Supercharge Your Innovation With Domain-Expert AI Agents!

Targeted drug-loading micelle loaded with copper ion chelating agent

A technology of drug-loaded micelles and copper ions is applied in the biological field to achieve the effect of reducing systemic toxicity

Pending Publication Date: 2022-03-01
FUDAN UNIV
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, there is an urgent need for a drug that can be delivered to the tumor area while tracking drug distribution information, which is still very challenging.

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
  • Targeted drug-loading micelle loaded with copper ion chelating agent
  • Targeted drug-loading micelle loaded with copper ion chelating agent
  • Targeted drug-loading micelle loaded with copper ion chelating agent

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Synthetic method of micellar building materials: Preparation of ring-opening polymerization monomer: Weigh 3g (10.7mmol) of Lys(Z) and 1.27g (4.28mmol) of triphosgene into a 100mL two-necked bottle, vacuumize with an oil pump, protect with nitrogen, and use a syringe Inject anhydrous THF (30 mL), and stir in an oil bath at 50° C. for 3 h. After the reaction was completed, it was cooled to room temperature, and the reaction solution was dropped into anhydrous n-hexane (150 mL) with continuous stirring, and white crystals were precipitated, which crystallized overnight at -20°C, and were filtered and dried to obtain a white solid Lys(Z)-NCA. Similarly, Phe 3g (18.2mmol) and triphosgene 2.69g (9.08mmol) were weighed, and a white solid Phe-NCA was obtained according to the above operation. use 1 The structures of the above two activated monomers were identified by H NMR.

[0049] Polymer mPEG-pLys-pPhe and N 3 -The synthesis of PEG-pLys-pPhe respectively with CH 3 O-PEG...

Embodiment 2

[0052] Monovalent copper ion chelating agent synthesis method: 2-hydroxyethyl sulfide (4.25g, 40mmol) and thiourea (3.05g, 40mmol) were added in hydrobromic acid (48wt%, 8.5mL, 75mmol), under argon Reflux under atmosphere overnight, then cool to room temperature, slowly add sodium hydroxide (3.2g, 80mmol) aqueous solution (10mL), reflux under argon atmosphere overnight, then cool to room temperature, slowly add hydrochloric acid (1M) until neutralized. Then extracted with dichloromethane (50mL×3), combined the organic phases, washed with water (100mL) and saturated brine (100mL) respectively, dried over anhydrous sodium sulfate, evaporated the solvent under reduced pressure to obtain compound 1 as a colorless oil , without purification can be directly put into the next reaction.

[0053] First scrape off the oxide layer on the surface of the sodium bar. Sodium (1.29g, 56mmol) and 2-ethylthioethanethiol (4.1g, 33.6mmol) were dissolved in absolute ethanol (60mL) and heated to r...

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 biology, and particularly relates to a targeted drug-loaded micelle loaded with a copper ion chelating agent. According to the targeted drug-loaded micelle, the copper ion chelating agent and the chemotherapeutic drug are jointly loaded in the same nano-drug system and are delivered to a tumor area in a targeted manner, and the purpose of inhibiting tumor growth is achieved through the cytotoxic effect of chelating copper ions in the tumor area and the chemotherapeutic drug; meanwhile, the copper ion chelating agent applied in the invention can emit near-infrared fluorescence after chelating copper ions. And finally, the aim of integrated diagnosis and treatment of tumors is fulfilled.

Description

technical field [0001] The invention belongs to the field of biological technology, and in particular relates to a targeted drug-loaded micelle loaded with a copper ion chelating agent. Background technique [0002] Tumor remains one of the biggest problems facing human health. The latest research has found that the content of copper ions in various tumors is abnormally increased, which is because copper ions play an important role in the occurrence, development, migration and proliferation of tumors (Cancer Treat.Rev.35(1)(2009)32 –46). In particular, copper ions play an important role in the process of tumor cells secreting pro-angiogenic growth factors. Studies have found that chelating copper ions can slow down tumor growth (Science 349(2015) 128–129). A well-known example is tetrathiomolybdic acid, which is undergoing clinical trials, which can slow down tumor growth by inhibiting new blood vessels (Arch. Neurol. 60 (2003) 379-385). Copper ion chelating agents are m...

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): A61K9/107A61K47/34A61K47/42A61K31/555A61K31/704A61K49/22A61P35/00
CPCA61K9/1075A61K47/34A61K47/42A61K31/555A61K31/704A61K49/227A61P35/00A61K2300/00
Inventor 孙涛蒋晨
Owner FUDAN 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