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Curcumin lipid carrier and preparation method thereof

A technology of curcumin lipid and lipid carrier, applied in liposome delivery, pharmaceutical formulation, drug delivery, etc.

Inactive Publication Date: 2009-04-01
NANJING MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The encapsulation efficiency of traditional solid lipid nanoparticles is only about 70%, and the drug in storage is degraded by the efflux carrier

Method used

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  • Curcumin lipid carrier and preparation method thereof
  • Curcumin lipid carrier and preparation method thereof
  • Curcumin lipid carrier and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Weigh 80mg of stearic acid, 20mg of Miglyol and 5mg of curcumin, melt and dissolve on a 70°C water bath, add a mixed solution of 0.4g of Tween 60 and 1.6g of ethanol at the same temperature and an appropriate amount of distilled water, and vortex on a vortex mixer for 1min After that, an O / W type transparent microemulsion can be formed. At a height of about 6cm from the cooling water surface, under electromagnetic stirring (1000r / min), drop the heat-insulating microemulsion into the water dispersion medium of 10 times the volume at 4°C at a rate of 5 seconds, cool and remove ethanol, and when the microemulsion After adding all the mixture, continue to keep stirring at 4°C for 15 minutes to obtain the nanostructured lipid carrier. The measured particle size and encapsulation efficiency were 208.4nm and 84.1%, respectively.

Embodiment 2

[0031] Weigh 80mg of glyceryl monostearate, 20mg of oleic acid and 5mg of curcumin, melt and dissolve on a water bath at 70°C, add a mixed solution of 0.4g of poloxamer 188 and 1.6g of 1,2-propanediol and an appropriate amount of distilled water at the same temperature , After vortexing on a vortex mixer for 1 min, an O / W transparent microemulsion can be formed. At a height of about 6cm from the surface of the cooling water, under electromagnetic stirring (1000r / min), drop the heat-preserved hot microemulsion into the water dispersion medium of 10 times the volume at 4°C at a rate of 5 seconds. When all the microemulsions are added, continue to Incubate and stir at 4°C for 15 minutes to obtain the nanostructured lipid carrier. The measured particle size and encapsulation efficiency were 179.1nm and 90.1%, respectively.

Embodiment 3

[0033] Weigh 80mg compritol 888, 20mg oleic acid and 5mg curcumin, melt and dissolve on a 70°C water bath, add 0.4g Cremophor RH40 and 0.8g 1,2-propanediol mixed solution and appropriate amount of distilled water at the same temperature, and vortex on a vortex mixer After spinning for 1 min, an O / W type transparent microemulsion can be formed. At a height of about 6cm from the surface of the cooling water, under electromagnetic stirring (1000r / min), drop the heat-preserved hot microemulsion into the water dispersion medium of 10 times the volume at 4°C at a rate of 5 seconds. When all the microemulsions are added, continue to Incubate and stir at 4°C for 15 minutes to obtain the nanostructured lipid carrier. The measured particle size and encapsulation efficiency were 159.2nm and 92.1%, respectively.

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Abstract

The invention provides a curcumin lipid carrier and a preparation method thereof for industrialized production. The curcumin lipid carrier comprises the effective remedy dosage of curcumin, lipid and the proper quantities of surface active agent, cosurfactant and additive. The curcumin lipid carrier prepared by the invention has small particle size and high drug loading efficiency and can improve the stability and bioavailability of the drug. The curcumin lipid carrier has good effects of protecting the nerve cell of experimental animal with cerebral ischemia reperfusion, keeping the integrality of the blood brain barrier and preventing and remedying post-stroke brain edema.

Description

technical field [0001] The invention belongs to the field of biomedical materials, in particular to a curcumin lipid carrier and a preparation method thereof Background technique [0002] Curcumin (Curcumin) [1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione] is derived from Curcuma L plant Curcuma longa, Zedoary, Curcuma It is a natural active ingredient extracted from the rhizomes of japonica, which has various pharmacological effects such as anti-tumor, anti-inflammation, anti-HIV, anti-bacterial, anti-oxidation, etc., and has low toxicity, which has the potential of clinical application. Because curcumin and its derivatives can prevent the activation of NF-κB, prevent the expression of inducible nitric oxide synthase (inducible nitric oxide synthase, iNOS) in cells, obviously remove the NO produced by it, and reduce the production of NO and some iron-containing substances. The enzymes form complexes, reduce the generation of peroxynitrite, and play a protectiv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K9/127A61K31/12A61P9/10A61P25/00
Inventor 朱东亚张青徐群为李瑞吴海银
Owner NANJING MEDICAL UNIV
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