Preparation method of drug-loaded water-soluble chitosan nano-particles

A technology of water-soluble chitosan and nanoparticles, which is applied in the direction of powder transportation, etc., can solve the problems affecting the cell survival rate and drug integrity, and achieve the effect of reducing the probability of particle adhesion

Inactive Publication Date: 2012-06-13
常州市晨光树脂有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Glutaraldehyde is often used as a cross-linking agent in this method, but glutaraldehyde has certain cytotoxicity, which affects the survival rate of cells and the integrity of drugs.

Method used

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  • Preparation method of drug-loaded water-soluble chitosan nano-particles
  • Preparation method of drug-loaded water-soluble chitosan nano-particles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Weigh 0.2 g of water-soluble chitosan, fully dissolve it in 20 mL of deionized water, prepare a 1% (w / v) chitosan aqueous solution, and filter. Add 2mL Span80 into 80mL liquid paraffin, and stir mechanically at 2000r / min for 30min to disperse evenly. The chitosan aqueous solution was added dropwise to the oil phase, heated in a water bath to control the temperature at 40° C. and stirred for 30 min. Add 1 mL of 2% genipin solution dropwise for cross-linking, and stir rapidly at 40°C for 30 min. With 1% NaHCO 3 The pH value of the reaction system was adjusted to 4, and the reaction was performed under rapid mechanical stirring at 40° C. for 3 hours. Repeatedly wash with petroleum ether and water. Centrifuge at 4500rpm and vacuum dry at 40°C. The obtained nanoparticles have an average particle diameter of 563 nm.

Embodiment 2

[0022] Weigh 0.1 g of water-soluble chitosan, fully dissolve it in 20 mL of deionized water, prepare a 0.5% (w / v) chitosan aqueous solution, and filter. Add 2mL Span80 into 80mL liquid paraffin, and stir mechanically at 2000r / min for 30min to disperse evenly. The chitosan aqueous solution was added dropwise to the oil phase, heated in a water bath to control the temperature at 40° C. and stirred for 30 min. Add 1 mL of 2% genipin solution dropwise for cross-linking, and stir rapidly at 40°C for 30 min. With 1% NaHCO 3 The pH value of the reaction system was adjusted by the solution to 5, and the reaction was performed under rapid mechanical stirring at 40° C. for 3 h. Repeatedly wash with petroleum ether and water. Centrifuge at 4500rpm and vacuum dry at 40°C. The average particle diameter of the obtained nanoparticles is 280nm.

Embodiment 3

[0024] Weigh 0.4 g of water-soluble chitosan, fully dissolve it in 20 mL of deionized water, prepare a 2% (w / v) chitosan aqueous solution, and filter. Add 3mL Span80 into 80mL liquid paraffin, and stir mechanically at 2000r / min for 30min to disperse evenly. The chitosan aqueous solution was added dropwise to the oil phase, heated in a water bath to control the temperature at 40° C. and stirred for 30 min. Add 1 mL of 2% genipin solution dropwise for cross-linking, and stir rapidly at 40°C for 30 min. With 1% NaHCO 3 The solution adjusted the pH value of the reaction system to 6.5, and reacted with rapid mechanical stirring at 40° C. for 4 hours. Repeatedly wash with petroleum ether and water. Centrifuge at 4500rpm and vacuum dry at 40°C. The obtained nanoparticles have an average particle diameter of 249 nm.

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Abstract

The invention relates to a preparation method of water-soluble chitosan nano-particles which can be used as drug carriers. The chitosan nano-particles are prepared by adopting an emulsification cross-linking process, which comprises the following steps of: adding a chitosan aqueous solution into liquid paraffin added with an emulsifier at first, preparing W / O type emulsion, adding a genipin solution to crosslink, then, adjusting a pH value by using a NaHCO3 solution, rinsing by using petroleum ether after reacting, and drying in vacuum to obtain the chitosan nano-particles. The nano-particles prepared by using the method disclosed by the invention are good in sphericity and low in toxicity and can be used as the drug carriers.

Description

technical field [0001] The invention relates to a method for preparing drug-loadable water-soluble chitosan nanoparticles. Background technique [0002] Chitosan is a partially deacetylated derivative of chitin, the only alkaline polysaccharide in nature, with good biocompatibility, biodegradability, bioadhesion and non-toxicity, so it is widely used in wound repair, Tissue engineering and drug controlled release and other fields. [0003] Since the drug-loaded nanoparticles are targeted to specific tissues and have drug-controlled and sustained-release effects, the preparation of drug-loaded nanoparticles has become a research hotspot in recent years. Cancer cells have more negative charges than normal cells, and the surface of nanoparticles prepared from chitosan has more positive charges. Using chitosan nanoparticles as a drug carrier has strong targeting, which can effectively improve the drug delivery rate. utilization rate. In addition, chitosan nanoparticles are hy...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/36
Inventor 黄天兴吕波陈力
Owner 常州市晨光树脂有限公司
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