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Delivery system capable of realizing co-loading gene and drug, preparation method of delivery system, and application

A gene and anti-tumor drug technology, applied in the field of nano-pharmaceutical preparations, can solve the problem of not considering the influence of the treatment effect, and achieve the effect of improving the encapsulation rate and drug loading capacity

Active Publication Date: 2017-05-31
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the vast majority of carriers are mainly based on the synergistic effect of drugs and genes, without considering the impact of the release sequence of the two on the therapeutic effect

Method used

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  • Delivery system capable of realizing co-loading gene and drug, preparation method of delivery system, and application
  • Delivery system capable of realizing co-loading gene and drug, preparation method of delivery system, and application
  • Delivery system capable of realizing co-loading gene and drug, preparation method of delivery system, and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] (1) Use divergence method or convergence method or divergence-convergence method to synthesize more than two generations of dendrimers (refer to the method described in the patent literature with publication number CN 103554923A), or use commercially available dendrimers molecular;

[0062] (2) Protect the peripheral functional groups of the resulting dendrimers containing amino groups and / or guanidine groups at the periphery, expose only one or two functional groups at one end, and then connect one end of the dendrimers through the exposed functional groups branch reduction sensitive keys;

[0063] (3) The other end exposed to the reduction-sensitive bond is grafted with a hydrophobic antineoplastic drug or its prodrug;

[0064] (4) Remove the amino and / or guanidine protecting groups on the periphery of the dendrimer to obtain a dual-response lipid prodrug.

[0065] As an alternative, in the above step (3), a hydrophobic antitumor drug with a suitable active group ca...

Embodiment 2

[0068] (1) Dissolve the plasmid DNA or RNA in sterile DEPC water (0.1% diethylpyrocarbonate) to prepare a gene solution of appropriate concentration; or mix the lipid prodrug prepared in Example 1 and the commercially available lipid Proteolytic molecules (DOPE, DSPE, cholesterol, etc.) or amphiphilic molecules that replace the hydrophobic groups of lipid prodrugs with alkane chains are mixed at a ratio of 1:0~1:1 and added to HBG buffer solution by solution dispersion method to prepare 0.1~10 mg / mL solution A.

[0069] (2) Mix the solution A obtained in the above steps with the gene solution, and incubate at room temperature for 20 minutes to obtain a cotransport drug delivery system.

[0070] Optionally, the mass ratio of the lipid prodrug to the gene is 0.1:1-50:1.

[0071] As an option, other drugs or magnetic nanoparticles can also be added in the above step (2) to prepare ternary or quaternary compounds.

[0072] Experiments have shown that the obtained co-transport dr...

Embodiment 3

[0073] Example 3: Preparation of second-generation arginine-cystamine-succinic anhydride-camptothecin (Arg(G2)-SS-SUC-CPT)

[0074] Take 1 mmol of camptothecin (CPT) and 3 mmol of succinic anhydride (SUC) at 0°C under nitrogen protection, add dichloromethane solvent, slowly drop 3 mmol of condensing agent (1,8-diazabicyclo [5.4.0] Undec-7-ene (DBU)); then react at room temperature for 4 hours, after the reaction, add water to terminate the reaction. The resulting solution was precipitated with 1% HCl solution. The precipitate was washed successively with 1% HCl solution and water to obtain succinic anhydride-camptothecin.

[0075] Take succinic anhydride-camptothecin, monoprotected cystamine, condensation agent (such as: 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride EDC, catalyst 1-hydroxybenzene Triazole (HOBt), base (N, N-diisopropylethylamine DIPEA) according to the molar ratio of 1: 1: 2: 2: 4, at 0 ° C, under nitrogen protection conditions, add dichlorometh...

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Abstract

The invention discloses a delivery system capable of realizing co-loading a gene and a drug, a preparation method of the delivery system, and application. The invention belongs to the technical field of nano-drug preparations. The delivery system capable of realizing co-loading the gene and the drug is formed by combining the gene and positive ion pharmacosomes formed by self-assembly of an environmental response type lipophilic prodrug. The lipophilic prodrug is formed by connecting the head of a hydrophilic dendrimer to a hydrophobic antineoplastic drug or a prodrug of the hydrophobic antineoplastic drug by using an environmentally sensitive bond. The environmentally sensitive bond can break under specific environmental conditions, so that the hydrophobic antineoplastic drug or the prodrug of the hydrophobic antineoplastic drug can be separated from the hydrophilic dendrimer, and the disassembly of the positive ion pharmacosomes is caused to release the gene. The gene can be compressed by the pharmacosomes to form the drug co-delivery system while the encapsulation rate and the drug loading capacity are improved by the pharmacosomes. The effects of gene and drug synergy therapy or sequential therapy can be realized.

Description

technical field [0001] The invention belongs to the technical field of nano-pharmaceutical preparations, and relates to a delivery system capable of realizing gene and drug co-loading, a preparation method and application thereof. [0002] technical background [0003] Due to the three characteristics of unlimited proliferation, transformation and easy transfer of tumor cells, the treatment of tumors has always been a major problem that plagues human health. However, with the deepening of tumor treatment research, it has been proved that a single chemotherapy method is difficult to achieve a good therapeutic effect. More and more evidence shows that the combination of drugs and genes is more effective than independent use of drugs or genes in inhibiting tumor proliferation and migration. At the same time, in order to obtain the greatest win-win effect, the optimal release sequence of the therapeutic agent is to release the gene first to complete the transfection, and then re...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/64A61K45/06A61K48/00A61K31/4745A61K31/4184A61P35/00A61P11/06A61P9/00C12N15/87
CPCA61K31/4184A61K31/4745A61K45/06A61K48/005C12N15/87
Inventor 聂宇姜倩顾忠伟陈晓冰梁鸿
Owner SICHUAN UNIV
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