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Methionine-polyesteramide high-molecular polymer with ROS responsiveness and application of methionine-polyesteramide high-molecular polymer

A technology of high molecular polymer and polyester amide, which is applied in the direction of organic active ingredients, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc.

Active Publication Date: 2021-02-05
SUN YAT SEN UNIV +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current research on the use of methionine-polyesteramide polymer materials as drug delivery carriers for encapsulating paclitaxel has not been reported.

Method used

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  • Methionine-polyesteramide high-molecular polymer with ROS responsiveness and application of methionine-polyesteramide high-molecular polymer
  • Methionine-polyesteramide high-molecular polymer with ROS responsiveness and application of methionine-polyesteramide high-molecular polymer
  • Methionine-polyesteramide high-molecular polymer with ROS responsiveness and application of methionine-polyesteramide high-molecular polymer

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Experimental program
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Effect test

Embodiment 1

[0097] Embodiment 1 is based on the synthesis of the polyester amide of methionine

[0098] 1. The preparation of high molecular polymer Met-PEA, the steps are as follows:

[0099] (1) Synthesis of N-x monomer (x represents the number of methylene groups on the diacid chloride)

[0100]①Here, take N-2 as an example. Add 0.0603mol triethylamine and 0.0603mol p-nitrophenol to 100ml acetone, stir and mix evenly at room temperature, then keep the acetone solution at -78°C with dry ice, after that, add 0.03mol (3.2ml) butane The acid chloride was added to 40ml of acetone, mixed evenly, added dropwise to the above frozen solution, and stirred at -78°C for 2h, then turned to room temperature and stirred overnight.

[0101] ②Pour the mixed solution obtained in step ① into 800ml of distilled water to precipitate the product, filter it, wash thoroughly with distilled water, dry it in vacuum at 50°C, and finally recrystallize and purify by acetonitrile three times to obtain dicarboxyli...

Embodiment 2

[0118] Example 2 Preparation and Screening of Methionine-Based Polyesteramide Polymers as Drug Carriers Encapsulating PTX Nanosystems

[0119] 1. Prepare the PTX@Met-PEA nano drug loading system through the following steps

[0120] (1) Dissolve the 12 kinds of Met-PEA prepared in Example 1 in DMSO respectively, make a solution of 25 mg / ml, take 200 μL for later use; dissolve the stabilizer DSPE-PEG2000 in dimethyl sulfoxide (DMSO) , made into a 15 mg / ml solution, and 100 μL was taken for later use; Paclitaxel (PTX) was dissolved in DMSO, and made into a 5 mg / ml solution, and 100 μL was taken for later use. At this time, DSPE-PEG2000 is 30% (mass percentage) of the Met-PEA dosage, and PTX is 10% (mass percentage) of the Met-PEA dosage.

[0121] (2) The above solutions were mixed to obtain 400 ul of the mixed solution as the organic phase. At a speed of 1000rpm, add the organic phase dropwise to 10ml of deionized water (the volume ratio of the organic phase to the water phase ...

Embodiment 3

[0129] Example 3 Stability and drug release of PTX@Met-PEA nanoparticles

[0130] 1. Study on the stability of PTX@Met-PEA nanoparticles

[0131] (1) Four kinds of drug-loaded nanoparticles prepared in Example 2 (PTX@N-2-Met-8 NPs, PTX@N-4-Met-8NPs, PTX@N-2-Met-10 NPs and PTX @N-4-Met-10 NPs) were taken out and dispersed in PBS buffer containing 10% (v / v) fetal bovine serum (FBS), placed at room temperature for seven days, and the corresponding particle size and PDI were measured every day. long-term stability of the particles.

[0132] (2) The result is as follows Figure 5 As shown, the particle size of PTX@N-2-Met-8 NPs and PTX@N-4-Met-8 NPs gradually increased in the PBS buffer containing 10% FBS, indicating that their stability was damaged and it was difficult to stable in the body. However, PTX@N-2-Met-10 NPs and PTX@N-4-Met-10 NPs can exist stably for more than 7 days in the same environment, which can prolong the cycle time of PTX to some extent. Therefore, throug...

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Abstract

The invention discloses a methionine-polyesteramide high-molecular polymer with ROS responsiveness and application of the methionine polyesteramide high-molecular polymer. The structural formula of the methionine polyesteramide high-molecular polymer is shown as a formula (I). The methionine-based polyesteramide polymer material is synthesized by taking methionine, diacid containing different methylene numbers, diol and the like as raw materials through melt phase polycondensation reaction, the method is high in repeatability and simple and convenient to operate, the used raw materials are non-toxic, economical and easy to obtain, the obtained high-molecular polymer material has excellent biosafety and biodegradability, can be used as a drug carrier, can be controllably released in a high-concentration H2O2 environment, effectively solves the problems of poor stability, poor biosafety, weak targeting property and the like of nano-drugs, and has a good prospect in biomedical applications such as tumor treatment and the like.

Description

technical field [0001] The invention relates to the field of nano drug carriers, in particular to a ROS-responsive methionine-polyesteramide polymer and its application. Background technique [0002] According to WHO's "Global Cancer Report", the number of cancer deaths in 2018 was 9.6 million, with an increase of 18.1 million cases, and the global cancer burden has further increased. At present, the most important treatment for cancer is surgical resection, but local residual tumors will greatly increase the chance of cancer recurrence. Radiotherapy and chemotherapy are commonly used to treat postoperative local residual tumors. However, radiotherapy will cause damage to normal cells, and chemotherapy will cause a series of problems such as drug resistance of tumor cells. The drug delivery system (DDS) can precisely target the tumor site through the high permeability and retention effect (EPR effect, namely enhanced permeability and retention effect) of solid tumors, impro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08G69/44A61K9/51A61K47/34A61K31/337A61P35/00
CPCC08G69/44A61K9/5146A61K31/337A61P35/00
Inventor 吴钧刘杰顾志鹏
Owner SUN YAT SEN UNIV
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