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A kind of nanoscale drug carrier loaded with methylprednisolone and preparation method thereof

A methylprednisolone and nano-scale technology, applied in the field of medicine, can solve the problems of lack of obvious curative effect, narrow treatment time window, and many complications in the treatment of spinal cord injury, so as to avoid toxic and side effects, high physiological safety performance, The effect of high tissue compatibility

Active Publication Date: 2019-01-29
AFFILIATED HOSPITAL OF NANTONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the administration of large doses of methylprednisolone can restore nerve function to a certain extent in acute central nervous system injury, it often leads to serious side effects
[0003] Side effects of methylprednisolone may be due to its high dose and toxicity
Conventional doses of methylprednisolone are not effective in the treatment of spinal cord injuries, and large doses of methylprednisolone for central nervous system injuries can cause serious side effects, including gastric bleeding, sepsis, pneumonia, acute cortical Steroid myopathy and wound infection, and only modest improvement in neurological recovery
And the application of methylprednisolone has many complications, and the treatment time window is narrow

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] A method for preparing a novel nanoscale drug carrier loaded with methylprednisolone, comprising two steps: the synthesis of ibuprofen-modified dextran nanospheres and the preparation of novel nanoparticles loaded with methylprednisolone , to complete the preparation of a novel nanoscale drug carrier loaded with methylprednisolone; the specific steps are as follows:

[0025] The synthetic concrete steps of ibuprofen modified dextran nano microspheres are as follows:

[0026] (1) Add 0.5g of ibuprofen into 4ml of dimethyl sulfoxide solvent and stir evenly at room temperature;

[0027] (2) Add 0.43g of N,N'-carbonyldiimidazole to the above mixture, and stir at room temperature for 0.5 hours;

[0028] (3) Add 0.5g of dextran to the mixture obtained in step (2), and stir and react at 75°C for 12 hours;

[0029] (4) Precipitate the mixed solution obtained in step (3) in 100ml of ice water, filter the precipitate, and wash the precipitate with double distilled water for 3 t...

Embodiment 2

[0036] A method for preparing a novel nanoscale drug carrier loaded with methylprednisolone, comprising two steps: the synthesis of ibuprofen-modified dextran nanospheres and the preparation of novel nanoparticles loaded with methylprednisolone , to complete the preparation of a novel nanoscale drug carrier loaded with methylprednisolone; the specific steps are as follows:

[0037] The synthetic concrete steps of ibuprofen modified dextran nano microspheres are as follows:

[0038] (8) Add 0.5g of ibuprofen into 10ml of dimethyl sulfoxide solvent, and stir evenly at room temperature;

[0039] (9) Add 0.43g of N,N'-carbonyldiimidazole to the above mixture, and stir at room temperature for 2 hours;

[0040] (10) Add 0.5 g of dextran to the mixture obtained in step (8), and stir and react at 85°C for 36 hours;

[0041] (11) Precipitate the mixed solution obtained in step (10) in 100ml of ice water, filter the precipitate, and use double distilled water to wash the precipitate f...

Embodiment 3

[0048]A method for preparing a novel nanoscale drug carrier loaded with methylprednisolone, comprising two steps: the synthesis of ibuprofen-modified dextran nanospheres and the preparation of novel nanoparticles loaded with methylprednisolone , to complete the preparation of a novel nanoscale drug carrier loaded with methylprednisolone; the specific steps are as follows:

[0049] The synthetic concrete steps of ibuprofen modified dextran nano microspheres are as follows:

[0050] (15) Add 0.5g of ibuprofen into 5ml of dimethyl sulfoxide solvent, and stir evenly at room temperature;

[0051] (16) Add 0.43g of N,N'-carbonyldiimidazole to the above mixture, and stir at room temperature for 1 hour;

[0052] (17) Add 0.5 g of dextran to the mixture obtained in step (16), and stir and react at 80°C for 24 hours;

[0053] (18) Precipitate the mixed solution obtained in step (17) in 100ml of ice water, filter the precipitate, and wash the precipitate with double distilled water for...

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Abstract

The invention discloses a novel nanometer drug carrier loaded with methyllprednisolone. The novel nanometer drug carrier comprises methyllprednisolone and a carrier, wherein the carrier is an ibuprofen modified dextran nanometer microsphere, the particle diameter of the novel nanometer drug carrier loaded with methyllprednisolone is 120 to 160 nanometers, the preparation method of the novel nanometer drug carrier loaded with methyllprednisolone comprises two steps of synthesizing the ibuprofen modified dextran nanometer microsphere and preparing novel nanoparticles loaded with methyllprednisolone. The novel nanometer drug carrier loaded with methyllprednisolone disclosed by the invention has the advantages that the nanometer microsphere synthesized by ibuprofen modified dextran is taken as the carrier, so that methyllprednisolone can be effectively and targetedly delivered to injured parts, the half-life of methylprednisolone drugs can be effectively prolonged, and methyllprednisolone and ibuprofen can play a synergistic role on promotion of central nervous system injury repair.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a novel nanoscale drug carrier loaded with methylprednisolone and a preparation method thereof. Background technique [0002] Central nervous system injuries caused by traffic accidents, violent blows or industrial production accidents are very common in clinical practice. After central nervous system injury, neurons will die, disintegrate and disappear; then inflammatory cells invade, glial cells and connective tissue hyperplasia, resulting in permanent motor and sensory dysfunction, which brings great difficulties to people's lives . Although many scholars have made a lot of efforts in this area, there is still no effective treatment for central nervous system injury. So far, methylprednisolone is an intermediate-effect glucocorticoid drug, and is currently recognized as an effective drug for spinal cord injury. It has a definite preventive effect on secondary spinal cord ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/54A61K9/16A61K31/573A61P25/00A61P25/28A61K31/192
CPCA61K9/1623A61K31/192A61K31/573A61K2300/00
Inventor 祁雷黄中伟蒋海燕张鲁中孙智超
Owner AFFILIATED HOSPITAL OF NANTONG UNIV
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