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目的 研究普通纳米脂质体、柔性纳米脂质体及胆酸钠 磷脂混合胶团对环孢素经小鼠皮肤给药的渗透机理。方法 将含药载体非封闭性应用于离体或在体小鼠皮肤 ,测定了皮肤、接收介质和血液中环孢素含量。结果离体条件下 ,应用柔性纳米脂质体和混和胶团后均能在接收液中检测到药物 ,但普通脂质体却不能。在体条件下 ,应用柔性纳米脂质体后 8h血药浓度到达峰值 ,而应用普通脂质体和混合胶团后在血中几乎未检测到药物。结论柔性纳米脂质体在皮肤水合压力下发生变形 ,携药透过皮肤 ;普通脂质体主要与皮肤发生融合产生蓄积作用 ;混合胶团在水溶液状态下发挥其渗透促进作用。
Objective To study the infiltration mechanism of cyclosporine administered to the skin of mice by ordinary nano-liposomes, flexible nano-liposomes and sodium cholate phospholipid micelles. Methods The non-blocking drug-containing carrier was applied to the skin of mice in vitro or in vivo, and the contents of cyclosporine in the skin, receiving medium and blood were measured. Results Under ex vivo conditions, the drug could be detected in the receiving solution after using flexible nanoliposomes and mixed micelles, but the ordinary liposomes could not. Under body conditions, the peak plasma concentration reached its peak at 8h after application of flexible nanoliposomes, whereas almost no drug was detected in the blood after application of the common liposomes and mixed micelles. CONCLUSION: The flexible nano-liposomes deform under the hydration pressure of the skin and carry the drug through the skin. The common liposomes have the effect of accumulating with the skin, and the mixed micelles exert their permeation promoting effect under the condition of the aqueous solution.