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Polycationic gene carriers formed of endogenous amino group-bearing monomers

An endogenous, cationic polymer technology, applied in the field of polycationic gene carriers formed by endogenous amino-carrying monomers, can solve the problems of complex structure and diverse metabolism in the carrier system.

Inactive Publication Date: 2011-06-01
金拓
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these types of macromolecules are often metabolized in vivo with complex structures and carrier systems.

Method used

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  • Polycationic gene carriers formed of endogenous amino group-bearing monomers
  • Polycationic gene carriers formed of endogenous amino group-bearing monomers
  • Polycationic gene carriers formed of endogenous amino group-bearing monomers

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1. Synthesis of polyspermine urethane with uncertain structure (see figure 1 A and 1B)

[0041] Spermine is polymerized via urethane bonds. Dissolve 1 equivalent of ethylene glycol dicarbamate or butylene glycol dicarbamate in chloroform, and slowly add dropwise to the stirred spermine dissolved in chloroform and triethylamine under a nitrogen atmosphere at 0°C In solution. After that, the reaction solution was warmed to room temperature and stirred for 12 hours. After evaporating and removing the solvent, the obtained polymer particles are dissolved in water and dialyzed with a dialysis bag (Mw=3500) to remove small molecular fragments. The final product was stored at -20°C after lyophilization.

Embodiment 2

[0042] Example 2. Synthesis of linear polyspermine urethane (see figure 2 A and 2B)

[0043] In order to synthesize linear polyspermine urethane, the two primary amino groups of spermine need to be protected, that is, under nitrogen, add trifluoroethyl acetate to the spermine solution (methanol as the solvent) at -78°C, and then Stirring was continued for 1 hour at 0°C. Product N 1 , N 14 -Bis(trifluoroacetyl)spermine is obtained by evaporating the solvent, and its polymer is obtained by the procedure of Example 1. After the completion of the polymerization reaction, the removal of the protective group of the amino group and the trifluoroacetate group was achieved by treating the polymerization product with 30wt% ammonia water (stored in a sealed state) at 60°C for 8 hours. The final polycation is finally obtained by removing small molecular fragments with a 3500 mass dialysis membrane.

Embodiment 3

[0044] Example 3. Synthesis of linear polyspermine amide (see image 3 )

[0045] The synthesis method of linear polyspermine amide bond is the same as that of polyspermine urethane, except that 1 equivalent of ethylene glycol dicarbamate or 1,4-butanediol dicarbamate is 1 equivalent Succinyl chloride instead.

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Abstract

The present invention is directed to a design of and a method to synthesize polycations for gene (DNA and RNA) delivery. According to this design, the polycations (also said cationic polymers) are formed by polymerization of endogenous monomers bearing sufficient amino groups through degradable bonds with linker molecules or with themselves. The amino group-bearing monomers are those naturally existing in or nontoxic to human body. The linker molecules are those which are not only degradable to nontoxic fragments but also able to release the amino group-bearing monomers in their native state upon degradation. Some examples for the endogenous amino group-bearing monomers are spermine, spermidine, serine or N,N-dimethyl serine, and histidine. Examples for the degradable chemical bonds formed between the amino group-bearing monomers are carbamate, imine, amide, carbonate, and ester. In order to improve degradability or proton sponging effect, low pKa (<8) amino group(s) or other electrondonating group(s) is incorporated in the linker between the two (or three) reactive groups for linking the amino group-bearing monomers. These polycationic carrier systems can be used for nano-encapsulation and transfection of gene materials.

Description

[0001] Cross-references and related applications [0002] This application claims the priority of U.S. serial number 61,023,426 filed on January 25, 2008 and U.S. serial number 61 / 087,958 filed on August 11, 2008. The contents of these two applications are incorporated into this application by reference. [0003] In this application, various publications are referenced. The contents of these publications are incorporated into this application in their entirety by reference to more fully describe the state of the technical field of the present invention. Invention field [0004] The present invention confirms the synthesis and assembly method and design concept of polycationic gene (and RNA) carrier that can be degraded into endogenous monomer. Background of the invention [0005] There is now enough evidence that nucleotides of a given sequence can be used as therapeutic agents for drug therapy, immunotherapy and tissue regeneration therapy by turning on (expressing) or turning off (...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12N11/08A61K9/50A61K47/30A61K48/00
CPCA61K9/1271A61K9/1272A61K48/00C12N15/87A61K47/34A61P43/00
Inventor 金拓杜子秀
Owner 金拓
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