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Method for preparing rapamycin/magnetic carboxymethyl chitosan nano drug-loaded microspheres

A technology of carboxymethyl chitosan and rapamycin is applied in the application field of biofunctional materials in the field of biomedicine, which can solve the problem of inability to solve normal tissue damage, failure to achieve optimal therapeutic effects, and drug-loaded microspheres. problems such as poor targeting, to achieve the effect of strengthening the effect of targeted therapy, low toxicity administration, and high drug loading

Inactive Publication Date: 2013-03-13
GUILIN UNIV OF ELECTRONIC TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The average particle size of the microspheres is 3.4±1.65μm, and the drug encapsulation rate reaches 73.95±5.43%, which preliminarily solves the problems of low water solubility of rapamycin and burst release of rapamycin, but there are still some deficiencies : For example, the prepared rapamycin drug-loaded particles are relatively large, on the one hand, it hinders the circulation of the drug in the blood vessel, and on the other hand, it is easy to cause the drug-loaded microspheres to be swallowed by the reticuloendothelial tissue, and the therapeutic effect cannot be achieved; Poor targeting of the ball, the drug cannot be accurately delivered to the lesion, and the damage to the normal tissue cannot be solved, and the best therapeutic effect cannot be achieved

Method used

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  • Method for preparing rapamycin/magnetic carboxymethyl chitosan nano drug-loaded microspheres
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  • Method for preparing rapamycin/magnetic carboxymethyl chitosan nano drug-loaded microspheres

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Experimental program
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Effect test

Embodiment 1

[0044] (1) Accurately weigh 0.4g of carboxymethyl chitosan (CMCS) and dissolve in 20ml of deionized water, stir to dissolve and filter, then add 0.4g of Fe 3 o 4 Nanoparticles, ultrasonic 5min to make them evenly dispersed; add 60ml of liquid paraffin oil (containing 1.8ml span-80) into a 250ml three-neck bottle, slowly add carboxymethyl chitosan solution drop by drop into the liquid paraffin oil while stirring , the mixture was sonicated for 30 minutes, fully stirred at 500 rpm for two hours, slowly added dropwise with 2ml of 25% glutaraldehyde solution, and stirred at 500 rpm for 2 hours. For magnetic separation, first wash thoroughly with petroleum ether for 2-3 times, then continue to wash with acetone for 3 times, so as to obtain clean nanoparticles, and dry them in a vacuum oven at 60°C for 12 hours to obtain Fe 3 o 4 / CMCS nanoparticles, spare.

[0045] (2) Accurately weigh 100mg of Fe 3 o 4 / CMCS nanoparticles, dispersed in 14ml of ultrapure water; weigh 11.9mg of r...

Embodiment 2

[0047] Accurately weigh the Fe prepared by 100mg embodiment 1 3 o 4 / CMCS nanoparticles were dispersed in 15ml of ultrapure water; 10mg of rapamycin (Rapa) was weighed and dissolved in 1ml of acetonitrile. Then the Rapa solution was slowly added dropwise to the Fe 3 o 4 / CMCS nanoparticle dispersion, stirred overnight with a magnetic stir bar at 600 rpm. First wash with ultrapure water, then magnetically separate; repeat the steps of ultrapure water washing and magnetic separation for 3 times, dry in vacuum freeze-drying equipment for 15 hours, and pulverize to obtain Fe 3 o 4 / CMCS-Rapa nanoparticles. Produced Fe 3 o 4 / CMCS-Rapa nanoparticles have a uniform particle size distribution, and the drug-loaded nanoparticles are regular spherical. The average encapsulation efficiency is 52.53%, and the drug-loading capacity is 5.2%.

Embodiment 3

[0049] Accurately weigh the Fe prepared by 100mg embodiment 1 3 o 4 / CMCS nanoparticles were dispersed in 15ml of ultrapure water; 12.5mg of rapamycin (Rapa) was weighed and dissolved in 1ml of acetonitrile. Then the Rapa solution was slowly added dropwise to the Fe 3 o 4 / CMCS nanoparticle dispersion, stirred overnight with a magnetic stirrer at 1500 rpm. Wash with ultrapure water first, and then magnetically separate; repeat the steps of ultrapure water washing and magnetic separation 5 times, freeze-dry for 12 hours, and grind to obtain Fe 3 o 4 / CMCS-Rapa nanoparticles. Produced Fe 3 o 4 / CMCS-Rapa nanoparticles have a uniform size distribution, and the drug-loaded nanoparticles are regular spherical. The average encapsulation efficiency is 46.36%, and the drug-loading capacity is 6.32%.

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Abstract

The invention relates to a method for preparing rapamycin / magnetic carboxymethyl chitosan nano drug-loaded microspheres. According to the method, synthesized Fe3O4 nanoparticles are added to liquid paraffin oil, the liquid paraffin oil is then mixed with carboxymethyl chitosan liquid, a crosslinking agent is added, nanospheres are collected through magnetic separation, and magnetic carboxymethyl chitosan nanospheres are obtained through washing and drying; aqueous dispersion liquid is prepared by using the obtained magnetic carboxymethyl chitosan nanospheres, rapamycin is dissolved in acetonitrile, and stirring is carried out so as to mix the rapamycin and the acetonitrile; and magnetic separation is carried out, a lower layer of precipitate is washed by using ultrapure water, and the rapamycin / magnetic carboxymethyl chitosan nano drug-loaded microspheres are obtained through freeze-drying and crushing. The nano drug-loaded microspheres prepared by the method have the characteristics of strong targeting, high drug loading capacity, good slow release performance, small particle size, low drug toxic and side effect and the like, and the tumor cell killing rate of rapamycin drugs can be remarkably increased; and the method is simple in process, mild in preparation conditions and easy in scale production.

Description

technical field [0001] The invention relates to the application of a biofunctional material in the field of biomedicine, in particular to a method for preparing nano drug microspheres by using magnetic carboxymethyl chitosan to fix rapamycin. Background technique [0002] Rapamycin (RAPA) is a new macrolide immunosuppressant isolated from the fermentation broth of Streptomyces hygroscopicus. It not only has anti-transplant immune rejection, but also has a strong inhibitory effect on prostate cancer, kidney cancer, breast cancer, colon cancer and liver cancer. RAPA can regulate gene expression by inhibiting the protein kinase catalytic activity of mammalian target of rapamycin (mTOR) and the phosphoinositide-3 kinase (PI3 K) / Akt signal transduction pathway , cell growth and proliferation, by blocking different cytokine receptor signal transduction, to block the progress of T lymphocytes and other cells from G1 phase to S phase, thereby exerting its immunosuppressive effect. ...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/436A61K47/36A61K47/04A61P37/06A61P35/00
Inventor 李桂银周治德黄勇操良丽陈真诚
Owner GUILIN UNIV OF ELECTRONIC TECH
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