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Amphipathy triblock polymer and preparation method and application thereof

A polymer, triblock technology, applied in the field of nanomedicine, can solve the problems of single function and limited application, and achieve the effect of wide application

Active Publication Date: 2013-05-08
SHENZHEN INST OF ADVANCED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, traditional amphiphilic block polymers can usually only load hydrophobic small molecule drugs and have a single function, which limits their further applications.

Method used

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  • Amphipathy triblock polymer and preparation method and application thereof
  • Amphipathy triblock polymer and preparation method and application thereof
  • Amphipathy triblock polymer and preparation method and application thereof

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preparation example Construction

[0055] In addition, this embodiment also provides a method for preparing an amphiphilic tri-block polymer, comprising the following steps:

[0056] Step 110, under a protective gas atmosphere, dissolving amino acid monomers and polyethylene glycol derivatives in N,N-dimethylformamide to obtain a mixed solution, and then reacting at a constant temperature at 30-50°C for 24-120 hours , wherein the amino acid monomer is formed by the internal anhydride of leucine (Leu-NCA), the internal anhydride of lysine containing a side chain protecting group, and the internal anhydride of glutamic acid containing a side chain protecting group The mixture, the ratio of the total moles of the mixture to the moles of the polyethylene glycol derivative is 10:1 to 200:1, and the concentration of the polyethylene glycol derivative in the mixture is 1 to 100 mg / mL.

[0057] Step 120, adding phenylalanine cyclic anhydride (Phe-NCA) to the reacted mixed solution, and reacting at a constant temperatur...

Embodiment 1

[0083] Preparation of P1 Amphiphilic Triblock Polymer

[0084]The closed round-bottomed flask was evacuated and filled with nitrogen; then 1 g of monomethyl ether amino polyethylene glycol (MPEG) with a molecular weight of 2000 was dissolved in 20 mL of N,N-dimethylformamide (DMF), and added into the above-mentioned round-bottomed flask; then add Lys(Z)-NCA, Glu(OBzl)-NCA and Leu-NCA three monomers to the above-mentioned round-bottomed flask, and react at a constant temperature of 40°C for 72 hours under nitrogen protection; After the end, add Phe-NCA monomer to the above-mentioned round-bottomed flask, and react at a constant temperature of 40°C for 48 hours under the protection of nitrogen; The amphiphilic triblock polymer of side chain protecting group, MPEG-b-P[Lys(Z)-co-Leu-co-Glu(OBzl)]-b-PPhe; Wherein, the total molar number of three kinds of monomers and The molar ratio of monomethyl ether amino polyethylene glycol is 30:1, and the molar ratio of Phe-NCA monomer to mo...

Embodiment 2

[0088] Preparation of P2 Amphiphilic Triblock Polymer

[0089] The closed round bottom flask was evacuated and filled with nitrogen; then 0.5 g of aminopolyethylene glycol carboxylic acid (NH 2 -PEG-COOH) was dissolved in 15mL DMF and added to the above round bottom flask; then three monomers, Lys(Z)-NCA, Glu(OBzl)-NCA and Leu-NCA were added to the above round bottom flask, Under the protection of nitrogen, react at a constant temperature of 30°C for 72 hours; after the reaction, add Phe-NCA monomer to the above-mentioned round bottom flask, and react at a constant temperature of 30°C for 72 hours under the protection of nitrogen; after the reaction, add 15 times The diethyl ether of the volume of reaction solution is precipitated, centrifuged, and dried to obtain an amphiphilic triblock polymer containing side chain protecting groups, HOOC-PEG-b-P[Lys(Z)-co-Leu-co-Glu(OBzl)]- b-PPhe; wherein, the ratio of the total moles of the three monomers to the moles of the aminopolyeth...

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Abstract

The invention relates to an amphipathy triblock polymer. The amphipathy triblock polymer is a linear compound comprising a hydrophilic chain section, an intermediate chain section and a hydrophobic chain section, wherein the hydrophilic chain section is a polyethylene glycol derivative; the intermediate chain section is a peptide polymer comprising lysine, leucine and glutamic acid; the hydrophobic chain section is polyphenylalanine; the polyethylene glycol derivative is connected with one end of the intermediate chain section through an amido bond; and the polyphenylalanine is connected with the other end of the intermediate chain section through a peptide bond. The amphipathy triblock polymer provided by the invention can be self-assembled in an aqueous solution to form a polymer nano-micelle with a three-layer structure; the polymer nano-micelle servicing as a vector has the characteristics of high stability, excellent biocompatibility and the like; the amphipathy triblock polymer is hardly removed by the immune system during circulating in a human body, and hydrophobic small molecule drugs, genetic materials and protein molecules can be effectively loaded at the same time, so that the amphipathy triblock polymer has a wide application prospect. In addition, the invention also provides a preparation method of the amphipathy triblock polymer.

Description

technical field [0001] The invention relates to the field of nanomedicine, in particular to an amphiphilic triblock polymer and its preparation method and application. Background technique [0002] As a drug-loaded nano-delivery system, nano-drug carriers are mainly used for controlled release of drugs, targeted delivery, increasing the solubility of hydrophobic drugs and reducing drug side effects, etc. It encapsulates drugs in nanoparticles to regulate release Increase the rate of drug, increase the permeability of biomembrane, change the distribution in the body, improve bioavailability, etc. [0003] With the development of technology, especially the development of gene therapy technology, nano-drug carriers need to load not only drugs in the traditional sense but also drugs in emerging senses such as genes and proteins. [0004] Gene therapy refers to the introduction of exogenous normal genes into target cells to correct or compensate diseases caused by gene defects a...

Claims

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Application Information

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IPC IPC(8): C08G69/40C08G69/10C08G69/14C08G69/46A61K47/42A61K45/00A61K45/06A61K48/00A61K9/107
Inventor 蔡林涛易虎强刘朋李萍王亚楠刘斌
Owner SHENZHEN INST OF ADVANCED TECH
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