Mesoporous silica nanoparticles modified by nucleic acid aptamer targeting polyethylene glycol and preparation method thereof

A mesoporous silica and nucleic acid aptamer technology, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, active ingredients of heterocyclic compounds, etc., can solve problems such as easy aggregation, precipitation, and large particle size, and achieve Good biocompatibility, improved water dispersibility and sustained release ability
CN109044993AInactive Publication Date: 2018-12-21SOUTH CHINA UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SOUTH CHINA UNIV OF TECH
Publication Date
2018-12-21
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses mesoporous silica nanoparticles modified by nucleic acid aptamer targeting polyethylene glycol and a preparation method thereof. The method comprises the following steps: synthesizing mesoporous silica through TEOS(tetraethyl orthosilicate), CTAB(cetyltrimethyl ammonium bromide), alkali and water; modifying amino on the surface of the mesoporous silica through APTES (aminopropyltriethoxysilane) in an ethanol solution; and connecting the primary amine end group of the mesoporous silica to the carboxyl group of polyethylene glycol by reacting, connecting the terminal carboxyl group of a nucleic acid aptamer to the amine group of the polyethylene glycol on the mesoporous silica by reacting, and carrying, by the mesoporous silica nanoparticles, a lipid-lowering drug such as atorvastatin. The mesoporous silica nanoparticles and the preparation method thereof have the characteristics that the nucleic acid aptamer is bound with the biological target with high affinityand high specificity, the polyethylene glycol can improve the water dispersion and the sustained release capability of the carrier, and the mesoporous silica can carry hydrophilic and hydrophobic drugs of different molecular weights due to the characteristics of unique mesoporous structure, huge specific surface area, easy surface modification and the like.
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Description

technical field

[0001] The invention belongs to the technical field of chemical medicines, and relates to a mesoporous silica nanoparticle modified with nucleic acid aptamer targeting polyethylene glycol and a preparation method thereof. Background technique

[0002] The formation of macrophage-derived foam cells is the main cytological change of atherosclerosis and can be used as a target for the diagnosis and treatment of atherosclerotic lesions. The formation of foam cells is due to the massive uptake of oxidized LDL, and scavenger receptors are responsible for 95% of the uptake of oxidized LDL. Nucleolin is a kind of scavenger receptor, and the nucleic acid aptamer AS1411 has a high degree of targeting to nucleolin. Therefore, it can target foam cells well by linking the AS1411 nucleic acid aptamer.

[0003] Mesoporous silica is an ordered mesoporous nanomaterial, which has the advantages of regular nanopore structure, continuously adjustable pore size from 2 to 50 nm,...

Claims

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