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Nano vesicles with pH and reduction dual sensitivity as well as preparation method and application thereof

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: 2018-03-27
SUN YAT SEN UNIV
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  • 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

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  • Nano vesicles with pH and reduction dual sensitivity as well as preparation method and application thereof
  • Nano vesicles with pH and reduction dual sensitivity as well as preparation method and application thereof
  • Nano vesicles with pH and reduction dual sensitivity as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

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

[0045]

[0046] Add 10.0 g β-aspartate benzyl ester (BLA) and 150 mL ethyl acetate into a three-necked flask; heat to reflux, and then slowly add 50 mL ethyl acetate solution dissolved in 6.0 g triphosgene (NCA) to In a three-necked flask; continue to reflux until it dissolves; after the reaction is completed, put the reaction flask in the refrigerator to cool down; then wash three times with 4℃ saturated sodium bicarbonate and once with 4℃ saturated saline; transfer the upper organic phase to a single-mouth bottle Add anhydrous magnesium sulfate to dry; filter, spin-evaporate and concentrate the filtrate to 50 mL; add 200 mL petroleum ether to a single-neck bottle, freeze to accelerate precipitation; restore room t...

Embodiment 2

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

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

Embodiment 3

[0073] A nanovesicle loaded with hydrophilic and hydrophobic anti-tumor 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 amino group to a 50 mL reaction flask m PEG 2000, filled with nitrogen; heated to 70℃, vacuumed for 4 hours to remove water; filled with nitrogen, cooled to room temperature; under the protection of nitrogen, add 4 mL DMF to remove the amino m PEG is dissolved; then add 1.00 g phenylalanine acid anhydride and 2.61 g benzyloxycarbonyl aspartic acid anhydride; after dissolving, add 20 mL of chloroform and react at 35℃ for 48 h; slowly add a large amount of the reaction solution Precipitate in water and ethanol; centrifuge, wash three times with absolute ethanol and three times with anhydrous ether; vacuum dry to obtain 3.05 g of white solid; 1 The total number of repeating units of BLA and Phe calculated by H NMR was 112, the degree of polymerizat...

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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 a preparation method and application thereof. Background technique [0002] Polymer vesicles are special self-assembled bodies with water-containing cavities formed by self-assembly of amphiphilic polymers in a certain way. They have high stability, adjustable membrane properties and can simultaneously encapsulate hydrophilic and The ability of hydrophobic ingredients. It is precisely because of these properties that polymer vesicles have broad application prospects in drug delivery, gene therapy and tissue engineering. Although these properties of polymer vesicles make them at the forefront of drug delivery applications, in order to obtain better therapeutic effects, it is necessary to develop polymer vesicles that target rapid drug release. [0003] In tumor cells, there is usually bot...

Claims

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Application Information

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Patent Type & Authority Applications(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
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