ABSORPTION AND TISSUE DISTRIBUTION OF DOXORUBICIN ENTRAPPED IN LIPOSOMES FOLLOWING INTRAVENOUS OR INTRAPERITONEAL ADMINISTRATION
ABSORPTION AND TISSUE DISTRIBUTION OF DOXORUBICIN ENTRAPPED IN LIPOSOMES FOLLOWING INTRAVENOUS OR INTRAPERITONEAL ADMINISTRATION
复制标题
DOI：
10.1159/000137805
复制
发表时间：
1983-01-01
期刊：
影响因子：
3.1
通讯作者：
CLEMENTI, F
中科院分区：
文献类型：
--
作者：
ROSA, P;CLEMENTI, F
研究了C57/B1/6小鼠经静脉或腹腔注射后，游离阿霉素（Dxn）和脂质体内包裹的阿霉素（Dxn）的吸收和组织分布。脂质体包封Dxn改变了其血浆动力学和组织分布。经静脉给药后，脂质体中的Dxn的半衰期比游离的Dxn长，主要被富含网状内皮细胞的组织吸收，如肝脏和脾脏。在心脏和肾脏脂质体中，Dxn的浓度低于游离Dxn。注射后，脂质体Dxn的组织分布发生显著变化。在组织中没有观察到高浓度的第一个峰。肝脏和脾脏中的Dxn含量降低，心脏中的Dxn浓度更低。脂质体包裹药物的给药途径可能改变其吸收动力学和组织分布，这可能导致不同的药理作用。
Absorption and tissue distribution of free doxorubicin (Dxn) and Dxn entrapped into liposomes have been examined after i.v. or i.p. injection into C57/B1/6 mice. Liposomal encapsulation of Dxn altered its plasma kinetics and tissue distribution. After i.v. administration Dxn in liposomes has a half-life longer than that of free Dxn and it is taken up mostly by tissues rich in reticuloendothelial cells, such as liver and spleen. In the heart and kidney liposomal Dxn reaches a lower concentration than free Dxn. After i.p. injection the tissue distribution of liposomal Dxn is drastically changed. The first peak of high concentration in the tissues was not observed. The Dxn content in liver and spleen is decreased and its concentration in heart is even more reduced. The route of administration of liposome-entrapped drugs may change both the kinetics of absorption and their tissue distribution and this could result in a different pharmacological effect.