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PH-sensitive pentablock linear polymer based on PDEAEMA and micelle

A linear polymer, pentablock technology, applied in the field of biomedical polymer materials, can solve the problems of limiting the application of polymer micelles, wide particle size distribution of micelles, too large particle size, etc., to enhance the encapsulation performance , The effect of increasing the package load and increasing the stability

Active Publication Date: 2015-05-27
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, this material still faces a series of problems, such as the micelles are diluted and easily disintegrated after entering the blood, and the micelles are too large to be swallowed by the reticuloendothelial system (RES) in the body or absorbed by tissues such as the liver and spleen. Micelles have a wide particle size distribution, etc.
The self-assembly of polymer micelles is a thermodynamically stable process, that is, the micellar structure remains stable only when its concentration is higher than the CMC value of the micelles, and it is easy to disintegrate when diluted to a concentration lower than the CMC value of the micelles in the current period, thereby loading drugs Burst release of drugs in micelles limits the application of polymer micelles in the human body

Method used

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  • PH-sensitive pentablock linear polymer based on PDEAEMA and micelle
  • PH-sensitive pentablock linear polymer based on PDEAEMA and micelle
  • PH-sensitive pentablock linear polymer based on PDEAEMA and micelle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Embodiment 1: the synthesis of macroinitiator Br-PEG-Br

[0067] The synthetic reaction formula is as follows:

[0068]

[0069] Synthesis of macromolecular initiator Br-PEG-Br: Put a magnetic stirrer in a 250mL round-bottomed reaction bottle, seal it with a reverse rubber stopper, evacuate it-pass argon three times, and place it in ice water. 0.4 g (3.28 mmol) of DMAP (Shanghai Covalent Chemical) and 2.0 mL (14.0 mmol) of TEA were dissolved in 20 mL of dichloromethane, and the solution was added to the reaction vial via syringe. 6.6 g (3.30 mmol) of PEG (Sigma-Aldrich) was dissolved in 80 mL of dichloromethane, and the PEG solution was injected into the reaction flask via a syringe. Add 1.6mL (6.60mmol) BMPB (J&K, Bailingwei) drop by drop to the reaction vial with a syringe, finish adding within one hour, keep the reaction at 0°C for 2 hours, remove the ice bath, and continue the reaction at room temperature for 24 hours . After the reaction is completed, use 5wt...

Embodiment 2

[0070] Example 2: pH Sensitive Pentablock Linear Polymer PEG-[b-PDEAEMA-b-PMMA] 2 Synthesis

[0071] The synthetic reaction formula is as follows:

[0072]

[0073]Put a magnetic stirrer, 26.8mg (0.12mmol) copper bromide and 2.2g (1mmol) macromolecular initiator Br-PEG-Br into a 50mL dry eggplant-shaped bottle, seal it with a reverse rubber stopper, vacuumize-argon Gas three times, inject 20mL of toluene, monomer DEAEMA (4.02mL, 20mmol) (J&K, Bailingwei), ligand HMTETA (0.31ml, 1.2mmol) (J&K, Bailingwei) into the bottle with a syringe in turn, and stir for 10 minutes to make the catalyst complex formation. Then 0.486g (1.2mmol) reducing agent Sn(Oct) 2 Dissolve in 2 mL of toluene and add to reaction flask. Then the reaction flask was transferred to 60° C. for 7 hours, and then 1.86 mL (17.5 mmol) of monomeric MMA (J&K, Braunwei) was added, and the reaction was continued for 12 hours. Cool the reaction solution to room temperature, add 50mL THF and stir to dissolve it, ...

Embodiment 3

[0074] Example 3: pH Sensitive Pentablock Linear Polymer PEG-[b-PDEAEMA-b-PMMA] 2 Synthesis

[0075] Put a magnetic stirrer, 17.9mg (0.08mmol) copper bromide and 1.76g (0.8mmol) macromolecular initiator Br-PEG-Br into a 50mL dry eggplant-shaped bottle, seal it with a reverse rubber stopper, vacuum-pass Argon gas was injected three times, and 20mL of toluene, monomer DEAEMA (5.02mL, 25mmol), and ligand HMTETA (0.21ml, 0.8mmol) were injected into the bottle in sequence, and stirred for 10 minutes to form a catalyst complex. Then 0.324g (0.8mmol) reducing agent Sn(Oct) 2 Dissolve in 2 mL of toluene and add to reaction flask. Then the reaction flask was transferred to 60° C. for 7 h, and then 2.12 mL (20 mmol) of monomeric MMA was added, and the reaction was continued for 12 h. Cool the reaction solution to room temperature, add 50mL THF and stir to dissolve it, then filter through a neutral alumina column to remove the catalyst CuBr 2 (with THF as eluent). The obtained eluat...

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Abstract

The invention belongs to the technical field of high polymer materials for biological medicines and discloses a pH-sensitive pentablock linear polymer based on PDEAEMA, a preparation method of the polymer and a micelle system obtained based on the polymer and the application of the micelle system. The polymer has the structure shown in a formula described in the specification, wherein x is equal to 45, y is equal to 19-37, and z is equal to 15-19. A symmetrical pentablock linear polymer is designed and synthesized, the drug encapsulation amount of the polymer can be obviously improved, the pH response range of the self-assembly micelle can be well regulated by virtue of the intermediate layer PDEAEMA so that the drug loading micelle can rapidly respond the change of the pH value in a tumor environment, the drug release can be effectively controlled, and burst release of the drug is avoided. A thick pH responsive intermediate layer is formed in the micelle formed by the polymer, the encapsulation capacity is improved, the drug release performance is improved, the particle size of the micelle after drug release is reduced, the drug discharge is facilitated, and the polymer can be widely applied to the field of medicines.

Description

technical field [0001] The invention belongs to the technical field of biomedical polymer materials, and in particular relates to a PDEAEMA-based pH-sensitive five-block linear polymer, a preparation method thereof, and a micelle system obtained based on the same and its application. Background technique [0002] Cancer (malignant tumor) is a disease caused by the abnormal mechanism of controlling cell growth and proliferation. However, in addition to uncontrolled growth, cancer cells also locally invade normal tissues of the human body and can easily transfer to other parts. According to the latest "World Cancer Report", among the 14 million new cancer cases in the world, 3.07 million are Chinese, accounting for 21.8%, and the new cancer cases rank first in the world. The proportion of deaths accounted for 26.9% of the global death toll. It can be seen that the treatment of cancer in China is still relatively backward, so the research on cancer treatment is also particular...

Claims

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Application Information

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IPC IPC(8): C08F293/00C08F220/34C08F220/14C08G65/332A61K47/34A61K9/107
Inventor 章莉娟陈全张灿阳姚娜吴文胜
Owner SOUTH CHINA UNIV OF TECH
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