Preparation method of genipin crosslinked chitosan drug-loaded microspheres

A technology of cross-linking chitosan and drug-loaded microspheres, which is applied in the fields of biology, food, and medical engineering. powerful effect

Inactive Publication Date: 2014-01-08
NANCHANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to overcome the defect that toxic crosslinking agent or organic solvent is introduced when preparing chitosan microspheres in the prior art, and the mechanical strength of prepared chitosan microspheres is not high, and to provide a safe, reliable, particle size adjustable The preparation method of chitosan drug-loaded microspheres with controllable surface state and biodegradable properties can significantly improve the mechanical strength of the microspheres; at the same time, further develop the application value of chitosan and broaden the scope of chitosan microspheres Through the continuous improvement of the preparation technology and theory of chitosan drug microspheres, more drugs with better efficacy can be prepared

Method used

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  • Preparation method of genipin crosslinked chitosan drug-loaded microspheres
  • Preparation method of genipin crosslinked chitosan drug-loaded microspheres
  • Preparation method of genipin crosslinked chitosan drug-loaded microspheres

Examples

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Comparison scheme
Effect test

Embodiment 1

[0022] Example 1. Take 50mL of liquid paraffin in a beaker, add 0.5g each of Tween-80 and Span-80, and stir for 30min at 30°C with a rotation speed of 660r / m to make an oily dispersion. Add 60mg of chitosan to 10mL of 2% acetic acid solution, then add 5mg of rhodiola rosea, after ultrasonic dissolution, add it to the above oil-containing dispersion at a uniform speed, stir for 30min at 30°C, and rotate at 660r / m, then slowly add 6mL of genipin absolute ethanol solution with a ratio of 70:1, and stir at 30°C for 3h at a speed of 660r / m, after standing for 2h, discard the supernatant to obtain the lower layer of sediment for centrifugation , washed three times with petroleum ether, acetone and absolute ethanol respectively. Finally, vacuum-dry at room temperature for 12 hours to obtain the chitosan drug-loaded microspheres of the present invention.

Embodiment 2

[0023] Example 2. Take 100mL of liquid paraffin in a beaker, add 1g each of Tween-80 and Span-80, and stir for 30min at 30°C with a rotation speed of 690r / m to make an oily dispersion. Add 120mg of chitosan to 20mL of acetic acid solution with a concentration of 2%, then add 10mg of salidroside, after ultrasonic dissolution, add it to the above oil-containing dispersion at a uniform speed, stir for 40min at 30°C, and rotate at a speed of 690r / m, then slowly add 12mL of genipin absolute ethanol solution with a ratio of 70:1, and stir at 30°C for 3.5h at a speed of 690r / m, after standing for 2h, discard the supernatant to obtain the lower precipitate Centrifuge and wash three times with petroleum ether, acetone and absolute ethanol respectively. Finally, vacuum-dry at room temperature for 12 hours to obtain the microspheres of the present invention.

Embodiment 3

[0024] Example 3: Take 150mL of liquid paraffin in a beaker, add 1.5mL each of Tween-20 and Span-80, and stir for 30min at 30°C with a rotation speed of 720r / m to make an oily dispersion. Add 180mg chitosan to 30mL acetic acid solution with a concentration of 2%, then add 15mg salidroside, after ultrasonic dissolution, add it to the above-mentioned oil-containing dispersion at a uniform speed, stir at 30°C for 50min, and rotate at a speed of 720r / m, then slowly add 18mL of genipin absolute ethanol solution with a ratio of 70:1, and stir at 30°C for 4h at a speed of 720r / m, after standing for 2h, discard the supernatant to obtain the lower layer of precipitate Centrifuge and wash three times with petroleum ether, acetone and absolute ethanol respectively. Finally, vacuum-dry at room temperature for 12 hours to obtain the microspheres of the present invention.

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Abstract

The invention relates to a preparation method of genipin crosslinked chitosan drug-loaded microspheres. The preparation method comprises the steps: after fully agitating water-insoluble oil-based substances with a surfactant evenly as an oil phase mixture by adopting an emulsion chemical-crosslinking method, adding a mixed solution with chitosan and loaded water-soluble drugs into the oil phase mixture as a water phase, fully agitating to an obtain a water-in-oil (W / O) type mixture, fully agitating and dropwise adding a crosslinking agent for crosslinking and curing through an injector, standing to remove the solution at the upper layer, centrifugally washing and drying the settling system at the lower layer respectively through an organic solvent to obtain the corresponding drug-loaded chitosan microspheres. The chitosan microspheres prepared by adopting the preparation method overcomes the defects and shortcomings existing in the traditional preparation method, are simple and easy in technique, low in toxic and side effects and high in mechanical strength, can be widely applied in the fields of food, biology, medical engineering and the like as a drug-use controlled-release carrier.

Description

[0001] technical field [0002] The invention belongs to the fields of food, biology, and medical engineering, and in particular relates to a chitosan-loaded chitosan with controllable particle size, controllable surface state, controllable swelling property, biodegradability, and can be used as a pharmaceutical slow-release carrier. Medicine microsphere, and preparation method thereof. Background technique [0003] Chitosan (chitosan) is the only basic amino polysaccharide that exists in the biological world. Its chemical name is (1,4)-2-amino-2-deoxy-β-D-glucan. It is abundant in nature. The chitin deacetylation product has many unique properties, such as good biocompatibility, biodegradability, bioadhesion, non-toxicity and antibacterial properties, etc., and is widely used in the fields of food, medicine and bioengineering materials. widespread attention. At the same time, it has recently been demonstrated as a controlled delivery system for active agents in the struct...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/36A61K31/7032
Inventor 熊华王素芳彭海龙宁方建陈莎罗美赵强朱雪梅黎文建
Owner NANCHANG UNIV
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