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Preparation method of polymaleic anhydride-phosphatidyl ethanolamine graft polymer nano-photosensitive carrier

A technology of phosphatidylethanolamine and polymaleic anhydride, which is applied in the field of medicine, can solve the problems of limiting the further application of photodynamic therapy, strong hydrophobicity of photosensitizer, and low utilization rate of drugs, and achieve high drug loading efficiency, short preparation cycle, The effect of simple and fast preparation process

Inactive Publication Date: 2015-05-20
TIANJIN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although photodynamic therapy technology has obtained a large number of clinical applications, it still has many defects and deficiencies that are difficult to overcome. Phototoxicity of normal tissues such as skin
These defects undoubtedly limit the further application of photodynamic therapy in tumor therapy.

Method used

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  • Preparation method of polymaleic anhydride-phosphatidyl ethanolamine graft polymer nano-photosensitive carrier
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  • Preparation method of polymaleic anhydride-phosphatidyl ethanolamine graft polymer nano-photosensitive carrier

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Experimental program
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Effect test

Embodiment 1

[0034] Synthesis of polymaleic anhydride-phosphatidylethanolamine graft polymer:

[0035] (1) The mass ratio of the raw materials is as follows: 100 mg of poly(1-octadecene / maleic anhydride) and 1000 mg of fatty acylethanolamine are weighed and added to the reactor. Under magnetic stirring conditions, add solvent tetrahydrofuran (THF) into the reactor to completely dissolve the raw materials. Heated to 70°C, condensed and refluxed for 2 days.

[0036] (2) After the reaction is finished, lower the temperature and put the product into a dialysis bag for dialysis for 3 days. The dialyzed solution was filtered and freeze-dried to obtain an amphiphilic polymaleic anhydride-phosphatidylethanolamine graft polymer, and the graft ratio of the prepared polymer was 22.6%.

[0037] figure 2 : according to the synthetic polymaleic anhydride-phosphatidylethanolamine graft polymer infrared spectrogram of embodiment 1.

Embodiment 2

[0039] Synthesis of polymaleic anhydride-phosphatidylethanolamine graft polymer:

[0040] (1) The mass ratio of the raw materials is as follows: 50 mg of poly(1-octadecene / maleic anhydride) and 1000 mg of fatty acylethanolamine are weighed and added to the reactor. Under magnetic stirring conditions, add solvent tetrahydrofuran (THF) into the reactor to completely dissolve the raw materials. Heated to 30°C, condensed and refluxed for 3 days.

[0041] (2) After the reaction is finished, lower the temperature and put the product into a dialysis bag for dialysis for 7 days. The dialyzed solution was filtered and freeze-dried to obtain an amphiphilic polymaleic anhydride-phosphatidylethanolamine graft polymer, and the graft ratio of the prepared polymer was 10%.

Embodiment 3

[0043] Synthesis of polymaleic anhydride-phosphatidylethanolamine graft polymer:

[0044] (1) The mass ratio of the raw materials is as follows: 200 mg of poly(1-octadecene / maleic anhydride) and 6000 mg of fatty acylethanolamine are weighed and added to the reactor. Under magnetic stirring conditions, add solvent tetrahydrofuran (THF) into the reactor to completely dissolve the raw materials. Heated to 46°C, condensed and refluxed for 1 day.

[0045] (2) After the reaction is finished, lower the temperature and put the product into a dialysis bag for dialysis for 5 days. The dialyzed solution was filtered and freeze-dried to obtain an amphiphilic polymaleic anhydride-phosphatidylethanolamine graft polymer, and the graft ratio of the prepared polymer was 30%.

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Abstract

The invention relates to a preparation method of a polymaleic anhydride-phosphatidyl ethanolamine graft polymer nano-photosensitive carrier. The preparation method comprises the following steps: (1) synthesizing a polymaleic anhydride-phosphatidyl ethanolamine graft polymer, namely, firstly performing ring opening by using poly(1-octadecene / maleic anhydride), taking poly(1-octadecene / maleic anhydride) and phosphatidyl ethanolamine as raw materials, and performing ring-opening reaction to prepare a polymaleic anhydride-phosphatidyl ethanolamine amphiphilic polymer; and (2) preparing a polymaleic anhydride-phosphatidyl ethanolamine graft polymer nano-photosensitive preparation according to a thin film dispersion method. The preparation method disclosed by the invention is simple and convenient to operate, strong in applicability and low in cost; the polymaleic anhydride-phosphatidyl ethanolamine graft polymer nano-photosensitive carrier has relatively good solubility in water and a variety of organic solvents, and ensures that the grafting efficiency can reach 10-30%; the effective particle size of the photosensitive preparation is between 50nm and 150nm, and more uniform particle sizes can be achieved; the photosensitive preparation is good in stability and can be stored in an aqueous solution for at least more than 2 months; and the medicine loading ratio of the photosensitive preparation can keep 10-20%, and the photosensitive preparation is high in yield and is suitable for large batch production.

Description

technical field [0001] The invention relates to a preparation method of a polymaleic anhydride-phosphatidylethanolamine grafted polymer nanometer photosensitive carrier, belonging to the technical field of medicine. Background technique [0002] Malignant tumors have the characteristics of fast growth, strong metastasizing ability, and high recurrence rate. It is difficult to cure cancer by any single treatment method while taking into account the quality of life of patients. Compared with the existing commonly used clinical treatment methods, such as surgery, radiotherapy, chemotherapy and immunotherapy, photodynamic therapy has become a new method in tumor diagnosis and treatment due to its unique advantages and good compatibility. It plays an important role in the comprehensive treatment of tumors. Photodynamic therapy (Photodynamic Therapy, PDT) is a new technology that uses photodynamic effect for disease diagnosis and treatment. The principle of the process is that ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K41/00A61K47/32A61P35/00C08F222/06C08F210/14C08F8/40
Inventor 王汉杰侯贝贝常津宫晓群苏琳郑斌
Owner TIANJIN UNIV
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