Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Targeting element and preparation method and application thereof

A targeting and component technology, applied in the field of medicine, can solve the problems of no active targeting, poor absorption of target organs in the body for targeted drug delivery, and reduced utilization rate.

Active Publication Date: 2019-12-03
CHENGDU RIBOCURE PHARMATECH CO LTD
View PDF6 Cites 3 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Thermosensitive liposomes can directly kill tumor cells, but heating for too long can also cause damage to normal tissues
Molecularly targeted liposomes also have problems such as directional delivery of drugs and poor absorption of target organs in vivo.
[0005] In summary, the primary problem to be solved in the research and development of targeted drugs is to maintain the stability of nanocarriers during transportation without being destroyed. Ordinary nanoparticles or liposomes do not have active targeting (some may have passive targeting). sex), easy to be cleared by the endothelial system, reducing the utilization rate, and may cause unnecessary toxic and side effects

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Targeting element and preparation method and application thereof
  • Targeting element and preparation method and application thereof
  • Targeting element and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0109] Example 1 Material

[0110]

[0111]

[0112] The material of lipid is cholesterol, egg yolk lecithin, soybean lecithin, cephalin, sphingomyelin, PC (phosphatidylcholine), EPG (egg phosphatidylglycerol), SPG (soybean phosphatidylglycerol), Distearoylphosphatidylethanolamine (DSPE), dipalmitoylphosphatidylethanolamine (DPPE), dipalmitoylphosphatidylcholine (DPPC), dioleoylphosphatidylcholine (DOPC), distearoylphosphatidylcholine Alkaline (DSPC), Dimyristoylphosphatidylcholine (DMPC), Dilinoleoylphosphatidylcholine (DLPC), Dioleoylphosphatidylglycerol (DOPG), Dipalmitoylphosphatidylglycerol (DPPG), Dimely Myristoylphosphatidylcholine (DMPC), Dilauroylphosphatidylglycerol (DLPG), Cetyltrimethylammonium Bromide (CTAB), Dimethyl Dioctadecylammonium Bromide (DDAB), One or more of 1,2-dioleoyl-3-trimethylammoniumpropane (chloride salt) (DOTAP).

[0113] In this embodiment, the amino acid of the spacer material is one of arginine, asparagine, aspartic acid, glutamic aci...

Embodiment 2

[0114] Example 2 Preparation of Targeting Elements

[0115] The targeting material and spacer material in Example 1 were synthesized, and the synthesis of mannose and PEGn was taken as an example here.

[0116] Take diethylene glycol, p-toluenesulfonyl chloride and triethylamine, dissolve in DCM, react at room temperature for 24 hours, and separate the product TosOC by column chromatography 2 h 4 OC 2 h 4 OH (compound 1). Take compound 1 and pentaacetylated mannose and its derivatives and boron trifluoride ether (BF 3 ·Et 2 O) dissolved in DCM, reacted at room temperature for 24h, separated by column chromatography to obtain the product Aco-M-OC 2 h 4 OC 2 h 4 OTos (compound 2), M is mannose and its derivatives.

Embodiment 3

[0117] Example 3 Preparation of Targeting Vector

[0118] The targeting element in Example 2 was further synthesized with the basic nano-preparation material, and the synthesis of mannose, PEGn and cholesterol was taken as an example here.

[0119] Take the compound prepared in Example 2 and sodium azide, dissolve in DMF, react at 60°C for 24h, and separate by silica gel column chromatography to obtain the solid product Aco-M-OC 2 h 4 OC 2 h 4 N 3 (Compound 3). Dissolve compound 3 in a methanol solution of sodium methoxide, react at room temperature for 3 h, and concentrate to obtain the product M-OC 2 h 4 OC 2 h 4 N 3 (compound 4). Cholesterol, propyne bromide and sodium hydrogen were dissolved in a mixed solution of ether and DMF, reacted at room temperature for 24 hours, and separated by silica gel column chromatography to obtain the solid product Chol-CH 2 CCH (Compound 5). Dissolve compound 4, compound 5 and cuprous iodide in DMF, react at room temperature for...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention belongs to the technical field of medicines, and particularly relates to a targeting element with a targeting function and a preparation method thereof, a method for improving the drug delivery capacity of a targeting carrier, a method for improving the transfection efficiency of a transfection reagent, a compound, a targeting oil phase and a water phase. The targeting element is composed of a targeting material and a spacing material, and the targeting material is mannose and / or a mannose derivative. The targeting element and the targeting carrier can well target a mannose receptor, and can be efficiently combined with the mannose receptor on a target cell; the preparation cost is low, the synthesis is easy, the universality is realized, various targeting nano preparations can be synthesized, and the purification and characterization are facilitated; and the targeting element can be used for improving the transfection efficiency of the transfection reagent and applied toscientific research and business.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a targeting element with a targeting function and a preparation method thereof, a method for improving the ability of the targeting carrier to deliver drugs, and a method for improving the transfection efficiency of a transfection reagent And a complex, targeting oil and water phases. Background technique [0002] In recent years, drug receptor-mediated targeted drug delivery systems have been extensively studied. Targeted drug delivery systems can improve their specific targeting and overcome the problems of wide distribution of drugs in vivo and serious side effects. Among them, lectin receptors are a kind of glycoproteins, glycolipids or carbohydrate complexes distributed on the surface of cell membranes, which can specifically recognize and bind to some sugar groups. Mannose receptor is the most important high-efficiency endocytic lectin receptor. Its functions i...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K47/26A61K47/10A61K47/54A61K47/60A61K39/00A61K48/00A61K31/704A61K31/352A61K31/337A61P35/00A61P9/10A61P29/00
CPCA61K47/26A61K47/10A61K47/549A61K47/60A61K39/00A61K48/005A61K31/704A61K31/352A61K31/337A61P35/00A61P9/10A61P29/00A61K9/127A61K47/6911A61K47/6917A61K47/6907A61K47/6929B82Y5/00A61K31/4745A61K31/475A61K31/7048A61K31/519A61K31/513A61K31/5377A61K31/17C12N15/88A61K48/0041A61K9/1271A61K47/34B82Y40/00
Inventor 宋相容魏于全
Owner CHENGDU RIBOCURE PHARMATECH CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com