β-榄香烯脂质体的制备及其在大鼠体内的组织分布

目的:研制β-榄香烯脂质体并考察其在大鼠体内的组织分布。方法:采用薄膜分散法制备β-榄香烯脂质体,考察其形态、粒径、Zeta电位、药物含量及包封率。并以榄香烯注射液为对照,大鼠尾静脉注射给药,考察β-榄香烯脂质体在血浆及心、肝、脾、肺、肾的分布特征。结果:制备的β-榄香烯脂质体均匀圆整,粒径为(158±s 37)nm,Zeta电位为(-67±4)mV,药物含量为(5.76±0.21)g·L~(-1),包封率为(45.08±0.15)%(n=3)。大鼠尾静脉注射β-榄香烯脂质体和榄香烯注射液后,2种制剂在心、肝、脾、肾中的AUC_(0-t)均有显著差异,其中β-榄香烯脂质体在肝、脾、肾组织中分布相对较多,在心脏中分布较少。结论:薄膜分散法制备β-榄香烯脂质体方法可行,β-榄香烯脂质体在大鼠体内的分布特性有不同程度的改变,可提高疗效,降低心脏毒性。

Preparation of β-elemene liposomes and their tissue distribution in rats

AIM:To study the preparation ofβ-elemene liposomes and their tissue distribution in rats.β-elemene liposomes were prepared by film dispersion method.Its physical properties,particle size,Zeta potential,content and its entrapment efficiency were detected.The tissue distribution(plasma,heart, liver,spleen,lung and kidney)ofβ-elemene liposomes and elemene injection(control)was measured after intravenous injection in rats.RESULTS:β-elemene liposomes were spherical vesicle with particle size of(158±s 37)nm,Zeta potential of(-67±4)mV,content of(5.76±0.21)g.L~(-1),entrapment efficiency of(45.08±0.15)%(n=3).There was significant difference in the AUC_(0-t)of heart,liver,spleen and kidney in rats betweenβ-elemene liposomes and elemene injection.Compared with elemene injection,β-elemene liposomes distributed mainly in liver,spleen and kidney while less in heart after intravenous injection in rats. CONCLUSION:The preparation ofβ-elemene liposomes by film dispersion method is feasible.There is a certain degree change ofβ-elemene liposomes distributed in rats,which can improve curative effects and reduce heart toxicity.