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

A nanovesicle with double sensitivity to pH and reduction and its preparation method and application

A dual-sensitivity, nanovesicle technology, applied in the fields of polymer chemistry and biomedical engineering, to achieve a good synergistic therapeutic effect and easy to control large-scale synthesis.

Active Publication Date: 2019-05-24
SUN YAT SEN UNIV
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are no reports on nanovesicles that can simultaneously load hydrophilic and hydrophobic drugs, achieve targeted release of drugs, and be easily degraded in the human body.

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
  • A nanovesicle with double sensitivity to pH and reduction and its preparation method and application
  • A nanovesicle with double sensitivity to pH and reduction and its preparation method and application
  • A nanovesicle with double sensitivity to pH and reduction and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] A method for preparing an amphiphilic polymer with dual sensitivity to pH and reduction, comprising the following steps:

[0044] 1. Synthesis of benzyloxycarbonyl aspartic acid anhydride (BLA-NCA), the reaction mechanism and reaction process are as follows:

[0045]

[0046] Add 10.0 g benzyl β-aspartate (BLA) and 150 mL ethyl acetate into a three-neck flask; heat to reflux, then slowly dropwise add 50 mL ethyl acetate solution containing 6.0 g triphosgene (NCA) to In the three-necked flask; continue to reflux until the solution is clear; after the reaction is completed, put the reaction bottle into the refrigerator to freeze and cool down; then wash with 4°C saturated sodium bicarbonate three times, and 4°C saturated saline once; transfer the upper organic phase to a one-necked bottle Add anhydrous magnesium sulfate to dry; filter, and concentrate the filtrate to 50 mL by rotary evaporation; add 200 mL of petroleum ether to a one-mouth bottle, and freeze to accelerat...

Embodiment 2

[0057] A nanovesicle loaded with hydrophilic and hydrophobic antitumor drugs (D-G-PDMP vesicle for short), prepared by the following method (such as figure 1 shown):

[0058] Weigh 20 mg of mPEG-P (Asp(DBA- co -MEA)-Phe), 1 mg hydrophobic antineoplastic drug Gefitinib (Gefitinib), dissolved in 3 mL chloroform; weighed 1.6 mg hydrophilic antineoplastic drug doxorubicin hydrochloride (DOX), dissolved in 0.4 mL Purified water; mix the two, and disperse into a uniform emulsion with an ultrasonic breaker; slowly add the emulsion to 30 mL of purified water, and disperse it with an ultrasonic breaker at the same time; remove chloroform by rotary evaporation, inject oxygen into the solution for 30 min, and then use 14 KDa The dialysis bag was dialyzed in PBS at pH 7.4; concentrated by ultrafiltration with a 100 KDa ultrafiltration tube; finally filtered with a 450 nm filter head to obtain nanovesicles loaded with gefitinib / doxorubicin hydrochloride, gefitinib The drug loading rates...

Embodiment 3

[0073] A nanovesicle loaded with hydrophilic and hydrophobic antitumor drugs is prepared by the following method:

[0074] 1. Synthesis of (BLA-NCA) and (Phe-NCA): same as Example 1.

[0075] 2,( m Synthesis of PEG-P(BLA-Phe)): Add 0.3272 g of aminom PEG 2000, filled with nitrogen; heated to 70°C, vacuumed for 4 h to remove water; filled with nitrogen, cooled to room temperature; added 4 mL DMF under nitrogen protection m Dissolve PEG; add 1.00 g of phenylalanine anhydride and 2.61 g of benzyloxycarbonyl aspartic anhydride; add 20 mL of chloroform after dissolution, and react at 35°C for 48 h; slowly add the reaction solution into a large amount of Precipitated in water and ethanol; centrifuged, washed three times with absolute ethanol and anhydrous ether three times; vacuum dried to obtain 3.05 g of white solid; 1 The total number of repeating units of BLA and Phe calculated by H NMR is 112, the degree of polymerization of BLA is 74, and the degree of polymerization of Phe ...

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
number average molecular weightaaaaaaaaaa
number average molecular weightaaaaaaaaaa
diameteraaaaaaaaaa
Login to View More

Abstract

The invention discloses a nano vesicle with pH and reduction dual sensitivity as well as a preparation method and application thereof, and belongs to the technical field of high polymer chemistry andbiomedical engineering. The nano vesicle contains an amphiphilic polymer with pH and reduction dual sensitivity, wherein the polymer is composed of a hydrophilic section, polyethylene glycol section and a hydrophobic section, poly(aspartyl (di-n-butyl ethylenediamine-co-mercaptoethylamine)-phenylalanine) section; the ratio of the hydrophilic section to the hydrophobic section is 1:11; the nano vesicle also contains a hydrophilic antitumor drug and a hydrophobic antitumor drug. The nano vesicle provided by the invention can bear hydrophilic and hydrophobic drugs at the same time to realize drugtarget release and high-efficiency cooperative treatment on the tumor part, and can be used in vivo for a long time.

Description

technical field [0001] The invention relates to the technical fields of polymer chemistry and biomedical engineering, in particular to a nanovesicle with dual sensitivity to pH and reduction and its preparation method and application. Background technique [0002] Polymer vesicles are a special self-assembled body with a water-containing cavity formed by self-assembly of amphiphilic polymers in a certain way. It has high stability, adjustable membrane properties, and can simultaneously encapsulate hydrophilic and The ability of hydrophobic components. It is precisely because of these properties that polymersomes have broad application prospects in drug delivery, gene therapy and tissue engineering. Although these properties of polymersomes put them at the forefront of drug delivery applications, in order to obtain better therapeutic effects, it is necessary to develop targeted polymersomes for rapid release of drugs. [0003] In tumor cells, there is usually a decrease 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): C08G69/48C08G69/10A61K9/127A61K47/34A61K45/00A61K31/5377A61K31/704A61P35/00
CPCA61K9/1273A61K31/5377A61K31/704A61K45/00A61K47/34C08G69/10C08G69/48
Inventor 帅心涛陈燕桂王勇李博程度
Owner SUN YAT SEN UNIV
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