Oba N, Sugimura H, Umehara Y, Yoshida M, Kimura T, Yamaguchi T
First Department of Surgery, Hamamatsu University School of Medicine, Japan.
Lipids. 1992 Sep;27(9):701-5. doi: 10.1007/BF02536028.
A water-in-oil-in-water (W/O/W) emulsion composed of oleic acid was used as a carrier of carboxyfluorescein (CF) via the enteral route, as a model for future drug transport. The absorption of CF in the small intestine of rats given the emulsion (W/O/W group) was compared with the absorption in a group administered CF alone (CF group), and a group administered a mixed micelle of oleic acid and a surface-active agent in CF solution (MM group). Higher amounts of CF were absorbed in the W/O/W and MM groups than in the CF group. At 120 min, the amount of CF remaining in the intestinal tract was smaller in the MM group than in the W/O/W group. In the early period, CF excretion into bile was higher in the MM group than in the W/O/W group, but from 120 to 360 min, CF excretion in the W/O/W group was higher than in the MM group (non-specific). The blood CF level was significantly higher at 240 and 360 min in the W/O/W group than in the other two groups. The highest concentration in lymph was found in the W/O/W group. The W/O/W emulsion was considered superior to the micelles because it maintained a higher blood level of CF over long periods and transferred it to the lymph. This suggests that the W/O/W emulsion is applicable as a drug carrier via the enteral route.
一种由油酸组成的水包油包水（W/O/W）乳液通过肠内途径用作羧基荧光素（CF）的载体，作为未来药物运输的模型。将给予该乳液的大鼠（W/O/W组）小肠中CF的吸收与单独给予CF的组（CF组）以及在CF溶液中给予油酸和表面活性剂混合胶束的组（MM组）的吸收进行比较。W/O/W组和MM组中吸收的CF量高于CF组。在120分钟时，MM组肠道中剩余的CF量低于W/O/W组。在早期，MM组胆汁中CF的排泄高于W/O/W组，但在120至360分钟期间，W/O/W组中CF的排泄高于MM组（非特异性）。在240和360分钟时，W/O/W组的血液CF水平显著高于其他两组。在W/O/W组中发现淋巴中的浓度最高。W/O/W乳液被认为优于胶束，因为它能长时间维持较高的CF血液水平并将其转移至淋巴。这表明W/O/W乳液可作为肠内途径的药物载体。
