Long-circulated thermal sensitive liposome containing 7-ethyl-10-hydroxycamptothecin and preparation method thereof
A technology of hydroxycamptothecin and heat-sensitive liposomes, which is applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of large side effects and low solubility, and achieve improved therapeutic index, Increase lipophilic effect
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Embodiment 1
[0021] prescription:
[0022]
[0023] Preparation Process:
[0024] Take the prescribed amount of 7-ethyl-10-hydroxycamptothecin, soybean lecithin, distearoylphosphatidylglycerol, distearylethanolamine-polyethylene glycol 2000 copolymer, cholesterol, α-tocopherol dissolved in Water ethanol, then add a small amount of PBS solution containing octadecylamine, spin the film at 40-45 ° C, hydrate with 10 mL of pH 5.0 PBS containing 3% lactose, ultrasonicate in a water bath, and cycle through the nanomachine for 6 times, with a pore size of 0.22 μm microporous filter membrane, and then divided into vials, pre-frozen at -18°C for 24 hours, transferred to a freeze dryer for freeze-drying, and obtained.
Embodiment 2
[0026] prescription:
[0027]
[0028] Preparation Process:
[0029] Take the prescribed amount of 7-ethyl-10-hydroxycamptothecin, egg yolk lecithin, distearoylphosphatidylglycerol, distearylethanolamine-polyethylene glycol 2000 copolymer, cholesterol, α-tocopherol and place in eggplant In a shaped bottle, add an appropriate amount of mixed solution of chloroform and methanol (3:1) to dissolve, then add a small amount of PBS solution containing octadecylamine, remove the organic solvent under reduced pressure in a water bath in a rotary evaporator, add an appropriate amount of PBS (pH7. 4) - Lactose solution, 50°C, hydration with rotation for 30 minutes, degassed under reduced pressure, placed in a high-pressure homogenizer, passed through polycarbonate membranes of 200 nm, 100 nm, and 80 nm in sequence, and freeze-dried to obtain the product.
Embodiment 3
[0031] prescription:
[0032]
[0033]
[0034] Preparation Process:
[0035] Dissolve the prescription amount of 7-ethyl-10-hydroxycamptothecin, soybean lecithin for injection, vitamin E, cholesterol, dipalmitoylphosphatidylcholine in chloroform: methanol (2: 1) and pour into a pear-shaped bottle, Then add a small amount of buffer solution containing octadecylamine, and evaporate the organic solvent to dryness in a water bath at 60°C to form a dry film on the wall of the glass bottle. Rotate hydration in a shaped bottle at 40 rpm at room temperature until the dry film on the wall of the bottle is completely eluted, and hydrate the resulting coarse suspension at room temperature for 1 hour. The resulting coarse suspension was passed through a 0.8 μm microporous membrane for 1 time, a 0.45 μm microporous membrane for 3 times, a 0.22 μm microporous membrane for 3 times, and a 0.1 μm microporous membrane for 3 times to obtain the final suspension. bottle, sealed with nitr...
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