Star polymer drug carrier and preparation method thereof

A technology of star-shaped polymers and drugs, which can be used in pharmaceutical formulations, medical preparations of non-active ingredients, emulsion delivery, etc. It can solve problems such as easy immune response and insufficient stability of micelles, and achieve good biocompatibility , the effect of long cycle times

Inactive Publication Date: 2021-04-06
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although PEG is widely used in amphiphilic block copolymers, it also has many disadvantages. For example, the micelles made of PEG are not stable enough to easily cause immune reactions, etc., while the zwitterionic polymer PMPC (poly-2-methyl Acryloyloxyethylphosphorylcholine) can effectively avoid these problems and form a stable, biocompatible micellar structure

Method used

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  • Star polymer drug carrier and preparation method thereof
  • Star polymer drug carrier and preparation method thereof
  • Star polymer drug carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Synthesis of the macromolecular initiator 4-arm-PEG-Br: First, weigh 300mg 4-arm-PEG-OH and place it in a three-neck flask equipped with a nitrogen inlet, a nitrogen outlet and a constant pressure dropping funnel, and pour into it Add 10mL CH 2 Cl 2 . Then 0.022g DMAP and 17uL TEA were added thereto. Add 37uL BIBB and 10mL CH to the constant pressure dropping funnel 2 Cl 2 , when BIBB is completely dissolved in CH 2 Cl 2 Afterwards, it was slowly added dropwise to a three-neck flask under ice bath and nitrogen protection conditions. After the dropwise addition was completed, the reaction was carried out at room temperature for 24 h. After the reaction was completed, the solvent CH was evaporated by rotary evaporation2 Cl 2 After removal, the product was dissolved in distilled water, dialyzed in distilled water for 48 hours with a dialysis bag (Mw=1000), and freeze-dried to obtain 4-arm-PEG-Br.

[0029] Synthesis of 4-arm-PEG-PMPC block copolymer: Weigh 4.3mg Cu...

Embodiment 2

[0032] Synthesis of the macromolecular initiator 4-arm-PEG-Br: First, weigh 300mg 4-arm-PEG-OH and place it in a three-neck flask equipped with a nitrogen inlet, a nitrogen outlet and a constant pressure dropping funnel, and pour into it Add 10mL CH 2 Cl 2 . Then 0.022g DMAP and 17uL TEA were added thereto. Add 37uL BIBB and 10mL CH to the constant pressure dropping funnel 2 Cl 2 , when BIBB is completely dissolved in CH 2 Cl 2 Afterwards, it was slowly added dropwise to a three-neck flask under ice bath and nitrogen protection conditions. After the dropwise addition was completed, the reaction was carried out at room temperature for 24 h. After the reaction was completed, the solvent CH was evaporated by rotary evaporation 2 Cl 2 After removal, the product was dissolved in distilled water, dialyzed in distilled water for 48 hours with a dialysis bag (Mw=1000), and freeze-dried to obtain 4-arm-PEG-Br.

[0033] Synthesis of 4-arm-PEG-PMPC block copolymer: Weigh 4.3mg ...

Embodiment 3

[0036] Synthesis of the macromolecular initiator 4-arm-PEG-Br: First, weigh 300mg 4-arm-PEG-OH and place it in a three-neck flask equipped with a nitrogen inlet, a nitrogen outlet and a constant pressure dropping funnel, and pour into it Add 10mL CH 2 Cl 2 . Then 0.033g DMAP and 34uL TEA were added thereto. Add 55.5uL BIBB and 15mL CH to the constant pressure dropping funnel 2 Cl 2 , when BIBB is completely dissolved in CH 2 Cl 2 Afterwards, it was slowly added dropwise to a three-neck flask under ice bath and nitrogen protection conditions. After the dropwise addition was completed, the reaction was carried out at room temperature for 24 h. After the reaction was completed, the solvent CH was evaporated by rotary evaporation 2 Cl 2 After removal, the product was dissolved in distilled water, dialyzed in distilled water for 48 hours with a dialysis bag (Mw=1000), and freeze-dried to obtain 4-arm-PEG-Br.

[0037] Synthesis of 4-arm-PEG-PMPC block copolymer: Weigh 4.3m...

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Abstract

The invention provides a star-shaped polymer drug carrier and a preparation method thereof. The carrier is an amphiphilic star-shaped polymer material. Firstly, star-shaped multi-armed polyethylene glycol-poly-2-methacryloyloxyethylphosphonium was synthesized by esterification reaction and atom transfer radical polymerization (ATRP) using star-shaped multi-armed polyethylene glycol as raw material Acylcholine (PEG‑PMPC) compound, which has good hydrophilicity, and then introduces a polyacrylate compound with a hydrophobic segment to form a drug carrier with hydrophobic drugs. The polymer of the invention can be used as a drug carrier to form a drug-loaded micelle through self-assembly in water, and is applied to tumor treatment.

Description

technical field [0001] The invention relates to the technical field of preparation of controlled-release drug carriers, in particular to a star-shaped polymer drug carrier and a preparation method thereof. Background technique [0002] Block copolymers have a wide range of applications in the fields of drug carriers and fluorescence / nuclear magnetic imaging. Amphiphilic block copolymers can self-assemble in water to form nanoscale micelles, which has attracted extensive attention. PEG and PMPC are commonly used hydrophilic segments in amphiphilic polymers. In the core-shell micelles with hydrophobic segments as the core and hydrophilic segments as the shell formed with hydrophobic segments, PEG and PMPC have strong hydrophilic Water-based, prevents the protein in the blood from adsorbing the micelles, thereby reducing the conditioning effect, reducing the phagocytosis of the micelles by macrophages and prolonging the circulation time in the blood. [0003] Although PEG is ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08F287/00C08F220/18C08F293/00A61K47/32A61K9/107
CPCA61K9/1075A61K47/32C08F287/00C08F293/00C08F220/1804
Inventor 侯信陈宁李思迪原续波赵瑾龙丽霞
Owner TIANJIN UNIV
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