Polypeptide and nucleic acid drug nanoparticles containing same

Abstract

The invention discloses a polypeptide and nucleic acid drug nanoparticles containing the same. The polypeptide comprises a first fragment with positive charges and a second fragment with a targeting function. The polypeptide is used as a nucleic acid drug transfer carrier; the first fragment of the polypeptide is combined with the nucleic acid gathering negative charges through the static effect to form a complex, and the second fragment is combined with a receptor on the surface of a liver cancer cell; the nucleic acid is concentrated on the liver cancer tissue through passive targeting and active targeting, thereby greatly improving the targeting property of the nucleic acid drug and reducing the dosage of the nucleic acid drug; the polypeptide-nucleic acid nanoparticles prepared by the method have good stability and high medication safety, and the size is 20-300nm; the preparation process is simple and controllable, and the production is easy to expand in a large scale.

Description

technical field [0001] The invention relates to a nucleic acid drug preparation, in particular to a polypeptide and nucleic acid drug nanoparticles containing the polypeptide. Background technique [0002] Liver cancer is one of the most common and most malignant tumors in the world, ranking sixth in the incidence of malignant tumors worldwide and third in its fatality rate. The number of cases of liver cancer in China accounts for 55% of the world, and it has become the second most lethal malignant tumor. More than 300,000 liver cancer patients die every year. One way to treat cancer is to use gene silencing caused by RNA interference. RNA interference (RNA interference, RNAi) is a phenomenon discovered and named in 1998 to inhibit the expression of homologous genes. It forms RNA-induced silencing complex (RISC) through small nucleic acid molecules and endogenous mRNA, and rapidly degrades targeted mRNA, thereby efficiently and specifically inhibiting the expression of ta...

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Problems solved by technology

[0003] However, RNA interference technology has not entered clinical tumor treatment for a long time, the main reasons are: (1) To realize the materials used in RNA interference technology, such as siRNA, microRNA, short hairpin RNA, duplex RNA, etc. It enters the cell, but RNA is a hydrophilic molecule with a high negative charge, and its fat solubility is extremely poor, so it cannot penetrate the cell membrane or be endocytosed by the cell. In vitro studies can use physical or chemical transfection reagents (such as lipofectamine) to allow RNA to enter cells, but it is difficult to achieve in vivo; (2) RNA has poor stability, and its half-life in plasma is only a few minutes. At the same time, due to its immunogenicity, it will be recognized by the immune system and quickly (3) RNA lacks targeting, even after entering the body, it cannot target specific tissues (such as tumor cells)

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