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Modified chitosan drug carrying microsphere and method for preparing same

A technology of drug-loaded microspheres and chitosan, which is applied in the direction of pharmaceutical formulations, antibacterial drugs, and medical preparations of non-active ingredients, etc., can solve the problem of serious drug burst release effect, anti-genotoxicity, and low density of microsphere skeleton etc. to achieve low cost, avoid cytotoxicity, and mild reaction conditions

Inactive Publication Date: 2012-09-19
HANGZHOU INST OF ADVANCED MATERIAL BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Glutaraldehyde is often used as a crosslinking agent in the preparation of microspheres by emulsification crosslinking, and proteins or peptides will react with glutaraldehyde to make them resistant to genotoxicity. Therefore, the application of this method to protein and peptide drugs is very limited.
The density of the microsphere skeleton formed by ion cross-linking is low, which is caused by the weak ionic bond, and the drug is mainly distributed on the surface of the microsphere, and the drug burst release effect is serious

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Weigh 2g of hyroxymecoumarin, 1g of methyl 10-bromodecanoate and 0.8g of potassium carbonate in 30mL of acetone, and stir at 70°C for 4h. Suction filtration, rotary distillation to remove the product, then react the product with 5% NaOH, acidify the system with 3mol / L HCl until the pH value of the system is 5, and wash with water repeatedly. Weigh 0.5 g of the above product, soak in water for 10 min, add 0.15 g of EDC and 0.1 g of NHS successively, and magnetically stir for 0.5 h to activate the carboxyl group. Weigh chitosan 0.13g and dissolve in 2% acetic acid solution, and drop the activated solution into the chitosan solution. The reaction was protected from light at room temperature for 24 h. Adjust the pH value of the reaction system to 8 with 1mol / L NaOH solution, and precipitate the product in acetone. Get 40 mg of the product and dissolve it in 100 mL of PBS buffer solution with a pH of 6 and a concentration of 0.01 mol / L, then add 20 mg of penicillin to it, ...

Embodiment 2

[0021] Weigh 2 g of hyroxymecoumarin, 1 g of methyl 10-bromodecanoate and 0.8 g of potassium carbonate in 30 mL of DMF, and stir at 70° C. for 4 h. Suction filtration, rotary distillation to remove the product, then react the product with 5% NaOH, acidify the system with 3mol / L HCl until the pH value of the system is 5, and wash with water repeatedly. Weigh 0.5 g of the above product, soak in water for 10 min, add 0.15 g of EDC and 0.1 g of NHS successively, and magnetically stir for 0.5 h to activate the carboxyl group. Weigh chitosan 0.13g and dissolve in 2% acetic acid solution, and drop the activated solution into the chitosan solution. The reaction was protected from light at room temperature for 24 h. Adjust the pH value of the reaction system to 8 with 1mol / L NaOH solution, and precipitate the product in acetone. Get 40 mg of the product and dissolve it in 100 mL of PBS buffer solution with a pH of 6 and a concentration of 0.01 mol / L, then add 20 mg of penicillin to i...

Embodiment 3

[0023] Weigh 2g of hyroxymecoumarin, 1g of methyl 10-bromodecanoate and 0.8g of potassium carbonate in 30mL of acetone, and stir at 70°C for 4h. Suction filtration, rotary distillation to remove the product, then react the product with 2% NaOH, acidify the system with 3mol / L HCl until the pH value of the system is 5, and wash with water repeatedly. Weigh 0.5 g of the above product, soak in water for 30 min, add 0.15 g of EDC and 0.1 g of NHS successively, and stir magnetically for 0.5 h to activate the carboxyl group. Weigh chitosan 0.13g and dissolve in 2% acetic acid solution, and drop the activated solution into the chitosan solution. React in the dark for 24 hours at room temperature. Adjust the pH value of the reaction system to 8 with 1mol / L NaOH solution, and precipitate the product in acetone. Get 40 mg of the product and dissolve it in 100 mL of PBS buffer solution with a pH of 6 and a concentration of 0.01 mol / L, then add 20 mg of penicillin to it, homogenize with ...

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PUM

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Abstract

The invention relates to the preparation of a modified chitosan drug carrying microsphere. Firstly, hymecromone is modified to obtain a hydrophobic group, the modified hymecromone is then used for modifying chitosan into an amphipathic chitosan which has a hydrophilic chain and a hydrophobic chain at the same time, an antibacterial agent is then added, and the chitosan drug carrying microsphere is produced by adopting a self-assembly method. The method has a simple preparation technology and moderate reaction conditions, and is lower in cost, and the prepared modified chitosan has amphipathy, the antibacterial agent is added, the drug carrying microsphere can be self assembled without adding a crosslinking agent, so the cytotoxicity is avoided. Moreover, the added antibacterial agent is the natural biological extract, so beneficial fungi and normal cells in the human body can be prevented from being damaged.

Description

technical field [0001] The invention relates to modified chitosan drug-loaded microspheres and a preparation method thereof Background technique [0002] Chitosan is an alkaline polysaccharide obtained by removing more than 55% of its N-acetyl group. It is the only naturally occurring hydrophilic cationic biodegradable polysaccharide with good biocompatibility. Its decomposition products Can be completely absorbed by the human body, therefore, chitosan is a good carrier for drug sustained release. The methods for preparing chitosan drug-loaded microspheres mainly include emulsification cross-linking method, ion gelation method, molecular self-assembly method and so on. Glutaraldehyde is often used as a crosslinking agent in the preparation of microspheres by emulsification crosslinking, and proteins or peptides will react with glutaraldehyde to make them resistant to genotoxicity. Therefore, the application of this method to protein and peptide drugs is very limited. . Th...

Claims

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Application Information

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IPC IPC(8): A61K47/36A61K9/16A61K45/00A61P31/04
Inventor 聂俊朱晓丹马贵平
Owner HANGZHOU INST OF ADVANCED MATERIAL BEIJING UNIV OF CHEM TECH
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