Small molecule-polymer conjugate self-assembled drug-loaded nanoparticles and preparation method thereof

A drug-loaded nano and polymer technology, applied in the cross field of chemistry and biomedicine, achieves high efficiency, improved therapeutic effect, and good biocompatibility

Active Publication Date: 2020-06-12
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] At present, there are no relevant patent reports on small molecule-polymer conjugate self-assembled nanoparticles loaded with anticancer drugs and nitric oxide prodrugs and capable of simultaneously releasing anticancer drugs and nitric oxide in tumor cells

Method used

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  • Small molecule-polymer conjugate self-assembled drug-loaded nanoparticles and preparation method thereof
  • Small molecule-polymer conjugate self-assembled drug-loaded nanoparticles and preparation method thereof
  • Small molecule-polymer conjugate self-assembled drug-loaded nanoparticles and preparation method thereof

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Embodiment 1

[0042] This embodiment relates to a small molecule-polymer conjugate self-assembled drug-loaded nanoparticle and its preparation method, including the following steps:

[0043] Such as figure 1Shown is a schematic diagram of the preparation process of the self-assembled drug-loaded nanoparticles of the small molecule-polymer conjugate of the present invention. Dissolve 2 mmol of polylactic acid in 40 mL of dichloromethane at room temperature, and add 2.8 mmol of N,N'-diisopropylcarbodiimide and 2 mmol of triethylamine to obtain a mixed solution with a polylactic acid concentration of 50 μmol / mL. Then stir in an ice bath for 40 minutes; dissolve 2 mmol of fluoxuridine and 1.5 mmol of 4-dimethylaminopyridine in 40 mL of dichloromethane, stir and mix at room temperature to obtain a solution with a concentration of fluoxuridine of 50 μmol / mL; Dissolve 0.4mmol of acrylated azocenediol in 5mL of dichloromethane, stir and mix at room temperature to obtain a solution with a concentra...

Embodiment 2

[0045] This embodiment relates to a small molecule-polymer conjugate self-assembled drug-loaded nanoparticle and its preparation method, including the following steps:

[0046] Dissolve 1.5 mmol of polycaprolactone in 50 mL of chloroform at room temperature, and add 2 mmol of N,N'-dicyclohexylcarbodiimide and 1.5 mmol of triethylamine to obtain a mixture with a polylactic acid concentration of 30 μmol / mL solution, and then stirred in an ice bath for 30 minutes; 1.5mmol irinotecan and 1mmol 4-dimethylaminopyridine were dissolved in 50mL of dichloromethane, stirred and mixed at room temperature to obtain a solution with an irinotecan concentration of 30 μmol / mL; Dissolve 0.3mmol of acrylated azenene glycol in 5mL of dichloromethane, stir and mix at room temperature to obtain a solution with a concentration of 60μmol / mL; mix the above three solutions together, and store at room temperature and under dark conditions Stirring and reacting for 36 hours, the reaction product was filt...

Embodiment 3

[0048] This embodiment relates to a small molecule-polymer conjugate self-assembled drug-loaded nanoparticle and its preparation method, including the following steps:

[0049] Dissolve 1 mmol (lactic acid-caprolactone) copolymer in 25 mL of chloroform at room temperature, and add 1 mmol 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and 0.75 mmol triethyl amine, to obtain a mixed solution with a (lactic acid-caprolactone) copolymer concentration of 40 μmol / mL, and then stir in an ice bath for 60 minutes; dissolve 1 mmol gemcitabine and 0.7 mmol 4-dimethylaminopyridine in 25 mL chloroform, and Stir and mix evenly to obtain a solution with a gemcitabine concentration of 40 μmol / mL; mix 0.3 mmol O 2 - Dissolve vinylazocenediol in 6 mL of chloroform, stir and mix at room temperature to obtain a solution with a concentration of 50 μmol / mL; mix the above three solutions together, and stir and react at room temperature and protected from light After 54 hours, the reaction product wa...

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Abstract

The invention discloses micromolecule-macromolecule conjugate self-assembly drug-loaded nanoparticles and a preparation method thereof. The preparation method comprises the steps that micromolecular anti-cancer drugs and macromolecular chains are connected together through specific groups through a simple and efficient method to form self-assembly nanomicelles, nitric oxide prodrugs are wrapped into macromolecular chain segments through hydrophobic interaction, and then the drug-loaded nanoparticles with the acidic sensitivity are obtained; the drug-loaded nanoparticles can be stably delivered into the tumor tissue, be decomposed under stimulation of an acidic environment in tumor cells to release the anti-cancer drugs and nitric oxide and achieve synergistic therapy on tumors. Compared with the prior art, the micromolecule-macromolecule conjugate self-assembly drug-loaded nanoparticles can release the anti-cancer drugs and nitric oxide simultaneously in the internal environment of the tumor cells, the multi-drug resistance of the tumor cells is effectively reduced, the tumor treatment effect is obviously promoted, and therefore the micromolecule-macromolecule conjugate self-assembly drug-loaded nanoparticles have a wide application prospect on tumor treatment.

Description

technical field [0001] The invention belongs to the interdisciplinary field of chemistry and biomedicine, and in particular relates to a self-assembled drug-loaded nanoparticle of a small molecule-macromolecule conjugate and a preparation method thereof. Background technique [0002] Nitric oxide (NO) is a chemically very active free radical gas, which acts as a messenger molecule and a regulator in the physiological and pathological processes of the body. NO can participate in and regulate cell apoptosis, cell cycle, angiogenesis, metastasis and invasion related to the occurrence and development of tumors. Existing studies have shown that the combined action of NO and anticancer drugs on tumor cells can significantly improve the killing effect of anticancer drugs on tumor cells, because a certain concentration of NO can inhibit the production of tumor cell P-glycoprotein (P-gp). Overexpression reduces multidrug resistance (MDR) and increases drug concentration in tumor cel...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/59A61K9/107A61K31/655A61P35/00A61K31/7068A61K31/7072A61K31/4745
CPCA61K31/4745A61K31/655A61K31/7068A61K31/7072A61K33/00A61K2300/00
Inventor 谭连江沈玉梅
Owner SHANGHAI JIAO TONG UNIV
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