Elemene and cabazitaxel double-targeted biomimetic liposome as well as preparation method and application thereof

A technology of cabazitaxel and elemene, which is applied in the field of elemene and cabazitaxel double-targeted bionic liposome and its preparation, can solve the problems of high toxicity targeting efficiency and the like, and improve the uptake of glioma cells rate, uniform particle size distribution, targeting efficiency and efficacy enhancement

Active Publication Date: 2021-12-10
HANGZHOU NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to overcome the problems of high toxicity and low targeting efficiency of cabazitaxel for the treatment of glioma, the present invention provides an elemene cabazitaxel dual-target To biomimetic liposomes, elemene, cabazitaxel, DSPE-PEG2000-transferrin, cell membrane protein, TPGS, etc. The BBB penetration rate of the drug and the uptake rate of glioma cells are improved, and the targeted efficacy is significantly enhanced; at the same time, the toxic side effects of cabazitaxel and the irritation of elemene are significantly reduced, the safety is significantly improved, and the effect on Side effects of normal brain cells and other tissues and organs

Method used

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  • Elemene and cabazitaxel double-targeted biomimetic liposome as well as preparation method and application thereof
  • Elemene and cabazitaxel double-targeted biomimetic liposome as well as preparation method and application thereof
  • Elemene and cabazitaxel double-targeted biomimetic liposome as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Example Embodiment

[0042] Example 1 (elemene content 0.4%, absolute ethanol 1.25%, cabazitaxel 0.04%, oil 0.5%, polyethylene glycol derivative 0.5%, phospholipid 2.5%, cholesterol 0.1%, DSPE-PEG2000-transfer iron Egg 0.05%, tumor cell membrane protein 0.025%)

[0043] An elemene-cabazitaxel double-targeted biomimetic liposome, calculated in 20 mL, comprises the following raw materials: cabazitaxel 8 mg, absolute ethanol 0.25 mL, MCT 100 mg, TPGS 100 mg, soybean lecithin 500 mg, elemene 80 mg, DSPE-PEG2000-transferrin 10mg, cholesterol 20mg, tumor cell membrane protein 5mg, glycerol 520mg, and the rest are water.

[0044] The preparation method of the above-mentioned elemene-cabazitaxel double-targeted biomimetic liposome is:

[0045] (1) Oil phase preparation: take cabazitaxel and dissolve it in absolute ethanol by ultrasonic, add MCT, TPGS, soybean lecithin, elemene, cholesterol, DSPE-PEG2000-transferrin, and dissolve in a water bath at 80°C;

[0046] (2) Preparation of water phase: dissolve gly

Example Embodiment

[0048] Example 2 (elemene content 0.15%)

[0049] The difference from Example 1 is that the amount of elemene is 30 mg.

Example Embodiment

[0050] Example 3 (elemene content 0.75%)

[0051] The difference from Example 1 is that the amount of elemene is 150 mg.

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Abstract

The invention relates to the field of tumor chemotherapy drugs, and provides an elemene and cabazitaxel double-targeted biomimetic liposome aiming at solving the problems of high toxicity and low targeting efficiency when cabazitaxel is used for treating glioma. Every 100mL of the elemene and cabazitaxel double-targeted biomimetic liposome contains 0.15-0.75g of elemene, 0.5-2.5mL of absolute ethyl alcohol, 0.015-0.07g of cabazitaxel, 0.25-1g of oil, 0.25-1g of polyethylene glycol derivatives, 1-5g of phospholipid, 0.05-0.2g of cholesterol, 0.025-0.1g of DSPE-PEG2000-transferrin, 0.005-0.025g of tumor cell membrane protein and the balance water. The two drugs have a synergistic effect, so that the BBB transmittance and the glioma cell uptake rate of the drugs are improved, and meanwhile, the toxic and side effects of cabazitaxel and the irritation of elemene are reduced. The invention further provides a preparation method and application of the liposome.

Description

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Claims

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Application Information

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Owner HANGZHOU NORMAL UNIVERSITY
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