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High-stability non-vesicle-type nano particle and application of same in therapy of helicobator pylori infection

A nanoparticle, non-vesicular technology, applied in the application of nanoparticles in the treatment of Helicobacter pylori infection, the field of highly stable, non-vesicular nanoparticles can solve the problem of affecting practical application value, producing drug-resistant strains, issues of limited stability

Inactive Publication Date: 2017-04-05
ALAYA SHANGHAIBIOSCI CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of the drugs in these nanoparticles are traditional antibiotics, so it is still inevitable that drug-resistant strains will arise
Moreover, the preparation process of the nanoparticles used is complicated, the cost is high, and the stability is limited, which seriously affects the practical application value of this class of drugs.

Method used

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  • High-stability non-vesicle-type nano particle and application of same in therapy of helicobator pylori infection
  • High-stability non-vesicle-type nano particle and application of same in therapy of helicobator pylori infection
  • High-stability non-vesicle-type nano particle and application of same in therapy of helicobator pylori infection

Examples

Experimental program
Comparison scheme
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preparation example Construction

[0102] Preparation method of non-vesicular nanoparticles of the present invention

[0103] The non-vesicular nanoparticles of the present invention can be prepared by the following method, comprising the following steps:

[0104] 1). Surfactants and optional lipids are suspended in water;

[0105] 2). Stir the suspension obtained in 1) until a homogeneous suspension is formed;

[0106] 3). Heating the homogeneous suspension obtained in 2) above the melting point of the surfactant and optional lipid it contains;

[0107] 4). Add the fatty acid to the hot suspension obtained in 3) and stir;

[0108] 5). Lower the temperature and let stand the suspension obtained in 4), so as to obtain the non-vesicular nanoparticle suspension of the present invention.

[0109] In a specific embodiment, the melting temperature in the method is 20-80°C, such as 20°C, 30°C, 40°C, 50°C, 60°C, 70°C or 80°C.

[0110] In further embodiments, the method may further comprise measuring the hydrodynami...

Embodiment 1

[0149] Embodiment 1 Preparation and characterization of nanoparticles of the present invention

[0150] Nanoparticles of the invention were prepared as described in the "Materials and Methods" section.

[0151] The present inventors prepared nanoparticles of the present invention with different myristoleic acid loadings ranging from 0.1-4% w / v, such as figure 1As shown, an optimal yield of nanoparticles was thus selected while maintaining an acceptable nanoparticle size (approximately 9 nm). The inventors found that when the initial loading concentration of myristoleic acid increased, the nanoparticle size also increased ( figure 2 ). The best formulation chosen for subsequent experiments was 0.3% w / v myristoleic acid (2:1 mass ratio lipid to surfactant) with an average particle size of approximately 8.6 nm, below the threshold of 10 nm. The quality of the nanoparticles was detected by dynamic light scattering and characterized by the polydispersity parameter. The PDI of ...

Embodiment 2

[0153] Example 2. In vitro antibacterial activity of nanoparticles of the present invention

[0154] The effect of the nanoparticles of the present invention on Helicobacter pylori (Sydney strain 1, HPSS1) was determined by the MIC (defined as the lowest concentration that inhibits bacterial growth) and MBC (defined as the lowest that kills 99.9% of target bacteria) values ​​against Helicobacter pylori. In vitro antibacterial activity.

[0155] For determination of MIC, 0.05OD 600 (corresponding to 5×10 6 CFU / mL) of Helicobacter pylori were co-cultured with different concentrations (0 to 0.012% w / v) of the nanoparticles of the present invention. To quantify bacterial growth, after 18 hours of incubation, determine the OD of the bacterial culture 600 value, records the change value compared to the initial value. The change value reflects the growth of bacteria under the influence of the nanoparticles of the invention. Such as Figure 5 As shown, when the concentration of ...

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Abstract

The invention provides a high-stability non-vesicle-type nano particle and an application of same in therapy of helicobator pylori infection. The non-vesicle-type nano particle is composed of a C13-C15 fatty acid, a surfactant, and optionally lipids. The non-vesicle-type nano particle has significant antibacterial activity on helicobator pylori, has excellent stability and is free of induction of generation of a drug resistant strain, so that the nano particle can be used as an excellent antibacterial medicine.

Description

technical field [0001] The present invention relates to the field of medicine. Specifically, the present invention relates to a highly stable, non-vesicular nanoparticle and the application of the nanoparticle in the treatment of Helicobacter Pylori infection. Background technique [0002] Helicobacter pylori is the most common bacterial pathogen in the world, infecting more than half of the world's population. Helicobacter pylori infection leads to a variety of gastric diseases, including chronic gastritis, gastric ulcer and gastric cancer. [0003] At present, the general treatment plan for Helicobacter pylori infection in the world is triple therapy, that is, two antibiotics (clarithromycin + amoxicillin or metronidazole) combined with a proton pump inhibitor. However, due to the rapid emergence of H. pylori strains resistant to existing antibiotics, their eradication rates with current treatment regimens are rapidly declining. For example, triple therapy has reduced H...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K47/12A61K47/24A61K47/10A61K47/14A61K47/26A61K47/20A61K47/28A61K45/00A61P31/04A61P31/00
Inventor 谈贇
Owner ALAYA SHANGHAIBIOSCI CO LTD