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A kind of bowl-shaped ISP composite functional nanoparticles and its preparation method and application

A composite nanoparticle and nanoparticle technology, applied in the field of nanosystems, can solve the problems of limiting the development of photodynamic therapy, toxic and side effects of healthy tissues, limiting the activity of photosensitizers, etc., and achieve good catalytic ability, efficient treatment, and improve the activity of photosensitizers Effect

Active Publication Date: 2022-06-28
NANJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In photodynamic therapy, due to the easy removal of drugs in the blood circulation and the poor targeting of drugs, the toxic and side effects on healthy tissues caused greatly limit the development of photodynamic therapy.
In addition, phthalocyanine photosensitizers will consume oxygen through light, and the insufficient supply of oxygen limits the activity of photosensitizers and reduces their anti-tumor effect in cells

Method used

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  • A kind of bowl-shaped ISP composite functional nanoparticles and its preparation method and application
  • A kind of bowl-shaped ISP composite functional nanoparticles and its preparation method and application
  • A kind of bowl-shaped ISP composite functional nanoparticles and its preparation method and application

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Experimental program
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Effect test

Embodiment 1

[0044] Preparation of bowl-shaped PEG-b-PS: PEG-b-PS block polymer according to figure 2 Synthesis as shown, specifically, poly(ethylene glycol) monomethyl ether (6.00 g, 2.00 mmol) with a molecular weight of 3000 was dissolved in 20 mL of tetrahydrofuran uniformly, then triethylamine (1.04 mL, 7.5 mmol) was added, and the mixture was cooled at 0°C on ice 2-Bromoisobutyryl bromide (620 μL, 5.00 mmol) was added dropwise under a water bath and nitrogen protection for 24 hours. After the reaction, suction filtration to obtain a white precipitate, and vacuum drying to obtain PEG-Br. PEG-Br was dissolved in 1.5ml anisole, and CuCl (45mg, 0.45mmol) and PMDETA (α-bromoisobutyrate, N,N,N',N",N"-Pentamethyldiethylenetriamine, 66μL were added under anhydrous and anoxic conditions. 0.32 mmol), anhydrous and oxygen-free reaction at 90 °C for 12 hours, in an argon atmosphere during the feeding period, and the low temperature state of the raw materials is maintained by placing the reactio...

Embodiment 2

[0046] superparamagnetic Fe 3 O 4 Nanoparticle preparation: 1.42g Fe(acac) 3 After dissolving evenly in 50 mL of triethylene glycol, N 2 Under the protection, gradient heating was carried out from room temperature to 200 °C, then to 250 °C, and finally to 280 °C. Each stage was kept stable for 10 min, and the reaction was carried out at 280 °C for 0.5 h to obtain superparamagnetic Fe. 3 O 4 Nanoparticle triethylene glycol solution. prepared Fe 3 O 4 Electron microscope image of nanoparticles Figure 4 shown.

Embodiment 3

[0048] ZnPc synthesis: Synthesis of side-chain tetra-substituted benzoic acid sodium salt phthalocyanine derivatives Figure 5 Follow the steps shown. p-Hydroxybenzoic acid (500 mg, 3.62 mmol) and 4-nitrophthalonitrile (658 mg, 3.8 mmol) were dissolved in N,N-dimethylformamide (8 mL), potassium carbonate (561.2 mg, 4.06 mmol) In mixed solvent, N 2 Under the protection conditions, the reaction generated compound 1; compound 1 (500 mg, 1.89 mmol) and zinc acetate (217 mg, 1.18 mmol) were catalyzed by DBU (0.38 mL, 2.82 mmol), and reacted in n-amyl alcohol (8 mL) solution at 140 ° C for 12 h , to generate compound 2; compound 2 (200 mg, 0.18 mmol) was reacted with sodium hydroxide (16 mg, 0.4 mmol) in ethanol (10 mL) for 24 h to finally generate a side-chain tetra-substituted benzoic acid sodium salt phthalocyanine derivative (ZnPc).

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Abstract

The invention discloses a bowl-shaped ISP composite functional nanoparticle and its preparation method and application, which are loaded with Fe after self-assembly of a block polymer 3 o 4 Particles and photosensitizer ZnPc are formed; the block polymer is bowl-shaped polyethylene glycol block polystyrene (PEG-b-PS). The bowl-shaped ISP functional composite nanoparticles prepared by the present invention have a magnetic targeting function, which can increase the enrichment of ZnPc in tumor tissue sites, and the new bowl-shaped ISP composite functional nanoparticles of the present invention can be magnetically targeted to tumor tissue sites , to enhance the activity of photosensitizers by catalyzing oxygen production to achieve efficient treatment of PDT. The preparation method of the invention is simple and convenient, has wide sources of raw materials and high bioavailability, and the prepared nano particles are used as photosensitizers and carriers in the preparation of photodynamic medicines.

Description

technical field [0001] The invention belongs to the technical field of nanometer systems that can improve photodynamic activity, and in particular relates to a bowl-shaped ISP composite functional nanoparticle and a preparation method and application thereof, in particular to a functional composite nanoparticle with magnetic targeting and its application. Application of photosensitive therapy in tumor. Background technique [0002] Photodynamic therapy (PDT) is a new type of tumor treatment. The photosensitizer is injected into the human body through intravenous injection, and then the photosensitizer located at the tumor site is excited by light of a specific wavelength, reacts with the surrounding oxygen to generate reactive oxygen species, and oxidizes and damages the biological macromolecules in the tumor cells, killing the tumor cells to achieve the goal of tumor treatment. Effect. PDT has received extensive attention due to its low toxicity, drug resistance, and reus...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K41/00A61K9/51A61K47/32A61K47/02A61P35/00
CPCA61K41/0071A61K9/5146A61K9/5115A61K9/0019A61P35/00
Inventor 魏少华张鹏周林
Owner NANJING NORMAL UNIVERSITY