【摘要】 药物分子的结构与性质对脂质体载药性能密切相关,本工作选择水溶性抗癌药环胞苷(Ⅰ)为模型药物,对其结构进行修饰,将环胞苷与棕榈酸反应,得到单棕榈酸酯(Ⅱ)及双棕榈酸酯(Ⅲ)二种衍生物,将上述三者分别包载于脂质体中,比较其载药性能,实验表明(Ⅱ)和(Ⅲ)的HLB值降低,与(Ⅰ)相比在脂质体中由载于内水相转到脂膜相,包封率由21％上升到86.5％和93.7％,且在脂质体中稳定性也大大提高,尤其是(Ⅲ),37℃显示包封率几乎不随时间改变,从而极大改善了(Ⅰ)的包封率差稳定性低的问题。这是由于在脂质体分散系中,水相和脂相体积相差极大(约50～500倍),包封于内水相的水溶性药物有可能透过双分子膜、漏入外水相,本工作对水溶性药物进行疏水性修饰,为脂质体载药提供一理想途径。更多还原

【Abstract】 Antitumor drug Cyc-c(1),its monopalmitoyl ester( Ⅱ ) and dipalmitoyl ester (Ⅲ) were entrapped in liposomes respectively.The encapsulation percentage Ep% of ( 1 ) was only 21% and ease to leak.On the contrary, the Ep% of ( Ⅱ ) (Ⅲ) were increased to 86.5% and 93.7%.The leakage rates were dramatically decreased. Therefore, the hydrophobic modification of water soluble drug is a good way to improve drug entrapped in liposomes更多还原