Imidazole ring modified acid-sensitive polycarbonate material as well as preparation and application thereof
A polycarbonate, acid-sensitive technology, applied in the field of polycarbonate materials and its preparation and its application as a drug carrier in drug delivery, can solve the problems of increasing toxic and side effects, and achieve simple preparation, good stability, good Antitumor Prospect Effect
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Embodiment 1
[0041] m PEG-PCC-Im preparation.
[0042] (a) Monomer preparation: 45.0g (0.338mol) 2,2-dimethylolpropionic acid (I), equimolar mass KOH (88%, 21.5g, 0.338mol) was dissolved in a 500ml eggplant-shaped bottle of DMF250ml , reacted at 100°C for 2h, and stirred vigorously until all the crystals were dissolved. 46ml (0.404mol) of excess benzyl chloride was slowly added dropwise to the eggplant-shaped flask with stirring. It was refluxed and stirred at 100°C for 18 hours. After filtration, distill out DMF from the filtrate under reduced pressure at 70-100°C. Dissolve the product with 600ml of organic phase (n-hexane-ethyl acetate 1:1) and 200ml of aqueous phase, and separate the layers. Keep the upper organic phase and wash it twice with 200ml distilled water. Pour the organic phase into a beaker filled with a large amount of anhydrous sodium sulfate and stir for 1 h to remove residual water. filter. The filtrate was rotary evaporated to obtain a yellow solid. Heat an approp...
Embodiment 2
[0052] 2.1 Preparation of drug-loaded micelles:
[0053] Medicine (docetaxel) and the carrier (mPEG) prepared in embodiment 1 113 -PCC 32 -Im) (1:4, w / w) the carrier is dissolved in dichloromethane at the same time, drop into the water phase and stir (500rpm) for 5min, probe ultrasonic (400W, 3min) under ice bath, stir at 500rpm for 12h to remove the organic solvent .
[0054] 2.2 Screening of drug to carrier ratio (weight ratio):
[0055] Table 1. Comparison of micellar properties for different drug to carrier ratios
[0056]
[0057] The results showed that: when the ratio of drug to carrier was 1:1-1:4, the drug loading capacity and encapsulation efficiency were increased, and when the ratio of drug to carrier was 1:3-1:4, the The drug dosage can reach more than 80%, and the encapsulation rate can reach more than 15%.
[0058] 2.3 Screening of the ratio (v / v) of organic phase (dichloromethane) to aqueous phase:
[0059] Control other conditions unchanged, prepare d...
Embodiment 3
[0093] Determination of critical micelle concentration of mPEG-PCC-Im polymer:
[0094]The determination of critical micelle concentration widely adopts pyrene fluorescent probe method. Pyrene is a fat-soluble fluorescent probe with weak fluorescence in polar environment and strong fluorescence in nonpolar environment. When there are micelles or hydrophobic regions in the polar solvent, pyrene will spontaneously transfer from the polar environment to the non-polar environment, resulting in enhanced fluorescence. Usually, this characteristic of pyrene is reflected by the ratio of the intensity of the first excitation peak to the third excitation peak. When this ratio increases significantly, it means that pyrene migrates from a polar environment to a non-polar environment, that is, micelles or hydrophobic region generated.
[0095] will be 6×10 -6 The mol / L pyrene solution in absolute ethanol was added to a 20mL stoppered flask, and the absolute ethanol was removed by drying...
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