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Chitosan microemulsion for curcumin transdermal delivery and preparation method thereof

A technology of chitosan and curcumin, applied in the field of biomedical materials, can solve problems affecting drug stability, low bioavailability, strong skin irritation, etc., to reduce skin irritation, high-efficiency skin permeability, and promote skin penetration sexual effect

Active Publication Date: 2022-04-01
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, a large number of surfactants in traditional microemulsions will affect the stability of the drug and have strong skin irritation, causing irreversible damage to the skin
[0004] Curcumin is a yellow pigment extracted from the rhizome of turmeric, which has the effects of lowering blood fat, anti-tumor, anti-inflammation, choleretic, and anti-oxidation, but due to its chemical instability, poor solubility, low bioavailability, etc. , specific applications are limited

Method used

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  • Chitosan microemulsion for curcumin transdermal delivery and preparation method thereof
  • Chitosan microemulsion for curcumin transdermal delivery and preparation method thereof
  • Chitosan microemulsion for curcumin transdermal delivery and preparation method thereof

Examples

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Effect test

Embodiment 1

[0034] 1) Place 0.4ml of epichlorohydrin and 1ml of N,N-dimethyl n-dodecylamine in a water bath, heat up to 50°C, and stir for 2 hours to prepare epoxy long-chain alkyl quaternary ammonium salt;

[0035] 2) Add 5ml of isopropanol into 15ml of deionized water, and stir evenly to obtain an isopropanol solution. Get 1g carboxymethyl chitosan and add in isopropanol solution, stir at room temperature to obtain chitosan solution;

[0036] 3) Slowly add the epoxy long-chain alkyl quaternary ammonium salt prepared in step 1) dropwise into the chitosan solution in step 2), and stir while adding dropwise until the mixture is evenly stirred;

[0037] 4) Dissolve 1.45g of sodium hydroxide in 2ml of deionized water, stir evenly to obtain a sodium hydroxide solution, slowly add the sodium hydroxide solution dropwise to the mixture in step 3), stir while adding, dropwise add After completion, keep the mixture in a water bath at 50°C for 24 hours with stirring, and the product is dialyzed wi...

Embodiment 2

[0043] 1) Place 0.4ml of epichlorohydrin and 1ml of N,N-dimethyl n-octadecylamine in a water bath, heat up to 50°C, and stir for 2 hours to prepare epoxy long-chain alkyl quaternary ammonium salt;

[0044] 2) Take 5ml of isopropanol and add it to 15ml of deionized water, stir evenly to obtain an isopropanol solution, take 1g of carboxymethyl chitosan and add it to the isopropanol solution, stir at room temperature to obtain a chitosan solution;

[0045]3) Slowly add the epoxy long-chain alkyl quaternary ammonium salt prepared in step 1) dropwise into the chitosan solution in step 2), and stir while adding dropwise until the mixture is evenly stirred;

[0046] 4) Dissolve 1.45 g of sodium hydroxide in 2 ml of deionized water, stir evenly to obtain a sodium hydroxide solution, slowly add the sodium hydroxide solution dropwise to the mixture in step 3), and stir while adding dropwise. After the dropwise addition was completed, the mixture was kept stirring in a water bath at 50° ...

Embodiment 3

[0052] 1) Place 0.4ml of epichlorohydrin and 1ml of N,N-dimethyl n-octadecylamine in a water bath, heat up to 50°C, and stir for 2 hours to prepare epoxy long-chain alkyl quaternary ammonium salt;

[0053] 2) Take 5ml of isopropanol and add it to 15ml of deionized water, stir evenly to obtain an isopropanol solution, take 1g of carboxymethyl chitosan and add it to the isopropanol solution, stir at room temperature to obtain a chitosan solution;

[0054] 3) Slowly add the epoxy long-chain alkyl quaternary ammonium salt prepared in step 1) dropwise into the chitosan solution in step 2), and stir while adding dropwise until the mixture is evenly stirred;

[0055] 4) Dissolve 1.45 g of sodium hydroxide in 2 ml of deionized water and stir evenly to obtain a sodium hydroxide solution. The sodium hydroxide solution was slowly added dropwise to the mixture in step 3), stirring while adding dropwise. After the dropwise addition was completed, the mixture was kept stirring in a water b...

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Abstract

The invention discloses a chitosan microemulsion for curcumin transdermal drug delivery and a preparation method thereof, and the preparation method comprises the following steps: 1) reacting long-chain alkyl tertiary amine with epoxy chloropropane to prepare epoxy long-chain alkyl quaternary ammonium salt; 2) dissolving the water-soluble chitosan derivative in a mixed solution of isopropanol and water, adding epoxy long-chain alkyl quaternary ammonium salt under an alkaline condition, and reacting to obtain an amphiphilic chitosan derivative; 3) dissolving the amphiphilic chitosan derivative in the water phase, adding the oil phase, uniformly stirring, and adding a cosurfactant to prepare a chitosan microemulsion; and 4) adding 0.1-3.5 mg / ml of curcumin into the chitosan micro-emulsion, and carrying out ultrasonic treatment until the curcumin is completely dissolved to obtain the drug-loaded chitosan micro-emulsion. The microemulsion has a stable nanometer size, can efficiently entrap drugs, and improves the transdermal permeability of the drugs. The microemulsion can effectively entrap curcumin to achieve a solubilizing effect, meanwhile, the stability of the curcumin is improved, the skin permeability of the curcumin is promoted, and finally the efficient percutaneous treatment effect is achieved.

Description

technical field [0001] The invention relates to the technical field of biomedical materials, in particular to a chitosan microemulsion for transdermal administration of curcumin and a preparation method thereof. Background technique [0002] Common routes of administration mainly include oral administration, intramuscular injection, intravenous injection, respiratory tract administration, and transdermal administration. Oral administration is safe and convenient, but due to the hepatic first-pass effect, the bioavailability of the drug is low. The injection method has a higher risk because the injection site is close to the nerve and the instantaneous high blood concentration. The disadvantage of the respiratory route of administration is that the dose is not easy to control and the daily administration is not convenient enough. Transdermal drug delivery is the third largest drug delivery system after oral administration and injection. It refers to a type of drug delivery ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/12A61K47/36A61P3/06A61P35/00A61P29/00A61P1/16A61P39/06
CPCY02A50/30
Inventor 曹晓东张洁
Owner SOUTH CHINA UNIV OF TECH