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A dendritic gene drug carrier and its preparation and application

A dendritic and product technology, applied in gene therapy, drug combination, anti-tumor drugs, etc., can solve the problems of cytotoxicity and poor degradation

Inactive Publication Date: 2017-02-22
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is a certain contradiction between the transport efficiency and self-toxicity of dendrimers. High-generation dendrimers have good transport efficiency, but exhibit obvious cytotoxicity due to poor degradation.

Method used

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  • A dendritic gene drug carrier and its preparation and application
  • A dendritic gene drug carrier and its preparation and application
  • A dendritic gene drug carrier and its preparation and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Example 1: Preparation of the carrier material 8armPEG-SS-PEG-Dendrimer G2 (PSPG2s) and carrying drugs and genes. (Dendrimer is AB3-Dendrimer G2, 8armPEG is 15000Da, NHS-PEG-OH is 2000Da, linker is CDI, drug is doxorubicin, gene is blank reporter gene DNA)

[0080] (1) AB 3 - Synthesis of Dendeimer G2

[0081] Weigh 445.6 mg of compound 1 and dissolve it in 15 ml of dichloromethane, add 871 mg of 1-hydroxy-7-azobenzotriazole (HOAt) and 3 ml of triethylamine, stir at room temperature for 10 minutes, then add 2.1 g of N-tert-butoxycarbonylethylenediamine, then slowly add 4.05 g of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDCI) at 0°C After the addition, keep the temperature at 0°C for 1 hour, and then react at room temperature for 4 hours. After the reaction was completed, 30 milliliters of ethyl acetate was added to the reaction solution, and 20 milliliters of the organic phase was washed three times with 0.4 mol / liter hydrochloric acid, three time...

Embodiment 2

[0097] Example 2: Characterization of materials

[0098] (1) AB 3 -Characterization of Dendrimer G2

[0099] figure 2 for AB 3 -H NMR and C NMR spectra of Dendrimer G2, image 3 for AB 3 -The high-resolution mass spectrum (MALDI-TOF MS) spectrum of Dendrimer G2 is basically consistent with the theoretical molecular weight of 5604, indicating that AB 3 - The preparation method of Dendrimer G2 is feasible.

[0100] (2) Synthesis and characterization of 8armPEG-SS-PEG-Dendrimer G2

[0101] Figure 4 It is eight-branched polyethylene glycol (8arm-PEG), eight-branched polyethylene glycol (8arm-PEG-SS-PEG) linked by disulfide bonds to straight-chain polyethylene glycol, and the second generation of AB 3 type dendrimers (AB 3 -Dendrimer G2), the final product dendritic polycation material (8armPEG-SS-PEG-Dendrimer G2, PSPG2s) H NMR spectrum, the displacement of each inactive hydrogen atom in the figure is shown in the figure, the NMR of the final product PSPG2s The hydroge...

Embodiment 3

[0102] Example 3: Ability of Compounds to Carry Genes

[0103] Image 6 (a) is Dendrimer G2 / DNA and PSPG2s / DNA with 4 access ratios (PSPG2s-2 / 4 / 6 / 8 respectively represent the molar ratio of 8arm-PEG and Dendrimer G2 in the dendritic polycation compound PSPG2s is 2 / 4 / 6 / 8) Retardation test of agarose gel electrophoresis carrying DNA at different N / P ratios. The figure shows that compounds such as PSPG2s can effectively carry DNA, and the efficiency is higher than that of Dendrimer G2 that exists alone. Figure (b) is the agarose gel electrophoresis retardation test of PSPG2s-2 / 4 / 6 / 8 carrying RNA under different N / P ratios. The figure shows that compounds such as PSPG2s can also effectively carry RNA.

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Abstract

The invention provides biodegradable dendritic cationic polymer with a high efficiency and low toxicity. Low-algebraic dendritic cationic polymer with low toxicity is linked to a water-soluble core with good biocompatibility through disulfide bonds to form polymer with a high molecular weight. The biodegradable dendritic cationic polymer is high in gene and drug delivery efficiency, is degradable in cells and effectively relieves contradiction between the delivery efficiency and toxicity of the dendritic cationic polymer. Multi-branch water-soluble polymer and the low-algebraic dendritic cationic polymer which are easily available and simple are adopted as raw materials, so that the cost is low. A synthetic method is simple, mostly comprises room-temperature reactions, and is free of rigorous reaction conditions such as no water and no oxygen. Post-treatment generally adopts extraction or dialysis as a separation method, and operation is simple. A structure formula of the biodegradable dendritic cationic polymer is shown in the specification.

Description

technical field [0001] The invention belongs to the field of biotechnology, and relates to a class of high-efficiency and low-toxicity biodegradable dendritic gene drug carriers, in particular to a class of dendritic polycation materials and their preparation methods and applications. Background technique [0002] Gene drug therapy is a method for treating cancer that has emerged in the past two decades. Its basic strategy is to introduce foreign genes or anticancer drugs into target cells through carrier transport and exert their effects, so as to achieve the purpose of treating cancer. In gene drug therapy, the transport of genes and drugs is a very important part. For the transport carrier, it is important to efficiently transport a certain amount of target genes and drugs to target cells so that they can play a role in a safe, effective and stable manner. the bare minimum. The vectors currently used in gene therapy are mainly divided into two categories: viral vectors a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G81/00C08G65/48C08G83/00A61K48/00A61K47/48A61P35/00
Inventor 王凯汤谷平周峻
Owner ZHEJIANG UNIV
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