Glutaryl cholesterol and liposome thereof and application of liposome as vaccine adjuvant
A technology of glutaryl cholesterol and vaccine adjuvant, which is applied in the directions of liposome delivery, medical preparations containing inactive ingredients, and medical preparations containing active ingredients, etc. Complex production process and other issues
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Embodiment 1
[0027] Synthetic method of glutaryl cholesterol
[0028] 1. Add 300mg (3mmol) of glutaric anhydride, 290mg (0.75mmol) of cholesterol, 351mg (1.5mmol) of DMAP into a 100ml eggplant-shaped bottle, and add an appropriate amount of CH 2 Cl 2 Dissolve, reflux and stir in a water bath at 75°C for 96 hours, and filter to obtain glutaryl cholesterol.
[0029] 2. Put the above product in a clean separatory funnel, wash the above product three times with HCl, three times with saturated brine, and add dried Na 2 SO 4 Absorb water, stand still, and filter with suction.
[0030] 3. The product was washed again with dichloromethane, and the filtrates were combined, rotary evaporated, and suction filtered to obtain a purified product.
[0031] 4. Using petroleum ether: ethyl acetate: methanol (2:1:0.1) as a developing solvent and 20% ethanol-sulfuric acid as a developing reagent, the product was detected by TLC.
[0032] 5. The purified product is weighed, and the yield and purity are c...
Embodiment 2
[0035] The preparation method of glutaryl liposome:
[0036] Accurately weigh 90 mg of soybean lecithin and 30 mg of glutaryl cholesterol, put them in a 250 ml eggplant-shaped bottle, add 3 ml of absolute ethanol to dissolve lecithin and cholesterol. Rotate at 37°C water bath temperature for 1 hour to evaporate the organic solvent, so that the lipid forms a uniform film on the wall of the vessel. Add 12ml of 5% mannitol as a hydration solution, wash the membrane by rotation at room temperature, and hydrate for 30 minutes. The hydrated suspension was sonicated in a water bath for 20 minutes to obtain liposomes with an average particle size of 180-230 nm.
Embodiment 3
[0038] Referring to the preparation method of Example 2, the difference is that the organic solvent used for dissolving lecithin and cholesterol is replaced by diethyl ether, and the volume of 5% mannitol in the hydration solution is increased to 15ml. The average particle diameter of the prepared liposome is 220-260nm.
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Abstract
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