Preparation method for novel drug-loaded chitosan nano-microspheres

A technology of chitosan nano- and drug-loaded microspheres, which is applied in the field of preparation of chitosan drug-loaded microspheres, can solve the problems of unsatisfactory slow-release and controlled-release effects, uneven size, poor dispersion, etc., and achieve sustained release Effective, easy to remove, good sphericity

Inactive Publication Date: 2012-04-25
AGRI PRODS PROCESSING RES INST CHINESE ACAD OF TROPICAL AGRI SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the commonly used preparation method of chitosan drug-loaded microspheres mainly adopts chemical cross-linking method, that is, formaldehyde, glutaraldehyde, sodium tripolyphosphate and sodium sulfate are used as cross-linking agents. Some of these cross-linking agents have strong At the same time, some prepared microspheres have a loose structure, uneven size, poor dispersion, unsatisfactory slow-release and controlled-release effects of drugs, and the phenomenon of "burst release" is more obvious

Method used

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  • Preparation method for novel drug-loaded chitosan nano-microspheres
  • Preparation method for novel drug-loaded chitosan nano-microspheres
  • Preparation method for novel drug-loaded chitosan nano-microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] First, dissolve 100mg of chitosan with a viscosity of 300mpa.s and a degree of deacetylation of ≥90% and 5mg of pentafluorouracil in 5g of 1% acetic acid solution. After fully dissolving, add slowly as an aqueous phase to 25g containing In the liquid paraffin oil phase of 2% sorbitol sesquioleate, stir quickly at room temperature for 60 minutes to form a white milky water-in-oil (W / O) emulsion; then add 24 g of 2.5% Put vanillin and acetone solution into the reaction system and continue to stir for 5h; finally, centrifuge at 10000rpm for 10min, collect the prepared drug-loaded nanospheres, and wash them thoroughly with petroleum ether and acetone, respectively, and freeze-dry to obtain light Yellow chitosan drug-loaded nanosphere powder. The microsphere has a particle size of 100-150 nm, a good sphericity, an encapsulation rate of 91.9%, and a drug loading rate of 21.8%.

Embodiment 2

[0030] First, dissolve 200mg of chitosan with a viscosity of 300mpa.s and a degree of deacetylation of ≥90% and 20mg of pentafluorouracil in 10g of a 1% acetic acid solution. After fully dissolving, add slowly as an aqueous phase to 50g containing In the liquid paraffin oil phase of sorbitan sesquioleate with a mass fraction of 2%, quickly stir at room temperature for 60 minutes to form a white milky water-in-oil (W / O) emulsion; then add 40g of 2.5% by mass Put vanillin and acetone solution into the reaction system and continue to stir for 5h; finally, centrifuge at 10000rpm for 10min, collect the prepared drug-loaded nanospheres, and wash them thoroughly with petroleum ether and acetone, respectively, and freeze-dry to obtain light Yellow chitosan drug-loaded nanosphere powder. The microsphere has a particle size of 100-150 nm, a good sphericity, an encapsulation rate of 95.7%, and a drug loading rate of 21.4%.

Embodiment 3

[0032] First, dissolve 300mg of chitosan with a viscosity of 300mpa.s and a degree of deacetylation of ≥90% and 30mg of pentafluorouracil in 12g of 1% acetic acid solution. After fully dissolving, add slowly as an aqueous phase to 60g containing In the liquid paraffin oil phase of sorbitan sesquioleate with a mass fraction of 2%, stir quickly at room temperature for 60 minutes to form a white milky water-in-oil (W / O) emulsion; then add 48g of a 2.5% mass fraction Put vanillin and acetone solution into the reaction system and continue to stir for 5h; finally, centrifuge at 10000rpm for 10min, collect the prepared drug-loaded nanospheres, and wash them thoroughly with petroleum ether and acetone, respectively, and freeze-dry to obtain light Yellow chitosan drug-loaded nanosphere powder. The microsphere has a particle size of 100-150 nm, a good sphericity, an encapsulation rate of 92.5%, and a drug loading rate of 19.9%.

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Abstract

The present invention discloses a method for preparing drug-loaded chitosan nano-microspheres, wherein sorbitan sesquioleate is adopted as an emulsifying agent, vanillin is adopted as a cross-linking agent, and an emulsifying and cross-linking method is adopted. The method comprises: dissolving a certain amount of chitosan and a certain amount of 5-fluorouracil in a certain amount of an acetic acid solution with a mass fraction of 1%; after completely dissolving, slowly adding the resulting solution to a certain amount of a liquid paraffin oil phase, and rapidly stirring at a room temperature to form a white emulsus water-in-oil emulsion, wherein the resulting solution is adopted as the water phase, the liquid paraffin oil phase contains a certain amount of an emulsifying agent; adding a certain amount of a cross-linking agent solution to the reaction system, and continuously stirring for a certain time; carrying out centrifugal separation, collecting the prepared drug-loaded nano-microspheres, completely washing respectively by petroleum ether and acetone, carrying out freeze drying to obtain the yellowish drug-loaded chitosan nano-microsphere powder, wherein the particle size of the prepared drug-loaded chitosan nano-microspheres is 100-150 nm, the sphericity is good, the controlled release effect is good, the encapsulation efficiency is 90-96%, the drug loading rate is 20-25%, and the drug-loaded chitosan nano-microspheres can meet clinical oral requirements and injection requirements. In addition, the method has a simple process, and is applicable for the large-scale production.

Description

【Technical Field】 [0001] The invention relates to a preparation method of chitosan drug-loaded microspheres, in particular to a method for preparing chitosan nano drug-loaded microspheres by adopting an emulsion cross-linking method. 【Background technique】 [0002] Chitosan is also known as chitosan, and its chemical name is (1,4)-2-amino-2-deoxy-β-D-glucose. It is a cationic high molecular natural polymer. Chitosan has many physiological activities. At the same time, due to its good biocompatibility and biodegradability, and the degradation products in the body are non-toxic, it is used in the medical field, especially as chemical drugs, peptide and protein drugs, and gene drugs. The application of carriers has received more and more attention. Chitosan can wrap the drug through chemical cross-linking, electrostatic adsorption, etc., forming a semi-permeable membrane on the surface of the drug. Since the barrier of the macromolecular framework must be overcome when the drug is...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/513A61K47/36A61P35/00
Inventor 李普旺杨子明王光彭政黄茂芳高为民孔令学
Owner AGRI PRODS PROCESSING RES INST CHINESE ACAD OF TROPICAL AGRI SCI
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