Nano-drug of hybrid membrane loaded oxidative phosphorylation inhibitor and preparation method of nano-drug

An oxidative phosphorylation, nano-drug technology, applied in nano-drugs, nano-technology for materials and surface science, nano-technology, etc., can solve the problems of limiting the development of nano-drug delivery systems, toxic side effects, etc. The effect of improving biocompatibility

Active Publication Date: 2021-11-12
HENAN UNIVERSITY
View PDF11 Cites 4 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, as foreign substances in the body, traditional nano-drugs are easily recognized and cleared by the immune system in the body, and have certain potential toxic side effects on the liver and kidneys, which greatly limits the development of nano-drug delivery systems.

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
  • Nano-drug of hybrid membrane loaded oxidative phosphorylation inhibitor and preparation method of nano-drug
  • Nano-drug of hybrid membrane loaded oxidative phosphorylation inhibitor and preparation method of nano-drug
  • Nano-drug of hybrid membrane loaded oxidative phosphorylation inhibitor and preparation method of nano-drug

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0074] The invention provides a preparation method of a nano-medicine loaded with an oxidative phosphorylation inhibitor on a mitochondrial-tumor cell mixed membrane, which includes: mixing a mixed membrane of mitochondrial membrane and tumor cell membrane with an inner core so that the mixed membrane wraps around the inner core. Coating of the inner core with the hybrid film can be accomplished by means of ultrasound and / or extrusion. The ultrasonic frequency is 100-110W, at 36-38°C, ultrasonic treatment is performed for 8-10min.

[0075] In one embodiment, after the mixed membrane of mitochondrial membrane and tumor cell membrane is mixed with the inner core, ultrasonic treatment (for example, ultrasonic treatment for 1-10 min) is performed first, and then repeatedly squeezed under 800nm, 400nm, and 200nm filter membranes successively 7 Second-rate.

[0076] In a preferred embodiment of the application of the present invention, the above-mentioned preparation method also in...

Embodiment 1

[0086] This example provides a nano-drug containing an oxidative phosphorylation inhibitor loaded on a heterogeneous membrane and a preparation method thereof.

[0087] The preparation method is as follows:

[0088] (1) Synthesis of benzyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)acrylate (HB).

[0089]First, 4-(hydroxymethyl) phenylboronic acid pinacol ester was dissolved in dry dichloromethane, transferred to a three-necked flask, and then a certain amount of triethylamine was added. Under ice-bath conditions, methacryloyl chloride dissolved in anhydrous dichloromethane was slowly dropped into the three-necked flask through a constant-pressure dropping funnel. After the dropwise addition, the stirring reaction was continued for 10 hours (h) at room temperature. The insoluble reaction product was removed by filtration, and the volume of the filtrate was reduced by rotary evaporation, then diluted with ethyl acetate, and washed three times with saturated brine. After ...

experiment example 1

[0102] In this experimental example, the structures of HB, PEG-CPADN, and PEG-PHB prepared and synthesized in Example 1 were characterized. Figure 5 Figures of NMR results for structural characterization. (a) Synthesized by HB 1 H-NMR (CDCl 3 ), using 4-hydroxymethylphenyl borate and methacryloyl chloride as raw materials, the ROS-sensitive HB monomer was synthesized with a yield of 80%; (b) PEG-CPADN synthesized 1 H-NMR (CDCl 3 ), RAFT is activated and interacts with PEG-NH 2 Reaction at room temperature generates PEG-CPADN, and its grafting rate is 100%; (c) PEG-PHB synthetic 1 H-NMR (DMSO), PEG-CPADN and HB monomer were synthesized by RAFT reaction to obtain polymer nanocarrier PEG-PHB, the degree of polymerization of PHB was about 11, the polymerization molecular weight was 3.3k, the total molecular weight of PEG-PHB was 5.3k, The degree of polymerization can be calculated by the area of ​​the characteristic peak of the NMR results.

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
particle sizeaaaaaaaaaa
particle diameteraaaaaaaaaa
Login to view more

Abstract

The invention discloses a nano-drug of a hybrid membrane loaded oxidative phosphorylation inhibitor and a preparation method of the nano-drug, and relates to the technical field of drug carriers. The nano-drug comprises an inner core and a shell; the outer shell covers the periphery of the inner core; the inner core comprises ROS-responsive drug-loaded nano-particles; drugs loaded by the ROS-responsive drug-loaded nano-particles are oxidative phosphorylation inhibitors; and the shell is a mixed membrane of a mitochondrial membrane and a tumor cell membrane. The nano-drug can cross BBB and reach a tumor site by virtue of homologous targeting of the tumor cell membrane, and can perform homologous target and can enter mitochondria by virtue of the mitochondrial membrane, the ROS-responsive drug-loading nano-particle is in a high-level ROS environment of the mitochondria, the core swells and degrades to release the loaded substance oxidation phosphorylation inhibitor, therefore, safe and efficient targeted drug therapy is realized. Through wrapping of the shell, the defect that the half-life period of the loaded medicine in the blood is short is avoided, and long circulation of the medicine in the blood is protected to a great extent.

Description

technical field [0001] The invention relates to the technical field of drug carriers, in particular to a nanometer drug loaded with an oxidative phosphorylation inhibitor on a heterogeneous membrane and a preparation method thereof. Background technique [0002] Mitochondria, a double-membrane organelle present in most cells, are the powerhouse and energy provider of mammals. In addition to providing energy to cells, it is also involved in processes such as cell differentiation, cell messaging, and apoptosis. In recent years, targeting mitochondria has been considered as a promising strategy for cancer treatment. [0003] At present, Gboxin is a glioma (GBM)-specific inhibitor of mitochondrial oxidative phosphorylation. The mechanism of action is: Gboxin binds to ATP synthase on the inner membrane of mitochondria, thereby inactivating ATP synthase. In addition, Gboxin can also block the electron transfer in the process of oxidative phosphorylation, resulting in the change ...

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): A61K9/51A61K31/4184A61K47/46A61K47/34A61P35/00B82Y5/00B82Y30/00B82Y40/00
CPCA61K9/5068A61K31/4184A61K47/34B82Y5/00B82Y30/00B82Y40/00A61P35/00A61K9/5073A61K9/5146A61K9/5176
Inventor 邹艳孙雅静师冰洋郑蒙郝明聪
Owner HENAN UNIVERSITY
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap