【摘要】 采用离子对复合物方法制备三磷酸腺苷二钠(ATP-2Na)脂质体以提高包封率,并考察其对心肌缺血小鼠组织能量状态的影响。ATP-2Na与十六烷基三甲基溴化铵(hexadecyl trimethyl ammonium bromide,HTAB)形成离子对复合物后用乙醇注入法制备脂质体,测定载药脂质体的粒径、表面电位等理化参数;以ATP-2Na溶液为对照,测定给药后心肌缺血小鼠血液及各组织中ATP浓度,评价脂质体对提高心肌缺血小鼠组织能量状态的作用。结果表明,ATP-2Na脂质体的平均粒径为(144.0±2.7)nm,表面电位为(+16.2±1.6)mV,包封率为(85.02±2.31)%,体外释药遵循Weibull方程。ATP-2Na脂质体与ATP-2Na溶液相比显著地提高了心肌缺血小鼠血液中的ATP浓度;ATP-2Na脂质体与生理盐水相比显著提高了缺血心肌及肝组织中的ATP浓度,而游离ATP-2Na却无此效果。表明ATP-2Na脂质体对提高心肌缺血动物的组织能量状态有一定的应用价值。更多还原

【Abstract】 The aim of this study is to improve liposome encapsulation efficiency of water soluble drug ATP-2Na with hydrophobic ion pairing method, and evaluate its effect on tissues energy state in myocardial ischemia mice. Ion pair complex of ATP-2Na with HTAB was prepared first; then the liposomes were prepared by ethanol injection method. The size and zeta potential of ATP-2Na liposome were investigated. Its effect on tissues energy state in myocardium ischemia mice was evaluated by detecting ATP-2Na concentration in tissues and blood after injection in comparison to ATP-2Na solution. The diameters and zeta potential of ATP-2Na liposomes were (144.0 ± 2.7) nm and (+16.2 ± 1.6) mV, respectively. The encapsulation efficiency was (85.02 ± 2.31) %. The in vitro drug release pattern from liposomes matches with Weibull equation. Compared with ATP-2Na solution, ATP-2Na liposome increased the ATP concentration of blood in myocardial ischemic mice very significantly; compared with blank, ATP-2Na liposome increased ATP content of myocardium and liver in myocaridal ischemic mice significantly, but ATP-2Na solution didn’t show this effect. ATP-2Na liposome might have an advantage in improving tissue energy state on myocaridal ischemic animals.更多还原