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Polymer nanoparticles capable of treating rheumatoid arthritis

A technology of polymer and polymer glue, applied in the field of polymer and biomedical materials

Active Publication Date: 2019-08-30
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently, in the clinical treatment of RA, TNF-α antibody drugs (such as etanercept, adalimumab, etc.), as well as IL-1, IL-6 and B cell-targeted drugs are commonly used. These drugs are effective for about 40% of patients. There is no effect, and long-term TNF-α antibody drug treatment will lead to the transformation of RA into systemic lupus erythematosus, type I diabetes and even cardiovascular disease

Method used

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  • Polymer nanoparticles capable of treating rheumatoid arthritis
  • Polymer nanoparticles capable of treating rheumatoid arthritis
  • Polymer nanoparticles capable of treating rheumatoid arthritis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0107] Embodiment 1 prepares amphiphilic block copolymer PLGA-b-PDMA 463 and cationic polymer micelles containing it

[0108] The cationic amphiphilic block copolymer used to prepare micelles in this example is PLGA-b-PDMA 463 , whose structure is as follows:

[0109]

[0110] 1. PLGA-b-PDMA 463 The preparation process is as follows:

[0111] S1. To 9 g ester-terminated PLGA (commercially available; M η =8000; with 1 M calculated by HNMR n =12000, the molar weight is 0.75mmol), add 90mL toluene, azeotropic water removal;

[0112] S2. Cool the ester-terminated PLGA after removing water to room temperature, add 50mL CH 2 Cl 2 , 0.08mL triethylamine (1.28mmol); Take 0.06mL 2-bromoisobutyryl bromide (1.28mmol) and wash with 2.5mL CH 2 Cl 2 Dilute and add dropwise to the flask filled with PLGA and triethylamine under ice-water bath cooling, remove the ice bath 4 hours after the drop, and react for 48 hours;

[0113] S3. The product obtained in S2 is extracted once wit...

Embodiment 2

[0126] With reference to the method of Example 1, prepare amphiphilic block copolymer PLGA-b-PDMA 347 , whose structure is as follows:

[0127]

[0128] With reference to the method of embodiment 1, based on PLGA-b-PDMA 347 Preparation of cationic polymer micelles cNP 347 , with an average particle size of 66nm and a Zeta potential of +14mV.

Embodiment 3

[0130]With reference to the method of Example 1, prepare amphiphilic block copolymer PLGA-b-PDMA 202 , whose structure is as follows:

[0131]

[0132] With reference to the method of embodiment 1, based on PLGA-b-PDMA 202 Preparation of cationic polymer micelles cNP 202 . Its average particle size is 97nm and its Zeta potential is +11mV.

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Abstract

The invention belongs to the field of macromolecule and biomedical materials, and relates to a polymer nanoparticle capable of treating rheumatoid arthritis, in particular to a cationic polymer micelle, a method for preparing the polymer micelle and a pharmaceutical composition containing the polymer micelle. The micelle provided by the invention can bind with cf-DNA, reduce the concentration of cytokines and enzymes related to rheumatoid arthritis, and be used for the treatment of rheumatoid arthritis.

Description

technical field [0001] The invention belongs to the field of polymers and biomedical materials, and relates to a polymer nanoparticle that can be used for treating rheumatoid arthritis, in particular to a cationic polymer micelle, a method for preparing the polymer micelle, and A pharmaceutical composition containing the polymer micelles. Background technique [0002] The core of rheumatoid arthritis (RA) lies in the activation of FLS (Synovial Fibroblasts-like) and the accumulation of immune cells and cytokines in joints. The activation of FLS leads to the expression of specific matrix degrading enzymes (such as matrix metalloproteinase MMP-3, MMP-14), adhesion factors (such as CD130, etc.) and cytokines, resulting in cartilage deformation and destruction. Currently, in the clinical treatment of RA, TNF-α antibody drugs (such as etanercept, adalimumab, etc.), as well as IL-1, IL-6 and B cell-targeted drugs are commonly used. These drugs are effective for about 40% of patie...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/34A61K31/785A61P29/00A61P19/02
CPCA61K9/1075A61K31/785A61K47/34A61P19/02A61P29/00A61K9/107
Inventor 刘利新梁慧怡董聪彭勃陈永明
Owner SUN YAT SEN UNIV
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