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Molecular design and preparation technique of novel multifunctional targeted nanocapsule anticancer drug

A technology of nanocapsules and anticancer drugs, which is applied in the field of design and synthesis of new multifunctional targeted nanocapsule anticancer drugs, which can solve the problems of toxicity and lack of targeting, so as to avoid toxic effects, enhance recognition and Pro-apoptotic effect, enhance the effect of TRAIL protein receptor

Inactive Publication Date: 2017-01-25
HUBEI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the combined use of paclitaxel and other chemotherapy drugs can increase the TRAIL protein receptor on the surface of non-sensitive tumor cells, it still lacks targeting and has toxicity problems

Method used

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  • Molecular design and preparation technique of novel multifunctional targeted nanocapsule anticancer drug
  • Molecular design and preparation technique of novel multifunctional targeted nanocapsule anticancer drug
  • Molecular design and preparation technique of novel multifunctional targeted nanocapsule anticancer drug

Examples

Experimental program
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Effect test

Embodiment 1

[0041] 1. Add 200 mg of F127 to 200 mL of anhydrous toluene and stir until F127 is completely dissolved to form solution A. 0.2 g of succinic anhydride was added to solution A, and solution B was formed after stirring. The solution B was heated in a boiling bath at 150°C for 5 hours, the toluene was distilled off under reduced pressure, the distillation residue was washed with dichloromethane, and then precipitated with ether, and then recrystallized with ether to obtain the product F127-COOH.

[0042] 2. Accurately weigh 180 mg of P123 and 90 mg of F127-COOH, dissolve them in 1 mL of chloroform solution by ultrasonic, add 4 mg of paclitaxel, and disperse by ultrasonic for 15 min at 100 W. The obtained mixed solution was vacuum dried at 75° C. until the chloroform was completely evaporated to obtain a nano film. Add 4 mL of deionized water to the film and disperse by 200 W ultrasonic for 12 min to obtain nanomicelles containing paclitaxel. Take 35 μL of tetramethoxysilane ultra...

Embodiment 2

[0045] First, prepare TRAIL protein-coupled drug-loaded nanocapsules according to Example 1, and then take 1 mL of the prepared drug-loaded nanocapsules, add 2 mL of acetonitrile to ultrasonically swell, use Shimadzu spectrophotometer to measure the absorbance at 229nm, and combine with paclitaxel concentration- The absorbance standard curve was used to calculate the paclitaxel content and the capsule drug loading, encapsulation efficiency and drug loading concentration. Drug loading = actual content of PTX in the drug-loaded capsule / capsule mass, encapsulation rate = actual content of PTX in the drug-loaded capsule / content of paclitaxel added in the reaction, drug loading concentration = actual PTX content of the drug-loaded capsule / Volume of capsule solution. Take 3 mL of the prepared drug-loaded nanocapsules into a dialysis bag with a molecular weight cut-off of 8000 g / mol, and place them in a PBS (pH 7.4) solution containing 0.1% Twain80 for dialysis at 0.5h, 1h, 2h, 4h, 6...

Embodiment 3

[0047] First, prepare TRAIL protein-coupled drug-loaded nanocapsules according to Example 1, and then use DMEM complete medium (containing 10% fetal calf serum, 1% penicillin-streptomycin) to culture hepatoma cell HepG2, and the culture conditions are 37°C, 5% CO 2 . After the cells have grown to the logarithmic phase, trypsinize them, collect the cells by centrifugation and resuspend them in DMEM complete medium (containing 10% fetal bovine serum, 1% penicillin-streptomycin), and inoculate 96 cells at a density of 8000 cells / well Well plate (LAB-TEK, Chambered Coverglass System), each well contains 100 μL of cell culture medium, at 37℃, 5% CO 2 Cultured for 8 h under the conditions to make the cells adhere to the wall. Add 10 μL of TRAIL drug-loaded nanocapsules of different concentrations, add 10 μL of cck-8 solution after co-cultivation for 24 hours, and use Bio-RAD microplate reader to measure the absorbance and calculate the cell survival rate after 1 hour of color reactio...

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Abstract

The invention provides a molecular design and preparation technique of a novel multifunctional targeted nanocapsule anticancer drug. The technique comprises the following steps: wrapping paclitaxel with a carboxylated block copolymer F127-COOH and P123 to form a nano micelle, and forming a silicon-dioxide-shell stable micelle structure in the micelle by using tetramethoxysilane to form drug-carrying nanocapsules; and coupling carboxyl groups on the nanocapsule surface with amino groups on the TRAIL protein surface by using a coupling agent to form the surface-TRAIL-protein-coupled drug-carrying nanocapsules. The technique has the advantages of favorable repetitiveness and mild conditions. The prepared multifunctional targeted nanocapsule anticancer drug has the advantages of high stability, wide anticancer spectrum and obvious curative effects.

Description

Technical field [0001] The invention relates to the design and synthesis technology of a new type of multifunctional targeted nanocapsule anticancer drug, in particular to an anticancer that is coupled to the surface of a nanocapsule containing paclitaxel and coupled to the tumor necrosis factor-related apoptosis-inducing ligand TRAIL protein Drug design and preparation. Background technique [0002] On a global scale, the treatment of malignant tumors is a difficult point in the field of life science research today. Chemotherapy is one of the main methods of current tumor treatment. The commonly used drugs for chemotherapy include paclitaxel (PTX), doxorubicin, daunorubicin, mitomycin, etc. However, due to the low selectivity of chemotherapy drugs, they are killing cancer At the same time, the cells will inevitably damage the normal cells of the human body. Adverse drug reactions often occur, and there are problems of toxicity, non-specificity and drug resistance. [0003] Tumor...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/60A61K47/69A61K47/10A61K47/04A61K47/42A61K31/337A61K38/17A61P35/00
CPCA61K9/5115A61K9/5146A61K9/5169A61K31/337A61K38/1761A61K2300/00
Inventor 王行国刘欣顾豪爽李岳彬
Owner HUBEI UNIV
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