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pH-responsive 6-arm star block copolymer and preparation method and application thereof

A technology of block copolymers and polymers, which can be used in pharmaceutical combinations, pharmaceutical formulations, and medical preparations with inactive ingredients, etc., and can solve the problems of insufficient stability and controlled release performance of multi-arm star block copolymers. , to achieve the effect of improving pH response sensitivity and release efficiency, controlling drug release, and improving controlled release performance

Inactive Publication Date: 2012-10-03
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These existing multi-arm radial block copolymers are not perfect in terms of stability and controlled release properties

Method used

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  • pH-responsive 6-arm star block copolymer and preparation method and application thereof
  • pH-responsive 6-arm star block copolymer and preparation method and application thereof
  • pH-responsive 6-arm star block copolymer and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0068] (1) Synthesis of polymers grafted with hydrophobic groups: Put a stirrer and 0.254g of pentaerythritol in a reaction bottle, seal it and pump it in a vacuum-argon three times, then add 12g of monomer e-CL and 0.012g of Sn (October) 2 , after three cycles of freezing-pumping-heating with liquid nitrogen, stir the reaction in an oil bath at 120°C under the protection of argon for 36h, after the completion of the reaction, cool to room temperature, evaporate toluene under reduced pressure, add 50mL THF to dilute, and then use 300mL methanol / water (1:1 volume ratio) at 0°C was precipitated and dried in vacuum at 45°C for 24 hours to obtain a white powder, which was the polymer 6AS-PCL grafted with hydrophobic groups, with a yield of 93%. M n =12322, PDI=1.59;

[0069] (2) Synthesis of macromolecular initiators: take a baked and dried 250mL three-neck flask, add 12g 6AS-PCl and 150mL THF, seal it and pass argon for 10min, inject 3.04g TEA after sealing, cool to 0°C with an...

Embodiment 2

[0080] (1) Synthesis of 6AS-PCL: Put a stirrer and 0.254g of pentaerythritol in the reaction bottle, seal it and pump it to a vacuum-argon three times, then use a syringe to inject 10g of monomer e-CL and 0.020g of Sn(Oct) 2 Add it into the reaction flask, use liquid nitrogen for three times of freezing-pumping-heating cycle, and stir the reaction in an oil bath at 140°C under the protection of argon for 24 hours. After the reaction is completed, cool to room temperature, evaporate toluene under reduced pressure, and add 50mL THF Diluted, then precipitated with 300mL 0°C methanol / water (1:1 volume ratio), and dried in vacuum at 45°C for 24h to obtain a white powder, 6AS-PCL, with a yield of 86%. M n =10918, PDI=1.62;

[0081] (2) Synthesis of 6AS-PCL-Br: Take a baked and dried 250mL three-neck flask, add 10g 6AS-PCl and 150mL THF, seal it and pass argon for 10min, inject 2.43g TEA after sealing, cool to 0°C with an ice-water bath, Then add 5.52g of 2-bromoisobutyryl bromide,...

Embodiment 3

[0084] (1) Synthesis of 6AS-PCL: Put a stirrer and 0.254g of pentaerythritol in the reaction bottle, seal it and pump the vacuum-argon gas three times, then inject 16g of monomer e-CL and 0.008g of Sn(Oct) 2 Add it into the reaction flask, use liquid nitrogen for three times of freezing-pumping-heating cycle, and stir the reaction in an oil bath at 110°C under the protection of argon for 48h. After the reaction is completed, cool to room temperature, evaporate the toluene under reduced pressure, and add 50mL THF Diluted, then precipitated with 300mL 0°C methanol / water (1:1 volume ratio), and dried in vacuum at 45°C for 24h to obtain a white powder, 6AS-PCL, with a yield of 89%. M n =17543, PDI=1.60;

[0085] (2) Synthesis of 6AS-PCL-Br: Take a baked and dried 250mL three-neck flask, add 16g 6AS-PCl and 150mL THF, seal it and pass argon for 10min, inject 3.64g TEA after sealing, cool to 0°C with an ice-water bath, Then add 8.28g of 2-bromoisobutyryl bromide, react at 0°C for ...

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Abstract

The invention discloses a pH-responsive 6-arm star block copolymer and a preparation method and application thereof. In the structure of the copolymer, pentaerythritol is adopted as a kernel, and each arm is connected with a hydrophobic group, a pH-responsive group and a hydrophilic group. The preparation method comprises the steps of: carrying out ring opening polymerization of the pentaerythritol to obtain a hydrophobic group polymer, carrying out acylation of the end of the hydrophobic group polymer to prepare a macromolecular initiator, carrying out sequential initiation of regeneration of an electron transfer activator for a pH-responsive monomer and the hydrophilic group, i.e. radical polymerization for atom transfer, thereby obtaining the pH-responsive 6-arm star block copolymer. The polymer is self-assembled into nano micelles in aqueous solution, the dissolution of water-insoluble drugs can be enhanced effectively, the polymer can be applied in preparation of a micelle carrying system for water-insoluble anticancer drugs, and the drugs can be released slowly when the pH of normal tissues is 7.4 and rapidly in a controlled way under acidic conditions when the pH of tumor cells is 5-6; and the proportion of functional groups can be easily adjusted, the synthesis process is simple, and the yield is higher.

Description

technical field [0001] The invention belongs to the field of high-molecular polymer materials for biomedicine, and relates to a high-molecular polymer material and its preparation method and application, in particular to a pH-responsive 6-arm star-shaped block copolymer and its preparation method and application. Background technique [0002] Star polymers are multi-arm branched polymers formed by at least three linear polymer chains connected to the same central core through chemical bonds. Compared with linear polymers, star polymers have compact structures and molecular surface functions Unique properties such as high degree of crystallinity, low crystallinity, hydrodynamic volume and easier microphase separation. Amphiphilic block copolymers refer to copolymers that contain two or more blocks and the solubility of these blocks in solvents is quite different. Amphiphilic block copolymers self-assemble at or above the critical micelle concentration to form various micelle...

Claims

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Application Information

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IPC IPC(8): C08F293/00C08F220/34C08F220/28C08G63/91C08G63/08A61K47/34A61K9/19A61K45/00A61P35/00
Inventor 章莉娟杨友强蒋薇杨楚芬
Owner SOUTH CHINA UNIV OF TECH
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