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

Bone-targeting hypoxic response nano-micelle loaded with anti-cancer drug and preparation method thereof

A technology of anticancer drugs and nano micelles, which is applied in anticancer drugs, drug combinations, and pharmaceutical formulations, etc., can solve the problems of bone metastases with little effect, achieve inhibition of tumor cell growth, easy entry into tumor cells, and difficulty in leakage Effect

Active Publication Date: 2020-01-10
NANTONG UNIVERSITY
View PDF3 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although non-bone-targeted drug-loaded nanocarriers can treat solid tumors, they have little effect on bone metastases like traditional drugs.

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
  • Bone-targeting hypoxic response nano-micelle loaded with anti-cancer drug and preparation method thereof
  • Bone-targeting hypoxic response nano-micelle loaded with anti-cancer drug and preparation method thereof
  • Bone-targeting hypoxic response nano-micelle loaded with anti-cancer drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-1

[0049] Preparation of bone-targeted hypoxia-responsive polymers:

[0050] (1) Dissolve 50 mg (1 equivalent) of polyethylene glycol (HOOC-PEG-NHS, MW=1000) in 5 mL of dichloromethane, add 6.8 mg (1.3 equivalents) of 4,4-azodiphenylamine (AZO ), stirred and reacted in the dark at room temperature for 24 hours, and then used 20 mL of glacial ether to precipitate the product to obtain carboxypolyethylene glycol azobenzene (HOOC-PEG-AZO);

[0051] (2) Dissolve 50 mg (1 equivalent) HOOC-PEG-AZO in tetrahydrofuran (THF), add 124 mg (16 equivalents) N-benzyloxycarbonyl-L-lysine-N-carboxylic acid anhydride (zLL-NCA) at room temperature React for 72 hours under light stirring to obtain a polyethylene glycol-polylysine block copolymer (HOOC-PEG-AZO-PBLL) with benzyloxycarbonyl groups on the surface;

[0052] (3) Dissolve 150mg (1 equivalent) HOOC-PEG-AZO-PBLL in 5mL trifluoroacetic acid (TFA), add 1mL 33% hydrogen bromide acetic acid solution (HBr / ACOH), stir and react at 0°C for 1h to ...

Embodiment 1-2

[0056] Preparation of bone-targeted hypoxia-responsive polymers:

[0057] Dissolve 50 mg (1 equivalent) of polyethylene glycol (HOOC-PEG-NHS, MW=2000) in 5 mL of dichloromethane, add 6.8 mg (1.3 equivalents) of 4,4-azodiphenylamine (AZO), and After stirring for 24 hours in the dark, the product was precipitated with 20 mL of glacial ether to obtain carboxypolyethylene glycol azobenzene (HOOC-PEG-AZO); the rest of the steps were the same as in Example 1-1.

Embodiment 1-3

[0059] Preparation of bone-targeted hypoxia-responsive polymers:

[0060] Dissolve 50 mg (1 equivalent) of polyethylene glycol (HOOC-PEG-NHS, MW=5000) in 5 mL of dichloromethane, add 6.8 mg (1.3 equivalents) of 4,4-azodiphenylamine (AZO), and After stirring for 24 hours in the dark, the product was precipitated with 20 mL of glacial ether to obtain carboxypolyethylene glycol azobenzene (HOOC-PEG-AZO); the rest of the steps were the same as in Example 1-1.

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
particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention discloses a bone-targeting hypoxic response nano-micelle loaded with an anti-cancer drug and a preparation method thereof. The preparation method disclosed by the invention comprises thefollowing steps: carrying out copolymerization reaction on polyethylene glycol and a low-oxygen response group (4, 4-diaminoazobenzene) to obtain carboxyl polyethylene glycol azobenzene; carrying outring-opening polymerization reaction on the carboxyl polyethylene glycol azobenzene and N-carbobenzoxy-L-lysine-N-carboxylic anhydride to obtain a polyethylene glycol-polylysine segmented copolymer with carbobenzoxy on the surface, and removing the carbobenzoxy to obtain a polyethylene glycol-polylysine segmented copolymer; carrying out copolymerization reaction on the polyethylene glycol-polylysine segmented copolymer and a bone-targeting group (alendronate) to obtain a bone-targeting hypoxic response polymer; and synthesizing the bone-targeting hypoxic response nano-micelle loaded with theanti-cancer drug by a dialysis method. The nano-micelle prepared by the preparation method disclosed by the invention is stable in structure and not easy to decompose, has a targeting effect on bone tissues, and can also play a role in low-oxygen controlled release of drugs.

Description

technical field [0001] The invention relates to the technical field of nano-pharmaceuticals, in particular to a bone-targeted hypoxia-responsive nano-micelle loaded with anticancer drugs and a preparation method thereof. Background technique [0002] Bone is the third most preferred metastatic site for cancer cells excluding lung and liver, and some cancers display marked osteotropism. Since bone metastases often have multiple nodules, it is difficult to completely eliminate them with localized radiation therapy or surgical resection. For chemotherapy, because the bone blood flow is low, there will not be enough drug concentration in the bone after administration, and the treatment effect is poor when used in large doses, and the toxic and side effects are strong. [0003] Drug delivery through nanocarriers is one of the important means of treating tumors. Nanocarriers will not change the physical and chemical properties of the loaded drugs, and can also continuously releas...

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 Applications(China)
IPC IPC(8): A61K9/107A61K47/34A61K31/704A61K31/337A61K31/4745A61P35/00C08G65/333C08G69/40C08G69/48
CPCA61K9/1075A61K31/337A61K31/4745A61K31/704A61K47/34A61P35/00C08G65/33313C08G69/40C08G69/48
Inventor 陈忠平龙朦朦翁凌燕陆敏朱俐陈秋萍
Owner NANTONG UNIVERSITY
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