TISSUE DISTRIBUTION OF LIPOSOMES EXHIBITING LONG HALF-LIVES IN THE CIRCULATION AFTER INTRAVENOUS-INJECTION
TISSUE DISTRIBUTION OF LIPOSOMES EXHIBITING LONG HALF-LIVES IN THE CIRCULATION AFTER INTRAVENOUS-INJECTION
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DOI：
10.1016/0304-4165(85)90174-6
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发表时间：
1985-01-01
期刊：
影响因子：
--
通讯作者：
GREGORIADIS, G
中科院分区：
文献类型：
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作者：
SENIOR, J;CRAWLEY, JCW;GREGORIADIS, G
进一步研究了先前建立的注射动物循环中不带电的小单层脂质体的长半衰期与血浆存在下截留溶质的渗透性降低之间的直接关系。囊泡的大小和表面电荷决定了囊泡清除率的膜渗透性。对于较大的囊泡或表面带负电荷的囊泡，在血浆中几乎不可渗透的脂质体的半衰期要短得多。111In标记的含博来霉素的具有长半衰期的小单层脂质体在注射后以小得多的程度在肝脏中累积（例如，26%）比类似的脂质体（剂量的55%）表现出更短的半衰期。大部分注射的长寿命脂质体（约35%）在动物尸体中回收。尸体扫描显示放射性在骨中定量蓄积，推测为骨髓的吞噬细胞。长寿命脂质体似乎适合于药物递送到骨髓或骨髓成像。
The previously established direct relationship between long half-life of uncharged small unilamellar liposomes in the circulation of injected animals and reduced permeability to entrapped solutes in the presence of blood plasma was investigated further. Vesicle size and surface charge override state of membrane permeability in determining rates of vesicle clearance. Half-lives of liposomes that were practically impermeable in plasma were much shorter for larger vesicles or vesicles with a negative charge on their surface. 111In-labeled bleomycin-containing small unilamellar liposomes with long half-lives accumulated in the liver after injection to a much lesser extent (e.g., 26%) than similar liposomes (55% of the dose) exhibiting a shorter half-life. Much of the injected long-lived liposomes (about 35%) were recovered in the carcass of the animals. Scanning of the carcasses revealed quantitative accumulation of radioactivity in the bones, presumably the phagocytic cells of the bone marrow. Long-lived liposomes appear suitable for drug delivery to, or imaging of the bone marrow.