A photoreduction degradation composition and its preparation method and application
A technology of a composition and a reducing agent, applied in the field of photoreduction and degradation composition and its preparation, can solve the problems of low drug release efficiency, inability to adjust, synergistic response, etc. Compatibility effect
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Embodiment 1
[0052] Taking Example 1 as an example, the present invention provides a photoreduction degradation composition, which includes a photosensitive o-nitrobenzene (ONB) group-modified dithiothreitol (DTT) reducing agent, and simultaneously includes two The reduction sensitive polyurethane of sulfur bond; This photoreduction degradation composition can respond to the GSH (10mM) of level in tumor cell to realize the scission of main chain in normal reductive physiological environment; And in the absence of reducing agent, this polymer can The ONB is removed under light conditions, and the reducing agent molecule DTT is generated in situ to attack the reduction-sensitive polyurethane containing disulfide bonds, thereby achieving the reductive degradation of the reduction-sensitive polyurethane.
[0053] The photoreductive degradation composition provided in Example 1 can produce the reducing agent DTT under exogenous light stimulation; since DTT is generated in situ near the disulfide...
Embodiment 2
[0061] In this example, photoreduction degradation composition 2 was prepared.
[0062] Get dithioerythritol (3.08g) dissolved in NaOH ethanol solution (40mL), ice bath cooling; dropwise add 2-(1-bromobutyl)-1,3-dinitrobenzene (13.9g) in ethanol The solution (40 mL) was naturally returned to room temperature and reacted for 6 hours, and the formed precipitate was suction-filtered, freeze-dried, and stored in the dark to obtain the modified reducing agent 2.
[0063] Dissolve modified reducing agent 2 (5 mg) and polyurethane (10 mg) containing diselenide bonds in tetrahydrofuran (1 mL), slowly add it dropwise to rapidly stirred deionized water (9 ml) at a speed of 30 s / d, dropwise After finishing, continue to stir overnight, make tetrahydrofuran volatilize completely; Then liquid is transferred to the dialysis bag that molecular weight cut off is 3500, dialyzes in deionized water 3 days, changes water once every 3 hours; Then liquid centrifugation (3500r / min ), filtered (0.45 ...
Embodiment 3
[0065] In this example, photoreduction degradation composition 3 was prepared.
[0066] Get glutathione (6.14g) dissolved in NaOH ethanol solution (40mL), ice bath cooling; dropwise add N-dodecyl-2-iodo-2-(6-nitro-3,4-methylene Dioxyphenyl)-acetamide (9.1g) in ethanol solution (40mL), naturally returned to room temperature and reacted for 6 hours, the product was concentrated, precipitated with ether, purified by column chromatography, stored in the dark, and modified Reductant 3.
[0067] Dissolve the modified reducing agent 3 (10 mg) in acetone, add it to the vial, and blow it dry with nitrogen; then add polyester-polyethylene glycol copolymer micelles (10 mL) containing disulfide bonds, and ultrasonicate for 4 hours; then The liquid was transferred to a dialysis bag with a molecular weight cut-off of 3500, dialyzed in deionized water for 3 days, and the water was changed every 3 hours; then the liquid was centrifuged (3500r / min), filtered (0.45μm), and constant volume to o...
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