Nicholas A R, Jones M N
Biochim Biophys Acta. 1986 Sep 11;860(3):600-7. doi: 10.1016/0005-2736(86)90559-6.
Two types of sonicated vesicle have been prepared from dipalmitoylphosphatidylcholine (DPPC) by incorporation of phosphatidylinositol (PI) to give negatively charged vesicles and stearylamine to give positively charged vesicles. The absorption of the vesicles by rat liver has been investigated by perfusion techniques. A steady state of vesicle absorption is rapidly established in approx. 2 min and the initial rates of absorption decrease with PI content of the vesicles and increase with stearylamine content. In the steady state, the uptake of vesicles by the liver is similarly dependent on vesicle charge, being inhibited by PI and enhanced by incorporation of stearylamine in the vesicles. Fractionation of the liver into subcellular fractions following perfusion showed that most of the vesicular lipid could be found associated with a nuclear (plus plasma membrane) fraction. The suppression of vesicle absorption by PI may be of value as a means of bypassing the liver in relation to the use of vesicles as a delivery system.
通过掺入磷脂酰肌醇(PI)制备了两种由二棕榈酰磷脂酰胆碱(DPPC)制成的超声处理囊泡,以得到带负电荷的囊泡,通过掺入硬脂胺制备带正电荷的囊泡。已通过灌注技术研究了大鼠肝脏对这些囊泡的吸收情况。在大约2分钟内迅速建立了囊泡吸收的稳态,吸收的初始速率随囊泡中PI含量的增加而降低,随硬脂胺含量的增加而升高。在稳态下,肝脏对囊泡的摄取同样取决于囊泡电荷,PI会抑制摄取,而在囊泡中掺入硬脂胺则会增强摄取。灌注后将肝脏分离成亚细胞组分表明,大部分囊泡脂质可与核(加质膜)组分相关联。就将囊泡用作递送系统而言,PI对囊泡吸收的抑制作用可能作为一种绕过肝脏的手段具有价值。