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Polyethylene glycol vitamin e succinate modified tigecycline silver nanoparticles and its preparation and application

A technology of polyethylene glycol and succinate, applied in the direction of active ingredients of tetracycline, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve problems such as the prevalence of Acinetobacter, reduce toxicity, Improve the bacteriostatic effect and reduce the effect of the minimum inhibitory concentration

Active Publication Date: 2019-10-29
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0002] In recent years, with the wide application of antibacterial drugs in clinical practice, multidrug-resistant and pan-drug-resistant strains are increasing, and Acinetobacter has appeared multidrug-resistant or even fully drug-resistant strains, leading to outbreaks of Acinetobacter epidemics in some hospitals, causing clinical infections. The treatment of
Tigecycline (Tigecycline), as the first (June 2005) approved by the U.S. Food and Drug Administration (Food and Drug Administration, FDA) a new generation of broad-spectrum glycylcycline antibacterial drugs, can overcome the bacterial Tetracycline resistance caused by efflux and ribosome protection maintains good antibacterial activity against common pathogenic bacteria or multidrug-resistant bacteria, and becomes the "last choice" for controlling clinical multidrug-resistant or pan-drug-resistant Acinetobacter infections. However, some studies have also found that Acinetobacter is also resistant to tigecycline, and its drug resistance mechanism may be related to the active efflux of the efflux pump system

Method used

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  • Polyethylene glycol vitamin e succinate modified tigecycline silver nanoparticles and its preparation and application
  • Polyethylene glycol vitamin e succinate modified tigecycline silver nanoparticles and its preparation and application
  • Polyethylene glycol vitamin e succinate modified tigecycline silver nanoparticles and its preparation and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Example 1 Preparation of Tigecycline Silver Nanoparticles Modified with Polyethylene Glycol Vitamin E Succinate

[0021] Polyethylene glycol vitamin E succinate modified tigecycline silver nanoparticles were synthesized in two steps. The first step was to obtain polyethylene glycol vitamin E succinate modified silver nanoparticles. Take 15.6 mL of deionized water and set In a 30mL vial, placed in an ice-water bath ultrasonic pulverizer, first add 0.9mL silver nitrate aqueous solution (10mM), then add 120μL polyethylene glycol vitamin E succinate aqueous solution (40mM, polyethylene glycol chain polymerization degree n =23) Ultrasonic mixing, and then adding sodium hydroxide aqueous solution, the reaction solution quickly becomes pale yellow, and the pH value of the solution rises to about 12, at which point silver oxide nanocrystals are formed. Quickly add freshly prepared 1.08mL sodium borohydride solution (10mM) to the obtained silver oxide nanocrystal solution, the s...

Embodiment 2

[0032] Example 2 Preparation of Tigecycline Silver Nanoparticles Modified with Polyethylene Glycol Vitamin E Succinate

[0033] Polyethylene glycol vitamin E succinate modified tigecycline silver nanoparticles were synthesized in two steps. The first step was to obtain polyethylene glycol vitamin E succinate modified silver nanoparticles. Take 15.6mL deionized water and set In a 30mL vial, placed in an ice-water bath ultrasonic pulverizer, first add 0.9mL silver nitrate aqueous solution (10mM), then add 120μL polyethylene glycol vitamin E succinate aqueous solution (40mM, polyethylene glycol chain polymerization degree ( n)=230) ultrasonic mixing, and then adding sodium hydroxide aqueous solution, the reaction solution quickly becomes light yellow, the pH value of the solution rises to about 12, and silver oxide nanocrystals are formed at this time. Add freshly prepared 1.08mL sodium borohydride solution (10mM) rapidly to the obtained silver oxide nanocrystal solution, the sol...

Embodiment 3

[0044] Example 3 Preparation of Tigecycline Silver Nanoparticles Modified with Polyethylene Glycol Vitamin E Succinate

[0045] Polyethylene glycol vitamin E succinate modified tigecycline silver nanoparticles were synthesized in two steps. The first step was to obtain polyethylene glycol vitamin E succinate modified silver nanoparticles. Take 15.6mL deionized water and set In a 30mL vial, placed in an ice-water bath ultrasonic pulverizer, first add 0.9mL silver nitrate aqueous solution (10mM), then add 120μL polyethylene glycol vitamin E succinate aqueous solution (40mM, polyethylene glycol chain polymerization degree n =23) Ultrasonic mixing, and then adding sodium hydroxide aqueous solution, the reaction solution quickly becomes pale yellow, and the pH value of the solution rises to about 12, at which point silver oxide nanocrystals are formed. Quickly add 1.08 mL of freshly prepared sodium borohydride solution (10 mM) to the obtained silver oxide nanocrystal solution, cont...

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Abstract

The invention provides polyethylene glycol vitamin E succinate modified tigecycline loading silver nanoparticles. First, under the stabilizing effect of polyethylene glycol vitamin E succinate, hollow silver nanoparticles are formed through kirkendall effect, and polyethylene glycol vitamin E succinate modified silver nanoparticles are synthesized, thus the stability of the hollow silver nanoparticles is improved, and toxicity caused by oxidation of the silver nanoparticles is reduced. An antibacterial drug tigecycline is effectively loaded by the hollow structure of polyethylene glycol vitamin E succinate modified tigecycline loading silver nanoparticles. With relatively small particle size, the nanoparticles can penetrate through the cell wall of bacteria, destroy cell membrane and enter cytoplasm; and through the synergistic antibacterial effect of silver nanoparticles and tigecycline, the minimal inhibitory concentration and minimal bactericidal concentration of a drug are remarkably reduced, and the drug resistance of escherichia coli against tigecycline is overcome. The silver nanoparticles can serve as a novel antibacterial nano material for preparing antibacterial drug-resistant drugs and is applied to the field of life science and pharmacy.

Description

technical field [0001] The invention belongs to the preparation of nanoparticles, and relates to silver nanoparticles loaded with tigecycline, in particular to silver nanoparticles modified with polyethylene glycol vitamin E succinate and a preparation method thereof, and polyethylene glycol vitamin E succinate modified silver nanoparticles Application of silver nanoparticles in the preparation of anti-drug-resistant bacteria drug tigecycline. Background technique [0002] In recent years, with the wide application of antibacterial drugs in clinical practice, multidrug-resistant and pan-drug-resistant strains are increasing, and Acinetobacter has appeared multidrug-resistant or even fully drug-resistant strains, leading to outbreaks of Acinetobacter epidemics in some hospitals, causing clinical infections. treatment poses serious challenges. Tigecycline (Tigecycline), as the first (June 2005) approved by the U.S. Food and Drug Administration (Food and Drug Administration, F...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/22A61K31/65A61K33/38A61P31/04
CPCA61K9/5146A61K31/65A61K33/38A61K2300/00Y02A50/30
Inventor 杜永忠康旭琪姜赛平应晓英
Owner ZHEJIANG UNIV
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