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Carrier-free nano delivery system loaded with banoxantrone and preparation method of carrier-free nano delivery system

A delivery system and carrier-free technology, applied in nanotechnology, nanotechnology, nanomedicine, etc., can solve the problems of low drug loading, complex synthesis process, and low bioavailability

Pending Publication Date: 2021-09-10
CHONGQING MEDICAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the most important type of treatment targeting tumor hypoxia is hypoxia-activated prodrugs, such as Banox antrone (AQ4N), Tirapazamine (TPZ), etc. Selective and highly toxic to hypoxic cells, while exhibiting low toxicity to oxygen-rich areas such as normal tissues and cells, but low bioavailability after simple administration
Nano-delivery systems can effectively improve its bioavailability, but the reported nano-delivery systems have the defects of low drug loading and complex synthesis process
[0003] Triblock copolymer nanosystems containing polyethylene glycol (PEG) and polycaprolactone (PLC) studied by Jiong Li et al. can load banoxantrone (AQ4N) and glucose oxidase (GOD) [“Adv Healthc Mater", (10):e1801627, (2019)], but the synthesis process is complicated, and the drug loading of AQ4N is only 8.17%

Method used

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  • Carrier-free nano delivery system loaded with banoxantrone and preparation method of carrier-free nano delivery system
  • Carrier-free nano delivery system loaded with banoxantrone and preparation method of carrier-free nano delivery system
  • Carrier-free nano delivery system loaded with banoxantrone and preparation method of carrier-free nano delivery system

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preparation example Construction

[0032] The invention provides a carrier-free nano-delivery system loaded with banoxantrone, the preparation method of which comprises the following steps:

[0033] (1) Add banoxantrone·dihydrochloride (AQ4N·HCl) into water, stir to dissolve fully;

[0034] (2) Add manganese dichloride solution in the solution of step (1), stir and react, then add triethylamine, stir and react, to remove HCl;

[0035] (3) slowly drop the reaction solution obtained in step (2) into water, stir for reaction, and finally dialyze to remove uncoordinated banoxantrone to obtain the nano-delivery system loaded with banoxantrone.

[0036] Further, in the steps (1) and (2), the mass ratio of banoxantrone dihydrochloride to manganese dichloride is 20-50:1, preferably 20-30:1, more preferably 20 :1.

[0037] Further, in the step (1), the concentration of banoxantrone is 2 mg / mL.

[0038] Further, in the step (1), the stirring time is 1-2h, preferably 1h.

[0039] Further, in the step (2), the concentr...

Embodiment 1

[0050] The preparation method of the carrier-free nano-delivery system loaded with banoxantrone in this example comprises the following steps:

[0051] (1) Take 2 mg of banoxantrone · dihydrochloride (AQ4N · HCl) in a brown glass bottle, add 1 mL of deionized water to dissolve, and stir magnetically.

[0052] (2) After stirring for 1 hour, 100 μl of 1 mg / mL manganese dichloride solution was added dropwise. After stirring for 4 hours, 450 μL of triethylamine was added dropwise, and the stirring was continued overnight to remove HCl.

[0053] (3) Then, into a round bottom flask filled with 10 mL of deionized water, 2 mL of the reaction solution obtained in step (2) was slowly added dropwise, and magnetically stirred for 2 h.

[0054] (4) Finally, dialyze the reaction solution obtained in step (3) with a dialysis bag to remove uncoordinated banoxantrone to obtain a nano-delivery system loaded with banoxantrone.

[0055] During the above process, the reaction needs to be protecte...

Embodiment 2

[0057] The preparation method of the carrier-free nano-delivery system loaded with banoxantrone in this example comprises the following steps:

[0058] (1) Take 2 mg of banoxantrone · dihydrochloride (AQ4N · HCl) in a brown glass bottle, add 1 mL of deionized water to dissolve, and stir magnetically.

[0059] (2) After stirring for 2 hours, add 100 μL of 1 mg / mL manganese dichloride solution dropwise, and after stirring for 3 hours, add 450 μL triethylamine dropwise, and continue stirring overnight to remove HCl.

[0060] (3) Then, into a round bottom flask filled with 10 mL of deionized water, 2 mL of the reaction solution obtained in step (2) was slowly added dropwise, and magnetically stirred for 2 h.

[0061] (4) Finally, dialyze the reaction solution obtained in step (3) with a dialysis bag to remove uncoordinated banoxantrone to obtain a nano-delivery system loaded with banoxantrone.

[0062] During the above process, the reaction needs to be protected from light throug...

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Abstract

The invention discloses a carrier-free nano delivery system loaded with banoxantrone and a preparation method of the carrier-free nano delivery system. The preparation method comprises the following steps: (1) adding banoxantrone dihydrochloride into water, and uniformly stirring; (2) adding a manganous chloride solution into the solution in the step (1), stirring for reaction, then adding triethylamine, and stirring for reaction to remove HCl; and (3) slowly dropwise adding the reaction solution obtained in the step (2) into water, stirring for reaction, and finally dialyzing to remove uncoordinated banoxantrone, thereby obtaining the banoxantronee-loaded nano delivery system. A metal organic framework (MOFs) is directly formed by banoxantrone and metal manganese ions through a metal coordination method, a banoxantrone-loaded carrier-free nano delivery system (AMMOFs) is prepared, the AMMOFs can effectively release drugs in a tumor cell endosome subacid environment, radiography imaging and treatment effects are achieved, the drug loading capacity is high, and the synthesis process is simple.

Description

technical field [0001] The invention relates to the technical field of tumor treatment and nano-drug delivery, in particular to a carrier-free nano-delivery system loaded with banoxantrone and a preparation method thereof. Background technique [0002] Malignant tumor is the number one killer threatening human life and health. Hypoxia is a prominent feature of most solid tumors and an important reason for tumor development, metastasis, and treatment failure. Treating tumor hypoxia has become a new direction for research on tumor diagnosis and treatment. At present, the most important type of treatment targeting tumor hypoxia is hypoxia-activated prodrugs, such as Banox antrone (AQ4N), Tirapazamine (TPZ), etc. It has selectivity and high toxicity to hypoxic cells, but shows low toxicity to oxygen-rich areas such as normal tissues and cells, but the bioavailability of simple administration is low. Nano-delivery systems can effectively improve their bioavailability, but the ...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/14A61K47/52A61K49/22A61P35/00B82Y5/00B82Y20/00B82Y40/00C08G83/00
CPCA61K31/14A61K47/52A61K49/221B82Y5/00B82Y20/00B82Y40/00A61P35/00C08G83/008A61K9/143
Inventor 李桦楠孙廷宇曾超李婧男黄楠涂道月
Owner CHONGQING MEDICAL UNIVERSITY
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