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Hepatocarcinoma targeting lipid nanoparticle as well as preparation method and application

A technology for targeting lipids and nanoparticles, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. It can solve problems such as restrictive design, achieve strong lipophilicity and enhance drug efficacy. Effect

Active Publication Date: 2017-08-18
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Oxaliplatin is slightly soluble in aqueous solvents and insoluble in ethanol, which limits its clinical application and the design of its drug delivery system

Method used

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  • Hepatocarcinoma targeting lipid nanoparticle as well as preparation method and application
  • Hepatocarcinoma targeting lipid nanoparticle as well as preparation method and application
  • Hepatocarcinoma targeting lipid nanoparticle as well as preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Take 10 mg of A54 polypeptide, accurately weigh it, dissolve it in 0.5 mL of anhydrous dimethyl sulfoxide, and prepare a solution with a concentration of 20 mg / mL. Add 4 μL of di-tert-butyl dicarbonate reagent to the A54 polypeptide solution, stir magnetically (300 rpm), and react for 12 hours at room temperature in the dark. Add 5 mg of carbodiimide and 3 mg of N-hydroxysuccinimide, and stir at room temperature for 1.5 h to obtain reaction solution 1. Another 17.6 mg of polyethylene glycol containing amino groups at both ends was taken, accurately weighed, and dissolved in 200 μL of anhydrous dimethyl sulfoxide. The reaction liquid 1 was added dropwise to the polyethylene glycol solution, and the reaction was stirred at room temperature for 12 h. Add 3 mg of N,N-disuccinimidyl carbonate, and stir at room temperature for 9 hours to obtain reaction solution 2. Take 2.36 mg of stearylamine, accurately weigh it, and ultrasonically dissolve it in 300 μL of absolute ethano...

Embodiment 2

[0021] Take 10 mg of A54 polypeptide, accurately weigh it, dissolve it in 0.5 mL of anhydrous dimethyl sulfoxide, and prepare a solution with a concentration of 20 mg / mL. Add 6 μL di-tert-butyl dicarbonate reagent to the A54 polypeptide solution, stir magnetically (300 rpm), and react at room temperature in the dark for 12 hours. Add 5 mg of carbodiimide and 3 mg of N-hydroxysuccinimide, and stir at room temperature for 1.5 h to obtain reaction solution 1. Another 17.6 mg of polyethylene glycol containing amino groups at both ends was taken, accurately weighed, and dissolved in 200 μL of anhydrous dimethyl sulfoxide. The reaction liquid 1 was added dropwise to the polyethylene glycol solution, and the reaction was stirred at room temperature for 12 h. Add 3 mg of N,N-disuccinimidyl carbonate, and stir at room temperature for 9 hours to obtain reaction solution 2. Take 2.36 mg of stearylamine, accurately weigh it, and ultrasonically dissolve it in 300 μL of absolute ethanol i...

Embodiment 3

[0023] Take 10 mg of A54 polypeptide, accurately weigh it, dissolve it in 0.5 mL of anhydrous dimethyl sulfoxide, and prepare a solution with a concentration of 20 mg / mL. Add 6 μL di-tert-butyl dicarbonate reagent to the A54 polypeptide solution, stir magnetically (300 rpm), and react at room temperature in the dark for 12 hours. Add 6 mg of carbodiimide and 3.6 mg of N-hydroxysuccinimide, and stir at room temperature for 1.5 h to obtain reaction solution 1. Another 17.6 mg of polyethylene glycol containing amino groups at both ends was taken, accurately weighed, and dissolved in 200 μL of anhydrous dimethyl sulfoxide. The reaction liquid 1 was added dropwise to the polyethylene glycol solution, and the reaction was stirred at room temperature for 12 h. Add 3 mg of N,N-disuccinimidyl carbonate, and stir at room temperature for 9 hours to obtain reaction solution 2. Take 2.36 mg of stearylamine, accurately weigh it, and ultrasonically dissolve it in 300 μL of absolute ethanol...

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Abstract

The invention provides a hepatocarcinoma targeting lipid nanoparticle, which encapsulates an anti-tumor drug oxaliplatin and targets a hepatocarcinoma cell BEL-7402. The lipid nanoparticle is prepared from A54 polypeptide-polyethylene glycol-eighteen-carbon chain graft, polyethylene glycol monostearate, an oxaliplatin phospholipid compound and glycerol monostearate, wherein the proportion of the A54 polypeptide-polyethylene glycol-eighteen-carbon chain graft is 5.3wt% to 18.2wt%; the proportion of the polyethylene glycol monostearate is 5.2wt% to 18.2wt%; the proportion of the oxaliplatin phospholipid compound is 15.2wt% to 35.0wt%; the proportion of the glycerol monostearate is 45.6wt% to 60.6wt%. The lipid nanoparticle provided by the invention can generate specific binding with the hepatocarcinoma cell to realize targeting action through A54 polypeptide on a surface, encapsulates an oxaliplatin granulesten compound, and enhances the anti-tumor-cell pharmacodynamic action of oxaliplatin.

Description

technical field [0001] The invention belongs to targeting lipid nanoparticles and a preparation method thereof, and mainly relates to liver cancer targeting lipid nanoparticles and a preparation method thereof. Background technique [0002] Lipid nanoparticles mainly use solid lipid or a small amount of liquid oil at room temperature as the carrier, and the drug is dispersed or encapsulated in the lipid core to form a solid micelle drug delivery system with a particle size of about 50-1000nm, forming a lipid nanoparticle drug delivery system. Lipid nanoparticles have good biocompatibility, can improve the stability of unstable drugs, and have slow and controlled release and long-acting effects. A certain proportion of liquid oil or mixed lipid can be used as a component to overcome the shortcomings of solid lipid materials such as high crystallinity and low drug loading, and realize the effective encapsulation of various drugs. The surface of lipid nanoparticles can also b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/42A61K47/10A61K47/06A61K31/555A61P35/00
CPCA61K9/5123A61K9/5146A61K9/5169A61K31/555
Inventor 胡富强孟廷廷袁弘邵士红
Owner ZHEJIANG UNIV
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