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A supramolecular assembly and preparation method for targeted delivery of small interfering RNA

A supramolecular assembly and targeted delivery technology, applied in the fields of genetic material components, drug combinations, pharmaceutical formulations, etc., can solve the problems of high cost, low efficiency of gene transfection, and the lack of widespread development of viral vectors. Positive enhancement, improved gene transfection efficiency, and low cytotoxic side effects

Inactive Publication Date: 2018-01-23
NANKAI UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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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 developed, so the design and construction of targeted gene delivery systems with biocompatibility and controlled release functions and high gene transfection efficiency have become the forefront research hotspots

Method used

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  • A supramolecular assembly and preparation method for targeted delivery of small interfering RNA
  • A supramolecular assembly and preparation method for targeted delivery of small interfering RNA
  • A supramolecular assembly and preparation method for targeted delivery of small interfering RNA

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Embodiment

[0031] A supramolecular assembly for targeted delivery of small interfering RNA, a quaternary supramolecular assembly based on β-cyclodextrin modified hyaluronic acid, adamantane polyamine compound, cucurbituril [6] and small interfering RNA synthesis, The molecular formula of β-cyclodextrin modified hyaluronic acid is (C 14h 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, and the chemical formula of the adamantane polyamine compound is C 32 h 56 Br 4 N 6 o 4 ; The quaternary supramolecular assembly is based on the strong non-covalent interactions between β-cyclodextrin and adamantane and the adamantane polyamine chain and cucurbituril [6], and the electrostatic interaction between the adamantane polyamine chain and small interfering RNA Based on the interaction, supramolecular nanoparticles with hydrophilic hyaluronic acid as the shell are formed, and the particle size of the nanoparticles is 30-40nm....

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Abstract

A supramolecular assembly targeting delivery of small interfering RNA, which is a quaternary supramolecular assembly based on β-cyclodextrin modified hyaluronic acid, adamantane polyamine compound, cucurbituril [6] and small interfering RNA synthesis, The quaternary supramolecular assembly is characterized by strong non-covalent interactions between β‑cyclodextrin and adamantane, adamantane polyamine chains and cucurbituril [6], and electrostatic interactions between adamantane polyamine chains and small interfering RNAs. Based on the action, supramolecular nanoparticles with hydrophilic hyaluronic acid as the shell are formed. The advantages of the present invention are: the supramolecular assembly has simple synthesis and construction routes, low production cost and high yield, and is suitable for scale-up synthesis and practical production applications; the hyaluronic acid receptor overexpressed on the surface of malignant tumor cells is The endocytosis of the mediator brings the quaternary supramolecular assembly into cancer cells in a targeted manner, achieving effective silencing of exogenous gene expression, and at the same time significantly reducing toxic and side effects.

Description

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

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K48/00A61K47/61A61P35/00
Inventor 刘育张瀛溟杨洋
Owner NANKAI UNIV
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