Hashida N, Murakami M, Yoshikawa H, Takada K, Muranishi S
J Pharmacobiodyn. 1984 Mar;7(3):195-203. doi: 10.1248/bpb1978.7.195.
The absorption of carboxyfluorescein (CF) entrapped in liposomes from the small intestine was investigated in vivo using bile fistula rats. Within the intestine CF was not metabolized, but 32% of the entrapped CF was released for 3 h from the liposomes when incubated with luminal incubation solution. The data of CF disappearance from the intestinal lumen and of CF plasma concentration showed that no apparent difference was observed between administration of the liposomal CF and that of free dye. Especially in initial 60 min after administration of liposomal CF, the plasma concentration was obviously lower than that in free CF administration. On the contrary, the coadministration of 40 mM lipid-surfactant mixed micelles induced a remarkable promotive effect on the absorption of free CF already in the early periods of the initial 60 min. When liposomal CF was administered into the intestinal lumen of thoracic duct-cannulated rats, the concentration in lymph was lower than that in plasma. Intramural injection of liposomal CF into intestinal wall, however, showed a much higher concentration in lymph than that in plasma. These findings suggest that liposomal entrapment of CF has rather difficulty to be absorbed through the intestinal mucosa, while lipid-surfactant mixed micelles exert a remarkable promotive effect on the absorption of CF.
利用胆瘘大鼠在体内研究了包裹于脂质体中的羧基荧光素（CF）从小肠的吸收情况。在肠道内CF未发生代谢，但当与肠腔孵育液一起孵育时，32%包裹的CF在3小时内从脂质体中释放出来。CF从肠腔消失的数据以及CF血浆浓度的数据表明，脂质体CF给药与游离染料给药之间未观察到明显差异。特别是在脂质体CF给药后的最初60分钟内，血浆浓度明显低于游离CF给药时的血浆浓度。相反，共同给予40 mM脂质 - 表面活性剂混合胶束在最初60分钟的早期阶段就对游离CF的吸收产生了显著的促进作用。当将脂质体CF注入胸导管插管大鼠的肠腔时，淋巴中的浓度低于血浆中的浓度。然而，将脂质体CF壁内注射到肠壁中时，淋巴中的浓度比血浆中的浓度高得多。这些发现表明，CF的脂质体包裹很难通过肠黏膜吸收，而脂质 - 表面活性剂混合胶束对CF的吸收具有显著的促进作用。
