Rowland R N, Woodley J F
Biochim Biophys Acta. 1980 Dec 5;620(3):400-9. doi: 10.1016/0005-2760(80)90131-9.
If liposomes are to be effective as carriers for the oral administration of insulin they must be able to withstand passage through the stomach and small intestine. Multilamellar liposomes, some identical in composition to those used in reported in vivo studies on the uptake of orally administered insulin, were tested in vitro for their stability in the presence of bile salts, pancreatic lipase, and variations in pH. While low or high pH had little effect on most liposomes, 10 mM bile salts caused the release of over 80% of entrapped marker from all liposomes tested except those composed of distearoyl phosphatidylcholine/cholesterol and those composed of dipalmitoyl phosphatidylethanolamine/cholesterol/dicetylphosphate. However, the latter were unstable at low pH. The distearoyl phosphatidylcholine/cholesterol liposomes were also resistant to pancreatic lipase, and therefore may be suitable for use in the oral administration of therapeutic agents.
如果脂质体要作为胰岛素口服给药的有效载体，它们必须能够耐受通过胃和小肠。多层脂质体，其某些成分与已报道的关于口服胰岛素摄取的体内研究中所使用的脂质体相同，在体外针对其在胆汁盐、胰脂肪酶存在以及pH值变化情况下的稳定性进行了测试。虽然低pH值或高pH值对大多数脂质体影响不大，但10 mM胆汁盐导致除了由二硬脂酰磷脂酰胆碱/胆固醇组成的脂质体以及由二棕榈酰磷脂酰乙醇胺/胆固醇/十六烷基磷酸酯组成的脂质体之外，所有测试脂质体中超过80%的包封标记物释放出来。然而，后者在低pH值下不稳定。二硬脂酰磷脂酰胆碱/胆固醇脂质体也对胰脂肪酶具有抗性，因此可能适用于治疗剂的口服给药。
