Low-density lipoprotein coupled N-succinyl chitosan nanoparticle vector, and preparation method and application thereof

A technology of succinyl chitosan and low-density lipoprotein, which is applied in the field of pharmaceutical preparations, can solve problems such as low encapsulation efficiency, difficulty in large-scale production, and high requirements for fat solubility, so as to reduce toxic and side effects, increase distribution, and slow release sex good effect

Inactive Publication Date: 2013-11-20
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, LDL has high requirements for the lipid solubility of loaded drug molecules, and the encapsulation efficiency is low. As an independent drug carrier, it is difficult to apply to large-scale production. Polymeric nanoparticles can solve these problems

Method used

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  • Low-density lipoprotein coupled N-succinyl chitosan nanoparticle vector, and preparation method and application thereof
  • Low-density lipoprotein coupled N-succinyl chitosan nanoparticle vector, and preparation method and application thereof
  • Low-density lipoprotein coupled N-succinyl chitosan nanoparticle vector, and preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0049] (1) Frozen plasma was dissolved at 37°C, refrigerated and centrifuged at 9000rpm for 30 minutes, and the top white chylomicrons were carefully sucked off. Calculate the amount of dry potassium bromide that needs to be added by the Radding-Steining formula:

[0050]

[0051] in, d 0 and V 0 are the initial plasma density and initial volume, respectively, d 1 is the plasma density to be adjusted, and 0.312 is the specific volume of KBr (mL g -1 ), X It is the mass (g) of KBr to be added. According to d=m / v, the initial density of plasma is measured by weighing method d 0 , weigh a certain amount of dry KBr to adjust the plasma density to 1.3g·mL -1 . After the solid KBr is completely dissolved, inject 4 mL of plasma into the centrifuge tube with a syringe, and carefully spread along the tube wall to a density of 1.006 g·mL -1 3.5mL of NaCl solution, balanced by ultracentrifugation at 55000rpm for 4h, plasma lipoproteins have been separated after centrifugat...

Embodiment 2

[0055] Weigh 0.05g of Suc-CS and dissolve it in 50mL of distilled water, add 0.01g of doxorubicin hydrochloride (Dox·HCl) to fully dissolve, 500r·min -1 Preheat in a water bath at 30°C for 20min under magnetic stirring, and the concentration is 1.2mg·mL -1 The TPP aqueous solution was dropped into it drop by drop at a rate of 1 drop every 2 seconds until the solution just produced opalescence. Doxorubicin N-succinyl chitosan nanoparticles (Dox-SCS-NPs) were obtained by passing through a 0.22 μm microporous membrane. Take 5 mL of Dox-SCS-NPs prepared according to the optimal prescription, add 5 mL of PBS (pH 5.5) dissolved with 25 mg EDC·HCl and 5 mg NHS, stir at room temperature for 15 min, and adjust the pH of the solution to 7.4 to terminate the activation. Add 1 mL of LDL (dialyzed in borate buffer with pH 9.4) and stir at room temperature for 2 h, and filter through a 0.45 μm microporous membrane to obtain LDL-coupled doxorubicin N-succinyl chitosan polymer nanoparticles...

Embodiment 3

[0057] Weigh 0.1 g of Suc-CS and dissolve it in 50 mL of distilled water, add poloxamer 188 at a final concentration of 0.5%, and preheat in a water bath at 40 °C for 20 min under magnetic stirring at 500 r / min as the water phase. In addition, weigh egg yolk lecithin with a final concentration of 1.2% in a small beaker, add ethyl acetate and acetone (v / v=3:1) to dissolve phospholipids as the oil phase, and the volume ratio of oil to water is 1:5. The oil phase was quickly injected into the water phase under stirring, and the stirring was continued for 20 min after the white color of the solution faded. N-succinyl chitosan nanoparticles (SCS-NPs) were obtained by passing through a 0.22 μm microporous membrane. Take 5 mL of SCS-NPs prepared according to the optimal prescription, add 5 mL of PBS (pH 5.5) dissolved with 25 mg of EDC·HCl and 5 mg of NHS, stir at room temperature for 15 min, and adjust the pH of the solution to 7.4 to terminate the activation. Add 1mL of LDL (dialy...

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Abstract

The invention discloses a low-density lipoprotein coupled N-succinyl chitosan nanoparticle vector, and a preparation method and application thereof as a vector of an active anti-tumor targeting drug delivery system. Chitosan is modified into N-succinyl chitosan with good water solubility and then the N-succinyl chitosan is prepared into nanoparticles; with a succinyl group as a connecting arm, the nanoparticles is in covalently binding to active amino acid of apoB-100 in low-density lipoprotein, so as to obtain low-density lipoprotein mediated and tumor tissue targeted polymer nanoparticles. By adopting the preparation method, drug-loaded polymer nanoparticles are prepared by taking adriamycin as a model drug. Experiments prove that the nanoparticles are high in encapsulation efficiency and drug loading amount and have slow release effect; cells are effectively ingested through a low-density lipoprotein receptor pathway, thereby increasing the treatment effect; the toxic and side effects are reduced; and targeted treatment is realized. A novel drug vector and a preparation form are provided for building of the anti-tumor targeting drug delivery system.

Description

technical field [0001] The invention relates to a modified N-succinyl chitosan polymer nanoparticle, a preparation method and its application, in particular to the application of the nanoparticle as a carrier in anti-tumor drug receptor targeting nano-preparations, belonging to field of pharmaceutical preparations. Background technique [0002] With the sharp increase in the incidence and mortality of tumors, malignant tumors have become the main killer threatening human life and health, and the treatment of tumors has also become an urgent problem to be solved. In the treatment of tumor diseases, the treatment of chemotherapy drugs lacks selectivity. More than 90% of the drugs are distributed in normal tissues, and only 2%–5% are taken up by tumor tissues, resulting in poor efficacy of anticancer drugs. Moreover, the anti-tumor chemotherapeutic drugs used in clinical practice have a certain degree of toxic and side effects, and also cause great damage to the normal body du...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/36A61K47/42A61P35/00
Inventor 张学农朱巧玲杨舒迪张春歌
Owner SUZHOU UNIV
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