Evaluation of an oleic acid water-in-oil-in-water-type multiple emulsion as potential drug carrier via the enteral route.
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.
Oba
N
N
First Department of Surgery, Hamamatsu University School of Medicine, Japan.
Sugimura
H
H
Umehara
Y
Y
Yoshida
M
M
Kimura
T
T
Yamaguchi
T
T
D000284:Administration, Oral; D000818:Animals; D001646:Bile / Q000378:metabolism; D004337:Drug Carriers; D004655:Emulsions / Q000378:metabolism; D004750:Enteral Nutrition; D005069:Evaluation Studies as Topic; D005452:Fluoresceins / Q000493:pharmacokinetics*; D007408:Intestinal Absorption; D008196:Lymph / Q000378:metabolism; D008297:Male; D019301:Oleic Acid; D009829:Oleic Acids / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D017208:Rats, Wistar; D014867:Water
D004337:Drug Carriers; D004655:Emulsions; D005452:Fluoresceins; D009829:Oleic Acids; D014867:Water; D019301:Oleic Acid; C024098:6-carboxyfluorescein