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
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, under normoxic conditions, the efficiency will decrease

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • 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

Examples

Experimental program
Comparison scheme
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...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
Login to view more

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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap