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Sugar-containing photodynamic therapy nano particles with blood stability and target ability and preparing method of sugar-containing photodynamic therapy nano particles

A photodynamic therapy and nanoparticle technology, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, and materials for wave energy or particle radiation treatment. problems such as poor performance and lack of targeting, to achieve the effect of simple operation

Active Publication Date: 2016-03-23
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Small molecule photosensitizers generally have poor water solubility and no targeting, which limits their application

Method used

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  • Sugar-containing photodynamic therapy nano particles with blood stability and target ability and preparing method of sugar-containing photodynamic therapy nano particles
  • Sugar-containing photodynamic therapy nano particles with blood stability and target ability and preparing method of sugar-containing photodynamic therapy nano particles
  • Sugar-containing photodynamic therapy nano particles with blood stability and target ability and preparing method of sugar-containing photodynamic therapy nano particles

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1: Preparation of sugar-containing photodynamic therapy nanoparticles with blood stability and targeting

[0040] The steps are as follows:

[0041] 1) Synthesis of DMA and DMAEMA copolymer: Weigh 0.3g (0.0013) mol of DMA and 1.0g (0.0064mol) DMAEMA into the ampoule, add 1.6μl (0.013mmol) EBIB, 10.8mg (0.039mmol) chain transfer Dissolve α-dithionaphthoic acid isobutyronitrile and 2.5mg (0.013mmol) Cu powder in 2mlDMSO, pass through Ar for 15min to remove the air, add 8.3μl (0.039mmol) PMEDTA, seal the tube, at 20℃ without oxygen Under the conditions of reaction for 7h, after the reaction was finished, it was diluted with 5mlTHF and passed through Al 2 o 3 The chromatographic column removes unreacted Cu powder and Cu 2+ , coagulated in ether to obtain a dark green solid, which was filtered by suction and dried to obtain a copolymer. The molecular weight of the polymer obtained above is 12300, and the molecular weight distribution is about 1.32.

[0042]2) Pr...

Embodiment 2

[0049] Example 2: Preparation of sugar-containing photodynamic therapy nanoparticles with blood stability and targeting

[0050] The steps are as follows:

[0051] 1) Synthesis of DMA and DMAEMA copolymer: Weigh 0.5g (0.0022mol) of DMA and 0.86g (0.0055mol) DMAEMA into the ampoule, add 1.6μl (0.013mmol) EBIB, 10.8mg (0.039mmol) chain transfer Dissolve α-dithionaphthoic acid isobutyronitrile and 2.5mg (0.013mmol) Cu powder in 2mlDMSO, pass through Ar for 15min to remove the air, add 24.9μl (0.117mmol) PMEDTA, seal the tube, at 20℃ without oxygen Under the condition of reaction for 6h, after the reaction was finished, it was diluted with 5mlTHF and passed through Al 2 o 3 The chromatographic column removes unreacted Cu powder and Cu 2+ , coagulated in ether to obtain a dark green solid, which was filtered by suction and dried to obtain a copolymer.

[0052] 2) Preparation of copolymer-coated photosensitizer nanoparticles: take 10 mg (0.000813 mmol) of the copolymer prepared ...

Embodiment 3

[0055] Example 3: Preparation of sugar-containing photodynamic therapy nanoparticles with blood stability and targeting

[0056] The steps are as follows:

[0057] 1) Synthesis of DMA and DMAEMA copolymer: Weigh 0.88g (0.0038mol) of DMA and 0.60g (0.0038mol) DMAEMA into the ampoule, add 1.6μl (0.013mmol) EBIB, 10.8mg (0.039mmol) chain transfer Dissolve α-dithionaphthoic acid isobutyronitrile and 2.5mg (0.013mmol) Cu powder in 2mlDMSO, pass through Ar for 15min to remove the air, add 8.3μl (0.039mmol) PMEDTA, seal the tube, at 20℃ without oxygen Under the condition of reaction for 6h, after the reaction was finished, it was diluted with 5mlTHF and passed through Al 2 o 3 The chromatographic column removes unreacted Cu powder and Cu 2+ , coagulated in ether to obtain a dark green solid, which was filtered by suction and dried to obtain a copolymer.

[0058] 2) Preparation of copolymer-coated photosensitizer nanoparticles: Take 10 mg (0.000813 mmol) of the copolymer prepared ...

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Abstract

The invention discloses sugar-containing photodynamic therapy nano particles with blood stability and target ability and a preparing method of the sugar-containing photodynamic therapy nano particles. The nano particles are formed by wrapping photosensitizer micromolecules with a synthesized copolymer of DMA and DMAEMA, and wrapping the outer layers of nano particles with glycopolymer layers, wherein the average particle size of the nano particles ranges from 180 nm to 300 nm. The preparing method of the sugar-containing photodynamic therapy nano particles comprises the steps that the copolymer of DMA and DMAEMA is subjected to self-assemblage in water to wrap the photosensitizer micromolecules to form the nano particles, the nano particles are mixed with a glycopolymer solution with an end group serving as carboxyl, and the glycopolymer is aggregated on the surfaces of the nano particles through electrostatic interaction to form the sugar-containing photodynamic therapy nano particles. According to the method, operation is easy and convenient, and various photodynamic reagents can be wrapped. The adopted polymer shows electropositivity and can be combined with various glucide polymers with negative electricity, meanwhile, the glycopolymer is aggregated on the surfaces of the nano particles, and thus blood stability, target ability and biocompatibility are achieved.

Description

technical field [0001] The invention relates to a polymer-coated photosensitizer nanoparticle, in particular to a sugar-containing photodynamic therapy nanoparticle with blood stability and targeting and a preparation method thereof. Background technique [0002] Photosensitizer (photosensitizer, PS) is a kind of substance that absorbs, transmits and converts light energy. If this kind of substance is enriched on the surface or inside of the cell to be acted on, it can generate photodynamic force when excited by a specific wavelength light source. effect thereby killing the cell. Based on the understanding of photosensitizers, people invented a new treatment method for tumors, that is, photodynamic therapy (PDI). The basic principle of this treatment technology is that the photosensitizer absorbs photon energy, transitions from the ground state to the excited state, and its physical de-excitation process generates fluorescence, which can be used for disease diagnosis throug...

Claims

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Application Information

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IPC IPC(8): A61K41/00A61K9/14A61K47/30A61K47/32A61P35/00
Inventor 陈高健张卫东陈奎
Owner SUZHOU UNIV
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