Supermolecular assembly for small interfering RNA targeting delivery and preparation method

A technology of supramolecular assembly and targeted delivery, which is applied in the direction of genetic material components, medical preparations of non-active ingredients, drug combinations, etc., and can solve the problem of the lack of extensive development of viral vectors, high cost, and low efficiency of gene transfection and other problems, to achieve the effect of low cytotoxicity and side effects, enhanced electropositivity, and improved gene transfection efficiency

Inactive Publication Date: 2015-08-19
NANKAI UNIV
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Problems solved by technology

However, the low efficiency of gene transfection has become a bottleneck restricting the wide application of this method.
Due to potential safety issues and high costs, viral vectors have not been widely devel

Method used

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  • Supermolecular assembly for small interfering RNA targeting delivery and preparation method
  • Supermolecular assembly for small interfering RNA targeting delivery and preparation method
  • Supermolecular assembly for small interfering RNA targeting delivery and preparation method

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Embodiment

[0031] A supramolecular assembly for targeted delivery of small interfering RNA is a quaternary supramolecular assembly based on β-cyclodextrin modified hyaluronic acid, adamantane polyamine compounds, cucurbituril [6] and small interfering RNA synthesis, The molecular formula of β-cyclodextrin modified hyaluronic acid is (C 14 H 21 NO 11 ) 98 (C 58 H 95 N 3 O 44 ) 17 , An average of 17 cyclodextrin units are modified on one polymer chain, the chemical formula of adamantane polyamine compound is C 32 H 56 Br 4 N 6 O 4 ; The quaternary supramolecular assembly uses strong non-covalent interactions between β-cyclodextrin and adamantane, as well as between adamantane polyamine chain and cucurbituril [6], and static electricity between adamantane polyamine chain and small interfering RNA Based on the interaction, supramolecular nanoparticles with hydrophilic hyaluronic acid as the shell are formed, and the diameter of the nanoparticles is 30-40nm.

[0032] A method for preparing the su...

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Abstract

The invention relates to a supermolecular assembly for small interfering RNA targeting delivery. The supermolecular assembly is a four-element supermolecular assembly synthesized on the basis of beta-cyclodextrin modified hyaluronic acid, an adamantine polyamine compound, cucurbituril [6] and small interfering RNA. The four-element supermolecular assembly is based on the strong non-covalent interaction between beta-cyclodextrin and adamantine and between adamantine polyamine chain and cucurbituril [6], and the electrostatic interaction between the adamantine polyamine chain and small interfering RNA, and forms supermolecular nanoparticles with hydrophilic hyaluronic acid as the shell. The supermolecular assembly provided by the invention has the advantages of simple synthesis and construction route, low production cost and high yield, and is suitable for amplified synthesis and actual production application. Through the endocytosis of a malignant tumor cell surface overexpressed hyaluronic acid receptor as a medium, the four-element supermolecular assembly can be brought into cancer cells targetedly, thus realizing effective silencing to exogenous gene expression and significantly reducing the toxic and side effect at the same time.

Description

【Technical Field】 [0001] The invention relates to the technical field of targeted gene delivery, in particular to a supramolecular assembly for targeted delivery of small interfering RNA and a preparation method. 【Background technique】 [0002] In today's society, due to the influence of haze, environmental pollution, ionizing radiation, food safety, genetics and other factors, the incidence of cancer is increasing year by year, which seriously threatens human health. For this reason, surgical treatment, chemotherapy and radiotherapy have been widely used as the main methods of clinical treatment of cancer. However, these therapies have not been able to conquer cancers by humans due to their poor therapeutic effects, easy recurrence, and serious side effects. Therefore, chemists, materials scientists and biomedical workers have developed various drug delivery systems such as liposomes, inorganic nanoparticles, vesicles and carbon nanomaterials to enhance the biocompatibility and...

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Application Information

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IPC IPC(8): A61K48/00A61K47/48A61P35/00
Inventor 刘育张瀛溟杨洋
Owner NANKAI UNIV
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