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Sensitively responsive polymer nano-particles, and preparation method and application thereof

A nanoparticle and polymer technology, applied in the fields of polymer chemistry and biomedical engineering, can solve the problems of poor biocompatibility and biodegradability of polymer particles, limiting the application of polymer nanocarriers, and easy leakage of ICG molecules. Achieve the effects of prolonging blood circulation time, simple and easy preparation method, good biocompatibility and biodegradability

Active Publication Date: 2014-12-24
SHENZHEN INST OF ADVANCED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the polymer particles in the prior art have: poor stability, easy to be cleared by the immune system, easy leakage of loaded ICG molecules, less accumulation at the target site, difficulty for ICG to enter tumor cells, and biocompatibility of the polymer particles. A series of disadvantages such as poor biodegradability limit the application of polymeric nanocarriers

Method used

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  • Sensitively responsive polymer nano-particles, and preparation method and application thereof
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  • Sensitively responsive polymer nano-particles, and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0078] A preparation method of a sensitive responsive polymer nanoparticle loaded with indocyanine green, comprising the following steps:

[0079] (1) The preparation of PEG-b-PLL (DMMA) polymer comprises the following steps:

[0080] (a) Vacuumize the polymerization tube and fill it with nitrogen to protect, and put 1g of CH with a molecular weight of 500Da 3 -PEG-NH 2 Dissolve in 20mL DMF and add to the polymerization tube to get CH 3 -PEG-NH 2 solution, under nitrogen protection, the CH 3 -PEG-NH 2 After the solution is heated to 30°C, add Lys(Z)-NCA monomer Obtain reaction solution, Lys(Z)-NCA monomer and CH 3 -PEG-NH 2 The molar ratio is 20:1, and the constant temperature reaction is carried out under the protection of nitrogen for 24 hours. After the reaction, ether with a volume 10 times the volume of DMF is added to precipitate, filter, and dry to obtain PEG-b-PLL (Z) block polymer One end of the polylysine segment is connected to the amino terminal of the ...

Embodiment 2

[0100] A preparation method of a sensitive responsive polymer nanoparticle loaded with indocyanine green, comprising the following steps:

[0101] (1) The preparation of PEG-b-PLL (DMMA) polymer comprises the following steps:

[0102] (a) Vacuumize the polymerization tube and fill it with nitrogen to protect, and 2 g of CH with a molecular weight of 1000 Da 3 -PEG-NH 2 Dissolve in 20mL DMF and add to the polymerization tube to get CH 3 -PEG-NH 2 solution, under nitrogen protection, CH 3 -PEG-NH 2 After the solution was heated to 50°C, Lys(Z)-NCA monomer was added to obtain a reaction solution, Lys(Z)-NCA monomer and PEG-NH 2 The molar ratio is 50:1, and the constant temperature reaction is carried out under the protection of nitrogen for 100 hours. After the reaction is completed, add ether with a volume 20 times the volume of DMF to precipitate, filter, and dry to obtain PEG-b-PLL (Z) block polymer; polylysine One end of the acid segment is connected to the amino termin...

Embodiment 3

[0115] A preparation method of a sensitive responsive polymer nanoparticle loaded with indocyanine green, comprising the following steps:

[0116] (1) The preparation of PEG-b-PLL (DMMA) polymer comprises the following steps:

[0117] (a) Vacuumize the polymerization tube and fill it with nitrogen protection, and add 0.1g of CH with a molecular weight of 10000Da 3 -PEG-NH 2 Dissolve in 100mL DMF and add to the polymerization tube to get CH 3 -PEG-NH 2 solution, the CH 3 -PEG-NH 2 After heating the solution to 40°C, add Lys(Z)-NCA monomer, Lys(Z)-NCA monomer and PEG-NH 2 The molar ratio is 200:1, under the protection of nitrogen, it is reacted at a constant temperature for 120 hours. After the reaction, add ether with a volume 10 times the volume of DMF to precipitate, filter, and dry to obtain PEG-b-PLL (Z) block polymer; polylysine One end of the acid segment is connected to the amino terminal of the polyethylene glycol segment through an amide bond;

[0118] (b) Disso...

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Abstract

The embodiment of the invention provides sensitively responsive polymer nano-particles which comprise poly(cystamine bisacrylamide-alt-spermine) and polyethylene glycol-b-polylysine(2,3-dimethyl maleate); in poly(cystamine bisacrylamide-alt-spermine), a cystamine bisacrylamide monomer and a spermine monomer are connected through a carbon-nitrogen bond; in polyethylene glycol-b-polylysine(2,3-dimethyl maleate), a polyethylene glycol chain segment is methyl-polyethylene glycol-amino; one end of a polylysine chain segment is connected with the amino end of the polyethylene glycol chain segment through an amide bond; and 2,3-dimethyl maleate is connected with amino on the side chain of the polylysine chain segment through an amide bond. The sensitively responsive polymer nano-particles are good in stability and can be effectively enriched at a tumor site; loaded medicinal molecules can enter tumor cells easily; in addition, the sensitively responsive polymer nano-particles are good in biocompatibility and easy to degrade.

Description

technical field [0001] The invention relates to the fields of polymer chemistry and biomedical engineering, in particular to a sensitive and responsive polymer nanoparticle and its preparation method and application. Background technique [0002] Cancer is a kind of disease that seriously threatens human health and has a high mortality rate. In the treatment of cancer, prevention and early diagnosis are an important means to improve the cure rate of cancer. Early diagnosis of cancer requires the use of various non-invasive imaging methods, including magnetic resonance imaging, ultrasound imaging, fluorescence imaging or X-ray imaging. [0003] As the only dye available in humans approved by the US Federal Drug Administration, indocyanine green (ICG) is a solid choice for diagnostic imaging of tumors. However, ICG has disadvantages such as poor photostability, low sensitivity and easy degradation in vivo. In order to overcome these shortcomings, the existing technology uses...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K47/34A61K49/00
Inventor 蔡林涛谢高峰易虎强王碧刘朋潘正银丁泽轩姬满祎
Owner SHENZHEN INST OF ADVANCED TECH
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