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Methylprednisolone-loading nanoparticles as well as preparation method and application thereof

A technology of nano-microspheres and methylprednisolone, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, and can solve the problem of methylprednisolone being unable to effectively target delivery, methylprednisolone high Dosage, side effects and other issues, to achieve the effect of prolonging the half-life of the drug, promoting central nervous system damage, and prolonging the half-life

Inactive Publication Date: 2014-04-09
NANTONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The purpose of the present invention is to provide a nano-microsphere loaded with methylprednisolone to solve the defects in the prior art that methylprednisolone cannot be effectively targeted and delivered to the damaged site and the high dose of methylprednisolone itself, toxicity and side effects

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  • Methylprednisolone-loading nanoparticles as well as preparation method and application thereof

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preparation example Construction

[0020] A method for preparing methylprednisolone-loaded nano-microspheres, using ibuprofen-modified inulin as a carrier, ibuprofen-modified inulin is composed of biocompatible inulin and anti-inflammatory drug ibuprofen, specifically prepared Including the following steps:

[0021] Step 1. Under stirring conditions, add N,N'-carbonyldiimidazole and ibuprofen into dimethyl sulfoxide solvent in a molar ratio of 1-1.3:1, and stir at room temperature for 1-3 hours;

[0022] Step 2, adding inulin to the reaction solution in step 1, and reacting at 60-100° C. for 12-48 hours; wherein, the molar ratio of the inulin unit to the ibuprofen in step 1 is 1-10:2;

[0023] Step 3: Pour the reaction solution in Step 2 into cold water to precipitate precipitates, wash with water, and dry to obtain ibuprofen-modified inulin. The preparation process of ibuprofen modified inulin is as follows:

[0024]

[0025] Step 4. Under stirring conditions, dissolve methylprednisolone and the ibuprofen...

Embodiment 1

[0030] Preparation of Ibuprofen Modified Inulin

[0031] Under stirring conditions, 0.43g N,N'-carbonyldiimidazole (2.65mmol) and 0.5g ibuprofen (2.42mmol) were added to 5mL dimethyl sulfoxide solvent, and the reaction was continued for 1h at room temperature. 0.5g of inulin (3.08mmol) was added to the above reaction solution, and the reaction was stirred at 80°C for 24h. The above reaction solution was poured into 100 mL of cold water, filtered with suction, washed with water, and dried to obtain ibuprofen-modified inulin.

[0032] Preparation of Nanoparticles Loaded with Methylprednisolone

[0033] Under stirring conditions, 5 mg of ibuprofen-modified inulin and 1 mg of methylprednisolone were dissolved in 1 mL of acetone, and added dropwise to 10 mL of 50°C hot water. Stir the above solution overnight to volatilize or evaporate acetone under reduced pressure, freeze-dry to obtain methylprednisolone-loaded nano-microspheres. The particle size range of the nano-microsphere...

Embodiment 2

[0035] Preparation of Ibuprofen Modified Inulin

[0036] Under stirring conditions, 0.43g N,N'-carbonyldiimidazole (2.65mmol) and 0.5g ibuprofen (2.42mmol) were added to 5mL dimethyl sulfoxide solvent, and the reaction was continued for 1h at room temperature. 0.39g of inulin (2.42mmol) was added to the above reaction solution, and stirred and reacted at 80°C for 24h. The above reaction solution was poured into 100 mL of cold water, filtered with suction, washed with water, and dried to obtain ibuprofen-modified inulin.

[0037] Preparation of Nanoparticles Loaded with Methylprednisolone

[0038] Under stirring conditions, 5 mg of ibuprofen-modified inulin and 1 mg of methylprednisolone were dissolved in 1 mL of acetone, and added dropwise to 10 mL of 50°C hot water. The above solution is stirred overnight to volatilize or acetone is aliquoted under reduced pressure, and freeze-dried to obtain methylprednisolone-loaded nano-microspheres. The particle size range of the nano-...

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Abstract

The invention discloses methylprednisolone-loading nanoparticles which consist of methylprednisolone and a carrier at a weight ratio of 1:(2-20), wherein the carrier is ibuprofen-modified ibuprofen and the grain size of the methylprednisolone-loading nanoparticles is 70-400nm. The invention further discloses a preparation method and application of the nanoparticles. The methylprednisolone-loading nanoparticles disclosed by the invention can be used for effectively transferring methylprednisolone to the injured part in a targeting manner, and have a very strong methylprednisolone slow-release function, so that side effects caused by high dosage and toxicity of methylprednisolone are avoided.

Description

technical field [0001] The invention relates to the field of preparation of drug-loaded nano-microspheres, in particular to a nano-microsphere loaded with methylprednisolone and its preparation method and application. Background technique [0002] Central nervous system injuries caused by traffic accidents, violent blows or industrial production accidents are very common in clinical practice. After the central nervous system is injured, neurons will die, disintegrate and disappear; then inflammatory cells invade, glial cells and connective tissue proliferate, 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 the only marketed drug for the treatment of acute spinal cord injury, and high-dose injection of methylprednisolone usually leads to neurological dysf...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/573A61K47/36A61P25/28
Inventor 张鲁中杨宇民周友浪李贵才王彩萍
Owner NANTONG UNIVERSITY
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