Compound and application thereof
A compound and drug compound technology, which is applied in the direction of drug combination, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of multi-drug resistance and toxicity, and achieve multi-drug resistance Effects of improving and promoting cell apoptosis and good application prospects
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Embodiment 1
[0041] Weigh 0.15mmol of cholic acid and dissolve in N,N-dimethylformamide, 0.1mmol of 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide and 0.1mmol of 1-hydroxybenzotriazole Dissolve in dichloromethane respectively, mix the three, stir for 1 hour, then dissolve 0.1mmol methoxypolyethylene glycol amine in dichloromethane, add dropwise to the above reaction solution, continue to react for 24 hours, add excess The product was precipitated with glacial diethyl ether, vacuum-dried overnight after suction filtration. Dissolved in pure water, dialyzed for 24 hours, and freeze-dried to obtain the cholic acid-polyethylene glycol material. The yield was 83.5%.
Embodiment 2
[0043] Weigh 24mg of cholic acid-polyethylene glycol, 56mg of vitamin E polyethylene glycol succinate, and 4mg of paclitaxel, mix and dissolve in dichloromethane, and evaporate the organic solvent at 45°C to form a film on the bottle wall. Add 5 mL of pure water to hydrate by rotating at 35°C, sonicate for 15 min with an ultrasonic cell disruptor at 200 W, and pass through the membrane to obtain paclitaxel micelles. The measured particle size is 281.62±2.66nm, PDI is 0.069±0.018, and zeta potential is -2.59±0.197mV. The encapsulation efficiency and drug loading were 28.78±0.049% and 1.42±0.025%, respectively.
Embodiment 3
[0045] Weigh 40mg of cholic acid-polyethylene glycol, 40mg of vitamin E polyethylene glycol succinate, and 4mg of paclitaxel, mix and dissolve in dichloromethane, and evaporate the organic solvent at 45°C to form a film on the bottle wall. Add 5 mL of pure water to hydrate by rotating at 35°C, sonicate for 15 min with an ultrasonic cell disruptor at 200 W, and pass through the membrane to obtain paclitaxel micelles. The measured particle size is 169.07±7.31nm, PDI is 0.163±0.04, and zeta potential is -0.787±0.555mV. The encapsulation efficiency and drug loading were 76.35±1.76% and 3.68±0.081%, respectively.
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