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Preparation method and application of drug-loaded polypyrrole nanoparticles

A pyrrole nanometer and nanoparticle technology, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problem of cancer cell chemistry- Photothermal combined therapy and other problems, to achieve the effect of enhancing the therapeutic effect of cancer cells, good photothermal effect, and good cytocompatibility

Inactive Publication Date: 2018-11-06
SOUTHWEST UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Search domestic and foreign literatures and patents about the application of polypyrrole nanoparticles in cancer treatment and find that: before the completion of the present invention, no polypyrrole / doxorubicin composite nanoparticles based on PEGylated polyethyleneimine stabilization have been found. Preparation and research report on combined chemical-photothermal therapy of cancer cells

Method used

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  • Preparation method and application of drug-loaded polypyrrole nanoparticles
  • Preparation method and application of drug-loaded polypyrrole nanoparticles
  • Preparation method and application of drug-loaded polypyrrole nanoparticles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Dissolve 200 mg of polyethyleneimine (PEI) in 5 ml of water, and stir it thoroughly with magnetic force. Add 25 μl of pyrrole monomer, and continue to stir and mix for 30 min. Add 1.12 mL of HCl (5 M) and 3.88 mL of distilled water, stir for 5 min and mix well. Add FeCl 3 · 6H 2O (250 mg / ml) 100 µl was stirred for 5 min, and the obtained solution was dialyzed (6 times, 1 L / time) for 24 h, and the water was changed at 0.5 h, 1.5 h, and 5.5 h during the dialysis. The obtained PPy-PEI nanoparticles were stored at 4°C for future use.

[0037] 1 The H NMR spectrum indicates the chemical environment and type of hydrogen atoms in each component. Refer to the attached figure 1 . 1 The H NMR spectrum shows that compared with pure PEI (attached figure 1 a), after wrapping polypyrrole nanoparticles (attached figure 1 b), The peak shape of PEI has changed somewhat, and there is some shift to the left.

Embodiment 2

[0039] Take 259.9 mg of polyethylene glycol (PEG) and dissolve it in 3 ml of distilled water. Under magnetic stirring, add 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDC) 1.682 mL (74.750 mg / mL) and N-hydroxysuccinimide (NHS) 1.730 mL (44.100 mg / mL), stirred at room temperature for 4 h.

[0040] Take 6.232 mL (40.469 mg / mL) of activated PEG prepared above and add it to the PPy-PEI nanoparticle aqueous solution (120 mL, 0.667 mg / mL) prepared in Example 1, and react with magnetic stirring for 48 h. After the reaction, the resulting solution was dialyzed against distilled water (6 times, 1 L / time) to obtain polyethylene glycol-modified polyethyleneimine-stabilized polypyrrole (PPy-PEI-PEG) nanoparticles, which were stored at 4 °C.

[0041] 1 H NMR spectrum (attached figure 1 The peak at around 3.6 ppm in c) is the proton peak of polyethylene glycol, indicating that it was successfully modified at the end of polyethyleneimine. UV-Vis spectrum (attached figu...

Embodiment 3

[0043] Take 5 mL (2 mg / mL) of PPy-PEI-PEG nanoparticles prepared in Example 2, and add 0.125 mL (8 mg / mL) of DOX aqueous solution according to the mass ratio of DOX / PPy-PEI-PEG nanoparticles as 1 / 10 ). After stirring for 5 min at room temperature in the dark, 1.21 µL of triethylamine was added. After stirring for 24 h, the product was centrifuged (4000 rpm, 4 min) to remove unloaded DOX. The collected supernatant is polyethylene glycol-modified polyethyleneimine-stabilized polypyrrole / doxorubicin (PPy-PEI-PEG / DOX) nanoparticles.

[0044] 1 H NMR spectrum (attached figure 1 The peak appearing between 2.0-1.0 ppm in d) is the characteristic peak of doxorubicin. UV-Vis spectrum (attached figure 2 b) shows that after loading doxorubicin, there is an obvious absorption peak around 490 nm. These data can demonstrate the successful loading of doxorubicin. The test results of laser particle size analyzer (DLS) showed the hydrodynamic size and uniformity of the obtained composi...

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Abstract

The invention relates to a preparation method and application of drug loaded polypyrrole nanoparticles. The preparation method comprises the following steps: preparing polypyrrole nanoparticles by taking polyethyleneimine as a stabilizer; carrying out polyethylene glycol modification through amino groups on the surface of polyethyleneimine; loading an anti-cancer drug-adriamycin by utilizing a cavity formed in polyethyleneimine; carrying out in-vitro cancer cell treatment performance evaluation on an obtained final product. The preparation method disclosed by the invention is simple and easy,prepared pegylated polyethyleneimine stabilized polypyrrole / adriamycin composite nanoparticles are good in photothermal effect, stability and biocompatibility, a good combined treatment effect is displayed aiming at cancer cells, and a potential cancer cell treatment application prospect is obtained.

Description

technical field [0001] The invention belongs to the field of preparation of therapeutic agents for cancer cells, and in particular relates to a preparation method of drug-loaded polypyrrole nanoparticles and its application in combined chemical-photothermal treatment of cancer cells in vitro. Background technique [0002] In recent years, the incidence of malignant tumors has gradually increased and has become an important killer affecting human health. At present, there are outstanding problems in the traditional cancer diagnosis and treatment methods used in clinical practice, and they are facing increasingly severe challenges. There is an urgent clinical need and great practical significance to develop a method with less toxic side effects and good cancer treatment effect. The development of nanotechnology provides a new great opportunity for the effective treatment of malignant tumors. Compared with traditional clinical methods, nanoparticle-based therapeutic methods s...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K47/60A61K41/00A61K31/704A61P35/00
CPCA61K31/704A61K41/0052A61K47/60A61K47/6933A61P35/00A61K2300/00
Inventor 刘辉谢围城蓝术航王静静
Owner SOUTHWEST UNIVERSITY
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