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Amphotericin B nano preparation

A technology of amphotericin and nano preparation, applied in the field of medicine, can solve the problems of high risk, many comorbidities, difficult to penetrate the blood-brain barrier, etc.

Inactive Publication Date: 2006-10-25
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Cryptococcal meningitis is a common deep fungal infectious disease. The biggest problem with AmB treatment is that it is not easy to pass through the blood-brain barrier. Direct intrathecal injection is not only inconvenient to operate, but also has high risks and complications. More, patients are unacceptable
Although clinically applied liposome formulations have been proven to be able to cross the blood-brain barrier, their widespread use is limited due to their high price and uncertain efficacy

Method used

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  • Amphotericin B nano preparation
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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Weigh 300mg of Dextran-70, put it in a beaker, add distilled water and stir to dissolve, adjust the pH value of the solution to 3.0 with 0.01mol / L hydrochloric acid, and set the volume to 50ml. Slowly add 0.5ml of BCA at room temperature under electromagnetic stirring to a final concentration of 1%. After stirring for 4 hours, adjust the pH to 8.5 with 0.1mol / L sodium hydroxide to obtain a blank PBCA nanoparticle colloidal solution. Measure 10ml of the blank nanoparticle colloidal solution, add 20mg of amphotericin B powder injection, measure the pH value to be about 7.5, and continue stirring for 4 hours to obtain the AmB-PBCA-NP colloidal solution. Finally, add 1% Tween-80 and incubate in a 37°C incubator for 2 hours to obtain the nano-preparation of the present invention. After testing, the encapsulation efficiency is 56.10%, the drug loading capacity is 82%, and the average particle size is 79.9nm.

Embodiment 2

[0027] Weigh 300mg of Dextran-70, put it in a beaker, add distilled water and stir to dissolve, adjust the pH value of the solution to 3.0 with 0.01mol / L hydrochloric acid, and set the volume to 50ml. Slowly add 0.5ml of BCA under electromagnetic stirring at room temperature to a final concentration of 1%. After stirring for 4 hours, adjust the pH to 7.5 with 0.1mol / L sodium hydroxide to obtain a blank PBCA nanoparticle colloidal solution. Measure 10ml of the blank nanoparticle colloidal solution, add 20mg of amphotericin B powder injection, and measure the pH value to be about 7.5, then add 20mg of cosolvent sodium deoxycholate, and continue stirring for 4 hours to obtain the AmB-PBCA-NP colloidal solution. Finally, add 1% Tween-80 and incubate in a 37°C incubator for 2 hours to obtain the nano-preparation of the present invention. After testing, the encapsulation efficiency is 23.1%, the drug loading capacity is 25%, and the average particle diameter is 90.7nm.

Embodiment 3

[0029] Weigh 300mg of Dextran-70 and 300mg of Poloxamer 188, put them in a beaker, add distilled water and stir to dissolve, adjust the pH value of the solution to 3.0 with 0.01mol / L hydrochloric acid, and dilute to 50ml. Slowly add 0.5ml of BCA at room temperature under electromagnetic stirring to a final concentration of 1%. After stirring for 4 hours, adjust the pH to 8.5 with 0.1mol / L sodium hydroxide to obtain a blank PBCA nanoparticle colloidal solution. Measure 10ml of the blank nanoparticle colloidal solution, add 20mg of amphotericin powder injection, measure the pH value to be about 7.0, and continue stirring for 4 hours to obtain the AmB-PBCA-NP colloidal solution. Finally, add 1% Tween-80 and incubate in a 37°C incubator for 2 hours to obtain the nano-preparation of the present invention. After testing, the encapsulation efficiency is 38.4%, the drug loading capacity is 92%, and the average particle diameter is 83.4nm.

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Abstract

The present invention relates to a nano preparation of antimycotic amphotericin B (AmB). Said invention is made up by using n-butyl poly cyanoacrylate as carrier material of AmB. The animal tests show that it can permeate through blood-brain barrier, the measured medicine concentration in brain tissue is higher than that of AmB liposome preparation in clinical application, said nano preparation of antimycotic amphotericin B (AmB) is superior to AmB liposome preparation in therapeutic effect.

Description

technical field [0001] The invention relates to the technical field of medicine, and is a nano preparation of antifungal amphotericin B. Background technique [0002] Amphotericin B (AmB), a macrocyclic polyene antibiotic, is the drug of choice for the treatment of deep fungal infections. Cryptococcal meningitis is a common deep fungal infectious disease. The biggest problem with AmB treatment is that it is not easy to pass through the blood-brain barrier. Direct intrathecal injection is not only inconvenient to operate, but also has high risks and complications. More, the patient is difficult to accept. Although liposome preparations in clinical application have been proved to be able to cross the blood-brain barrier, their widespread use is limited due to their high price and uncertain actual curative effect. Contents of the invention [0003] The invention uses poly(n-butyl cyanoacrylate) (PBCA) as the Am...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/7048A61K47/10A61K47/34A61P31/10
Inventor 陈江汉温海徐楠汪晓军徐赤宇
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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