Unlock instant, AI-driven research and patent intelligence for your innovation.

Preparation method of environment response type radial copolymer

A star-shaped copolymer, environment-responsive technology, applied in the fields of polymer materials and biomedical engineering, can solve problems such as large side effects, inability to distinguish between intracellular and extracellular environments, insufficient tumor cell therapy, etc. The effect of drug utilization

Active Publication Date: 2013-05-01
TONGJI UNIV
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, there are still some deficiencies in the treatment of tumor cells by drug sustained release.
For example, chemotherapeutic drugs generally need to enter the tumor cells to produce curative effect, while the drug release behavior of traditional nanocarriers has no obvious difference between the inside and outside of the cell, and most drugs are released outside the cell, resulting in low bioavailability of the drug , side effects
The current common stimuli-responsive nanomicelles cannot distinguish between intracellular and extracellular environments, so it is of great significance to study smart drug-loaded nanomicelles capable of intracellular drug delivery

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Preparation method of environment response type radial copolymer
  • Preparation method of environment response type radial copolymer
  • Preparation method of environment response type radial copolymer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Weigh 4.0 g of carboxyl-terminated polyethylene glycol monomethyl ether containing disulfide bonds with a molecular weight of 2000, 0.26 g of 2,2-bis(bromomethyl)-1,3-propanediol, N,N'-bicyclic Hexylcarbodiimide 2.0g, 4-dimethylaminopyridine 0.1g, dissolved in dichloromethane, reacted at room temperature for 20 hours, filtered to remove N,N'-bicycloethylurea, concentrated the filtrate and precipitated it twice with ether , filtered and vacuum-dried to obtain two-arm polyethylene glycol containing two bromine groups; the two-arm polyethylene glycol containing two bromine groups was dissolved in N,N'-dimethylformamide, Add 0.3g of sodium azide, react at 50°C for 12 hours, cool and filter. The filtrate was evaporated under reduced pressure to remove N,N'-dimethylformamide, dissolved in dichloromethane, filtered, and the filtrate was concentrated and precipitated in ether, filtered and dried in vacuo to obtain a two-arm polyethylene oxide containing two azide groups. Diol;...

Embodiment 2

[0028]Weigh 2.0 g of carboxy-terminated polyethylene glycol monomethyl ether containing disulfide bonds with a molecular weight of 1000, 0.26 g of 2,2-bis(bromomethyl)-1,3-propanediol, N,N'-bicyclic Hexylcarbodiimide 1.0g, 4-dimethylaminopyridine 0.1g, dissolved in tetrahydrofuran, reacted at room temperature for 20 hours, filtered to remove N,N'-bicycloethylurea, concentrated the filtrate, precipitated with ether, filtered and vacuum Dry to obtain two-arm polyethylene glycol containing two bromine groups; dissolve the two-arm polyethylene glycol containing two bromine groups in N,N'-dimethylformamide, add 0.5g alkene Sodium nitride, react at 80°C for 7 hours, cool and filter. The filtrate was evaporated under reduced pressure to remove N, N'-dimethylformamide, dissolved in dichloromethane, filtered, and the filtrate was concentrated and precipitated with ether, filtered and dried in vacuo to obtain a two-armed polyethylene glycol containing two azide groups. Alcohol; the two...

Embodiment 3

[0030] Weigh 8.0 g of carboxyl-terminated polyethylene glycol monomethyl ether with a molecular weight of 1900, 0.5 g of 2,2-bis(bromomethyl)-1,3-propanediol, N,N'-bicyclic Hexylcarbodiimide 3.0g, 4-dimethylaminopyridine 0.1g, dissolved in chloroform, reacted at room temperature for 32 hours, filtered to remove N,N'-bicycloethylurea, concentrated the filtrate, precipitated with ether, filtered and vacuum-dried to obtain two-arm polyethylene glycol containing two bromine groups; the two-arm polyethylene glycol containing two bromine groups was dissolved in N, N'-dimethylformamide, and 0.5 g sodium azide, reacted at 50°C for 17 hours, cooled and filtered. The filtrate was evaporated under reduced pressure to remove N,N'-dimethylformamide, dissolved in dichloromethane, filtered, and the filtrate was concentrated and precipitated in ether, filtered and dried in vacuo to obtain a two-arm polyethylene glycol containing two azide groups. Diol; the two-armed polyethylene glycol conta...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention belongs to the fields of polymer materials and biomedical engineering, and particularly relates to a preparation method of an environment response type radial copolymer. The preparation method comprises the specific step of: simultaneously grafting hydrophilic disulfide-bond-containing carboxy-terminated ethylene glycol monomethyl ether and hydrophobic polyamino acid to the same core to form an amphipathic four-branch radial copolymer. The prepared four-branch radial copolymer has amphipathicity and reduction environment responsiveness. When the four-branch radial copolymer is used for preparing nano micelles to be used as a medicament carrier, in internal reduction environment of tumor cells, the disulfide bond breaks, so the hydrophilic chain on the surface of the micellesfalls off, the structure of the micelles is destroyed, and a medicament is selectively released to the inside of the tumor cells, thus the utilization rate of the medicament is effectively improved.

Description

technical field [0001] The invention belongs to the fields of polymer materials and biomedical engineering, and in particular relates to a preparation method of an environment-responsive star-shaped copolymer. Background technique [0002] At present, in view of the shortcomings of fast drug metabolism in the body, short half-life, frequent and large doses, and poor targeting, drug carriers have begun to be widely studied. After the drug and the carrier form a drug-loading system, the absorption and distribution of the drug are affected by the physical and chemical properties of the carrier. Selecting appropriate carrier materials according to clinical requirements can not only deliver drugs to target organs, but also play a beneficial role in drug carrier properties and pharmacological activity. [0003] However, there are still some deficiencies in the treatment of tumor cells by drug sustained release. For example, chemotherapeutic drugs generally need to enter the tumo...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C08G69/40C08G69/08C08G65/48A61K9/00A61K47/34
Inventor 李建波任杰屈阳
Owner TONGJI UNIV