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Dual-response amphiphilic polyphosphazene targeted drug carrier material and preparation method thereof

A dual-response, polyphosphazene technology, applied in the field of medicine, can solve the problems of human toxicity and side effects, lack of specificity, etc.

Inactive Publication Date: 2018-09-04
YANBIAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Most chemotherapeutic drugs are lethal to both tumor cells and normal cells, that is, these anti-tumor drugs lack specificity between tumor tissue and normal tissue, and have serious toxic side effects on the human body during treatment

Method used

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  • Dual-response amphiphilic polyphosphazene targeted drug carrier material and preparation method thereof
  • Dual-response amphiphilic polyphosphazene targeted drug carrier material and preparation method thereof
  • Dual-response amphiphilic polyphosphazene targeted drug carrier material and preparation method thereof

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Embodiment 1

[0068] The invention provides a dual-response amphiphilic polyphosphazene-targeted drug-loaded polymer material, comprising an enzyme-responsive and pH-responsive dual-response amphiphilic polyphosphazene and at least one hydrophobic drug;

[0069] The double response type amphiphilic polyphosphazene is based on the polyphosphazene segment shown in formula (1), and is connected with a hydrophilic segment and a hydrophobic segment on the phosphorus atom; the hydrophilic The segment is polyethylene glycol monomethyl ether, and the hydrophobic segment is an enzyme-responsive pentapeptide H 2 N-GFLGK-OEt, the chemical formula is gly-phe-leu-gly-lys-OEt;

[0070]

[0071] The chemical formula of the double response type amphiphilic polyphosphazene obtained is:

[0072]

[0073] Among them, A is polyethylene glycol monomethyl ether, and B is an enzyme-responsive pentapeptide;

[0074] The hydrophobic drug is covalently bonded to the hydrophobic segment, and the hydrophobic d...

Embodiment 2

[0094] According to the preparation method of Example 1, the hydrophobic segment is designed to be a pentapeptide, and the molar ratio of MPEG and pentapeptide is 1.5:1, and the amount of each raw material component is modified therein;

[0095] In step (1), in step b, the normal temperature reaction time is 2h, in step c, according to the molar ratio of the hydrophilic segment MPEG and pentapeptide is 1.5:1, weigh the pentapeptide H after vacuum drying 2 N-GFLGK-OEt, add dropwise the tetrahydrofuran solution containing the pentapeptide and triethylamine to the above polyphosphazene-MPEG reaction solution, react at room temperature for 3h, then heat in an oil bath at 55°C, and continue the reaction for 50h, In step d, after the reaction, the oil bath was removed, cooled to room temperature, the polyphosphazene-MPEG-peptide chain reaction solution was spin-dried, then dissolved in methanol, filtered with diatomaceous earth, and centrifuged at a speed of 12000r / min Remove the in...

Embodiment 3

[0098] According to the preparation method of Example 1, the hydrophobic segment is designed to be a pentapeptide, and the molar ratio of MPEG and pentapeptide is 2.5:1, and the amount of each raw material component is modified therein;

[0099] In step (1), in step b, the normal temperature reaction time is 2h, in step c, according to the molar ratio of the hydrophilic segment MPEG and pentapeptide is 1.5:1, weigh the pentapeptide H after vacuum drying 2N-GFLGK-OEt, add dropwise the tetrahydrofuran solution containing the pentapeptide and triethylamine to the above polyphosphazene-MPEG reaction solution, react at room temperature for 3h, then heat in an oil bath at 50°C, and continue the reaction for 48h, In step d, after the reaction, the oil bath was removed, cooled to room temperature, the polyphosphazene-MPEG-peptide chain reaction solution was spin-dried, then dissolved in methanol, filtered with diatomaceous earth, and centrifuged at a speed of 11000r / min Remove the ins...

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Abstract

The invention provides a dual-response amphiphilic polyphosphazene targeted drug carrier polymer material. The dual-response amphiphilic polyphosphazene targeted drug carrier polymer material is grafted with a hydrophilic chain segment MPEG (Methoxy Polyethylene Glycol) and an enzyme-sensitive hydrophobic chain segment peptide chain, an acid-sensitive drug is bonded on a hydrophobic side chain, micelles can be easily formed in water through self-assembly, the micelles can be intravenously injected into a human body, can accumulate in a tumor site through an EPR (Enhanced Permeability and Retention) effect and can go into cells, the acidity of a physiological environment in tumor cells is stronger, the pH (Potential of Hydrogen) value is about 4.5 to 5.5, but the normal physiological pH value of the human body is 7.4; the cells contain a large amount of lysosomal enzyme, a micelle structure of a drug carrier polymer can be dissociated under dual functions of low pH and the lysosomal enzyme, free adriamycin can be released, and the adriamycin acts on DNA (Deoxyribonucleic Acid) to stop copying of the DNA, so that the tumor cell death is caused, and the purposes of targeted therapy and no toxic and side effects are finally achieved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a dual-response amphiphilic polyphosphazene targeting drug carrier material and a preparation method thereof. Background technique [0002] Polyphosphazene is an organic-inorganic functional polymer material. Its main chain is composed of nitrogen atoms and phosphorus atoms alternately arranged. Groups with different properties can be introduced through side chain derivatization. The diversity of side chains endows it with Special physical and chemical properties, such as degradability, good biocompatibility, non-carcinogenic, hydrophilic or hydrophobic, etc. Due to the controllability and diversity of polyphosphazene side groups, the functions of polyphosphazene derivatives are also diversified, and can be used as a drug control system in the fields of pharmacology and medical research. [0003] Most chemotherapeutic drugs are lethal to tumor cells as well as norma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/60A61K47/58A61K31/704A61P35/00C08G81/00
CPCA61K9/1075A61K31/704A61K47/60A61K47/605A61P35/00C08G81/00
Inventor 许景哲金成
Owner YANBIAN UNIV
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