Preparation process for glycyrrhizic acid-mediated hydroxycamptothecine albumin liver cancer targeting nanoparticle lyophilized powder

A technology of hydroxycamptothecin and targeting nanoparticles, which is applied in freeze-dried delivery, medical preparations containing active ingredients, powder delivery, etc., and can solve the problem that nanoparticles do not have active targeting and do not have active targeting , poor biocompatibility and other issues, to achieve the effect of low production cost, high drug loading and uniform distribution

Inactive Publication Date: 2013-12-11
NORTHEAST FORESTRY UNIVERSITY +1
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  • Summary
  • Abstract
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  • Claims
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AI Technical Summary

Problems solved by technology

Nanoparticles have the characteristics of slow release, low toxicity, long residence time in the body, high stability in solution phase, and small particle size, but they do not have active targeting
Patent CN201110135725.8 discloses the preparation method of hydroxycamptothecin invisible nanoparticle sustained-release preparation. Biodegradable materials are used as drug carriers. The prepared nanoparticles have the effect of sustained release and long-term effect, but the nanoparticles do not have active targeting Poor biocompatibility and poor biocompatibility of polymers as carrier materials

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0024] Dissolve 60 mg of glycyrrhizic acid-coupled albumin in 60 mL of water, dissolve 7.4 mg of hydroxycamptothecin in 2.4 mL of chloroform-absolute ethanol solution, ultrasonicate for 5 minutes, place the albumin aqueous solution under the rotor of a homogenizer, The homogenization speed is 5000rpm, dropwise add the organic phase dissolved in hydroxycamptothecin, homogenate for 1 minute after the dropwise addition, transfer the homogenized system to a homogenizer, and homogenize 7 times under 800bar pressure to obtain half Transparent system with light yellow opalescence. The organic phase is removed by rotary evaporation, and the obtained water dispersion is freeze-dried to obtain glycyrrhizic acid-coupled albumin-loaded hydroxycamptothecin nanoparticle freeze-dried powder. The average particle size of nanoparticles is less than 200nm, and the encapsulation efficiency and drug loading are 96.7% and 10.6%.

example 2

[0026] Dissolve 80 mg of glycyrrhizic acid-coupled albumin in 80 mL of water, dissolve 9.6 mg of hydroxycamptothecin in 3.2 mL of chloroform-absolute ethanol solution, ultrasonicate for 10 minutes, place the albumin aqueous solution under the rotor of a homogenizer, The homogenization speed is 5000rpm, dropwise add the organic phase dissolved in hydroxycamptothecin, homogenate for 1 minute after the dropwise addition, transfer the homogenized system to a homogenizer, and homogenize 7 times under 800bar pressure to obtain half Transparent system with light yellow opalescence. The organic phase is removed by rotary evaporation, and the obtained water dispersion is freeze-dried to obtain glycyrrhizic acid-coupled albumin-loaded hydroxycamptothecin nanoparticle freeze-dried powder. The average particle size of nanoparticles is less than 200nm, and the encapsulation efficiency and drug loading are 93.1% and 9.97%.

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Abstract

The invention relates to a preparation process for glycyrrhizic acid-mediated hydroxycamptothecine albumin liver cancer targeting nanoparticle lyophilized powder. The glycyrrhizic acid-mediated hydroxycamptothecine albumin liver cancer targeting nanoparticle lyophilized powder is obtained by the steps of reacting glycyrrhizic acid and albumin under a certain conditions to successfully couple glycyrrhizic acid and albumin; removing glycyrrhizic acid uncoupled with albumin by a dialysis method; then lyophilizing albumin coupled with glycyrrhizic acid to obtain lyophilized powder of albumin coupled with glycyrrhizic acid; dissolving albumin coupled with glycyrrhizic acid in water at a certain concentration and hydroxycamptothecine in a mixed solution of chloroform and ethanol; dropwise adding the hydroxycamptothecine solution to the albumin solution slowly; homogenizing at a certain rotation speed and time; homogenizing the homogenized mixed suspension for a certain times under a certain pressure to obtain an oil-in-water emulsion; removing organic solvents-ethanol and chloroform from the mixed suspension by a rotary evaporation method; and then removing water from the mixed suspension in a lyophilization manner.

Description

technical field [0001] The invention relates to glycyrrhizic acid-mediated hydroxycamptothecin albumin liver cancer targeting nanoparticle freeze-dried powder and its preparation process, in particular to the treatment of liver cancer with targeting, high drug loading, small average particle size and uniform distribution Preparation of glycyrrhizic acid-mediated hydroxycamptothecin-albumin liver cancer-targeting nanoparticles. technical background [0002] Glycyrrhizic acid is the main active ingredient in licorice. Glycyrrhizic acid has the function of protecting the liver, so it is often added as a liver-protecting ingredient in medicines. Glycyrrhizic acid can accumulate in the liver in large quantities. Domestic research shows that there are glycyrrhizic acid receptors on the surface of liver cells, and glycyrrhizic acid receptors exist on the surface of liver tumor cells. Receptors are expressed in large quantities, and the expression level is 1.5-5 times that of norma...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/4745A61K47/42A61P35/00A61P1/16
Inventor 祖元刚赵修华孟丽葛云龙张印邓怡平
Owner NORTHEAST FORESTRY UNIVERSITY
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