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Nanoparticles with high drug loading efficiency as well as preparation and application thereof

A nanoparticle and responsive technology, which is applied in the field of stimuli-responsive self-depolymerization polymers and their nano-assembly systems, can solve the problems of low drug loading rate of lapachone and low encapsulation rate of lapachone, and achieve the goal of promoting apoptosis. Death, enhance the effect of oxidative stress

Active Publication Date: 2022-01-14
UNIV OF SCI & TECH OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The low drug loading rate (2.2 wt%) of lapachone by conventional nanocarriers is due to the crystalline nature of lapachone
Therefore, a major obstacle to the limitation of lapachone nano-formulations is that the encapsulation efficiency of lapachone is too low

Method used

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  • Nanoparticles with high drug loading efficiency as well as preparation and application thereof
  • Nanoparticles with high drug loading efficiency as well as preparation and application thereof
  • Nanoparticles with high drug loading efficiency as well as preparation and application thereof

Examples

Experimental program
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Effect test

preparation example 1

[0026] The linear self-depolymerization polymer BP containing phenylboronic acid pinacol ester group as the trigger unit was prepared as follows pb -HFI:

[0027]

[0028] In the polymer, the phenylboronic acid pinacol ester group is used as a trigger unit, and the side group is a hexafluoroisopropanol group, with a hydrophilic PEG block and a hydrophobic SIP block.

[0029] The preparation method is as follows: polymer precursor M (1 g, 3.34 mmol) and dibutyltin dilaurate (106 mg, 0.17 mmol) were dissolved in anhydrous NMP (1.67 mL) after removing water by azeotropic toluene. The reaction system was stirred and reacted at 60°C for 6 hours in a nitrogen atmosphere. 4-Hydroxymethylphenylboronic acid pinacol ester (0.782g, 3.34mmol), which is a capping group, was dissolved in NMP (1.67mL) after azeotropic removal of water with toluene, added to the reaction system, and continued to react for 6 hours. After the polymerization, the reaction was quenched with liquid nitrogen, ...

preparation example 2

[0033] Nanoparticles were prepared using the nanoflash method. Self-depolymerization polymer BP triggered by ROS pb -HFI details the self-assembly process as an example: 2 mg of polymer was dissolved in 1 mL of DMSO, then quickly added to 9 mL of rapidly stirring deionized water. The organic solvent was removed by dialysis (MWCO: 3 kDa) for 8 hours.

[0034] Lappaquinone (Lap) load: the BP pb 、BP pb -HFB, BP pb -HFI and Lap were dissolved in DMSO respectively at a concentration of 2g / L and 1g / L, and the mixed system was quickly added to 9mL of rapidly stirred deionized water. The organic solvent was removed by dialysis (MWCO: 3 kDa) for 8 hours.

[0035] Doxorubicin (DOX) loading: the BP pb -HFI and DOX (deprotonated with 1.5 equivalents of TEA first) were dissolved in DMSO at a concentration of 2g / L and 1g / L respectively, and the mixed system was quickly added to 9mL of rapidly stirring deionized water. The organic solvent was removed by dialysis (MWCO: 3 kDa) for 8 ho...

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Abstract

The invention relates to nanoparticles with high drug loading efficiency as well as preparation and application thereof. Specifically, the invention relates to a brand new anti-tumor drug targeting delivery system based on self-depolymerization polymer nanoparticles. An amphiphilic block copolymer (BCP) P designed by the invention can be self-assembled into micelle nanoparticles in a water phase, and has a hydrophobic core and a hydrophilic shell structure. Therefore, a hydrophobic drug, such as lapachol, can be physically embedded in the hydrophobic core of the nanoparticle. The nanoparticles provided by the invention can greatly improve a drug loading capacity (DLC) and a drug loading efficiency (DLE) of the lapachol. The nanoparticles are kept stable in normal cells, and the drug cannot be released, so that toxicity is very small; and after being triggered by ROS up-regulated by tumor cells, an anti-oxidation system of the cells is destroyed, an oxidation pressure of the cells is improved, the tumor cells are killed, and cancers are treated. In addition, a tail end of the amphiphilic polymer is modified with a targeting group cRGD, and the nanoparticles can be actively targeted and enriched in tumor tissues.

Description

technical field [0001] The present invention relates to the field of macromolecular materials, more specifically to a stimulus-responsive self-depolymerization polymer and its nano-assembly system, which can physically embed hydrophobic drugs with higher drug-loading capacity and drug-loading efficiency. Depolymerization occurs in response to a stimulus. During this process, the main chain of the polymer is transformed into a small molecule active substance, quinone methylene, which can realize drug release, destroy the antioxidant system of tumor cells, increase the oxidative stress of tumor cells and have anti-tumor effects. Background technique [0002] At present, the strategy of using cancer-specific molecular targets combined with effective carriers for tumor-targeted drug delivery is of great significance for improving the effect of tumor chemotherapy. β-lapachone (Lap) is a novel anticancer drug flavoprotein extracted from plants, and its cytotoxicity is significant...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/34A61K31/352A61P35/00C08G65/333C08G65/337C08G65/334
CPCA61K9/5146A61K31/352A61P35/00C08G65/33351C08G65/337C08G65/3344
Inventor 刘世勇丁泽轩
Owner UNIV OF SCI & TECH OF CHINA
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