Nano-particle containing docetaxel and vitamin E TPGS (d-alpha tocopheryl polyethylene glycol 1000 succinate) and preparation method thereof
A technology of docetaxel and nanoparticles, which is applied in the field of nanoparticles containing docetaxel and vitamin E TPGS and its preparation, which can solve the problems that the preparation method needs to be improved, and achieve good chemical and physical stability and production cost Low, high ability effect
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[0077] 1. In the method of the present invention for preparing nanoparticles containing docetaxel and vitamin E TPGS, the vitamin E TPGS used can be used not only as an emulsifier, but also to exert a synergistic antitumor effect with docetaxel.
[0078] 2. The method for preparing nanoparticles containing docetaxel and vitamin E TPGS of the present invention uses ethanol, propanol, butanol, isopropanol and tert-butanol as organic solvents that are miscible with water and substantially non-toxic. These substances can be easily removed during freeze-drying, which increases the stability and safety of the nanoparticles containing docetaxel and vitamin E TPGS of the present invention; The preparation process also does not need to remove the organic phase by rotary evaporation and other processes, which greatly reduces the cost and is beneficial to industrial production.
[0079] 3. The prepared nano-particles containing docetaxel and vitamin E TPGS have a good shape, the average ...
Embodiment 1
[0084] Example 1. Preparation of docetaxel and TPGS synergistic anti-tumor albumin nanoparticles with isopropanol as the organic phase
[0085] Weigh 80 mg of multilineage paclitaxel and dissolve it in 30 ml of isopropanol as the organic phase, weigh 600 mg of human serum albumin, 80 mg of TPGS (polyethylene glycol number average molecular weight M n 1000), 200mg mannitol and 60mg sodium acetate were dissolved in 80ml double distilled water, stirred and dissolved as the water phase. Under the condition of high-speed mechanical stirring (2000rpm), the organic phase was slowly added to the water phase, and after stirring for a period of time, it was filtered and sterilized through a 0.22 μm microporous membrane filter. Freeze at -80°C and freeze-dry at -50°C to remove isopropanol and water to obtain a freeze-dried powder with good shape (particle size about 80 nm). The obtained powder can be easily reconstituted into a dispersion before freeze-drying with physiological saline, ...
Embodiment 2
[0086] Example 2. Preparation of docetaxel and TPGS synergistic anti-tumor albumin nanoparticles with isopropanol as the organic phase
[0087] Weigh 80 mg of multilineage paclitaxel dissolved in 30 ml of isopropanol as the organic phase, weigh 1000 mg of human serum albumin, 100 mg of TPGS (polyethylene glycol number average molecular weight M n 1000), 280mg mannitol and 65mg potassium acetate were dissolved in 100ml double distilled water, stirred and dissolved as the water phase. Under the condition of high-speed mechanical stirring (2000rpm), slowly add the organic phase to the water phase, and after stirring for a period of time, filter and sterilize through a 0.22 μm microporous membrane filter. Freeze at -80°C and freeze-dry at -50°C to remove isopropanol and water to obtain a freeze-dried powder with good shape (particle size about 80 nm). The obtained powder can be easily reconstituted into a dispersion before freeze-drying with physiological saline, and its particle...
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