Preparation and application of fucoidin self-assembled drug-loaded nanoparticles

A technology of fucoidan and drug-loaded nanometers, which is applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as high polymerization degree and low antioxidant capacity, and achieve Improve absorption, high drug loading efficiency, and reduce the number of administrations

Active Publication Date: 2022-06-21
QINGDAO UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The extremely strong ability to scavenge free radical ions endows proanthocyanidins with the basis for their biological activity, but high polymerization proanthocyanidins have extremely low antioxidant capacity and solubility in water due to their high degree of polymerization

Method used

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  • Preparation and application of fucoidin self-assembled drug-loaded nanoparticles
  • Preparation and application of fucoidin self-assembled drug-loaded nanoparticles
  • Preparation and application of fucoidin self-assembled drug-loaded nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Preparation of ferulic acid-fucoidan self-assembled nanoparticles

[0030] Accurately weigh 0.200g of fucoidan powder, dissolve it in 20ml of deionized water, dissolve by ultrasonic for 2min, stir at 500r / min for 2h, and set aside; accurately weigh 0.020g of ferulic acid powder, dissolve it in 1ml of ethanol Then, ultrasonically dissolve for 1 min, and at a stirring speed of 700 r / min, use a syringe to drop the ferulic acid-ethanol solution into the fucoidan-water solution dropwise; after the dropwise addition, continue to stir at 500 r / min for 1 h The fucoidan-ferulic acid self-assembled nanoparticles were obtained; the solvent evaporation method was used, and the ethanol was evaporated to dryness by continuing stirring for 2 hours at a rotation speed below 500 r / min, and the particle size was homogenized by filtration with a 220 nm microporous membrane. The obtained ferulic acid-fucoidan self-assembled nanoparticle solution had an average particle size of 136 nm.

Embodiment 2

[0032] Changes of body weight after cisplatin-induced kidney injury in mice

[0033] Mice were randomly divided into the following eight groups (n=6 per group): control group (physiological saline); ferulic acid (100 mg / kg); cisplatin (20 mg / kg) + saline; cisplatin (20 ng / kg) )+fucoidan; cisplatin (20ng / kg)+ferulic acid (50mg / kg); cisplatin (20ng / kg)+ferulic acid (100mg / kg); cisplatin (20ng / kg)+ferulic acid Acid-fucoidan nanoparticles (50mg / kg); cisplatin (20ng / kg) + ferulic acid-fucoidan nanoparticles (100mg / kg); the body weight changes before administration and before sacrifice were obtained such as image 3 .

Embodiment 3

[0035] Changes of serum urea nitrogen content in mice after kidney injury

[0036] Urea is the final product of protein metabolism in mice, and urea nitrogen in the blood comes from the liver and is excreted in the urine through the kidneys. Renal failure, nephritis, and urinary tract obstruction can increase blood urea nitrogen levels. The therapeutic potential of ferulic acid-fucoidan nanoparticles was further shown by detecting the changes of serum urea nitrogen content in mice.

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Abstract

The invention provides a preparation method of fucoidin self-assembled drug-loaded nanoparticles and application of the fucoidin self-assembled drug-loaded nanoparticles in prevention of renal injury. The preparation method comprises the following steps: connecting an indissolvable hydrophobic drug to fucoidin through a chemical bond, and then entrapping the hydrophobic drug through self-assembly to obtain the self-assembled nanoparticles, and specifically comprises the following steps: adding fucoidin powder into a proper amount of deionized water, carrying out ultrasonic-assisted dissolution and stirring to obtain a fucoidin solution with the concentration of 10 mg/ml; the preparation method comprises the following steps: dissolving a hydrophobic drug in a trace amount of ethanol (the volume ratio of ethanol to water is 1: 10-1: 20), dropwise adding the hydrophobic drug into a fucoidin solution by using an anti-solvent method to prepare self-assembled nanoparticles, and stirring and volatilizing ethanol by using a solvent volatilization method to obtain the nanoparticles with the pH value of 6-7, the particle size of about 150nm and the maximum drug loading capacity of 60%. According to the invention, fucoidin with good biocompatibility is used as a transport carrier, and the self-assembled nanoparticles containing hydrophobic drugs such as ferulic acid, caffeic acid and high polymer procyanidine are obtained. The carrier material selected by the method has functionality, so that the drug stability can be improved, and the dosage and toxicity can be reduced. The method is simple to operate, simple in equipment and suitable for industrial production, and has good social value and application prospect.

Description

technical field [0001] The invention relates to the field of biological materials and nanotechnology, in particular to a preparation method and application of self-assembly of hydrophobic medicines into nanometer medicines. Background technique [0002] Nanocarriers can increase solubility by increasing the dispersion and dissolution surface area of ​​poorly soluble active ingredients, improve membrane permeability through small particle size effects, improve bioavailability, and achieve controlled release in vivo. It can solve the problem of low bioavailability of some hydrophobic drugs and expand the application range of some hydrophobic drugs. [0003] The anti-solvent method is to use the different solubility of the drug in two different solvents to prepare nanoparticles. The drug is first dissolved in a good solvent, and then mixed with a poor solvent. When mixing, a local supersaturation state will be generated in the poor solvent, thereby causing Nucleation, nuclear ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/36A61K31/192A61K31/353
CPCA61K9/5161A61K31/192A61K31/353Y02A50/30
Inventor 郭传龙高新涛吴晓晨
Owner QINGDAO UNIV OF SCI & TECH
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