Polymer nano-drug and preparation method thereof
A technology of nano-drugs and polymers, applied in drug combinations, pharmaceutical formulations, anti-tumor drugs, etc., can solve the problems of low drug-loading rate, side effects of carriers, disassembly and leakage of drugs, etc., achieve high drug-loading rate, reduce side effects, The effect of simple operation
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[0068] R used in the embodiment of the preparation method of the present invention o1 , the synthesis steps are as follows:
[0069]
[0070] Dissolve 2,5-dihydroxy-4-methyl-2,5-dioxo-3-furanpropionic acid (1.84g, 10.0mmol) in 2mL of thionyl chloride and react at 40°C for 12 After 1 hour, the reaction solution was cooled to room temperature, concentrated, and 5 mL of dichloromethane and 50 μL of triethylamine were added. Then 1,12-dodecanediol (2.02g, 10.0mmol) was added to the mixture, and after reacting at room temperature for 12 hours, 30mL of dichloromethane was added, and the organic phase was washed successively with saturated ammonium chloride solution and saturated brine , dried the organic phase with anhydrous sodium sulfate, removed sodium sulfate by suction filtration, and concentrated. The mixture was purified by gradient elution of column chromatography, and the eluent component was a mixture of petroleum ether and ethyl acetate. Concentration of the eluent ...
Embodiment 1
[0092] The water phase monomer is R w1 , the oil phase monomer is R o1 .
[0093]
[0094] Weigh:
[0095] Water Phase Monomer R w1 : 3.56mg
[0096] Oil Phase Monomer R o1 : 1.07mg
[0097] The aqueous phase monomer R w1 Dissolved in 2mL of pure water (concentration: 1mmol / L), the oil phase monomer R o1 Dissolved in 50 μL of dichloromethane (concentration: 40 mmol / L), after the initial mixing of the two solutions, the emulsion interfacial polymerization of the two monomers occurred at a temperature of 30 °C and an ultrasonic power of 40 W, and the reaction time was 5 min. 4.58 mg polymer nanomedicine, yield 99%. Infrared spectrum characteristic absorption peak: 1680cm -1 (vs), 1520cm -1 (s), 1250-1150cm -1 (s), 810cm -1 (m), 750cm -1 (m), its infrared spectrum is as figure 1 shown. The particle size of the polymer nanomedicine is 78nm, and its particle size distribution is shown in figure 2 As shown, the transmission electron microscope image is shown in ...
Embodiment 2
[0099] The water phase monomer is R w1 , the oil phase monomer is R o2 .
[0100]
[0101] Weigh:
[0102] Water Phase Monomer R w1 : 1.78mg
[0103] Oil Phase Monomer R o2 : 1.20mg
[0104] The aqueous phase monomer R w1 Dissolved in 1mL of pure water (concentration: 1mmol / L), the oil phase monomer R o2 Dissolved in 25μL of dichloromethane (concentration: 40mmol / L), after the initial mixing of the two solutions, the emulsion interfacial polymerization of the two monomers occurred at a temperature of 10°C and an ultrasonic power of 80W, and the reaction time was 10min. 2.97mg polymer nanomedicine, yield 99%. Infrared spectrum characteristic absorption peak: 1657cm -1 (vs), 1546cm -1 (s), 1200-1132cm -1 (s), 800cm -1 (m), 722cm -1 (m), its infrared spectrum is as Figure 5 shown. The particle size of the polymer nanomedicine is 377nm, and its particle size distribution is shown in Figure 6 shown.
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