Oxidation-reduction stimulus response type nanometer medicine carrier as well as preparation method and application thereof
A nano-drug carrier and stimuli-response technology, which is applied in the direction of pharmaceutical formulations, medical preparations of non-active ingredients, emulsion delivery, etc., to achieve the effect of good application value and simple preparation process
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[0037] Example 1: Preparation of mPEG-CDP(IV)
[0038] Put mPEG(II)(M n =2000, 2.00g, 1mmol), CDP (III) (0.80g, 2mmol), DMAP (0.12g, 1mmol), added to 100ml of dichloromethane; EDC (0.40g, 2mmol) was dissolved in 30mL of dichloromethane It was added dropwise to the above system in an ice bath environment, and reacted at room temperature for 18 hours. After the reaction was completed, part of the solvent was evaporated, and the remaining liquid was added dropwise to cold ether to wash the precipitate, and repeated washing 3 After the second time, put the precipitate in a vacuum drying oven at 40°C overnight to obtain 2.11 g of the macromolecular RAFT reagent mPEG-CDP(IV) with a yield of 87%.
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[0039] Example 2: Preparation of PEG-b-PTMPM(V)
[0040] Add mPEG-CDP(IV) (0.48g, 0.2mmol), AIBN (11mg, 0.067mmol), TMPM (0.90g, 4mmol), and 5.5mL of dioxane to a 50mL single-necked round bottom flask. Pass N 2 After 30 minutes, react at 70°C for 24 hours. After the liquid obtained by the reaction is precipitated with petroleum ether, the precipitate is placed in a vacuum drying oven and dried overnight at 40°C to obtain 1.31 g of polymer PEG-b-PTMPM(V), yield 95%.
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[0041] Example 3: Preparation of PEG-b-PTMA (VI)
[0042] Add the polymer PEG-b-PTMPM(V) (1.0g, 2.92mmol containing secondary amine groups measured), Na 2 WO 4 ·2H 2 O (0.24g, 0.73mmol), EDTA (0.12g, 0.41mmol), 5mL of THF, stir at room temperature for 30min, then transfer to 60℃ oil bath, slowly add H 2 O 2 3.0 mL, reacted for 24 hours, after the liquid obtained by the reaction was precipitated with petroleum ether, the precipitate was placed in a vacuum drying cabinet and dried overnight at 40° C. to obtain 0.82 g of polymer PEG-b-PTMA (VI) with a yield of 80%.
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