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TPGS modified docetaxel liposome nano-drug delivery system and preparation method thereof, and application thereof

A drug delivery system, the technology of docetaxel, applied in the field of pharmaceutical preparations, can solve the problems of multiple skin and bone toxicity, neutropenia, limited application, etc., achieve excellent anti-tumor multidrug resistance, and increase solubility , the effect of reducing systemic toxic effects

Inactive Publication Date: 2019-01-18
NINGXIA MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as a cytotoxic anticancer drug, DTX has severe systemic toxicity, and patients will experience side effects such as neutropenia, peripheral neuropathy, and multiple skin and bone toxicity after taking it, which greatly limits its clinical application.

Method used

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  • TPGS modified docetaxel liposome nano-drug delivery system and preparation method thereof, and application thereof
  • TPGS modified docetaxel liposome nano-drug delivery system and preparation method thereof, and application thereof
  • TPGS modified docetaxel liposome nano-drug delivery system and preparation method thereof, and application thereof

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Experimental program
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Effect test

Embodiment 1

[0040] Embodiment 1: Preparation of DSPC-DTX-liposome nano drug delivery system by thin film dispersion method

[0041] Put DTX and DSPC at a mass ratio of 1:5~30; chol and DSPC at a mass ratio of 1:1~20 in a 50 ml round bottom flask, add sufficient chloroform / ethanol solution (appropriate volume ratio) Dissolve, and remove the organic solvent by rotary evaporation under reduced pressure under heating at 37°C in a water bath until a uniform lipid film is formed on the wall of the round-bottomed flask, and then inject 2 minN 2 , remove the residual solvent. Then add 3ml of PBS buffer solution (pH 5~8, concentration 1~20mmol / ml), stir in a water bath at 60°C for 30min~1h, ultrasonic cell pulverizer for 3min, and pass through a 0.22μm filter membrane to obtain DSPC-DTX-liposome with a particle size of 80 ~200nm, zeta is 0±30mV, encapsulation efficiency is 90.8±5.1%, drug loading is 6.0±0.1%.

Embodiment 2

[0042] Embodiment 2: Preparation of TPGS-DTX-liposome nano drug delivery system by thin film dispersion method

[0043] Put DTX and DSPC at a mass ratio of 1:5~30; TPGS and DSPC at a mass ratio of 1:8~50; chol and DSPC at a mass ratio of 1:1~20 in a 50 ml round bottom flask, add Dissolve a sufficient amount of chloroform / ethanol solution (appropriate volume ratio), and remove the organic solvent by rotary evaporation under reduced pressure under heating in a water bath at 37°C until a uniform lipid film is formed on the wall of the round-bottomed flask, and then inject 2 minN 2 , remove the residual solvent. Then add 3ml of PBS buffer solution (pH 5~8, concentration 1~20mmol / ml), stir in a water bath at 60°C for 30min~1h, ultrasonic cell pulverizer for 3min, and pass through a 0.22μm filter membrane to obtain TPGS-DTX-liposome with a particle size of 80 ~200nm, zeta is 0±30mV, encapsulation efficiency is 99.0±0.9%, drug loading is 8.4±0.01%.

Embodiment 3

[0044] Embodiment 3: Preparation of TPGS-DTX-liposome nano drug delivery system by freeze-drying method

[0045] Put DTX and DSPC at a mass ratio of 1:5~30; TPGS and DSPC at a mass ratio of 1:8~50; chol and DSPC at a mass ratio of 1:1~20 in a 50 ml round bottom flask, add Dissolve a sufficient amount of chloroform / ethanol solution (appropriate volume ratio), and remove the organic solvent by rotary evaporation under reduced pressure under heating in a water bath at 37°C until a uniform lipid film is formed on the wall of the round-bottomed flask, and then inject 2 minN 2 , remove the residual solvent. Then add 3ml of PBS buffer solution (pH 5~8, concentration 1~20mmol / ml), stir in a water bath at 60°C for 30min~1h, ultrasonic cell pulverizer for 3min, and pass through a 0.22μm filter membrane to obtain TPGS-DTX-liposome. 2% (m / V) mannitol was used as a freeze-drying agent, and then it was put into a -80°C refrigerator for 12 hours, and then it was taken out and placed in a va...

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Abstract

The invention relates to a TPGS modified docetaxel liposome nano-drug delivery system, a preparation method and an application thereof. The TPGS modified docetaxel liposome nano-drug delivery system uses phospholipid and cholesterol as membrane materials, Surfactant TPGS modified liposomes and docetaxel (DTX) as anticancer drug were prepared by membrane dispersion ethanol injection ultrasonic dispersion reverse evaporation and freeze drying. The particle size of nano-doxetaxel liposomes modified by TPGS is 80-200 nm, the zeta potential is 0+30 mV or 0-30 mV, the encapsulation efficiency is 75-99%, with a drug loading of 3-15%. The in vitro cell experiment and in vivo pharmacodynamic experiment of the TPGS modified docetaxel liposome nano-drug delivery system prepared by the invention showthat the nano-drug delivery system can inhibit P. Overexpression of gp, decrease of drug efflux, increase of drug enrichment in tumor cells, increase of cytotoxicity and apoptosis rate, increase of tumor therapeutic effect and reversal of multidrug resistance.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a TPGS-modified docetaxel liposome nano drug delivery system, a preparation method thereof, and an application in anti-tumor multi-drug resistance. Background technique [0002] Cancer is one of the diseases that cause human death. In recent years, comprehensive treatment options for cancer mainly include surgery, radiation therapy, and chemotherapy. Among them, chemotherapy plays a leading role in cancer treatment. However, chemotherapy can often cause multiple drug resistance (MDR) and severe systemic toxicity. Tumor multidrug resistance (MDR) refers to cancer cells that become resistant to one chemotherapeutic drug and are resistant to other different structures and Chemotherapy drugs with different mechanisms of action can also develop resistance. This seriously affects the efficacy of cancer treatment. The mechanism of MDR is complex, one of which is ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/69A61K47/60A61K31/337A61P35/00
CPCA61K47/60A61K47/6911A61P35/00A61K9/0019A61K31/337
Inventor 杨建宏刘强李娜侯延辉刘艳华
Owner NINGXIA MEDICAL UNIV
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