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a w 18 o 49 -Tirapazamine composite nanoparticles and their preparation method and application

A technology of composite nanoparticles and tirapazamine, which is applied in the field of W18O49-tirapazamine composite nanoparticles, can solve the problems of reduced efficiency and achieve the effects of high killing rate, exacerbation of anoxic area, and increase of anoxic area

Active Publication Date: 2020-12-08
NANJING DRUM TOWER HOSPITAL +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, under normoxic conditions, the efficiency will decrease

Method used

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  • a w <sub>18</sub> o <sub>49</sub> -Tirapazamine composite nanoparticles and their preparation method and application
  • a w <sub>18</sub> o <sub>49</sub> -Tirapazamine composite nanoparticles and their preparation method and application
  • a w <sub>18</sub> o <sub>49</sub> -Tirapazamine composite nanoparticles and their preparation method and application

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Experimental program
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Effect test

preparation Embodiment 1

[0037] The following steps are adopted to prepare the composite nanoparticles of the present invention:

[0038] (1) 50 mg of PEG-PCL (polyethylene glycol-polycaprolactone) was dissolved in dichloromethane (5-10 mL) to obtain solution a;

[0039] (2) Add 50-100 mL of pure water to solution a to obtain solution b;

[0040] (3) Add W to solution b 18 o 49 (5mg-10mg), and using a magnetic stirrer to stir for 10-20 minutes, the rotating speed of the magnetic rotor is 600 rpm to obtain solution c;

[0041] (4) Add tirapazamine TPZ (2-4mg) to solution c, and stir with a magnetic stirrer for 10-20 minutes, and the rotating speed of the magnetic rotor is 600 rpm to obtain solution d;

[0042] (5) get solution d ultrasonic 30-50 minute;

[0043] (6) centrifugation (14000 rpm), 10-20 minutes;

[0044] (7) Take the precipitate and add 20-50 mL of deionized water to wash, and centrifuge (centrifugation conditions are the same as step (6));

[0045] (8) Repeat (6) and (7) three times...

Embodiment 2

[0047] Get the composite nanoparticle (PL-W that embodiment 1 prepares 18 o 49 -TPZ NPs) for characterization:

[0048] 1. Observation of PL-W by scanning electron microscope 18 o 49 -TPZ NPs nanoparticles

[0049] Such as figure 1 As shown, it can be seen that the composite nanoparticle is a dispersed spherical structure with a particle size of 60-100nm (average 80nm).

[0050] 2. Using an inductively coupled plasma mass spectrometer (ICP-MS, NexION 300D, Perkin-Elmer Corporation, USA) to measure the tungsten concentration.

[0051] PL-W 18 o 49 -Drug loading in TPZ NPs is 2.99% (W 18 o 49 ) and 1.29% (TPZ).

[0052]3. Use Shimadzu UV-3100 spectrophotometer to measure TPZ, PEG-PCL NPs, W 18 o 49 and PL-W 18 o 49 -TPZ was carried out for UV absorption spectrum scanning.

[0053] Such as figure 2 As shown, the UV characterization results show that in PL-W 18 o 49 -TPZ NPs have W in the UV spectrum 18 o 49 and characteristic peaks of TPZ, demonstrating that ...

experiment Embodiment 7

[0089] When the tumor volume reaches 500mm 3 , the tumor model mice induced by HeLa cells were randomly divided into 4 groups, 8 in each group (i.e. saline group Saline, PL-W 18 o 49 Nanoparticle plus laser irradiation group PL-W 18 o 49 +Laser, PL-TPZ nanoparticles plus laser irradiation group PL-TPZ+Laser and PL-W 18 o 49 -TPZ nanoparticles plus laser irradiation group PL -W 18 o 49 -TPZ+Laser).

[0090] 8 hours after intravenous injection, PL-W 18 o 49 +Laser group, PL-TPZ+Laser group and PL-W 18 o 49 -TPZ+Laser group is irradiated with 808nm laser (1W / cm 2 )8min. Body weight and tumor volume were recorded.

[0091] After 12 days, the mice were sacrificed, and the tumors were collected, weighed, stained with hematoxylin-eosin (H&E) and TUNEL for cell apoptosis staining, and observed under a fluorescent microscope (IX71, Olympus).

[0092] Such as Figure 9 , Figure 10 Shown, PL-W 18 o49 -TPZ+Laser group passed PL-W 18 o 49 -TPZ NPs treatment, and after l...

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Abstract

The invention discloses a W 18 o 49 ‑Tirapazamine composite nanoparticles, the composite nanoparticles use PEG‑PCL as a carrier, and its internal load W 18 o 49 and tirapazamine; W 18 o 49 The drug loadings of Tirapazamine and Tirapazamine are 2.99% and 1.29% respectively; the composite nanoparticles are dispersed spherical structures with a particle size of 60-100nm. The invention can improve the therapeutic effect of TPZ.

Description

technical field [0001] The present invention relates to a kind of W with good tumor treatment effect 18 o 49 - Tirapazamine composite nanoparticles. Background technique [0002] Tumor hypoxia has been one of the main reasons for the failure of solid tumor radiochemotherapy (chemoradiotherapy resistance). There are 10%-50% hypoxic cells in solid tumors, and these hypoxic cells are 2.5-3 times more resistant to radiation and chemotherapeutic drugs than aerobic cells, which has become an important factor for tumor refractory, easy recurrence and metastasis one. [0003] Triapazamine (TPZ) is one of the most attention-grabbing hypoxic cytotoxic drugs. The mechanism of action of TPZ is that under hypoxic conditions, highly active TPZ free radicals can be mediated by topoisomerase II. Gain a hydrogen atom from DNA, causing single / double strand breaks, chromosome damage, and cell death. However, under normoxic conditions, the efficiency will decrease. Contents of the invent...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K41/00A61K9/51A61K47/34A61K31/53A61P35/00
CPCA61K9/5153A61K31/53A61K41/0052A61K2300/00
Inventor 何健张超周正扬任双双
Owner NANJING DRUM TOWER HOSPITAL
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