Methotrexate-entrapped iron-tannic acid complex, and preparation method and application thereof

A technology for carrying methotrexate and methotrexate is applied in the directions of non-active ingredients medical preparations, medical preparations containing active ingredients, and pharmaceutical formulas, and can solve the problems of low drug loading, complex preparation, and carrier materials Problems such as high consumption

Active Publication Date: 2020-10-27
CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the disadvantages of complex preparation of MTX nano drug delivery system, large consumption of carrier materials and low drug loading in the prior art, the present invention provides an iron-tannin complex loaded with methotrexate. Methotrexate and tannic acid in the complex form a drug-organic ligand bond through covalent coupling, and the drug-organic ligand bond and Fe 3+ Coordination Formation of Iron-Tannic Acid Complex Encapsulating Methotrexate

Method used

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  • Methotrexate-entrapped iron-tannic acid complex, and preparation method and application thereof
  • Methotrexate-entrapped iron-tannic acid complex, and preparation method and application thereof
  • Methotrexate-entrapped iron-tannic acid complex, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Dissolve 284.0mg of MTX, 119.8mg of EDC·HCl, and 85.1mg of TA in 10mL of DMSO, and stir in a 100mL round-bottomed flask at room temperature in the dark for 12 hours to obtain the MTX-TA reaction solution; place the MTX-TA reaction solution in an ice-water bath, add enough Measure ultrapure water to precipitate, filter with suction and collect the filter residue, which is a brown-red solid. The solid was suspended with an appropriate amount of PBS solution, transferred to a dialysis bag (MWCO=1000), placed in PBS solution (10 mM, pH 7.4) for dialysis at room temperature for 48 hours, and then transferred to ultrapure water for dialysis for 24 hours. The liquid in the dialysis bag was collected and freeze-dried to obtain the brown-yellow solid MTX-TA.

[0044] Take 4mL of MTX-TA solution (dissolved in PBS) with a concentration of 0.5mM in a 20mL beaker, add 4mL of FeCl with a concentration of 8mM (or 0.25mM, 0.5mM, 1mM, 2mM, 4mM, 10mM) 3 solution, stirred at room tempera...

Embodiment 2

[0046] Dissolve 531.6 mg mg MTX, 212.7 mg 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride EDC·HCl, 53.2 mg TA in 10 mL dimethyl sulfoxide DMSO in a 100 mL round bottom flask Stir at room temperature in the dark for 12 hours to obtain the methotrexate-tannin MTX-TA reaction solution, put the MTX-TA reaction solution in an ice-water bath, add enough ultra-pure water to cause precipitation, filter with suction and collect the filter residue, it is a brown-red solid . The solid was suspended with an appropriate amount of PBS solution, transferred to a dialysis bag (MWCO=1000), placed in PBS solution (10 mM, pH 7.4) for dialysis at room temperature for 42 hours, and then transferred to ultrapure water for dialysis for 28 hours. The liquid in the dialysis bag was collected and freeze-dried to obtain the brown-yellow solid MTX-TA.

[0047] Take 4mL of 0.5mM MTX-TA solution (dissolved in PBS) in a 20mL beaker, add 4mL of 8mM Fe 2 (SO 4 ) 3 solution, stirred at room temp...

Embodiment 3

[0049] Dissolve 284.0mg MTX, 119.8mg 1-ethyl-(3-dimethylaminopropyl)carbodiimide hydrochloride (EDC·HCl), 85.1mgTA in 10mL dimethyl sulfoxide (DMSO), in 100mL Stir in a round-bottomed flask at room temperature in the dark for 12 hours to obtain a methotrexate-tannic acid (MTX-TA) reaction solution, place the MTX-TA reaction solution in an ice-water bath, add sufficient ultrapure water to precipitate, filter and collect The filter residue is a brownish red solid. Suspend the solid with an appropriate amount of phosphate buffer (PBS solution), transfer it to a dialysis bag (MWCO=1000), place it in PBS solution (10mM, pH 7.4) and dialyze it at room temperature for 48h, then transfer the dialysis bag to ultrapure water Dialysis in 24h. The liquid in the dialysis bag was collected and freeze-dried to obtain the brown-yellow solid MTX-TA.

[0050] Take 4mL of 0.5mM MTX-TA solution (dissolved in PBS) in a 20mL beaker, add 4mL of 8mM FeCl 3 solution, stirred at room temperature for...

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Abstract

The invention relates to the technical field of biological medicines, in particular to a methotrexate-entrapped iron-tannic acid complex and a preparation method and application thereof. Methotrexateand tannic acid in the complex are covalently coupled to form a drug-organic ligand bond, the drug-organic ligand bond is coordinated with Fe<3+> to form the methotrexate-entrapped iron-tannic acid complex, and then a targeting ligand and the complex are combined through electrostatic interaction to form the targeting complex. The complex does not need to be added with other carrier materials, organic solvents and the like, the preparation process is simple, controllable, green and safe, and the drug is efficiently delivered to an inflammatory joint part under the dual mediation of passive targeting and active targeting, so that the complex is used for treating rheumatoid arthritis.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to an iron-tannic acid complex carrying methotrexate and its preparation method and application. Background technique [0002] Rheumatoid arthritis (RA) is an autoimmune disease characterized by chronic inflammatory lesions of joint tissues, mainly invading the small joints of the limbs of the whole body, and the incidence rate is as high as 1%. Its main pathological features are the formation of pannus and synovitis, pannus is aggressive, and synovitis leads to erosive hyperplasia of synovial tissue and infiltration of inflammatory cells and factors, which in turn erodes the surrounding cartilage and leads to progressive cartilage damage, eventually leading to Bone damage, loss of joint function and a series of complications. Drug therapy is currently the first choice for clinical treatment of RA. [0003] Methotrexate (MTX) has immunosuppressive and anti-inflammatory effects...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/54A61K47/61A61K31/519A61P29/00A61P19/02
CPCA61K47/6939A61K47/549A61K47/61A61K31/519A61P29/00A61P19/02
Inventor 周文虎郭丽娜
Owner CENT SOUTH UNIV
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