A kind of ursolic acid polymer drug-loaded nanoparticles and its preparation method and application
A technology of drug-loaded nanoparticles and ursolic acid, which is applied in pharmaceutical formulations, drug combinations, anti-tumor drugs, etc., can solve the problems of poor biosafety, poor drug targeting, and wide particle size distribution of drug-loaded nanoparticles. The effect of simple method, controllable delivery, good biocompatibility, and degradability
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Embodiment 1
[0065] The synthesis of embodiment 1 PUA
[0066] 1, the following examples use the catalysis of pyridine and thionyl chloride to make polyursolic acid (PUA) through ursolic esterification condensation, comprising the following steps:
[0067] (1) In a well-ventilated environment, add 10 mL of anhydrous pyridine to a clean and dry 25 mL round bottom flask, and stir in an ice bath for 5 min;
[0068] (2) Add 200 μL (2.76 mmol) of thionyl chloride so that the volume ratio of anhydrous pyridine to thionyl chloride is 10:0.2, and stir in an ice bath for 15 minutes;
[0069] (3) Add 0.42g (0.92mmol) UA, so that the molar ratio of thionyl chloride to ursolic acid is 3:1, and the reaction solution is stirred and reacted at room temperature for 1h. After washing and filtering, repeat 3 times to obtain a white filter cake, and freeze-dry to obtain the desired product PUA, 0.35 g (yield: 83.3%).
[0070] The reaction formula of PUA is as follows (n=10):
[0071]
[0072] 2. Result...
Embodiment 2
[0074] The synthesis of embodiment 2 PUA
[0075] Other conditions are identical with embodiment 1, only difference is: control the volume ratio of anhydrous pyridine and thionyl chloride to be 10:0.1, the molar ratio of thionyl chloride to ursolic acid is 1.2:1, and reaction solution is in Stirring and reacting at room temperature for 0.55h, polyursolic acid was successfully prepared.
Embodiment 3
[0076] The synthesis of embodiment 3 PUA
[0077] Other conditions are identical with embodiment 1, only difference is: control the volume ratio of anhydrous pyridine and thionyl chloride to be 10:0.3, the molar ratio of thionyl chloride to ursolic acid is 4.8:1, and reaction solution is in The reaction was stirred for 6 hours at room temperature, and polyursolic acid was successfully prepared.
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