Tumor targeted gene delivery system and application of same

Abstract

The invention discloses a tumor targeted gene delivery system which includes: a polyethyleneimine derivative connected with a difunctional peptide, wherein the polyethyleneimine derivative is pluronic-modified low-molecular-weight polyethyleneimine and the difunctional peptide contains DR5 oligopeptide having specifically affinity with a DR5 acceptor, and cell-penetrating peptide TAT. The invention also provides a preparation method and an application of the gene delivery system. The tumor targeted gene delivery system is high in transfection efficiency, is high in tumor cell and tissue targeting property and is excellent in safety and in-vivo and in-vitro stability, can achieve oriented killing effect on tumor cells, is low in toxic and side effects, is high in therapeutic index and has a wide application prospect.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to a bifunctional peptide-modified tumor-targeted gene delivery system and its application. Background technique [0002] Tumor has become a major disease that threatens human life and health, and there is still a lack of effective treatment methods. Traditional drugs for treating tumors have poor curative effect, large side effects and poor targeting effect. The biological cause of tumor development is gene mutation. Targeted therapy to diseased genes and tumor cells is currently the most powerful treatment method, and it is also the most active field of modern research on tumor treatment. [0003] To successfully implement gene therapy, three key factors must be in place: targeted therapeutic gene; gene delivery system; gene expression regulation system. Among them, the gene delivery system is the core technology of gene therapy. An ideal gene delivery carrier system should hav...

AI Technical Summary

Problems solved by technology

However, PEI still has two outstanding problems as a gene carrier: first, there is a contradiction between transfection efficiency and cytotoxicity

Although small molecule PEI has low cytotoxicity, it is easy to dissociate with DNA under physiological ion concentration, resulting in poor transfection effect; although PEI with a molecular weight above 20kDa has a relatively ideal transfection efficiency, because the surface of PEI is rich in positive High molecular weight PEI exhibits strong cytotoxicity due to its charge and non-degradability in vivo

Second, polyethyleneimine has poor targeting

[0006] However, the bifunctional peptide-modified polyethyleneimine derivatives composed of DR5 short peptides and TAT cell-penetrating peptides and their applications have not been reported at home and abroad.

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