Stomach- and Site-Selective Delivery of 5-Fluorouracil Following Its Application on the Gastric Serosal Surface in Rats

The present study was undertaken to elucidate the stomach- and site-selective delivery of 5-fluorouracil (5-FU) following its application on the gastric serosal surface in rats. An experimental system utilizing a cylindrical diffusion cell attached to the gastric serosal surface was established. To...

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Bibliographic Details
Published in:Biological & Pharmaceutical Bulletin 2005, Vol.28(6), pp.1049-1053
Main Authors: Nakamura, Junzo, Kobayashi, Kazuko, Fumoto, Shintaro, Nishi, Junya, Mukai, Takahiro, Nakashima, Mikiro, Sasaki, Hitoshi, Nishida, Koyo
Format: Article
Language:English
Subjects:
5-fluorouracil
Animals
chemotherapy
drug delivery system
Drug Delivery Systems - methods
Fluorouracil - administration & dosage
Fluorouracil - metabolism
gastric cancer
Gastric Mucosa - drug effects
Gastric Mucosa - metabolism
Male
rat
Rats
Rats, Wistar
Stomach - drug effects
stomach targeting
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Summary:The present study was undertaken to elucidate the stomach- and site-selective delivery of 5-fluorouracil (5-FU) following its application on the gastric serosal surface in rats. An experimental system utilizing a cylindrical diffusion cell attached to the gastric serosal surface was established. To evaluate the gastric distribution of 5-FU, the stomach was separated into the site under the diffusion cell (site 1) and the site not under the diffusion cell (site 2). Furthermore, the mucosal side at site 1 was separated from the serosal side. After intravenous and oral administration of 5-FU, the 5-FU concentrations at sites 1 and 2 until 240 min were similar. After gastric serosal surface application of 5-FU, however, the concentration of 5-FU at site 1 until 240 min was approximately 10-fold higher than that at site 2, and was sustained. Furthermore, the 5-FU concentration on the mucosal side at site 1 and the serosal side at site 1 were comparable after gastric serosal surface application. The blood concentration of 5-FU was low (
ISSN:0918-6158
1347-5215
DOI:10.1248/bpb.28.1049