Ariën A, Goigoux C, Baquey C, Dupuy B
INSERM U.306, Laboratoire Biophysique, Université de Bordeaux II, France.
Life Sci. 1993;53(16):1279-90. doi: 10.1016/0024-3205(93)90573-l.
Factors affecting liposome transport to the blood compartment after oral administration to rats were evaluated. A high entrapment of calcitonin (CT) was obtained when the vesicles were prepared by sonication and were composed of egg phosphatidylcholine, cholesterol and stearylamine. In vitro tests showed that the liposomes were stable in light acidic or basic buffers, but that they were partly lysed in pH 2.5, 10 mM bile salts and pancreatin. Oral administration of liposomes entrapping calcitonin in fasting rats showed that the vesicles facilitate transport of the hormone to the general circulation and that they increase the lifetime of 125I-CT in blood. Oral administration of liposomes entrapping radioactive indium in fasting rats did not induce radioactivity in blood. This could be explained by disruption of most of the vesicles in the enterocytes.
评估了口服给予大鼠后影响脂质体转运至血循环的因素。当通过超声处理制备由蛋黄卵磷脂、胆固醇和硬脂胺组成的脂质体时，可实现高含量的降钙素（CT）包封。体外试验表明，脂质体在轻度酸性或碱性缓冲液中稳定，但在pH 2.5、10 mM胆汁盐和胰酶中会部分裂解。对禁食大鼠口服包封降钙素的脂质体表明，脂质体有助于激素转运至体循环，并延长了血液中125I-CT的半衰期。对禁食大鼠口服包封放射性铟的脂质体后，血液中未检测到放射性。这可能是由于肠细胞中大多数脂质体被破坏所致。
