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Preparation method of composite particles wrapping quorum sensing inhibitor and product thereof

A quorum sensing and composite particle technology, which is applied to non-active ingredients in medical preparations, pharmaceutical formulations, active ingredients of hydroxyl compounds, etc. Better quorum sensing activity, improved encapsulation efficiency and stability, and reduced transport resistance

Active Publication Date: 2021-09-07
JIANGNAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003]Carvacrol is a highly lipophilic phenolic substance with low solubility in water, high volatility, and strong essential oil smell, so It is also difficult to use in a pure form in practical applications
[0004] At present, drug carriers are more or less effective in protecting active substances from adverse environmental conditions, improving solubility and bioavailability of fat-soluble substances, and improving controlled release. There are limitations
For example, when liposome is used as the encapsulation system, its outer membrane is thin, and the contents are prone to leakage. The organic solvent used in the preparation process of polymer nanoparticles cannot be completely removed, which limits the scope of application. Solid Lipid nanoparticles are prone to polymorphic transformation, resulting in low drug loading and unpredictable gelation tendency

Method used

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  • Preparation method of composite particles wrapping quorum sensing inhibitor and product thereof
  • Preparation method of composite particles wrapping quorum sensing inhibitor and product thereof
  • Preparation method of composite particles wrapping quorum sensing inhibitor and product thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0062] This example provides a preparation method for encapsulating quorum sensing inhibitor composite particles:

[0063] (1) Add sodium alginate to deionized water at 60°C, stir until completely dissolved to obtain an aqueous solution of sodium alginate; add montmorillonite powder to the aqueous solution of sodium alginate, mix well, and lower to 25°C, Stir for 1 hour, let it stand overnight to discharge air bubbles, and prepare a mixed solution of montmorillonite and sodium alginate, which is used as an aqueous phase for later use, wherein the mass fraction of montmorillonite is 2wt%, and the mass fraction of sodium alginate is 2wt%;

[0064] (2) Take monoglyceride stearate and heat it at 65°C to dissolve, add carvacrol after it is completely dissolved, and mix the two evenly as the oil phase, wherein the mass ratio of monoglyceride stearate to carvacrol is 2 :1;

[0065] (3) Heat the water phase prepared in (1) to 70°C, pour it into the beaker containing the oil phase in ...

Embodiment 2

[0070] Under the conditions of Example 1, the control conditions are: MMT (montmorillonite) content is 2% (w / w), Alg (sodium alginate) content is 2% (w / w), oil: carvacrol ( (mass ratio)=2:1, the oil-water ratio is (volume ratio) 1:5, other conditions are the same as embodiment 1, when exploring the oil phase is respectively liquid paraffin, beeswax and GMS (monoglycerol stearate) to microparticle preparation influences.

[0071] see results figure 1 .

[0072] figure 1 (a) and (b) are micrographs and SEM images of Pickering emulsions prepared using liquid paraffin as the oil phase. It can be seen that the particle size of the emulsion is about 20 μm, and the particle size difference after curing is large, and there is no fixed shape. This is because the preparation process of the microparticles needs to go through a large number of steps such as dilution, stirring, and centrifugation. The Pickering emulsion prepared by liquid paraffin will break and coalesce. More oil phas...

Embodiment 3

[0078] The influence of Alg mass fraction: under the condition of embodiment 1, control condition is: MMT (montmorillonite) content is 2% (w / w), GMS: carvacrol=2:1, oil-water ratio is 1:5 When the mass fraction of Alg was 1%, 1.5%, 2.0%, and 2.5%, the influence on the preparation of microparticles was studied, and other conditions were the same as in Example 2.

[0079] see results figure 2 , wherein, (a) is 1.0%, (b) is 1.5%, (c) is 2.0%, and (d) is the electron micrograph of 2.5%.

[0080] It can be seen that when the Alg content is low, there is not enough Alg and Ca 2+ Cross-linking will cause part of the shell layer of the solidified particle to not solidify into a network shape or the shell layer is thin, so that the outside of the particle does not have enough hardness and rigidity to resist external forces. Moreover, the fragile shell layer may be broken during solidification and dispersion, and the oil phase cannot be well wrapped, and a large number of particles a...

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Abstract

The invention discloses a preparation method of composite particles wrapping a quorum sensing inhibitor and a product thereof. The preparation method comprises the following steps: preparing a mixed solution of montmorillonite and sodium alginate as a water phase; preparing an oil phase containing the quorum sensing inhibitor; adding the oil phase into the water phase, and shearing and mixing to obtain microemulsion; and cooling and diluting the obtained microemulsion to obtain an aqueous dispersion of the emulsion, dropwise adding an ionic cross-linking agent solution, stirring and cross-linking after dropwise adding, standing, washing particles with deionized water, and freeze-drying to obtain the composite particles wrapping the quorum sensing inhibitor. According to the preparation method, the montmorillonite-based Pickering emulsion is used as a template to prepare the particles, the biotoxicity is low, the encapsulation efficiency and stability of the medicine are obviously improved, and the leakage of active ingredients in the storage process is reduced to a great extent.

Description

technical field [0001] The invention belongs to the technical field of preparation of antibacterial agents, and in particular relates to a preparation method and a product thereof for encapsulating quorum sensing inhibitor composite particles. Background technique [0002] Carvacrol is a monoterpenoid found in several aromatic plants such as oregano (Origanum vulgare), pepper grass (Lepidium flavum), and thyme (Thymus vulgaris). According to research reports, the sub-inhibitory concentration of carvacrol can reduce the motility and invasion of bacteria, and can also reduce the biofilm formation of Staphylococcus and Salmonella. The results showed that carvacrol interferes with the quorum-sensing signaling mechanism between bacterial cells, thereby reducing the ability to form biofilms. [0003] Carvacrol is a highly lipophilic phenolic substance with low solubility in water, high volatility, and strong essential oil smell, so it is difficult to use in pure form in practical...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/02A61K47/36A61K31/05A61P31/04
CPCA61K9/1652A61K9/1611A61K31/05A61P31/04Y02A50/30
Inventor 孙亚娟邓涵越杨成吕妍
Owner JIANGNAN UNIV
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