different molecular weights and different polyester monomers

[0084] Using the method of Example 1, by changing the amount of allyl glycidyl ether and polyester monomer, different polyester monomers and compounds containing different mercapto monomers, PEG- PEG / COOH -PCL block polymer, the specific results are shown in Table 1. The subscript after the polymer code in the table indicates the molecular weight of the block.

[0085] Table 1

[0086]

[0087] Note: In the table, CL stands for ε-caprolactone, LA stands for lactide, and GA stands for glycolide.

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Abstract

The invention provides a cross-linked biologically degradable carrier polymer, a micelle and a vesicle, and a preparation method and an application of the cross-linked biologically degradable carrier polymer, micelle and vesicle, belonging to the field of biological medical material and solving a poor stability problem of the existing polymer micelle and vesicle. The carrier polymer is an A-B-C tri-block polymer, wherein the block A is polyethylene glycol, the block B is the polyethylene glycol containing functional groups in a lateral chain, and the block C is biologically degradable polyester. The invention also provides the polymer micelle and vesicle, which is formed by self assembly of the carrier polymer, wherein the size of the polymer micelle is 20-1000nm, and the size distribution is 0.01-0.50; the size of the vesicle is 20-1000nm, and the size distribution is 0.01-0.50. The polymer micelle provided by the invention can package fat-soluble matters; and the polymer vesicle can package water-soluble matters and the fat-soluble matters at the same time; and the polymer micelle or the vesicle has better mechanical strength and stability because the polymer micelle or the vesicle contains a transitional layer formed by the cross-linked block B.

Description

technical field [0001] The invention relates to a drug carrier and a preparation method thereof, in particular to a cross-linked biodegradable carrier polymer, micelles and vesicles, a preparation method and application thereof, and belongs to the field of biomedical materials. Background technique [0002] A series of nanomaterials, such as spherical micelles, rod micelles or vesicles, can be obtained by self-assembly of amphiphilic block polymers in aqueous solution. Vesicles are spherical or elliptical unicellular or multi-cellular structures formed by closed bilayers, which are similar to the structure of cell membranes and have good biocompatibility. Vesicles made of amphiphilic block polymers have a structure similar to liposomes, consisting of a hydrophilic inner cavity and a bilayer molecular membrane. This polymer vesicle has the advantages of liposomes and nanoparticles and other drug delivery systems, and due to the large molecular weight of the polymer, its mech...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G63/91C08G63/08C08J3/12C08J3/24A61K47/34A61K9/51A61K9/19A61K49/00
Inventor 谢志刚景遐斌岳军晏乐三胡秀丽黄宇彬
Owner CHANGZHOU INST OF ENERGY STORAGE MATERIALS &DEVICES
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