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Silica nanocarrier delivery system for targeted activation of CD44 molecules, its preparation method and use

A nano-carrier and delivery system technology, which can be used in liposome delivery, preparations for in vivo tests, nano-drugs, etc., and can solve problems such as non-existence

Active Publication Date: 2021-02-26
BEIJING INNO MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the following problems will be encountered in the research and development of targeted drug delivery systems targeting CD44: if the affinity between CD44 and HA on the surface of target cells is not enough to provide significant specificity, then such targeted drug delivery systems will be difficult to obtain. There will be no specific targeting properties
[0014] So far, there is no report on the expression status of CD44 on the surface of macrophages, monocytes, endothelial cells, lymphocytes and smooth muscle cells mainly present in vulnerable plaques and its affinity for HA, nor does it exist. Any targeted drug delivery capable of stable and sustained release of drugs designed for the diagnosis or treatment of vulnerable plaques or diseases associated with vulnerable plaques using the interaction of HA and CD44 and the specific microenvironment of vulnerable plaques system prior art

Method used

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  • Silica nanocarrier delivery system for targeted activation of CD44 molecules, its preparation method and use
  • Silica nanocarrier delivery system for targeted activation of CD44 molecules, its preparation method and use
  • Silica nanocarrier delivery system for targeted activation of CD44 molecules, its preparation method and use

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specific Embodiment approach

[0149] The present invention will be further illustrated by specific examples below, but it should be understood that these examples are only used for more detailed description, and should not be construed as limiting the present invention in any form.

[0150] This section provides a general description of the materials and test methods used in the tests of the present invention. While many of the materials and methods of manipulation which are employed for the purposes of the invention are well known in the art, the invention has been described here in as much detail as possible. It will be apparent to those skilled in the art that, in the context and context, the materials used and methods of operation used in the present invention are known in the art unless otherwise indicated.

Embodiment 1

[0151] Synthesis of embodiment 1 siliceous body monomer C2

[0152] Silicosomal monomer C2 has a weakly polar small molecular structure and inorganic silicon-oxygen functional groups that can be easily inserted into the phospholipid bilayer membrane, and has a typical organic-inorganic composite lipid structure. It is selected as a representative class of silicon with weakly polar functional groups. Plastid monomer molecule.

[0153] C2 can be obtained according to the preparation method described in, and the preparation of cholesterol succinyl silane can be found in Biomaterials 32 (2011) 9300e9307. The chemical structure of siliceous monomer C2 is as follows:

[0154]

[0155] image 3 It is the NMR result of C2. Figure 4 It is the mass spectrum result of C2.

Embodiment 2

[0156] Example 2 Preparation of siliceous nanocarriers (CL2-(R)-SP) targeted at linking selectin (SP) and loading rosuvastatin (R)

[0157] 2.1 Preparation of siliceous nanocarrier CL2-(R) loaded with rosuvastatin (R)

[0158] Silica body monomer C2, dimyristoylphosphatidylethanolamine (DMPE), DSPC, (mass ratio 6:0.5:2), rosuvastatin (R) (feeding according to the ratio of drug to lipid 1:10) was placed in Round bottom flask, and add 10mL chloroform to dissolve. The organic solvent was completely removed by rotary evaporation (55° C. water bath, 90 r / min, 30 min), thereby forming a thin film on the container wall. The flask was placed in a constant temperature water bath at 50°C to fully hydrate the film for 30 minutes, and the siliceous body solution was formed by ultrasonication in a water bath for 10 minutes and a probe-type ultrasonic instrument for 5 minutes (amplitude 20, interval 3 s). The solution is placed in an oven at 50°C to promote the formation of the sol-gel pr...

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Abstract

A siliceous nanocarrier delivery system for targeting activated CD44 molecules and a preparation method thereof, the surface of the nanocarrier is partially modified by a targeting ligand, and the targeting ligand is capable of interacting with activated CD44 A ligand to which a molecule specifically binds. Use of the siliceous body nanocarrier delivery system in preparing medicines for diagnosing, preventing and treating vulnerable plaques or diseases related to vulnerable plaques.

Description

[0001] Cross References to Related Applications [0002] This application claims the priority of the Chinese invention patent application No. CN201810060265.9 submitted on January 22, 2018, which is incorporated herein by reference. technical field [0003] The invention belongs to the technical field of targeted drug delivery, and in particular relates to a nanocarrier for targeting and activating CD44 molecules, especially for targeting vulnerable plaques, in particular to a silicon plastid nanocarrier delivery system. The present invention also relates to the preparation method and use of the nanocarrier, especially the siliceous nanocarrier delivery system, especially in the diagnosis, prevention and treatment of vulnerable plaque or diseases related to vulnerable plaque. Background technique [0004] At present, acute cardiovascular events, mainly acute myocardial infarction and sudden cardiac death, have become the number one killer of human health. According to stat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61P7/00A61P9/00
CPCA61P7/00A61P9/00A61K51/1234A61K49/1812A61K49/0409A61K47/6911A61K47/6913A61K9/1271A61K9/1272A61K9/0019A61K9/127A61K47/10A61K47/42A61K47/36A61P9/10A61K49/0002A61K49/0084A61K49/04A61K45/06B82Y5/00
Inventor 马茜孙洁芳周玉杰
Owner BEIJING INNO MEDICINE CO LTD
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