A kind of preparation method of pH-sensitive polyion micelles and block polymers
A technology of block polymer and polyion, which can be used in medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc. , good antibacterial properties, the effect of improving bioavailability
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Embodiment 1
[0036] In this embodiment, a method for preparing a pH-sensitive block polymer is provided, and the synthesis steps are as follows:
[0037] (1) Synthesis of macromolecular initiator PEG-Br:
[0038] First, polyethylene glycol monomethyl ether PEG (Mn=2000, 2 g, 1 mmol) and triethylamine (417 μL, 3 mmol) were dissolved in 10 mL of dichloromethane, ice bathed for 15 minutes, and then 2-bromoisobutyl Acyl bromide (378 μL, 3 mmol). The mixed solution was first stirred for 2 hours under ice-bath conditions, and then reacted at room temperature for 24 hours. The reacted mixed solution was filtered to remove insoluble salts, and the filtered product was concentrated by a rotary evaporator to remove organic solvents. The obtained crude product was transferred to a small beaker, and a large amount of glacial ether was added for precipitation. Finally, the ether solvent was removed by suction filtration with a Buchner funnel, and the solid product was put into a vacuum oven for vacu...
Embodiment 2
[0055] In this example, the pH-sensitive degradation behavior of the citraconamide bond of the block polymer PEG-b-PAECOEMA / CA prepared in Example 1 was determined. The degradation rate of citraconamide bond was measured by fluorescamine method.
[0056] The block polymer PEG-b-PAECOEMA / CA was dissolved in ultrapure water to prepare a polymer solution with a concentration of 1 mg / mL. The above polymer solution was blended with pH 5.5 acetate buffer (10 mM) or pH 7.4 phosphate buffer (10 mM). The mixture was incubated at 37°C, and 50 μL of the mixture was dissolved in 3 mL of borate buffer (0.1 M) at pH 9.1 within a preset period of time, and then 50 μL of fluorescamine in DMF (0.5 mg / mL) was added. Incubate at room temperature for 10 minutes. The fluorescence intensity was measured by a fluorescence spectrophotometer (RF-6000, Shimadzu).
Embodiment 3
[0058] In the present embodiment, the preparation method of pH-sensitive polyion micelles is provided, and the steps are as follows:
[0059] The block polymer PEG-b-PAECOEMA / CA was dissolved in ultrapure water to prepare a solution with a concentration of 2 mg / mL. Then pass the polymer solution through a 220nm filter to remove possible impurities. Then, the diluted chlorhexidine gluconate solution (2 mg / mL) was slowly added dropwise into the above polymer solution using a micro-syringe pump, and stirred evenly. The resulting mixture was stirred for an additional 2.5 hours in an ice bath. A dialysis bag with a molecular weight cut-off of 1000 Da was selected, and the polyion micelles solution was dialyzed in an ice bath to remove unadsorbed antibacterial drugs. Finally, the pH-sensitive polyion micelle solution was collected.
[0060] Figure 4 It is the AFM figure of the pH-sensitive polyion micelles prepared in embodiment 3;
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