Six-arm star-shaped amphiphilic polymer and preparation method thereof, and nano hydrogel drug-loading system prepared from six-arm star-shaped amphiphilic polymer

An amphiphilic polymer and polymer technology, which can be used in organic active ingredients, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve problems such as responsive exploration, and achieve simple operation and high performance pH-responsive, mild reaction conditions

Active Publication Date: 2020-03-27
GUANGDONG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Patent application CN109431971A discloses a drug-loaded hydrogel that can be used for local injection, including but not limited to the treatment of solid tumors such as intratumoral injection and paratumoral injection, but has not further explored its responsiveness

Method used

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  • Six-arm star-shaped amphiphilic polymer and preparation method thereof, and nano hydrogel drug-loading system prepared from six-arm star-shaped amphiphilic polymer
  • Six-arm star-shaped amphiphilic polymer and preparation method thereof, and nano hydrogel drug-loading system prepared from six-arm star-shaped amphiphilic polymer
  • Six-arm star-shaped amphiphilic polymer and preparation method thereof, and nano hydrogel drug-loading system prepared from six-arm star-shaped amphiphilic polymer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] Example 1: Preparation of six-arm star-shaped amphiphilic polymer 6-AS-PCL-PAA-PPEGMA

[0063] (1) Preparation of macromolecular initiator 6-AS-PCL: get 100mL dry reaction bottle, cool after 10 minutes with alcohol lamp baking, stir bar, initiator dipentaerythritol (1.27g, 5mmol) are added in the reaction bottle, and use Sealed with a rubber stopper. After evacuating-argon for 3 times, add monomer ε-caprolactone (34.22g, 300mmol) under the protection of argon. After heating in an oil bath at 150°C for 20 minutes, add Sn(Oct) 2 (0.1wt%ofε-CL, 0.03g), then stop heating after 24h of reaction, cool the eggplant-shaped bottle, add 30mL of anhydrous THF to dissolve the white sticky solid, in 300mL of cold methanol / water (1:1, v / v) After precipitation, filter to remove unreacted monomer and catalyst, and obtain a white powdery solid after vacuum drying (or the product is vacuum dried at 40°C and 35mb for 24h). The synthetic reaction formula is shown in formula (1). The mol...

Embodiment 2

[0079] Example 2: Preparation of six-armed star-shaped amphiphilic polymer 6-AS-PCL-PAA-PPEGMA

[0080] (1) Preparation of macromolecular initiator 6-AS-PCL: get 100mL dry reaction bottle, cool after 10 minutes with alcohol lamp baking, stir bar, initiator dipentaerythritol (1.27g, 5mmol) are added in the reaction bottle, and use Sealed with a rubber stopper. After evacuating-argon for 3 times, add monomer ε-caprolactone (17.11g, 150mmol) under the protection of argon, and perform three freezing-pumping-heating cycles with liquid nitrogen, then place After heating in an oil bath at 130°C for 20 minutes, add Sn(Oct) 2 (0.1wt%ofε-CL, 0.03g), then stop heating after 24h of reaction, cool the eggplant-shaped bottle, add 30mL of anhydrous THF to dissolve the white sticky solid, in 300mL of cold methanol / water (1:1, v / v) After precipitation, filter to remove unreacted monomer and catalyst, and obtain a white powdery solid after vacuum drying (or the product is vacuum dried at 40°C a...

Embodiment 3

[0084] Example 3: Preparation of six-armed star-shaped amphiphilic polymer 6-AS-PCL-PAA-PPEGMA

[0085] (1) Preparation of macromolecular initiator 6-AS-PCL: get 100mL dry reaction bottle, cool after 10 minutes with alcohol lamp baking, stir bar, initiator dipentaerythritol (1.27g, 5mmol) are added in the reaction bottle, and use Sealed with a rubber stopper. After evacuating-argon for 3 times, add the monomer ε-caprolactone (51.33g, 450mmol) under the protection of argon. After heating in an oil bath at 130°C for 20 minutes, add Sn(Oct)2 (0.1wt% ofε-CL, 0.03g), then stop heating after 48 hours of reaction, cool the eggplant-shaped bottle, and add 30mL of anhydrous THF to dissolve the white Viscous solid, filtered after precipitation in 300 mL of cold methanol / water (1:1, v / v) to remove unreacted monomer and catalyst, gave a white powdery solid after vacuum drying (or product at 40 °C, 35 mb vacuum Dry 24h). The synthetic reaction formula is shown in formula (1).

[0086] ...

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Abstract

The invention belongs to the technical field of biomedical high-molecular polymer materials, and discloses a six-arm star-shaped amphiphilic polymer and a preparation method thereof, and a nano hydrogel drug-loading system prepared from the six-arm star-shaped amphiphilic polymer. The six-arm star-shaped amphiphilic polymer has a structure as shown in the following formula (I), wherein x is equalto 5-15, y is equal to 50-70, and z is equal to 4-10. The proportion of each block of the polymer is easy to control, and a polymer micelle solution with a stable structure and a small particle size can be prepared. The invention also provides a nano drug-loading hydrogel with a uniform structure prepared on the basis of the polymer micelle solution. The prepared nano drug-loading hydrogel with auniform structure is expected to be applied to a delivery system loaded with hydrophobic anti-tumor drugs. R4 is shown in the specification.

Description

technical field [0001] The invention belongs to the technical field of biomedical polymer materials, and in particular relates to a six-armed star-shaped amphiphilic polymer, a preparation method thereof, and a nanometer hydrogel drug-loading system based on the amphiphilic polymer. Background technique [0002] Hydrogel is a class of materials with three-dimensional cross-linked hydrophilic network formed by water or hydrophilic solvents. Using their structural characteristics, they can contain various guest molecules with different physical and chemical properties, and can be expanded by swelling, diffusion and Release it by degradation etc. In the past few decades, hydrogels have been intensively studied and widely used in drug release, sustained release of perfume, and controlled release of pesticides. Among the various methods for preparing hydrogels, hydrogels containing polymer nanoparticles, dendrimers, and polymer micelles are widely used in many fields because the...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F293/00C08F8/12A61K9/06A61K31/704A61K47/34A61P35/00
CPCC08F8/12A61K9/06A61K47/34A61K31/704A61P35/00C08F2438/01C08F293/005
Inventor 易国斌林文静赵倩怡黄云薇王琦雯王伟明
Owner GUANGDONG UNIV OF TECH
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