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ABA-type triblock aliphatic polyester copolymer, preparation method thereof and applications thereof

A terpolymer and polymer technology, applied in the field of polymer chemistry, can solve problems such as poor solubility and short half-life, and achieve the effects of prolonging the action time, avoiding phagocytosis, and improving hydrophilicity

Inactive Publication Date: 2014-02-26
NORTHWEST UNIV(CN)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The object of the present invention is to provide a kind of ABA type triblock aliphatic polyester copolymer, it can load hydrophobic drug and has excellent biocompatibility and biodegradability, to overcome the deficiency of poor solubility and short half-life of existing drug

Method used

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  • ABA-type triblock aliphatic polyester copolymer, preparation method thereof and applications thereof
  • ABA-type triblock aliphatic polyester copolymer, preparation method thereof and applications thereof
  • ABA-type triblock aliphatic polyester copolymer, preparation method thereof and applications thereof

Examples

Experimental program
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preparation example Construction

[0042] The preparation of the triblock copolymer of the present invention is carried out in three steps. First reference [Zhang S. P., et al.Biomacromolecules 2003 ,4: 437-445; Yang J., et al. Biomacromolecules 2004 ,5: 209-218] Synthesize polydiacid glycol esters with hydroxyl groups at both ends by polycondensation reaction with diacid or its derivatives (methyl ester, ethyl ester or aromatic ester) and linear diol—polymer (A) . The aliphatic polyester obtained through the polycondensation reaction in the present invention is used as a raw material for the subsequent reaction, and its ideal molecular weight range is 3000-8000, and the molecular weight is mainly controlled by the feeding ratio and the time of the polycondensation reaction. Then, the polymer (A) reacts with 2-bromoisobutyryl bromide by using the reactivity of the terminal hydroxyl group of the polymer (A) to generate a macroinitiator polymer (B) with a tertiary bromine at the end. The reaction uses anhydro...

Embodiment 1

[0045] 1. Synthesis of hydroxyl-terminated polybutylene succinate PBS

[0046] Add 5.9 g (50 mmol) dimethyl succinate and 5.4 g (60 mmol) 1,4-butanediol (molar ratio 1:1.2) into a three-necked flask treated with anhydrous and anaerobic treatment, and mix the above The system was placed in an oil bath with a preset temperature of 180°C, stirring was started, and the reaction system was protected by nitrogen. After 3 h, the reaction bottle was taken out, and after the reaction bottle was slightly cooled, the catalyst tetraisopropoxytitanium (1 / 500 of the molar number of dimethyl succinate) was added. After maintaining the temperature for 0.5 h, the pressure was reduced slowly and the reaction temperature was raised to 200 °C. The reaction was terminated after depressurizing for 3-5 h. Then, in a nitrogen atmosphere, the reaction product was quickly taken out and cooled to obtain a crude product. The above crude product was dissolved in an appropriate amount of chloroform, pre...

Embodiment 2

[0052] Similar to the synthesis method in Example 1, terpolymers with different structures can be obtained by changing the synthesis conditions. The structural formula is as follows:

[0053]

[0054] The structure of the synthesized terpolymer 1-1

[0055]

[0056] Structure of terpolymer 1-2

[0057]

[0058] Structure of terpolymer 1-3

[0059]

[0060] Structure of terpolymer 2

[0061]

[0062] Structure of Terpolymer 3

[0063]

[0064] Structure of Terpolymer 4

[0065]

[0066] Structure of terpolymer 5

[0067]

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Abstract

The invention discloses a terpolymer shown as the general formula (I), wherein x is 2, 4 or 6, y is 0, 2 or 4, m is an integer between 10 and 100, and n is an integer between 20 and 80. The amphiphilic triblock copolymer has excellent biocompatibility and capability of being partially biodegradable, and can form a nano medicine carrier with a structure imitating a cell outer membrane in water by self-assembly. The amphiphilic triblock copolymer has important research value and a broad application prospect in the field of controlled release of medicines. (I).

Description

technical field [0001] The invention relates to an ABA type tri-block amphiphilic copolymer, a preparation method thereof and the application of self-assembled nano micelles with an imitation cell outer membrane structure as a drug carrier, belonging to the technical field of macromolecular chemistry. Background technique [0002] In today's society, tumor has become the second largest disease that seriously endangers human health. At present, the drugs widely used clinically to treat tumors have little target distribution on human lesion sites, have large toxic and side effects, and most of them have poor water solubility. Therefore, improving the solubility of drugs, improving the bioavailability of drugs and reducing toxic and side effects are important issues to be solved urgently. [0003] Polymeric micelles are self-assembled structures formed spontaneously by amphiphilic polymers in water or body fluids driven by intermolecular hydrogen bonds, electrostatic interacti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08F283/02C08G63/91A61K47/32A61K9/107A61K9/19
Inventor 张世平张宇澄宫永宽何贵强赵婧
Owner NORTHWEST UNIV(CN)
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