A tumor-mitochondria dual-targeting polymer and its preparation method and application
A technology of polymers and mitochondria, applied in the direction of antineoplastic drugs, drug combinations, pharmaceutical formulations, etc., can solve problems such as tissue damage, and achieve good biological treatment prospects
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Embodiment 1
[0041] Example 1: Preparation of dual targeting polymer cRGD-P (DMA-co-CSMA)
[0042] (1) Synthesis of light absorber CSMA
[0043] CS-2 was prepared according to reference (J. Am. Chem. Soc. 2012, 134, 1200-1211). Weigh light absorber CS-2 (114mg, 0.203mmol), hydroxyethyl methacrylate (HEMA, 34mg, 0.261mmol), EDC·HCl (60mg, 0.314mmol), DMAP (33mg, 0.27mmol) and 3mL dry Dichloromethane in an ampoule. Freeze the ampoule bottle in liquid nitrogen, pump air with an oil pump, then seal the ampoule bottle, and stir overnight at room temperature. After the solvent was rotary evaporated, it was separated and purified by silica gel column chromatography, and eluted with dichloromethane:ethanol (V:V)=50:1 to obtain the light absorber monomer (CSMA) as a green solid (102.9g, yield: 62% ).
[0044] The reaction formula is:
[0045] (2) Synthetic polymer P(DMA-co-CSMA)
[0046] Add 147.5 mg of N,N-dimethylacrylamide, 2.67 mg of 4-cyanopentanoic acid dithiobenzoate, 0.49 mg of 2,2'...
Embodiment 2
[0049] Example 2: Preparation of targeted, photosensitive antitumor drug R848@cRGD-P(DMA-co-CSMA)
[0050] Dissolve 2 mg of cRGD-P (DMA-co-CSMA) and 0.8 mg of R848 (purchased from Anaiji) in 1.0 mL of N, N-dimethylformamide, stir magnetically at room temperature for 2 hours, and add deionized water dropwise 9mL (dropping rate is 4.5ml / h) and then continue to stir for 1 hour, then dialyze with deionized water, use a dialysis membrane with a molecular weight of 3.5KDa to remove the organic solvent, replace the deionized water every 1 hour during the 4 hours of dialysis, and dialyze Finally, nanoparticles R848@cRGD-P(DMA-co-CSMA) were obtained.
[0051] The ultraviolet absorption spectrum of the dual targeting polymer cRGD-P (DMA-co-CSMA) prepared in Example 1 and the R848@cRGD-P (DMA-co-CSMA) prepared in Example 2 is as follows figure 1 shown, from figure 1 As can be seen in , the dual targeting polymers cRGD-P(DMA-co-CSMA) and R848@cRGD-P(DMA-co-CSMA) have strong absorbance i...
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