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Amphiphilic waterborne segmented copolymer medicament carrier with pH responsiveness and biodegradability and preparation thereof

A block copolymer and degradability technology, applied in the field of dual hydrophilic block copolymer drug carrier and preparation thereof

Inactive Publication Date: 2012-12-05
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0018] However, there is no literature or patent report on the structure of the bihydrophilic block copolymer with pH responsiveness and biodegradability as described in the present invention and its application as a drug carrier.

Method used

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  • Amphiphilic waterborne segmented copolymer medicament carrier with pH responsiveness and biodegradability and preparation thereof
  • Amphiphilic waterborne segmented copolymer medicament carrier with pH responsiveness and biodegradability and preparation thereof
  • Amphiphilic waterborne segmented copolymer medicament carrier with pH responsiveness and biodegradability and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Embodiment one: prepare macromolecule ATRP initiator PEEP 32 The specific synthesis method of -Br:

[0075] (1) After drying the branched round-bottomed flask with a stirring bar in an oven at 120°C for at least 24 hours, plug it with a glass stopper, connect it to an oil pump through a latex tube, and pump it to room temperature, then introduce high-purity argon gas, and pump it again. Vacuum, so repeated three times.

[0076] (2) Inject a certain amount of initiator bromoisobutyrate-2-hydroxyethyl (HEBI) (0.14g, 0.66mmol) sequentially from the branch pipe with a dry syringe, 2-ethoxy-2-oxygen-1 , 3,2-dioxaphospholane (EEP) monomer (4g, 26mmol) and Sn(Oct) 2 (EEP monomer: Sn(Oct) 2 =1:0.002, mass ratio), anhydrous tetrahydrofuran (15 mL) was used as solvent. After the reaction flask was filled with argon, the reaction was stirred in an oil bath at 40° C. for 1 h.

[0077] (3) After the reaction, most of the solvent tetrahydrofuran was removed by rotary evaporation...

Embodiment 2

[0080] Embodiment two: diblock copolymer PEEP 32 -b-PHEMA 128 The specific preparation method:

[0081] (a) After treating the round-bottomed flask with branch tubes according to the above method, fill it with argon, quickly weigh and add PEEP 32 -Br (2.25g, 0.45mmol), cuprous bromide (0.06g, 0.45mmol) and bipyridine (0.14g, 0.45mmol) (the molar ratio of the three is 1:1:1), after repeated three times , inject 5 mL of solvent anhydrous methanol, stir until the mixture is completely dissolved and the solution turns brown.

[0082] (b) Move the round bottom flask to an oil bath, then add monomer hydroxyethyl methacrylate (HEMA) (8.7 g, 67.5 mmol) with a dry syringe, and use PEEP 32 The terminal bromine in the -Br homopolymer acts as an initiator to initiate the ATRP reaction, and the reaction is stirred in an oil bath at 30°C for 6h.

[0083] (c) After the reaction is over, contact with air to terminate the reaction, remove most of the solvent by rotary evaporation of the po...

Embodiment 3

[0084] Example Three: pH Responsive Double Hydrophilic Block Copolymer PEEP 32 -b-PSEMA 128 The specific synthesis method:

[0085] (1) After the branch tube round bottom flask was treated according to the above method, it was filled with argon, and the above two-block polymer PEEP dissolved in 10mL of anhydrous pyridine was quickly added. 32 -b-PHEMA 128 (3g, the molar number of hydroxyl (HO-) is 16.64mmol), add succinic anhydride under magnetic stirring (3.328g, 33.28mmol) (the molar ratio of hydroxyl to succinic anhydride is 1:2), and reacted at room temperature for 48h.

[0086] (2) After the reaction is over, the reaction solution is precipitated in 150 mL of ice anhydrous ether to remove solvent and unreacted monomers. After repeated precipitation for 3 times, the product obtained after the precipitation is dissolved in deionized water and then dialyzed (dialysis Bag interception 3500g mol -1 ) for 2 to 3 days, and finally the dialysis solution was freeze-dried to ...

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Abstract

The invention discloses an amphiphilic waterborne segmented copolymer medicament carrier with pH responsiveness and biodegradability and a preparation method thereof. An amphiphilic waterborne segmented copolymer consists of a chain segment which is modified with polyphosphoester and polymethacrylate hydroxyethyl and contains carboxyl. A polyanion chain segment can be reversely converted into a hydrophilic or hydrophobic chain segment by adjusting the pH value of a medium. The amphiphilic polymer is self-assembled into a micelle under the condition of certain PH, and a shell of the micelle formed by a hydrophilic polyphosphoester chain segment can be used for better stabilizing the micelle. A hydrophobic polyanionic chain segment is used for forming an inner core of the micelle, is used for coating a hydrophobic medicament, and serves as a medicament carrier. The polyphosphoester chain segment has high biocompatibility and high biodegradability, and long in-vivo circulation of a medicament-carrying micelle can be realized. Under a weakly alkaline condition, the aims of dissociating the micelle, releasing a medicament and realizing controllable release are fulfilled.

Description

technical field [0001] The invention belongs to the field of biomedical polymer materials, and in particular relates to a pH-responsive and biodegradable double-hydrophilic block copolymer drug carrier and a preparation method thereof. Background technique [0002] Double Hydrophilic Block Copolymers (Double Hydrophilic Block Copolymers) is a special class of block copolymers, which are composed of two different types of hydrophilic segments, one of which remains dissolved in water, and When the other segment is stimulated by the external environment in water, it will change its physical or chemical properties from a hydrophilic state to a hydrophobic state. External stimuli are mainly divided into two categories: physical stimuli and chemical stimuli. Physical stimuli include temperature, magnetic field, light, etc.; chemical stimuli include pH, ionic strength, etc. Dihydrophilic block copolymers can be designed and synthesized with different structures according to needs...

Claims

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Application Information

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IPC IPC(8): C08F293/00C08F8/14C08F6/06C08G79/04A61K47/34A61K9/10
Inventor 倪沛红卞姣张明祖郝莹
Owner SUZHOU UNIV
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