Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Biodegradable cationic polymer and application thereof

A cationic polymer, cationic technology, used in genetic material components, medical preparations with inactive ingredients, gene therapy, etc., can solve the problems of high toxicity in vivo, inability to compress siRNA well, low efficiency, etc., to strengthen the concentration of drugs. effect on symptoms

Inactive Publication Date: 2010-06-16
SUZHOU UNIV
View PDF0 Cites 13 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, PDMAEMA does not compress siRNA well and is inefficient in siRNA release
In addition, since PDMAEMA cannot be degraded in vivo, high molecular weight PDMAEMA is difficult to excrete from the body, and its toxicity in vivo is high.

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
  • Biodegradable cationic polymer and application thereof
  • Biodegradable cationic polymer and application thereof
  • Biodegradable cationic polymer and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Embodiment one, RAFT polymerization obtains triblock copolymer PDMAEMA 17 -PCL 32 -PDMAEMA 17

[0036] Under argon protection, the initiator AIBN (1.0 mg, 6.2 μmol), the macromolecular RAFT reagent CPADN-PCL 32 -CPADN (0.13 g, 31 μmol), N,N-dimethylmethacrylate (DMAEMA) monomer (0.19 g, 1.24 mmol) and 1.5 mL of tetrahydrofuran were added to a 10 mL Schlenk vacuum-sealed bottle, and argon After aeration for 30 minutes, the bottle was placed in an oil bath at 60° C., stirred and reacted for 24 hours, precipitated in n-hexane, filtered, and vacuum-dried for 48 hours to obtain a triblock copolymer with a yield of 80%. NMR results show that its structure is PDMAEMA 17 -PCL 32 -PDMAEMA 17 . m n (GPC)=9200, M w / M n (GPC) = 1.15.

Embodiment 2

[0037] Embodiment two, RAFT polymerization obtains triblock copolymer PDMAEMA 58 -PCL 32 -PDMAEMA 58

[0038] Under the protection of argon, the initiator AIBN (1.0 mg, 6.2 μmol), the macromolecular RAFT reagent CPADN-PCL-CPADN (0.13 g, 31 μmol), N, N-dimethyl methacrylate monomer DMAEMA (0.71 g, 4.65mmol) and 1.5mL of tetrahydrofuran were added to a 10mL Schlenk vacuum-sealed bottle, and the bottle was placed in an oil bath at 60°C after passing argon for 30 minutes. After stirring and reacting for 24 hours, it was precipitated in n-hexane and filtered. , dried in vacuum for 48 hours to obtain a triblock copolymer with a yield of 72%. NMR results show that its structure is PDMAEMA 58 -PCL 32 -PDMAEMA 58 . m n (GPC)=21100, M w / M n (GPC) = 1.42.

Embodiment 3

[0039] Embodiment three, RAFT polymerization obtains triblock copolymer PDMAEMA 30 -PCL 32 -PDMAEMA 30

[0040] Under the protection of argon, the initiator AIBN (1.0 mg, 6.2 μmol), the macromolecular RAFT reagent CPADN-PCL-CPADN (0.13 g, 31 μ.mol), N, N-dimethyl methacrylate monomer DMAE MA (0.36g, 2.33mmol) and 1.5mL of tetrahydrofuran were added to a 10mL Schlenk vacuum-sealed bottle, and after 30 minutes of argon gas, the bottle was placed in an oil bath at 60°C. After stirring for 24 hours, the reaction was carried out in n-hexane Precipitate, filter, and vacuum dry for 48 hours to obtain a triblock copolymer with a yield of 75%. NMR results show that its structure is PDMAEMA 30 -PCL 32 -PDMAEMA 30 . m n (GPC)=14200, M w / M n (GPC) = 1.31.

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 discloses a biodegradable cationic polymer micelle, preparation and application thereof. The biodegradable cationic polymer micelle consists of a triblock copolymer. The triblock copolymer at least comprises a cationic hydrophilic segment and a biodegradable hydrophobic segment, wherein the cationic hydrophilic segment forms a shell of the polymer micelle; and the hydrophobic segment forms a core of the polymer micelle. The polymer micelle can load siRNA through electrostatic compounding to obtain steady polymer / siRNA composite particles, and the particles can effectively inhibit the expression of specific genes during in vitro transfection experiments; and the polymer micelle loaded with a hydrophobic medicament can also load the siRNA through electrostatic compounding to realize a method for synchronously loading the medicament and the siRNA, and the method has the double effect on pharmacological treatment and gene therapy.

Description

technical field [0001] The invention relates to a biodegradable cationic polymer and its application, in particular to a biodegradable cationic polymer and the application of the polymer to prepare medicine or / and siRNA carrier. Background technique [0002] Small molecule RNA interference (siRNA) technology can specifically inhibit the expression of target genes, and has broad application prospects in the treatment of diseases caused by gene overexpression or mutation (see: Dorsett Y, TuschlT Nat Rev Drug Discov 2004; 3(4) : 318-329; de Fougerolles A, et al. Nat Rev Drug Discov 2007; 6: 443-453). However, siRNA molecules have dual characteristics of nucleic acid and small molecule compounds, and are easily degraded by nucleases; their hydrophilic and anionic properties make it difficult to pass through lipid cell membranes, and the cell transfection efficiency is low (see: Castanotto D, Rossi JJ Nature 2009;457(7228):426-433). At present, the main solutions are: using che...

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
IPC IPC(8): C08F293/00C08G63/91A61K47/32A61K47/34A61K48/00
Inventor 朱彩虹罗思彬孟凤华朱秀林钟志远
Owner SUZHOU UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com