EGCG (Epigallocatechin Gallate) functionalized chitosan derivative as well as EGCG functionalized chitosan derivative carried honokiol nano particle and preparation methods of EGCG functionalized chitosan derivative and EGCG functionalized chitosan derivative carried honokiol nano particle

A technology of honokiol and nanoparticles, which is applied in the direction of active ingredients of hydroxyl compounds, pharmaceutical formulations, drug combinations, etc., can solve the problems of unimproved biological activity, low bioavailability, and limited clinical application, and achieve favorable quality control, good biocompatibility, and significant sustained-release performance

Inactive Publication Date: 2017-02-22
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Honokiol has good antibacterial, anti-inflammatory, anti-oxidant, and anti-tumor activities, but due to its extremely poor water solubility and low bioavailability in the body, it needs to increase the dosage and take it for a long time, which greatly limits its clinical application
CN 104095817 A discloses a nanoparticle that directly uses chitosan to load magnolol and honokiol. The nanoparticle improves the solubility and dissolution rate of honokiol, but its biological activity is not improved

Method used

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  • EGCG (Epigallocatechin Gallate) functionalized chitosan derivative as well as EGCG functionalized chitosan derivative carried honokiol nano particle and preparation methods of EGCG functionalized chitosan derivative and EGCG functionalized chitosan derivative carried honokiol nano particle
  • EGCG (Epigallocatechin Gallate) functionalized chitosan derivative as well as EGCG functionalized chitosan derivative carried honokiol nano particle and preparation methods of EGCG functionalized chitosan derivative and EGCG functionalized chitosan derivative carried honokiol nano particle
  • EGCG (Epigallocatechin Gallate) functionalized chitosan derivative as well as EGCG functionalized chitosan derivative carried honokiol nano particle and preparation methods of EGCG functionalized chitosan derivative and EGCG functionalized chitosan derivative carried honokiol nano particle

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Embodiment 1

[0044] In the present embodiment, the preparation method of EGCG functionalized chitin derivatives and EGCG functionalized chitin derivatives loaded honokiol nanoparticles is provided, the steps are as follows:

[0045] (1) Dissolving chitin in the hydrochloric acid of 0.5wt% to form chitin concentration is the chitin hydrochloric acid solution of 2mg / mL, and epigallocatechin gallate (EGCG) is dissolved in water to form the concentration of 2mg / mL In the EGCG aqueous solution, honokiol is dissolved in an ethanol-water solution with a volume fraction of ethanol of 50% to form a solution with a honokiol concentration of 2 mg / mL.

[0046] (2) 100 parts by weight of chitin hydrochloric acid solution is added in the container, and then 5 parts by weight of H are dissolved with ascorbic acid 2 o 2 (Dissolving 1 part by weight of ascorbic acid in 8 parts by weight of H 2 o 2 middle), stirred magnetically at 20°C for 10 min, then added 15 parts of EGCG solution, stirred magneticall...

Embodiment 2

[0053] In the present embodiment, the preparation method of EGCG functionalized chitin derivatives and EGCG functionalized chitin derivatives loaded honokiol nanoparticles is provided, the steps are as follows:

[0054] (1) Chitin is dissolved in the hydrochloric acid of 5wt% to form the chitin hydrochloric acid solution that chitin concentration is 8mg / mL, and EGCG is dissolved in water and forms the EGCG aqueous solution that concentration is 6mg / mL, and magnolol is dissolved in ethanol The concentration of honokiol in 30% ethanol-water solution is 6mg / mL solution.

[0055] (2) Put 100 parts by weight of chitin hydrochloric acid solution into the container, then add 10 parts by weight of DMSO dissolved with ascorbic acid (dissolve 1 part by weight of ascorbic acid in 15 parts by weight of DMSO), stir magnetically at 30°C for 60 minutes, and then add 30 parts of EGCG solution were magnetically stirred for 60 min, and the resulting reaction solution was dialyzed 5 times and fr...

Embodiment 3

[0062] In the present embodiment, the preparation method of EGCG functionalized chitin derivatives and EGCG functionalized chitin derivatives loaded honokiol nanoparticles is provided, the steps are as follows:

[0063] (1) Chitin is dissolved in the hydrochloric acid of 10wt% to form the chitin hydrochloric acid solution that chitin concentration is 15mg / mL, and EGCG is dissolved in water and forms the EGCG aqueous solution that concentration is 10mg / mL, and magnolol is dissolved in ethanol The concentration of honokiol in 80% ethanol-water solution is 12 mg / mL solution.

[0064] (2) 100 parts by weight of chitin hydrochloric acid solution is added in the container, and then 20 parts by weight of H are dissolved with ascorbic acid 2 o 2 (dissolving 10 parts by weight of ascorbic acid in 30 parts by weight of H 2 o 2 Middle), magnetically stirred at 40°C for 50min, then 60 parts of EGCG solution was added, magnetically stirred for 90min, the resulting reaction solution was ...

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Abstract

The invention provides an EGCG (Epigallocatechin Gallate) functionalized chitosan derivative, an EGCG functionalized chitosan derivative carried honokiol nano particle and preparation methods of the EGCG functionalized chitosan derivative and the EGCG functionalized chitosan derivative carried honokiol nano particle. The structural formula of the EGCG functionalized chitosan derivative is as shown in the description; in the structural formula, the content of EGCG is 10 to 60 percent; the deacetylation degree is 50 to 98 percent; the content of amino is 50 to 98 percent. According to the EGCG functionalized chitosan derivative carried honokiol nano particle, the nano particle is prepared from the EGCG functionalized chitosan derivative and honokiol; the honokiol and the EGCG functionalized chitosan derivative form the nano particle through charge action; the honokiol is encapsulated inside the nano particle.

Description

technical field [0001] The invention belongs to the field of biomedical materials, and relates to EGCG functionalized chitin derivatives, honokiol nanoparticles loaded therein and a preparation method. Background technique [0002] Nanomedicine has become a research hotspot in recent years because of its special properties such as targeting, sustained release, and low toxicity. Chitin, which exists in large quantities in the shells of crustaceans, and its partially or fully deacetylated product chitosan has a large number of cations, has good biocompatibility and biodegradability, and nanoparticles based on chitin deacetylated products It has been practically applied in the fields of food and medicine. Chitosan drug-loaded nanoparticles have shown better solubilization or sustained-release effects, but the existing drug-loaded nanoparticles basically use chitosan (chitosan) directly as a carrier, and have no effect on the shell. The structural modification of polysaccharid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/05A61K47/36A61K47/22A61P35/00A61P31/04A61P31/10A61P29/00A61P39/06C08B37/08
CPCA61K9/19A61K9/0002A61K31/05A61K47/22A61K47/36C08B37/003
Inventor 李晖唐培潇
Owner SICHUAN UNIV
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