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Tumor targeted mitomycin C liposome and preparation method thereof

A technology for mitomycin and tumor targeting, applied in the field of pharmaceutical antitumor drug preparations, can solve problems such as poor stability, and achieve the effects of good stability, good targeting and sustained release characteristics

Active Publication Date: 2015-06-17
XIAMEN CHITOSAN BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But this preparation also involves characteristics such as poor stability

Method used

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  • Tumor targeted mitomycin C liposome and preparation method thereof
  • Tumor targeted mitomycin C liposome and preparation method thereof

Examples

Experimental program
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Effect test

example 1

[0028] Example 1: Weigh soybean lecithin and mitomycin (molar ratio: 4:1), place them in a round-bottom beaker, add an appropriate amount of tetrahydrofuran to dissolve, react in a water bath at 40°C for 4 hours, remove the reaction solvent tetrahydrofuran under reduced pressure, and then add Wash with an appropriate amount of chloroform, filter and collect the solution, rotary steam and dry to obtain a purple viscous substance mitomycin C and lecithin complex;

[0029] Dissolve the mitomycin C and lecithin complex in chloroform, slowly add it to the water phase as the oil phase, stir to remove the organic solvent and filter with a 1 micron microporous membrane to obtain mitomycin C Liposome solution;

[0030] The prepared mitomycin C liposome solution and DSPE-PEG-FA were mixed in a water bath at 60° C. for 0.5 h. The DSPE-PEG-FA accounted for 30% of the mass of the mitomycin C and lecithin complex. %, use a 3500 molecular weight dialysis bag to remove unreacted DSPE-PEG-FA, and ...

example 2

[0031] Example 2: Weigh soybean lecithin and mitomycin (molar ratio: 3:1), place them in a round-bottomed beaker, add appropriate amount of tetrahydrofuran to dissolve, react in a water bath at 40°C for 4 hours, remove the reaction solvent tetrahydrofuran under reduced pressure, and then add Wash with an appropriate amount of dichloromethane, filter and collect the solution, rotary steam and dry to obtain a purple viscous substance, namely mitomycin C and lecithin complex;

[0032] The compound of mitomycin C and lecithin was dissolved in dichloromethane and slowly added as an oil phase to the water phase. After stirring to remove the organic solvent, it was filtered with a 1 micron microporous membrane to obtain mitomycin C. Liposome solution;

[0033] The prepared mitomycin C liposome solution and DSPE-PEG-FA were mixed in a water bath at 50° C. for 0.5 h. The DSPE-PEG-FA accounted for 10% of the mass of the mitomycin C and lecithin complex. %, use a 3500 molecular weight dialys...

example 3

[0034] Example 3: Weigh soybean lecithin and mitomycin (molar ratio: 2:1), place them in a round bottom beaker, add an appropriate amount of tetrahydrofuran to dissolve, react in a water bath at 50°C for 3 hours, remove the reaction solvent tetrahydrofuran under reduced pressure, and add Wash with an appropriate amount of dichloromethane, filter and collect the solution, rotary steam and dry to obtain a purple viscous substance mitomycin C and lecithin complex;

[0035] The compound of mitomycin C and lecithin was dissolved in dichloromethane and slowly added as an oil phase to the water phase. After stirring to remove the organic solvent, it was filtered with a 1 micron microporous membrane to obtain mitomycin C. Liposome solution;

[0036] The prepared mitomycin C liposome solution and DSPE-PEG-FA were mixed in a water bath at 50° C. for 0.5 h. The DSPE-PEG-FA accounted for 5 percent of the mass of the mitomycin C and lecithin complex. %, use a 3500 molecular weight dialysis bag...

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Abstract

The invention relates to the pharmaceutical antitumor drug preparation field, and in particular relates to a tumor targeted mitomycin C liposome for prevention of malignant tumor growth and recurrence and a preparation method thereof. The tumor targeted mitomycin C liposome includes raw material drug mitomycin C, a carrier material and a targeted molecule, and the carrier material includes lecithin and DSPE (distearoyl-phosphatidylethanolamine)-PEG (polyethylene glycol), the target molecule is folic acid, the molar ratio of mitomycin C to lecithin is 1: 1 to 4, and the total mass of the DSPE-PEG and folic acid accounts for 5-40% of the total mass of mitomycin C and lecithin. The tumor targeted mitomycin C liposome is spherical, the diameter is between 100 to 500 nm, stability is good, and the tumor targeted mitomycin C liposome has low toxicity, long-term efficiency and high efficiency what the naked drug does not have, and has higher drug loading amount and high anti tumor effect and other characteristics.

Description

Technical field [0001] The invention relates to the field of pharmaceutical anti-tumor drug preparations, in particular to a tumor-targeted mitomycin C liposome for preventing the growth and recurrence of malignant tumors and a preparation method thereof. Background technique [0002] Mitomycin C (Mitomycin C, MMC), Mr334.37, aziridine derivatives, is an anti-tumor antibiotic isolated from the culture medium of Actinomyces Streptomyces caespitosus. It is a cell cycle non-specific anti-tumor Medicine, broad anti-tumor spectrum. MMC is a blue-purple crystal or crystalline powder, which is needle-like or columnar in an ampoule, soluble in water, and its aqueous solution is unstable to acid, alkali, light and heat, and is relatively stable at pH 6-9; easily soluble In strong polar solvents such as N,N dimethylformamide (DMF) and dimethyl sulfoxide (DMSO); slightly soluble in methanol, acetone, butyl acetate; slightly soluble in benzene, carbon tetrachloride, and ether; Insoluble in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K9/19A61K31/407A61K47/34A61P35/00A61K47/24
Inventor 侯鲁蔺金燕周水帆江倩
Owner XIAMEN CHITOSAN BIO TECH