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Tumor targeting nanometer micelle, preparation method and application of tumor targeting nanometer micelle as drug carrier

A nanomicelle, tumor targeting technology, applied in the field of biomedicine, can solve the problems of chemoresistant cancer cell clone and distant metastasis, chemotherapy can not achieve therapeutic effect, large side effects, etc., achieves good degradability, suitable for The effect of drug loading and easy operation

Active Publication Date: 2020-11-03
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to its poor selectivity, excessive side effects, easy induction of chemoresistant cancer cell clones and distant metastasis, chemotherapy still cannot achieve the desired therapeutic effect

Method used

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  • Tumor targeting nanometer micelle, preparation method and application of tumor targeting nanometer micelle as drug carrier
  • Tumor targeting nanometer micelle, preparation method and application of tumor targeting nanometer micelle as drug carrier
  • Tumor targeting nanometer micelle, preparation method and application of tumor targeting nanometer micelle as drug carrier

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] The synthesis of embodiment 1 chondroitin sulfate-rhein polymer:

[0080] (1) Synthesis of chondroitin sulfate-adipate dihydrazide: Weigh 0.5g chondroitin sulfate and dissolve it in 100mL distilled water, stir to make it fully swell and dissolve, then add 3.52g adipic acid dihydrazide to the solution in turn Hydrazide, 2.0g 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride and 0.8g N-hydroxysuccinimide, reacted at room temperature for 24 hours, dialyzed with distilled water for three days, The intermediate product chondroitin sulfate-adipate dihydrazide was obtained by freeze-drying.

[0081] (2) Weigh 30 mg of rhein and dissolve it in 10 mL of dimethyl sulfoxide, and sequentially add 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide equivalent to 5 times the molar amount of rhein Hydrochloride, N-hydroxysuccinimide equivalent to 5 times the molar amount of rhein, stirred at room temperature for 4 hours to activate rhein.

[0082] (3) Synthesis of chondroitin su...

Embodiment 2

[0086] Example 2 Preparation of cross-linked chondroitin sulfate-rhein-lipoic acid polymer nanomicelles loaded with docetaxel

[0087] (1) 50 mg of chondroitin sulfate-rhein-lipoic acid (prepared in Example 1) was ultrasonically dispersed in 10 mL of deionized water for subsequent use; another 15 mg of docetaxel was weighed and dissolved in 1 mL of methanol, and stirred vigorously Slowly add it dropwise to the above-mentioned chondroitin sulfate-rhein-lipoic acid polymer aqueous solution, and after stirring vigorously at room temperature for 4 hours in the dark, use probe-type ultrasonic treatment at 120W power three times, each time for 4min, pulse on for 2s and stop for 4s, Keep the temperature at 4°C-9°C, then transfer the solution to a dialysis bag and dialyze against water for 12 hours, then add a dithiothreitol solution containing 10% of the ester groups contained in the nanoparticles under strong stirring, and stir at room temperature for 12 hours After that, it was aga...

Embodiment 3

[0089] Example 3 In vitro release test of cross-linked chondroitin sulfate-rhein-lipoic acid nanoparticle micelles loaded with docetaxel

[0090] In this example, DTT is used to simulate the hyperoxic environment in the tumor tissue, and the release rate of the drug is measured by the reverse dynamic dialysis method: take 1 mL of the nano-micelle (prepared in Example 2) solution, and put it in a medium with a molecular weight cut-off of 3500 Daltons In a dialysis bag, use 40ml of phosphate buffered saline (PBS) with a pH of 7.4 containing 0.2% Tween 80 as the release medium, the stirring speed is 100r / min, the temperature is 37±0.5°C, and 1mL of the dialysis medium is taken at a predetermined time And add an equal amount of fresh release medium. After sampling, inject 20 μL of sample for HPLC determination, and calculate the cumulative release percentage, such as Figure 5 shown. The results showed that compared with docetaxel API, the cross-linked chondroitin sulfate-rhein-...

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Abstract

The invention particularly relates to a tumor targeting nanometer micelle, a preparation method and an application of the tumor targeting nanometer micelle as a drug carrier. Aiming at the defect thata traditional chemotherapy method is poor in selectivity, the invention aims to design a drug delivery carrier having the multifunctional targeting effect and an acoustodynamic effect and improve thedelivery efficiency of antitumor drugs. Based on the technical purpose, the invention provides a multifunctional targeting nanometer drug delivery system taking chondroitin sulfate as a skeleton, water-soluble chondroitin sulfate as a basic skeleton, and rhein and lipoic acid as hydrophobic modifications, and the formed nanometer micelle is relatively small in size and has a good drug loading effect and encapsulation efficiency. Disulfide bonds on the surface of the nanometer micelle can be specifically broken after reaching a tumor site, so that positioned release is achieved; and under thestimulation of ultrasonic waves, the nanometer micelle can promote the ability of the rhein to generate active oxygen, so that the utilization rate of the antitumor drugs is effectively increased. Thetumor targeting nanometer micelle provided by the invention is used as an anti-tumor drug carrier and has a good application prospect.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and specifically relates to a tumor-targeting nanomicelle with chondroitin sulfate as the basic skeleton and surface modified with rhein and lipoic acid, a preparation method of the tumor-targeting nanomicelle, and an anti-cancer drug. Application of tumor drug carrier. Background technique [0002] The information disclosed in this background section is only intended to increase the understanding of the general background of the present invention, and is not necessarily taken as an acknowledgment or any form of suggestion that the information constitutes the prior art already known to those skilled in the art. [0003] In recent years, the incidence and mortality of tumors have shown an obvious upward trend, and it has become a disease that seriously threatens human health, with the characteristics of high mortality and poor prognosis. Clinically, at present, chemotherapy is still one of th...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K47/36A61K47/54A61K47/22A61K41/00A61K31/337A61P35/00
CPCA61K9/1075A61K31/337A61K41/0033A61K47/22A61K47/36A61K47/542A61P35/00A61K2300/00
Inventor 翟光喜张雅楠赵小刚刘梦锐
Owner SHANDONG UNIV
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