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RAFT (reversible addition fragmentation chain transfer) preparation method of polylysine derivative

A technology of polylysine and its derivatives, which can be used in pharmaceutical formulations, genetic material components, gene therapy, etc. It can solve problems such as poor DNA burden capacity, poor molecular weight and distribution control, and achieve excellent biocompatibility , the effect of extensive application value

Inactive Publication Date: 2012-11-14
JIANGNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

In the current research on polylysine, there are few studies on polylysine derivatives obtained by free radical polymerization
However, the polymer obtained by traditional free radical polymerization has poor control over the polymer structure, molecular weight and distribution, and the cytotoxicity caused by high molecular weight polylysine and the poor ability to carry DNA at low molecular weight make it difficult to The control of polymer structure is particularly important

Method used

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  • RAFT (reversible addition fragmentation chain transfer) preparation method of polylysine derivative
  • RAFT (reversible addition fragmentation chain transfer) preparation method of polylysine derivative
  • RAFT (reversible addition fragmentation chain transfer) preparation method of polylysine derivative

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Effect test

Embodiment 1

[0014] Weigh 1.00g of hydroxyethyl methacrylate (HEMA) (7.684×10 -3 mol), trithiocarbonate 0.0839g (2.305×10 -4 mol), AIBN0.0128g (7.684×10 -5 mol), 4ml of tert-butanol, added to a 50ml reactor, protected by nitrogen gas for 30min before the reaction, heated up to 75°C under magnetic stirring, after 5h of reaction, cooled with ice water to stop the reaction, precipitated with cold ether three times, and then Under constant temperature drying to obtain homopolymer PHEMA, the product is white, molecular weight M n(GPC) =5.4×10 4 , the molecular weight distribution is 1.52.

Embodiment 2

[0016] Weigh Boc-protected lysine (Boc-L-lysine) 1.010g (2.15×10 -2 mol), PHEMA0.38g (7.6×10 -6 mol), DCC 0.793g (3.84×10 -3 mol), DMAP 0.0202g (1.65×10 -4 mol), DMF15ml, added to a 50ml reactor, kept the temperature at 25°C under magnetic stirring, after 24 hours of reaction, the solvent was distilled off under reduced pressure, and precipitated in ether to obtain PHEMA-co-PHEMA-Boc-L-lysine copolymer , the product is pale yellow.

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Abstract

The invention provides an RAFT (reversible addition fragmentation chain transfer) preparation method of polylysine derivative, belonging to the technical field of functional material. The preparation method comprises the following steps of: taking hydroxyethyl methacrylate (HEMA) and lysine (L-lysine) as raw materials, taking trithiocarbonate as a chain transfer agent, sequentially adopting a reversible addition fragmentation chain transfer (RAFT) free radical polymerization method to obtain PHEMA homopolymer with different chain segment lengths, wherein the molecular weight of the PHEMA homopolymer is controllable, and obtaining PHEM-co-PHEMA-Boc-L-lysine copolymer by an esterification. The preparation method is simple, the prepared PHEM-co-PHEMA-L-lysine copolymer has biocompatibility, the composite formed by the electrostatic interaction between the PHEM-co-PHEMA-L-lysine copolymer and the plasmid DNA (pDNA) can be widely applicable to the fields such as the drug slow-release system, the gene therapy and the like.

Description

technical field [0001] The invention discloses a RAFT preparation method of polylysine derivatives, which belongs to the technical field of functional materials. Background technique [0002] With the development and application of new technologies, various new polymer materials have sprung up, playing a pivotal role in people's production and life. However, while polymer materials bring convenience to people's lives and improve the quality of life, a large amount of waste after use is also increasing day by day, causing a non-negligible negative impact on the environment on which human beings depend. The used monomer hydroxyethyl methacrylate (HEMA) of the present invention is an environment-friendly raw material, and lysine (L-lysine) is an amino acid required by the human body, and the research on their copolymer preparation, structure and performance has caused extensive attention of researchers. Among them, hydroxyethyl methacrylate (HEMA) is a very important monomer,...

Claims

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Application Information

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IPC IPC(8): C08F8/14C08F120/28C08F2/38A61K47/34A61K48/00
Inventor 陈明清娄宇倪忠斌张明施东健
Owner JIANGNAN UNIV
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