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Triclosan-based nano antibiotic hydrogel and preparation method and application thereof

A triclosan and hydrogel technology, applied in the field of nano-biomedical materials, can solve the problems of reduced antibacterial activity and limited application

Active Publication Date: 2020-03-24
INST OF RADIATION MEDICINE CHINESE ACADEMY OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, triclosan has poor water solubility (about 10 µg / mL), and it is easy to aggregate in a physiological environment, resulting in a greatly reduced antibacterial activity, which limits its clinical application

Method used

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  • Triclosan-based nano antibiotic hydrogel and preparation method and application thereof
  • Triclosan-based nano antibiotic hydrogel and preparation method and application thereof
  • Triclosan-based nano antibiotic hydrogel and preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0063] (1) The preparation method of TCS-GA, the steps are as follows:

[0064] 1) Add GA (6 mmol, 684.6 mg) and DMAP (0.15 mmol, 18.3 mg) to 20 mL of anhydrous DCM solution, then add TCS (4 mmol, 1158.2 mg) to the mixed solution, and stir overnight at room temperature.

[0065] 2) After the reaction, add ultrapure water to the reaction solution and place the reaction solution in a separatory funnel for liquid separation, collect the insoluble organic layer, add anhydrous sodium sulfate to dry, and remove the organic solvent by rotary evaporation The pure product TCS-GA (a known compound) was obtained after purification by DCM and silica gel chromatography.

[0066] (2) The preparation method of TCS-GA-GFFY, the steps are as follows:

[0067] 1) Weigh 1 g of dichloro resin into the solid-phase reactor, then add DCM solvent to swell the dichloro resin for 10 min, and squeeze out the solvent in the solid-phase reactor with a suction ear ball.

[0068] 2) Weigh Fmoc-Tyr ( t Bu...

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Abstract

The invention discloses a triclosan-based nano antibiotic hydrogel TCS-GA-GFFY. By chemical bonding of TCS with self-assembled peptide, a polypeptide derivative TCS-GA-GFFY is prepared; and through the heating-cooling mode, TCS-GA-GFFY supramolecular hydrogel is formed and used as nano-antibiotic to enhance the effect of treating bacterial infection. The invention is characterized in that the preparation is simple, and the raw materials are easily available; and the product has good biocompatibility and is easy for clinical transformation. Meanwhile, the problem of poor water solubility of TCSis obviously improved, and the bioavailability of TCS is improved. Especially compared with free TCS, the TCS-GA-GFFY supramolecular hydrogel releases TCS through acid responsiveness and shows betterbacteria killing ability.

Description

technical field [0001] The invention belongs to the field of nano biomedical materials, and relates to a supramolecular hydrogel of self-assembled peptide chemically bonded with antibiotics, a preparation method thereof and an application in improving the therapeutic effect of bacterial infection. Background technique [0002] In recent years, the abuse of antibiotics and the rising rate of bacterial drug-resistant mutations have led to an increasing number of drug-resistant bacteria. At the same time, the development of new antibiotics to treat bacterial infections has struggled to keep pace with the evolution of bacteria. Therefore, it is imperative to modify and improve the existing antibiotics and develop more effective antibacterial agents to treat bacterial infections. Recently, many efforts have been made to modify existing antibiotics with various nanomaterials to improve their antibacterial effects. The formed "nanoantibiotics" can not only significantly improve t...

Claims

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Application Information

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IPC IPC(8): A61K47/64A61K9/06A61K31/085A61P31/04C07K5/103C07K1/16C07K1/06C07K1/04
CPCA61K47/64A61K9/06A61K31/085A61P31/04C07K5/1008Y02P20/55
Inventor 刘鉴峰侯小雪黄帆杨丽军刘金剑张玉民杨翠红任春华王忠彦张从柔
Owner INST OF RADIATION MEDICINE CHINESE ACADEMY OF MEDICAL SCI
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