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Preparation and application of nano medicine targeting at adhesion factor ICAM-1

A technology of ICAM-1 and adhesion factor, which is applied in the field of preparation of anti-tumor metastasis drugs, can solve the problems of poor water solubility and low bioavailability, and achieve the effects of growth inhibition, good therapeutic effect and high amplification effect

Active Publication Date: 2017-11-24
FUZHOU UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, due to limiting factors such as poor water solubility and low bioavailability of ursolic acid, its clinical development and application as an anticancer drug at home and abroad is limited.

Method used

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  • Preparation and application of nano medicine targeting at adhesion factor ICAM-1
  • Preparation and application of nano medicine targeting at adhesion factor ICAM-1
  • Preparation and application of nano medicine targeting at adhesion factor ICAM-1

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The preparation method of ICAM-1-CS-UA NPs comprises the following steps:

[0036] 1) Preparation of ursolic acid solution

[0037] Accurately weigh 60 mg of ursolic acid (UA), add 40 mL of DMSO to dissolve, then add 63.2 mg of EDC and 50.3 mg of NHS in turn and stir at room temperature for 2 h to obtain an activated UA solution;

[0038] 2) Preparation of ursolic acid-chitosan conjugates

[0039] Accurately weigh 40mg of chitosan with a molecular weight of 30KD, dissolve it in 10 mL of 1wt% acetic acid solution to obtain a chitosan solution; slowly add the activated UA solution to the constantly stirring chitosan solution, and freeze-dry after purification After that, the conjugate (CS-UA) of ursolic acid and chitosan was obtained; the specific purification method was as follows: after reacting at room temperature for 16 h, the above-mentioned mixture was placed in a dialysis bag with a molecular weight cut-off of 1000, placed in Containing 40% methanol, pH 7.4 in PBS ...

Embodiment 2

[0048] Dissolve the CS-UA conjugate in 0.1mol / L acetic acid solution to obtain a CS-UA solution with a concentration of 1mg / mL, adjust the pH of the CS-UA solution to 5.0, and stir magnetically at room temperature to obtain a concentration of 1mg / mL / mL of sodium tripolyphosphate (TPP) solution was slowly added dropwise to the CS-UA solution (V:V=5:1) until white opalescence appeared, stirring continuously during the dropping process, and the reaction was carried out for 2 hours , to obtain CS-UA nanoparticles (CS-UA NPs) prepared by ion cross-linking method.

Embodiment 3

[0050] Accurately weigh 6 mg of UA and dissolve in 1 mL of methanol, dissolve 4 mg of CS in 2 mL of 1% acetic acid-water solution, add 100 μL of methanol solution dropwise to CS acetic acid-water solution, stir magnetically for 30 min, centrifuge and take the supernatant obtained from assembled CS / UA nanomedicines (CS / UA NPs), where the molar ratio of CS to UA is 1:90.

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Abstract

The invention belongs to the field of preparation of anti-tumor metastasis medicines, and specifically relates to a chitosan nano medicine targeting at adhesion factor ICAM-1 and preparation and application thereof. Ursolic acid and chitosan are coupled to obtain a CS-UA conjugate, an ICAM-1-CS-UA conjugate is formed from the CS-UA conjugate and ICAM-1 through an amido bond, and finally an ICAM-1-CS-UA nano medicine is formed by ionic crosslinking method. The nano medicine has many advantages such as high specificity, low toxic and side effects and simple operation, and provides a good application prospect for the development of anti tumor and anti metastatic drugs in clinic.

Description

technical field [0001] The invention belongs to the field of preparation of anti-tumor metastasis drugs, and in particular relates to a chitosan nanometer drug targeting adhesion factor ICAM-1 and its preparation and application. Background technique [0002] Cancer is one of the diseases that seriously threaten human life and health. Tumor metastasis is the main cause of death of cancer patients, not only because the process of tumor metastasis is complicated and difficult to control, but also because metastases are difficult to surgically remove and drug resistance is more likely to form . Data show that 90% of the deaths of clinical tumor patients are caused by tumor metastasis. Therefore, the development of anti-tumor metastasis drugs is very important to improve the survival rate of cancer patients. The process of tumor metastasis involves cell shedding, infiltration, migration, implantation, angiogenesis, etc. As long as one or more of the above processes can be preve...

Claims

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Application Information

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IPC IPC(8): A61K47/68A61K31/56A61P35/00A61P35/04C08B37/08
CPCA61K31/56C08B37/003
Inventor 邵敬伟郭燕许爱笑
Owner FUZHOU UNIVERSITY
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