HEPATIC-UPTAKE AND DEGRADATION OF UNILAMELLAR SPHINGOMYELIN-CHOLESTEROL LIPOSOMES - A KINETIC-STUDY
HEPATIC-UPTAKE AND DEGRADATION OF UNILAMELLAR SPHINGOMYELIN-CHOLESTEROL LIPOSOMES - A KINETIC-STUDY
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DOI：
10.1073/pnas.77.7.4030
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发表时间：
1980-01-01
期刊：
影响因子：
--
通讯作者：
BEAUMIER, PL
中科院分区：
文献类型：
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作者：
HWANG, KJ;LUK, KFS;BEAUMIER, PL
研究了鞘磷脂/胆固醇（2：1，M/M）小单层脂质体在BALB/c小鼠肝脏的摄取和降解动力学。用闪烁光谱法测定脂质体的组织分布。组织中完整脂质体的百分比通过γ-半乳糖醛酸技术估计。射线扰动角相关建立了动力学模型对上述数据进行了分析。一个显着的协议之间的实验数据和相应的理论值。鞘磷脂/胆固醇单层脂质体在小鼠静脉给药后的循环中具有异常长的半衰期（t1/2），为16.5 h。脂质体在体外在37 ℃下的肝降解。C遵循一级动力学，t1/2为3.5 ±。0.2（SEM [平均值的SE]）h。脂质体在肝脏中的体内降解速率与体外相似，t1/2为3.6 ±。0.4 H.脂质体包封的药剂铟-111在肝脏中的释放速率不是恒定的，并且在约x时达到最大值。脂质体给药后8 h。在本研究中开发的方法是通用的，可以应用于调查的因素，可以控制释放的药物在任何组织。
The kinetics of hepatic uptake and degradation of sphingomyelin/cholesterol (2:1, M/M) small unilamellar liposomes were investigated in a BALB/c mouse. The tissue distribution of liposomes was determined by scintillation spectrometry. The percentage of intact liposomes in tissues was estimated by the technique of .gamma.-ray perturbed angular correlation. A kinetic model was developed to analyze the above data. A remarkable agreement was noted between the experimental data and the corresponding theoretical values. The sphingomyelin/cholesterol unilamellar liposomes had an unusually long half-life (t1/2) of 16.5 h in the circulation after i.v. administration to mice. The hepatic degradation of the liposomes in vitro at 37.degree. C followed 1st-order kinetics, with a t1/2 of 3.5 .+-. 0.2 (SEM [SE of mean]) h. The rate of the in vivo degradation of liposomes in the liver was similar to that in vitro, with a t1/2 of 3.6 .+-. 0.4 h. The rate of release of the liposome-encapsulated agent, indium-111, in the liver was not constant, and reached a maximum at .apprx. 8 h after the administration of liposomes. The approach developed in the present study is general and can be applied to the investigation of factors that may control the release of pharmacologically active agents in any tissue.