呋喃二烯脂质微球在小鼠体内的药动学及组织分布研究

考察了呋喃二烯(FDE)脂质微球在小鼠体内的药动学及组织分布.制备FDE脂质微球并考察其粒径、Zeta电位、含药量等指标.小鼠尾静脉给药,采用HPLC法测定血浆和组织中的FDE浓度,评价药动学及组织分布特征.结果表明FDE脂质微球各项指标均符合注射剂要求.FDE在血浆中Cmax为(33.38±5.13)μg.mL-1,脑组织可检测到Cmax为(23.35±1.20)μg.g-1,说明FDE脂质微球可透过血脑屏障,对治疗脑部肿瘤及疾病具有潜在优势.

Tissues Distribution and Pharmacokinetics of Furanodiene Lipid Microsphere in Mice

The in vivo pharmacokinetics of Furanodiene （FDE） lipid microsphere and its distribution in plasma, brain, heart, liver, lung and kidney of mice are investigated. The FDE lipid microsphere is prepared and its physi-cal properties including particle size, Zeta potential and drug loading are evaluated. After intravenous injection into mice, the tissue distribution of FDE lipid microsphere is evaluated through measuring the Cmax of FDE in various tis-sues （plasma, brain, heart, liver, lung and kidney） using HPLC. The results show that the physical properties of FDE lipid microsphere meet the requirements of injection. The Cm=of FDE is 33.38±5.13μg·mL^-1 in plasma and 23.35±1.20μg·g^-1 in brain tissues. The targeting efficiency of brain tissue is 19.67%. This suggests that FDE lipid microsphere can pass through blood-brain barrier and has potential advantages for brain tumors and dis-ease treatment.