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Carbataxel-elemene composite liposome and preparation method and application thereof

A technology of cabazitaxel and elemene, which is applied in the field of cabazitaxel-elemene composition complex liposome and its preparation, can solve the problems such as the performance to be improved, the scope of application is small, the curative effect is limited, etc. drug, easy for clinical use, low affinity effect

Active Publication Date: 2019-01-25
HANGZHOU NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] It is disclosed in the prior art that both cabazitaxel and elemene have certain anticancer effects, but their curative effects on tumors alone are limited, and there are certain toxic and side effects, especially for drug-resistant tumors. , so its scope of application is small, and its performance needs to be improved.

Method used

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  • Carbataxel-elemene composite liposome and preparation method and application thereof
  • Carbataxel-elemene composite liposome and preparation method and application thereof
  • Carbataxel-elemene composite liposome and preparation method and application thereof

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Experimental program
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Effect test

Embodiment 1

[0041] (1) Test preparation:

[0042] Cultivation of test cell lines

[0043] Take the frozen cells out of the liquid nitrogen tank for recovery, digest the cells, count them, dilute them with medium to form a suspension, and place them at 37°C, 5% CO 2 cultured in an incubator.

[0044] Preparation of drug mother solution

[0045] The raw material drug of cabazitaxel and the raw material drug of elemene are dissolved in DMSO respectively, and then an appropriate volume is taken and diluted with medium to form mixtures of different proportions.

[0046] (2) Test process

[0047] Cells were digested and counted to prepare tumor cell suspension MCF-7, MCF-7 / T (paclitaxel-resistant MCF-7 cells), A549, A549 / T (paclitaxel-resistant A549 cells), HCT-8, For HCT-8 / T (paclitaxel-resistant HCT-8 cells), MGC-803, PC-3, add 100 μl of cell suspension to each well of a 96-well cell culture plate;

[0048] Place the 96-well cell culture plate at 37°C, 5% CO 2 Cultivate in the incubat...

Embodiment 2

[0056] (1) Preparation of organic phase: Weigh 40 mg of cabazitaxel, add 2 ml of absolute ethanol, heat to dissolve at 60°C, then add 0.5 g of PEG-DSPE (2000), 50 mg of cholesterol, 2.5 g of soybean lecithin, 500 mg of elemene, 70 °C melting.

[0057] (2) Heat 2.25g of glycerin and 95g of water in a water bath at 60°C to obtain the water phase; then add the organic phase to the water phase, shear at 12,000r / min for 1 hour, and homogenize at 600bar for 5 minutes under high pressure, and finally divide and pack to obtain the complex lipid plastid.

[0058] The average particle diameter of the composite liposomes detected by particle size analyzer is 57 ± 8.9nm, D90 is 69nm, see the specific particle size diagram figure 1 shown.

Embodiment 3

[0060] (1) Preparation of organic phase: Weigh 40 mg of cabazitaxel, add 1 ml of absolute ethanol, heat to dissolve at 60°C, then add 0.5 g of PEG-DSPE (2000), 50 mg of cholesterol, 2.5 g of soybean lecithin, and 500 mg of β-elemene , 80 ° C melting.

[0061] (2) Heat 2.25g of glycerin and 95g of water in a water bath at 60°C to obtain the water phase, then add the organic phase to the water phase, shear at 12,000r / min for 1 hour, homogenize at 600bar for 5 minutes under high pressure, and finally divide and pack to obtain the compound Liposomes.

[0062] The average particle diameter of the composite liposomes detected by particle size analyzer is 55 ± 8.5nm, D90 is 67nm, see the specific particle size diagram figure 2 shown.

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Abstract

The invention discloses a capartasol-elemene composite liposome, preparation method and application thereof, and carbataxel-elemene composite liposome is prepared by dissolving carbataxel in absoluteethanol, adding polyethylene glycol derivative, cholesterol, phospholipid and elemene, and heating to 70-90 DEG C to melt to obtain organic phase; glycerol and water are mixed and heat preserve at 50-70 DEG C to obtain an aqueous phase; adding an organic phase into an aqueous phase, and homogenizing under high pressure after high-speed shearing to obtain the composite liposome; the mass ratio of carbataxel to elemene is 1:10-150. The obtained composite liposomes have small particle size and uniform particle size distribution, and can be used for the preparation and treatment of taxane-resistant tumors, which significantly improves the anti-drug resistance effect and curative effect to a variety of tumors, reduces the toxic and side effects of drugs, greatly alleviates the pain of tumor patients, and is very convenient for clinical use.

Description

technical field [0001] The invention relates to a composite liposome for improving the anti-drug resistance and curative effect of antitumor drugs, in particular to a composite liposome composed of cabazitaxel-elemene and its preparation method and application. Background technique [0002] The progression of many life-threatening diseases such as cancer is influenced by multiple mechanisms. Because of this complexity, success with single drug therapy has been limited. Therefore, drug combinations are often used to fight cancer and enhance the efficacy. For example, Yang Lei et al. found that the rare saponin component of ginseng-paclitaxel multi-component system inhibits the proliferation and growth of lung cancer A549 cells by promoting paclitaxel-induced apoptosis, reduces the dosage of paclitaxel, reduces the toxicity of paclitaxel, and enhances the anti-lung cancer effect. Effect (Yang Lei et al., Experimental study on the treatment of A549 lung cancer with ginseng ra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K47/24A61K47/28A61K47/22A61K31/337A61K31/015A61P35/00
CPCA61K9/1271A61K31/015A61K31/337A61K47/22A61K47/24A61K47/28A61P35/00A61K2300/00
Inventor 谢恬曾昭武曾义英曾义军张娜娜李晨曦
Owner HANGZHOU NORMAL UNIVERSITY
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