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Methotrexate-loaded magnetosome drug carrier and preparation method thereof

A technology of methotrexate and magnetosomes, which is applied in the direction of drug combinations, pharmaceutical formulas, medical preparations of non-active ingredients, etc., can solve the problems of toxic side effects, poor water solubility, etc., and achieve high drug loading and long release cycle , anti-inflammatory and therapeutic effects on soft tissue injuries

Inactive Publication Date: 2013-03-27
HUAQIAO UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
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AI Technical Summary

Problems solved by technology

However, its water solubility is poor, and it has different degrees of toxic and side effects on the gastrointestinal tract, liver, genitourinary system, respiratory system, blood system, central system, etc.

Method used

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preparation example Construction

[0024] The present invention also relates to a preparation method of a magnetosome drug carrier loaded with methotrexate, comprising the following steps:

[0025] Step 10, dispersing the purified and freeze-dried magnetosome particles in a solvent, and then adding methotrexate solution;

[0026] Step 20, ultrasonically dispersing the mixed liquid in step 10, and fully mixing;

[0027] Step 30, add the genipin solution, and continue to disperse evenly by ultrasonic;

[0028] Step 40, putting the mixed solution in step 30 into a shaker for cross-linking, and obtaining the magnetosome drug carrier loaded with methotrexate after the cross-linking is saturated.

[0029] The magnetosomes are extracted from magnetotactic bacteria.

[0030] Preferably, the solvent in step 10 is PBS buffer or physiological saline.

[0031] Preferably, the ultrasonic dispersion in step 30 is intermittent ultrasonic dispersion.

[0032] Preferably, the step 40 specifically includes: putting the mixed...

Embodiment 1

[0035] Disperse the purified and freeze-dried magnetosome particles in a PBS solution with a pH of 7.4 to obtain a magnetosome solution with a concentration of 0.1 mg / mL; then add an equal amount of methotrexate solution and ultrasonically disperse (50W, 5min). After fully mixing, add 10mg / mL genipin solution to make the concentration of genipin in the mixture 1mg / mL, continue intermittent ultrasonic dispersion (50W, 1min each time, 5min interval), repeat 10 times, and then put the mixture Into a 37°C, 60rpm shaker for cross-linking for 24h.

[0036] Finally, the drug loading capacity of the magnetosome drug carrier loaded with methotrexate was 48.6%, the encapsulation efficiency was 94.4%, the release amount in 0.5 hours was 4.8%, there was no burst release effect, and the cumulative release was two months The rate is 82.4%.

Embodiment 2

[0038] This embodiment is basically the same as Embodiment 1, except that the concentration of genipin in the mixed solution is 0.5 mg / mL.

[0039] Finally, the drug loading capacity of the magnetosome drug carrier loaded with methotrexate was 48.0%, the encapsulation efficiency was 86.6%, the release amount in 0.5 hours was 5.4%, there was no burst release effect, and the cumulative release was two months The rate is 82.1%.

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Abstract

The invention provides a methotrexate-loaded magnetosome drug carrier and a preparation method thereof. Methotrexate is crosslinked on a biological film of a magnetosome through genipin and the magnetosome is extracted from magnetotactic bacteria. The preparation method comprises the following steps of: 10, dispersing magnetosome particles after being subjected to purifying and freeze drying in a solvent and adding a methotrexate solution; 20, ultrasonically dispersing and fully mixing the mixed liquor obtained in the step 10; 30, adding a genipin solution and continuing the ultrasonic dispersion to be uniform; and 40, putting the mixed liquor obtained in the step 30 in a shaker to carry out crosslinking and obtaining the methotrexate-loaded magnetosome drug carrier after crosslinking saturation. According to the invention, a natural magnetic targeting antitumor drug delivering system can be constructed; and meanwhile, the utilization ratio of methotrexate can be increased and the toxic and side effects of methotrexate to normal cells and tissues can be reduced. The preparation method is simple in process and convenient for operation.

Description

【Technical field】 [0001] The invention relates to the technical field of biomedical drug carriers, in particular to a magnetosome drug carrier loaded with methotrexate and a preparation method thereof. 【Background technique】 [0002] The research on drug carriers has always been one of the hot spots in the field of medicine, in which the development and use of new materials plays an important role in the research of drug carriers. [0003] Magnetosomes are natural magnetic nanoparticles synthesized in vivo by magnetotactic bacteria. As the core structure of magnetotactic bacteria, magnetosomes consist of an outer lipid bilayer and an inner mineral crystal (Fe 3 o 4 or Fe 3 S 4 ) composed of cells arranged in chains. Among them, the thickness of the lipid bimolecular membrane on the surface of the magnetosome is 2-3nm, and there is abundant phosphatidylethanolamine on the magnetosome membrane, so that the surface is electronegativity. There are a large number of protein...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/519A61P35/00
Inventor 刘源岗王士斌谢茂彬邓琼嘉陈爱政
Owner HUAQIAO UNIVERSITY
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