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Rubimaillin/chitosan nanoparticle, and preparation method and application thereof

A nanotechnology of rubidin and chitosan, which is applied in the field of medicine, can solve the problems of large particle size of drug-loaded microspheres, high reaction conditions, and complicated preparation, and achieve anti-oxidation and inhibition of cancer cell activity with good repeatability , the effect of simple operation

Active Publication Date: 2014-11-05
WUHAN INSTITUTE OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are certain defects in the preparation methods of these chitosan drug-loaded microspheres, as some methods have used toxic reagents (glutaraldehyde), some methods are complicated to prepare, and the reaction conditions are higher (ion cross-linking method combined with secondary freeze-drying method), And the particle size of the obtained drug-loaded microspheres is relatively large, and the distribution is wide, etc.

Method used

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  • Rubimaillin/chitosan nanoparticle, and preparation method and application thereof
  • Rubimaillin/chitosan nanoparticle, and preparation method and application thereof
  • Rubimaillin/chitosan nanoparticle, and preparation method and application thereof

Examples

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Embodiment 1

[0026] The preparation method of rubidin / chitosan nano-microspheres of the present embodiment is as follows:

[0027] (1) Dissolve chitosan (deacetylation degree 82%, molecular weight 500,000) in an aqueous solution containing 0.1wt% poloxamer 188 and 1.5% (V / V) acetic acid to form a 1.0mg / mL shell The polysaccharide aqueous solution is then filtered through a microporous membrane with a pore size of 0.45 μm, and the resulting filtrate is adjusted to a pH value of 4.0 by a NaOH solution with a concentration of 1mol / L to obtain a chitosan component liquid;

[0028] (2) Dissolve rubikin in absolute ethanol to form a rubidin ethanol solution with a concentration of 1.0 mg / mL, and filter through a microporous membrane with a pore size of 0.45 μm to obtain the rubikin component liquid ;

[0029] (3) Add 1mL step (2) gained rubidin component liquid dropwise in 5mL step (1) gained chitosan component liquid, fully stir (stirring speed is 800r / min), and dropwise add 2mL1 .0mg / mL sodi...

Embodiment 2

[0033] The preparation method of rubidin / chitosan nano-microspheres of the present embodiment is as follows:

[0034] (1) Dissolve chitosan (deacetylation degree 97%, molecular weight 100,000) in an aqueous solution containing 0.3wt% poloxamer 188 and 1.0% (V / V) acetic acid to form a 1.2mg / mL shell The polysaccharide aqueous solution is then filtered through a microporous membrane with a pore size of 0.45 μm, and the resulting filtrate is adjusted to a pH value of 3.5 by a NaOH solution with a concentration of 1mol / L to obtain a chitosan component liquid;

[0035] (2) Dissolving rubikin in absolute ethanol to form a rubidin ethanol solution with a concentration of 3.0 mg / mL, and filter it through a microporous membrane with a pore size of 0.45 μm to obtain the rubikin component liquid ;

[0036](3) Add 1mL step (2) gained rubidin component liquid dropwise in 5mL step (1) gained chitosan component liquid, fully stir (stirring rate is 1200r / min), and dropwise add 2mL1 .5 mg / mL...

Embodiment 3

[0040] The preparation method of rubidin / chitosan nano-microspheres of the present embodiment is as follows:

[0041] (1) Dissolve chitosan (deacetylation degree 90%, molecular weight 300,000) in an aqueous solution containing 0.5wt% poloxamer 188 and 1.2% (V / V) acetic acid to form a 3.0mg / mL shell The polysaccharide aqueous solution is then filtered through a microporous membrane with a pore size of 0.45 μm, and the resulting filtrate is adjusted to a pH value of 4.5 by a NaOH solution with a concentration of 1mol / L to obtain a chitosan component liquid;

[0042] (2) Dissolving rubikin in absolute ethanol to form a rubidin ethanol solution with a concentration of 5.0 mg / mL, and filter it through a microporous membrane with a pore size of 0.45 μm to obtain the rubikin component liquid ;

[0043] (3) Add 1mL step (2) obtained rubidin component liquid dropwise in 5mL step (1) gained chitosan component liquid, fully stir (stirring speed is 1600r / min), and add dropwise 2mL3 .0 m...

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Abstract

The invention discloses a rubimaillin / chitosan nanoparticle, and a preparation method and an application thereof. The nanoparticle is a three-dimensional reticular structure formed by crosslinking chitosan with sodium tripolyphosphate, rubimaillin is fixed in the nanoparticle in a molecular form, the rubimaillin encapsulation rate is 4.58-14.64%, the average particle size of the nanoparticle is 96-467nm, and the polydispersity index, the drug loading capacity and the Zeta potential of the nanoparticle are 0.25-0.27, 5.73-28.153[mu]g / mg and 45.07-48.73mV respectively. The preparation method of the rubimaillin / chitosan nanoparticle comprises the following steps: 1, preparing a chitosan component liquid; 2, preparing a rubimaillin component liquid; and 3, adding the rubimaillin component liquid into the chitosan component liquid in a dropwise manner, fully stirring, and adding an aqueous solution of sodium tripolyphosphate of 1.0-3.0mg / mL in a dropwise manner in order to prepare the rubimaillin / chitosan nanoparticle. The nanoparticle prepared in the invention has the advantages of regular shape, small particle size, good dispersion, and obvious anti-oxidation and cancer cell inhibition effects, and is a potential antioxidant and antitumor preparation.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a rubiacin / chitosan nano-microsphere and a preparation method and application thereof. Background technique [0002] Rubia cordifolia L. is a Chinese herbal medicine with broad application prospects in medicine, and mollugin is the main active ingredient in Rubiaceae plants. Studies have found that rubidin has good biological activities such as anti-tumor, anti-oxidation, anti-mutagenesis, anti-virus, anti-bacterial, anti-inflammatory, anti-rheumatic, nerve protection, inhibition of fat accumulation, and hemostasis. It is used for arthritis, dysmenorrhea, massive bleeding, It is a plant active substance with broad research value and market prospect for the treatment of diseases such as rheumatism and urinary system disorders. However, due to the existence of phenolic hydroxyl groups in rubidin, the compound is unstable and easily oxidatively degraded in organic solvents; moreover...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/352A61K47/36A61P39/06A61P35/00
Inventor 陈嵘杨红红王雅萍杨浩吕中
Owner WUHAN INSTITUTE OF TECHNOLOGY
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