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Drug-loaded nano-particles with core-shell structure as well as preparation method and application of drug-loaded nano-particles

A drug-loaded nanotechnology, core-shell structure technology, applied in pharmaceutical formulations, medical formulations with non-active ingredients, and medical formulations containing active ingredients, etc. The wide application of antibacterial peptides can achieve the effect of improving antibacterial effect, promoting physiological activity and simple preparation process.

Active Publication Date: 2022-07-05
CHANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the non-target toxicity of antimicrobial peptides is one of the reasons that hinder the wide application of antimicrobial peptides.
In addition, in the face of complex infection environments, especially in the presence of biofilms, a single antimicrobial peptide cannot achieve the expected therapeutic effect

Method used

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  • Drug-loaded nano-particles with core-shell structure as well as preparation method and application of drug-loaded nano-particles
  • Drug-loaded nano-particles with core-shell structure as well as preparation method and application of drug-loaded nano-particles
  • Drug-loaded nano-particles with core-shell structure as well as preparation method and application of drug-loaded nano-particles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] 1. Preparation of antimicrobial peptide AMP-Cy3

[0042] Firstly, using α-amino acid as raw material and 200mg MBHA resin as carrier, it was synthesized by Fmoc solid-phase synthesis method, that is, 5 times equivalents of amino acids of MBHA resin, 5 times equivalents of condensing agents HBTU and HOBT were weighed and dissolved in 4mL DMF. 400 μL of DIEA was added and cross-linked with the resin for 45 min.

[0043] Next, piperidine / DMF (20%, v / v) was added to react for 30 min to cleave the Fmoc protecting group on the amino acid. A color check was performed using ninhydrin at each step, and the above steps were repeated until the sequence was synthesized.

[0044] Then use piperidine / DMF (20%, v / v) to cut off the Fmoc group at the N-terminus of glycine, and the exposed amino group at the N-terminus reacts with 5 times the equivalent of Cy3 and an equimolar ratio of EDC and HOBT in the dark for 12h to form a sequence. AMP-Cy3. The target peptide chain was left to r...

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Abstract

The invention belongs to the field of biological medicine, and particularly relates to a drug-loaded nanoparticle with a core-shell structure and a preparation method and application thereof.The nanoparticle is of a shell-core structure composed of gelatin nanoparticles, Cypate and fluorescently-labeled antibacterial peptide, A-type gelatin and a photothermal agent Cypate coupled with the A-type gelatin jointly form a nano shell, and Cy3-labeled antibacterial peptide (AMP-Cy3) serves as an embedded core. When the antibacterial peptide exists in a gelatinase microenvironment of an infected part, a gelatin shell is degraded, and the internal fluorescent antibacterial peptide is released in a responsive manner, so that the non-target toxicity of the antibacterial peptide is reduced. In addition, heat generated by the photothermal agent Cypate irradiated by near-infrared light can also provide a good bactericidal synergistic effect for the antibacterial peptide, so that the purpose of selectively and rapidly eradicating bacteria at an infected part is achieved. The composite nanoparticles are simple and convenient to synthesize, high in biocompatibility and excellent in bactericidal effect, and have potential clinical conversion value as an antibacterial agent.

Description

technical field [0001] The invention belongs to the field of biomedicine, and particularly relates to a drug-carrying nanoparticle with a core-shell structure and a preparation method and application thereof. Background technique [0002] Staphylococcus aureus (S. aureus) infects about 30% of the total population and is a major cause of foodborne illness. During wound healing, cascades of hemostasis, inflammation, proliferation, and remodeling occur in an orderly fashion. Bacterial infection disrupts these steps of skin repair, and delayed wound healing, in turn, leads to persistent wound site infection, leading to Worsening of infection. [0003] Under the circumstance that the effect of antibiotic treatment is declining day by day, it is necessary to actively seek various new antibacterial drugs with alternative effects to fight against the evolving multidrug-resistant bacteria. At the same time, it is not easy to induce bacteria to develop drug resistance, and it is con...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/64A61K38/08A61K41/00A61P17/02A61P31/04
CPCA61K38/08A61K47/6435A61K41/0052A61P31/04A61P17/02A61K9/5169A61K2300/00
Inventor 王建浩李孟金周心霈惠泽轩邱琳崔朋飞周舒文王程胡华安子
Owner CHANGZHOU UNIV
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