Curcumenol solid lipid nano-particle and its preparation method
A technology of solid lipid nanoparticles and curcumitol, which is applied in the directions of liposome delivery, pharmaceutical formulations, and medical preparations containing active ingredients, etc., can solve problems such as solid lipid nanoparticles without physical and chemical properties, and improve bioavailability. , the effect of reducing the dosage of the drug and improving the therapeutic index
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Embodiment 1
[0050] Dissolve 10mg of curcumol and 50mg of stearic acid in 8ml of acetone, dissolve 30mg of soybean lecithin in 2ml of ethanol, and mix the two parts to form the organic phase. 100 mg of Poloxamer 188 was dissolved in 40 ml of distilled water to constitute the aqueous phase. Heat the organic phase and the water phase to 75°C respectively, and slowly inject the organic phase into the water phase with a No. 6 needle under the stirring condition of 1500 rpm to form a translucent system; evaporate the translucent system under reduced pressure with a rotary evaporator The organic solvent was removed and concentrated to 2 / 5 volume. The concentrated system was quickly mixed in the water phase at 0°C, stirred and cooled for 2 hours, and then processed by a high-pressure homogenizer at a working pressure of 800 Bar in an ice bath for 3 cycles to obtain a solid lipid nanoparticle suspension. Add 100 mg of excipient mannitol to the obtained nanoparticle suspension to dissolve, filter ...
Embodiment 2
[0053] Dissolve 10mg of curcumol, 900mg of glyceryl monostearate in 8ml of acetone, 800mg of dipalmitoylphosphatidylcholine in 2ml of ethanol, and mix the two parts to form the organic phase. 2000 mg of Poloxamer 188 was dissolved in 40 ml of distilled water to form the aqueous phase. The preparation process is the same as in Example 1, except that the high-pressure homogeneous working pressure is changed to 1000 Bar, the translucent system is concentrated to the original 1 / 2 volume, the amount of excipient trehalose added to the suspension is 2 g, and the spray-drying method is used to dry.
[0054] Detection: the average particle diameter of curcumol solid lipid nanoparticles is 216.2nm, and the encapsulation efficiency is 72.56%.
Embodiment 3
[0056] Dissolve 10mg curcumol, 100mg triolein in 8ml acetone, 100mg soybean lecithin in 2ml ethanol, and mix the two parts to form the organic phase. 200 mg of Poloxamer 188 was dissolved in 40 ml of distilled water to form the aqueous phase. The preparation process is the same as in Example 1, except that the working pressure of the high-pressure homogenization is changed to 1000 Bar, and the amount of excipient glucose added to the suspension is 300 mg.
[0057] Detection: the average particle diameter of curcumol solid lipid nanoparticles is 123.4nm, and the encapsulation efficiency is 73.64%.
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