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PH response four-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, improving controlled release performance, and controlling drug release

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 response four-arm star block copolymer and preparation method and application thereof
  • PH response four-arm star block copolymer and preparation method and application thereof
  • PH response four-arm star block copolymer and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] (1) Synthesis of polymers grafted with hydrophobic groups: put a stirrer and 0.136g of pentaerythritol in a reaction bottle, seal it and vacuumize it - blow argon three times, then use a syringe to pour 20mL of solvent toluene, 12g of monomer e-CL and 0.012g 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 120°C under the protection of argon for 36h. 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), dried in vacuum at 45°C for 24h, and obtained a white powder, which was the polymer 4AS-PCl grafted with hydrophobic groups, with a yield of 91%. M n =13898, PDI=1.35;

[0070] (2) Synthesis of macromolecular initiator: Take a dry three-necked flask, add 12g 4AS-PCl and 150mL THF, seal it and pass argon for 10 minutes, inject 2....

Embodiment 2

[0078] (1) Synthesis of 4AS-PCl: Put a stirrer and 0.136g of pentaerythritol in the reaction flask, seal it and pump it in vacuum-argon three times, then add 20mL of solvent toluene, 10g of monomer e-CL and 0.020g of Sn( Oct) 2 , after three cycles of freezing-pumping-heating with liquid nitrogen, the reaction was stirred in an oil bath at 140°C under the protection of argon for 24 hours. After the reaction was completed, it was cooled to room temperature, the toluene was distilled off under reduced pressure, diluted with 50mL THF, and then used 300mL of methanol / water (1:1 volume ratio) at 0°C was precipitated and dried in vacuum at 45°C for 24h to obtain a white powder which was the product 4AS-PCl with a yield of 92%. M n =11036, PDI=1.60;

[0079] (2) Synthesis of 4AS-PCL-Br: Take a dry three-necked flask, add 10g 4AS-PCl and 150mL THF, seal it and pass argon for 10min, then add 1.62g TEA after sealing, cool to 0°C with an ice-water bath, then add 3.68g 2-Bromoisobutyry...

Embodiment 3

[0082] (1) Synthesis of 4AS-PCl: Put a stirrer and 0.136g of pentaerythritol in the reaction bottle, seal it and pump it with argon for three times, then add 20mL of solvent toluene, 18g of monomer e-CL and 0.018g of Sn( Oct) 2 , after three cycles of freezing-pumping-heating with liquid nitrogen, stir the reaction in an oil bath at 130°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 of methanol / water (1:1 volume ratio) at 0°C was precipitated and dried in vacuum at 45°C for 24h to obtain a white powder which was the product 4AS-PCl with a yield of 86%. M n =18025, PDI=1.59;

[0083] (2) Synthesis of 4AS-PCL-Br: Take a dry 250mL three-neck flask, add 18g 4AS-PCl and 150mL THF, seal it and pass argon for 10min, add 2.02g TEA after sealing, cool to 0°C with an ice-water bath, and then add 4.6g of 2-bromoisobutyryl bromide was first reac...

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Abstract

The invention discloses pH response four-arm star block copolymer and a preparation method and application thereof. According to the copolymer, pentaerythritol is used as an inner core, each arm is connected with a hydrophobic group, a pH response group and a hydrophilic group; and the preparation method comprises the following steps of: performing ring opening polymerization on pentaerythritol to obtain hydrophobic group copolymer, performing acylation on the tail end of the hydrophobic group copolymer, and sequentially initiating pH response monomer and the hydrophilic group to perform electron transfer activating agent regeneration-atom transfer radical polymerization by using hydrophobic group copolymer of which the tail end is subjected to acylation and which is used as macroinitiator to obtain the pH response four-arm star block copolymer. The copolymer is self-assembled into nano micelle in an aqueous solution, so that insoluble medicines can be effectively solubilized; the copolymer is used for preparing a micelle medicine carrying system for insoluble anti-cancer medicines, and the medicines can be kept to be slowly released when pH of normal tissues is 7.4, and can be quickly released in a controllable way under the faintly acid condition that pH of cancer cells is 5 to 6; and the proportion of foundational groups of the copolymer is easy to control, and the copolymer is simple in synthesis process and high in yield.

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 4-arm star-shaped block copolymer and its preparation method and application. Background technique [0002] A star polymer is a class of polymers in which several or more polymer chains emanate from a fulcrum or core. Due to its compact structure, spherical shape and block structure inside the molecule, it exhibits different properties from linear polymers. , such as: the molecular chain is not easy to entangle, the viscosity of the solution and bulk is significantly lower than that of the linear polymer of the same molecular weight, and the end of the molecular chain has a large number of functional groups for further modification. The particularity of the structure makes it have a unique microphase morphology, as well as some special prope...

Claims

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Application Information

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IPC IPC(8): C08F293/00A61K47/32A61K45/00A61K9/19A61P35/00
Inventor 章莉娟杨友强蒋薇钱宇张灿阳
Owner SOUTH CHINA UNIV OF TECH
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