Application of ITCNs assembling body loaded anti-tumor compound
A compound and anti-tumor technology, applied in the application field of ITCNs assembly loaded with anti-tumor compounds, can solve the problems of chemotherapy failure, tumor multidrug resistance, neglect of stromal cells and tumor cell heterogeneity, etc., to improve the therapeutic effect , good therapeutic effect
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Embodiment 1
[0041] The present embodiment provides a kind of PEG-PEI, and its structural formula is as follows:
[0042]
[0043] This example provides a preparation method of PEG-PEI: first, dissolve mPEG (MW: 2,000, 0.059g; 0.194mmol) in 5mL of dichloromethane, then add 0.038g (0.053mmol) methanesulfonic acid chloride and 0.04 g (0.21mmol) 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride, reacted at room temperature for 24h under stirring, and then dialyzed for 24-96h with a dialysis bag (MW: 1000), Preparation of methylsulfonated methoxypolyethylene glycol.
[0044] Then, dissolve methylsulfonated methoxypolyethylene glycol in 5 mL of methanol / triethyl orthoformate ratio 10 / 1 mixed solvent, then add 0.243 g of polyethyleneimine (0.0097 mmol) and stir at room temperature for 48 h . The resulting reaction solution was dialyzed for 24-96 hours using a dialysis bag (MW: 3500), and then freeze-dried to obtain a Schiff base-linked PEG-PEI copolymer.
[0045] This example prov...
Embodiment 2
[0060] The method and basic steps for the evaluation of antitumor multidrug resistance of the ITCNs assembly loaded with antitumor compounds used in this example are basically the same as those in Example 1, except that the antitumor compound loaded is docetaxel (DTX). The tumor cell line used in this example is a drug-resistant human breast cancer cell, MCF7 / MDR.
[0061] This example provides a method for preparing docetaxel-loaded ITCNs assemblies loaded with anti-tumor compounds (DTXITCNs): 10 mg of DTX, IND, and PEG-PEI are co-dissolved in 1 mL of methanol or other water-soluble organic solvents (such as dimethyl sulfoxide or dimethylformamide), mixed under stirring or ultrasonication, and the obtained mixed solution was dialyzed in an aqueous solution for 12-24 hours to obtain an aqueous solution of the assembly. Figure 9 Its transmission electron microscope picture.
[0062] The detection result of this embodiment sees Figure 10 . according to Figure 10 It can be...
Embodiment 3
[0064] The method and basic steps for evaluating the anti-tumor multidrug resistance of ITCNs self-assembled in this example are basically the same as those in Example 1, except that the loaded anti-tumor compound is doxorubicin (DOX). In this example, human melanoma cell line B16F10 drug-resistant cell line and sensitive line were used.
[0065] This embodiment provides a preparation method of ITCNs self-assembly (DOX ITCNs) loaded with doxorubicin: 10 mg of DOX, IND and PEG-PEI are co-dissolved in 1 mL of methanol or other water-soluble organic solvents (such as dimethyl methylene sulfone or dimethylformamide), mixed under stirring or ultrasonic action, and the obtained mixed solution was dialyzed in the aqueous solution for 12-24 hours to obtain an aqueous solution of the assembly. Figure 11 Its transmission electron microscope picture.
[0066] The detection result of this embodiment sees Figure 12 . according to Figure 12 It can be seen that according to the result...
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