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Double-drug co-loaded liposome containing erianin and doxorubicin as well as preparation and application of double-drug co-loaded liposome

A technology of erianin and doxorubicin, which is applied in the field of medicine, can solve the problems of unfavorable large-scale commercial production, uncertain synergistic effect, unfavorable absorption and utilization, etc., to improve the targeting of cancer cells and reduce the amount of natural extracts As well as the total drug dosage and the effect of reducing biological safety hazards

Active Publication Date: 2021-04-09
ZHEJIANG UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Erianin has the following problems: the solubility in the water phase is low, which is not conducive to the absorption and utilization in the body; compared with synthetic chemotherapy drugs, the extraction cost is higher, which is not conducive to large-scale commercial production
However, the two liposomal drugs are limited to conventional chemotherapy drugs that have been clinically used, and it is not sure whether they have synergistic effects

Method used

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  • Double-drug co-loaded liposome containing erianin and doxorubicin as well as preparation and application of double-drug co-loaded liposome
  • Double-drug co-loaded liposome containing erianin and doxorubicin as well as preparation and application of double-drug co-loaded liposome
  • Double-drug co-loaded liposome containing erianin and doxorubicin as well as preparation and application of double-drug co-loaded liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] In vitro cytotoxicity test to screen the optimal ratio of erianin (ER) and doxorubicin hydrochloride (DOX) synergistic effect;

[0083] (1) Use trypsin to digest the cells in the logarithmic growth phase, and dilute the cells to 5*10 with DMEM medium 3 cells / ml, inoculate 100 μl of cell suspension into each well of a 96-well plate after pipetting evenly, and culture overnight;

[0084] (2) After the cells adhere to the wall, discard the old medium in step 1, add 100 μl of DMEM medium containing two drugs at different concentrations to each well, set 3 parallel wells for each concentration, and add blank medium to the control well, Cultivate for 48 hours;

[0085] (3) Discard the cell culture medium in step 2, add 100 μl of DMEM medium containing 10% CCK-8 reagent to each well, and incubate in the incubator for 2 hours;

[0086] (4) Use a microplate reader to detect the absorbance of the 96-well plate in step 3, and the test wavelength is 450nm;

[0087] (5) Calculate...

Embodiment 2

[0096] Preparation of dual drug-loaded liposomes;

[0097] (1) Weigh 132mg of folic acid, 184.16mg of NHS, 268.38mg of EDC·HCl, dissolve in 30ml DMSO and activate in the dark for 4h; weigh 150mg of chitosan and add it to 30ml of 1% acetic acid solution and stir until dissolved;

[0098] (2) Add the folic acid solution in step 1 dropwise to the chitosan solution, and after stirring for 16 hours in the dark, adjust the pH to 9 with 0.1mol / L NaOH solution;

[0099] (3) Transfer the solution in step 2 to a dialysis bag with a molecular weight cut-off of 1 kDA, and dialyze for 2 days using a PBS solution of pH 7.2 and distilled water respectively; after the solution is centrifuged, freeze-dried and precipitated to obtain a folic acid-chitosan cross-linked product;

[0100] (4) Weighing 189.5mg lecithin, 28.95mg cholesterol, and 1.04mg erianin were dissolved in a mixed solvent of 4ml chloroform and 4ml absolute ethanol to obtain an organic phase;

[0101] (5) Remove the organic sol...

Embodiment 3

[0105] (1) Weigh 176mg of folic acid, 230.2mg of NHS, 383.4mg of EDC·HCl, dissolve in 30ml DMSO and activate in the dark for 4h; weigh 300mg of chitosan and add it to 30ml of 1% acetic acid solution and stir until dissolved;

[0106] (2) Add the folic acid solution in step 1 dropwise to the chitosan solution, and after stirring for 16 hours in the dark, adjust the pH to 9 with 0.1mol / L NaOH solution;

[0107] (3) Transfer the solution in step 2 to a dialysis bag with a molecular weight cut-off of 2 kDA, and dialyze for 2 days using a PBS solution of pH 7.4 and distilled water respectively; after the solution is centrifuged, freeze-dried and precipitated to obtain a folic acid-chitosan cross-linked product;

[0108] (4) Weighing 94.75mg of lecithin, 19.3mg of cholesterol, 0.26mg of Erianin dissolved in a mixed solvent of 6ml of chloroform and 2ml of absolute ethanol to obtain an organic phase;

[0109] (5) Remove the organic solvent by vacuum rotary evaporation of the solution ...

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Abstract

The invention discloses a double-drug co-loaded liposome containing erianin and doxorubicin as well as preparation and application of the double-drug co-loaded liposome. The double-drug co-loaded liposome containing erianin and doxorubicin is composed of a liposome loaded with erianin and doxorubicin hydrochloride and a folic acid-chitosan cross-linked polymer modified outer layer. The invention provides the application of the double-drug co-loaded liposome containing erianin and doxorubicin in preparation of anti-cancer drugs. The two drugs are loaded on the same carrier to be delivered, the cancer cell inhibiting capacity can be enhanced, the application cost is reduced, and the toxic effect on normal cells is weak.

Description

[0001] (1) Technical field [0002] The invention relates to the field of medicaments, and relates to a liposome containing dendrobium extract erianin-doxorubicin double-drug co-loading and a preparation method and application thereof. [0003] (2) Technical background [0004] Cancer is a disease that seriously endangers human health. With the development of modern society, it has become one of the main causes of human death. Among them, breast cancer is a malignant tumor originating from the epithelium of the mammary duct or acinar epithelium. There are more than 1.5 million new cases of breast cancer every year in the world, and the incidence rate ranks first among female malignant tumors. In the past few decades, a variety of cancer treatment methods have emerged, among which surgery, radiation therapy, and chemotherapy have become the main means. Chemotherapy refers to the use of chemical drugs to treat cancer, which is the most variable and fastest-growing field in cance...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61K47/69A61K47/61A61P35/00A61K31/09
CPCA61K31/09A61K31/704A61K47/6911A61K47/61A61P35/00A61K2300/00
Inventor 邵平谢华凌徐靖孙培龙
Owner ZHEJIANG UNIV OF TECH
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