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Soluble thrombin nano-particle, and preparation method and application thereof

A nanoparticle and thrombin technology, applied in the field of biomedicine, can solve the problems of low solubility, low drug efficacy, and high toxicity, and achieve high bioavailability, reduced drug dosage, and good stability

Inactive Publication Date: 2014-06-04
SUN YAT SEN MEMORIAL HOSPITAL SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to overcome the disadvantages and deficiencies of low efficacy, low solubility, and high toxicity of thrombin-loaded drugs in the prior art, the primary purpose of the present invention is to provide a preparation method for soluble thrombin nanoparticles;

Method used

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  • Soluble thrombin nano-particle, and preparation method and application thereof
  • Soluble thrombin nano-particle, and preparation method and application thereof
  • Soluble thrombin nano-particle, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Preparation of amylose-polylysine nanoparticles:

[0046] (1) Synthesis of the first-generation dendritic polylysine by amidation reaction: 1.73g L-2,6-di-tert-butoxycarbonyllysine (5mmol) and 350μL propargylamine (5.5mmol) were co-dissolved in 20mL In anhydrous N,N dimethylformamide (DMF) solution, stir under nitrogen for 10min, then cool to 0°C, add 2.18g (5.5mmol) benzotriazole-N,N,N to the solution ', N'-tetramethyluronium hexafluorophosphate (HBTU) and 0.74g (5.5mmol) 1-hydroxybenzotriazole (HOBT), continue to stir at room temperature for 16h, after the reaction, add 200mL ethyl acetate Ester (EtOAc), with saturated NaHCO 3 solution, 0.1mol / L NaHSO 4 , saturated NaHCO 3 Solution and brine were rinsed sequentially, and then dried by rotary evaporation. The obtained crude product was purified by column chromatography (silica gel, chloroform-methanol=5:1), and then rotary evaporation could obtain 90% of the first generation dendrimer lysine.

[0047] (2) Synthesi...

Embodiment 2

[0051] Take 20 mg of amylose-polylysine nanoparticles obtained in Example 1, put them into a three-neck flask, add 500 ml of acetic acid aqueous solution with a mass percentage of 2%, and stir to make it dissolve completely; company) 3000u, add phosphate buffer (pH7.4) 100ml, stir to dissolve, and form a thrombin buffer solution; stir at a speed of 100-800 rpm at room temperature, and add the thrombin buffer solution dropwise to the linear chain Into the starch-polylysine acetic acid aqueous solution, the dropping time is 30min, the temperature is raised to 40°C, 30ml of glutaraldehyde solution with a mass fraction of 0.1% is added dropwise, stirring continuously at a speed of 200r / min for 30min, the stirring is stopped, and poured Put it into 500ml of liquid paraffin, stir for 25min, add 50ml of Tween 80, and stir at a high speed of 500 rpm for 4 hours to emulsify; take the emulsion and add 100ml of glutaraldehyde solution with a mass fraction of 25%, and stir for 30min to mak...

Embodiment 3

[0053] Take 40 mg of amylose-polylysine nanoparticles obtained in Example 1, put them into a three-necked flask, add 1500 ml of acetic acid aqueous solution with a mass fraction of 2%, and stir to make it dissolve completely; company) 6000u, add 150ml of phosphate buffer (pH7.4), stir to dissolve, and form a thrombin buffer solution; stir at a speed of 100-800 rpm at room temperature, and add the thrombin buffer solution dropwise to the above linear Into the starch-polylysine acetic acid aqueous solution, the dropping time is 40min, the temperature is raised to 40°C, 40ml of glutaraldehyde solution with a mass fraction of 0.1% is added dropwise, and the stirring is continued for 40min at a speed of 300 rpm, the stirring is stopped, and it is poured Put it into 500ml of liquid paraffin, stir for 35min, add 100ml of Tween 80, and stir at a high speed of 500 rpm for 4 hours to emulsify; take the emulsion and add 150ml of glutaraldehyde solution with a mass fraction of 25%, and sti...

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Abstract

The invention belongs to the field of biomedicines, and discloses a soluble thrombin nano-particle, and a preparation method and application thereof. The soluble thrombin nano-particle is of a core-shell structure, wherein the core is thrombin, and the shell is a nano-particle formed by crosslinking of cations of water soluble amylose-polylysine. The core-shell structure is advantageous to maintain the bioactivity of thrombin, can be preserved stably at room temperature, has the function of sustained release, is long in duration of drug-acting, cannot be easily degraded when entering a body, and is economical and safe. According to the nanoparticle, the particle diameter is 150-250nm preferably, so that the bioactivity of the thrombin can be well maintained, and the stability and sustained release function of nano-thrombin can be further improved. The encapsulation efficiency of the nano-thrombin is 50-75 percent preferably to well improve the stability and sustained release function of the nano-thrombin.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a soluble thrombin nanoparticle and a preparation method and application thereof. Background technique [0002] Thrombin is a highly specific serine proteolytic enzyme, it can hydrolyze the peptide bond of fibrinogen, produce insoluble fibrin, make the blood into gel and coagulate, and make the blood rapidly Coagulate and fill the bleeding point to achieve the purpose of hemostasis. Because of its advantages of fast hemostasis and no side effects, it is widely used in wounds, clinical surgical wounds, and bleeding and oozing of digestive tract mucosa, etc., with good hemostatic effect and definite curative effect. However, ordinary thrombin is a kind of protease reagent, which is easily affected by light, temperature, humidity, and especially microbial contamination factors, resulting in decreased or even lost biological activity. At room temperature, the aqueous solution...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K38/48A61K47/36A61P7/04C08G81/00
Inventor 陈汝福庄宝雄
Owner SUN YAT SEN MEMORIAL HOSPITAL SUN YAT SEN UNIV
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