Unlock instant, AI-driven research and patent intelligence for your innovation.

Preparation method and application of a multi-stage liver-targeting intelligent nano-drug delivery system

A technology of actively targeting groups and polysaccharides, which can be used in pharmaceutical formulations, preparations for in vivo tests, medical preparations of non-active ingredients, etc. Poor sex and other problems, to achieve the effect of promoting selective recognition into cells, good biocompatibility, and reducing side effects

Inactive Publication Date: 2018-10-19
SICHUAN UNIV
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The main reason why this stubborn fortress has not been conquered is that besides the unsatisfactory pharmacological effect of the therapeutic drug itself, the drug is not effectively delivered to the lesion of the liver, that is, the liver targeting of the drug is poor.

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
  • Preparation method and application of a multi-stage liver-targeting intelligent nano-drug delivery system
  • Preparation method and application of a multi-stage liver-targeting intelligent nano-drug delivery system
  • Preparation method and application of a multi-stage liver-targeting intelligent nano-drug delivery system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1: Preparation of a multi-stage liver-targeted reduction-sensitive nano drug delivery system

[0059] In this example, the multi-stage liver-targeted reduction-sensitive nano drug delivery system was prepared through the following steps.

[0060] Add propargylamine (1g), Boc-L-Lys(Boc)-OH (6.92g), HBTU (3.82g) and HOBT (2.70g) into the reaction flask and dissolve them in 52mL of redistilled dichloromethane. Under protection, add 12mL of DIEA and react at room temperature for 48h, rotary steam, add chloroform to dilute, and then successively wash with saturated NaHCO 3 solution, washed with HCl (1M) and saturated NaCl solution, anhydrous MgSO 4 Compound a was separated by column after drying overnight.

[0061] Under nitrogen protection, compound a (4.5 g, 24.5 mmol) was dissolved in 18 mL CH 2 Cl 2 , then added TFA 18mL, reacted at room temperature for 5h, rotary steamed, diethyl ether precipitated, removed diethyl ether to obtain white powder compound b.

...

Embodiment 2

[0071] Example 2: Preparation of a multi-stage liver-targeted pH-sensitive nano drug delivery system

[0072] In this example, the multistage liver-targeted pH-sensitive nano drug delivery system was prepared through the following steps.

[0073] After adding H-Lys-OMe·2HCl (2.5g), Boc-L-Lys(Boc)-OH (12.81g), HBTU7.0g) and HOBT (5.0g) into the reaction flask, use 80mL of redistilled dichloro Dissolve methane, under the protection of nitrogen, add 10.2mL DIEA, react at room temperature for 48h, rotary evaporate, add chloroform to dilute, and then successively wash with saturated NaHCO 3 solution, washed with HCl (1M) and saturated NaCl solution, anhydrous MgSO 4 After drying overnight, it was purified by column separation to obtain compound 1.

[0074] Under nitrogen protection, the above product Compound 1 (1.82 g, 2 mmol) was dissolved in 6 mL of CH 2 Cl 2 , then added 7mL of trifluoroacetic acid (TFA), reacted at room temperature for 7h, then rotary evaporated, diethyl e...

Embodiment 3

[0087] Example 3: Preparation of a multi-stage liver-targeted MMP enzyme-sensitive nano drug delivery system

[0088] In this example, the multi-stage liver-targeting MMP enzyme-sensitive nano drug delivery system was prepared through the following steps.

[0089] Add H-Lys-OMe·2HCl (2.5g), Boc-L-Lys(Boc)-OH (12.81g), HBTU (7.0g) and HOBT (5.0g) into the reaction flask and use 80mL of distilled distilled Chloromethane was dissolved, and under the protection of nitrogen, 10.2mL DIPEA was added and reacted at room temperature for 48h, rotary steamed, diluted with chloroform, and then saturated NaHCO 3 solution, washed with HCl (1M) and saturated NaCl solution, anhydrous MgSO 4 After drying overnight, it was purified by column separation to obtain compound 1.

[0090] Under nitrogen protection, the above product Compound 1 (1.82 g, 2 mmol) was dissolved in 6 mL of CH 2 Cl 2 , then added 7mL of trifluoroacetic acid (TFA), reacted at room temperature for 7h, then rotary evapora...

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

PropertyMeasurementUnit
molecular weightaaaaaaaaaa
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention discloses a multi-stage liver-targeted intelligent nano drug delivery system, and belongs to the field of biological materials. The nano drug delivery system comprises hydrophobic dendrimers, hydrophilic natural macromolecular polysaccharides, active targeting groups and hydrophobic drug molecules. According to the nano drug delivery system provided by the invention, the hydrophobic dendrimers are linked to the hydrophilic natural macromolecular polysaccharides by virtue of environment-responsive chemical bonds, so that amphipathic molecules are formed; then, hydrophobic drugs are encapsulated in hydrophobic cavities of nanoparticles formed by the amphipathic molecules under hydrophilic and hydrophobic actions as well as a [pi]-[pi] stacking action; and the active targeting groups, which have a tumor specific recognition function, are linked to the natural macromolecular polysaccharides by virtue of stable covalent bonds. According to the drug delivery system, intelligent nanoparticles having an environment-responsive performance can be formed through self-assembling; the drug delivery system is good in biocompatibility and biodegradability, multi-stage liver targeting can be achieved, and the drug delivery system is applicable to delivery of such hydrophobic molecules as antineoplastic drugs, fluorescent molecules, photosensitizers and the like.

Description

technical field [0001] The invention belongs to the field of biological materials, in particular to a preparation method and application of a multi-stage liver-targeting intelligent nano drug delivery system. technical background [0002] Cancer is a leading cause of death in today's world. According to the World Health Organization, approximately 840 million people died of cancer between 2005 and 2015. The three major means of treating cancer include chemotherapy, radiotherapy, and surgery. Among them, chemotherapy has led to the failure of cancer treatment due to poor water solubility of therapeutic drugs, narrow therapeutic window, and toxic side effects on normal tissues. Our nano-delivery system has unique conditions to solve the above problems, but how to realize the specific recognition of tumor tissue by the delivery system and the accurate release of drugs in tumor cells, and reduce the side effects on normal tissues still needs to be solved. solve. [0003] In ...

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
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/36A61K47/12A61K47/42A61K49/00A61P35/00C08B37/00A61K31/704
CPCA61K9/5161A61K31/704A61K49/0054A61K49/0093C08B37/0018
Inventor 顾忠伟何一燕周洁马胜男姜倩岳冬
Owner SICHUAN UNIV
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com