Regional intestinal absorption of FITC–dextran 4,400 with nanoparticles based on β-sitosterol β-d-glucoside in rats
✍ Scribed by Koji Nakamura; Kozo Takayama; Tsuneji Nagai; Yoshie Maitani
- Publisher
- John Wiley and Sons
- Year
- 2003
- Tongue
- English
- Weight
- 122 KB
- Volume
- 92
- Category
- Article
- ISSN
- 0022-3549
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✦ Synopsis
Nanoparticles (NP) are potential carriers for drug delivery to the targeted intestine. NP based on beta-sitosterol beta-D-glucoside (Sit-G) enhanced the colon-specific absorption of FITC-dextran 4,400 (FD-4), because the concentration-dependent increase of bioavailability appeared in only the colon. In a permeation study, the absorption enhancement in the colon was suppressed in the following conditions: (1) the addition of Sit-G NP to serosa; (2) a permeation study at 4 degrees C; (3) the addition of endocytosis inhibitor, cytochalasin B. NP based on sitosterol, the aglycon of Sit-G, did not increase the FD-4 colonic permeation. The addition of Sit-G NP to the mucosal side induced a decrease of transepithelial resistance (TEER), but this phenomenon was suppressed by an inhibitor of Na(+)-dependent specific glucose transporter, phrolidzin, which did not affect FD-4 permeation. These findings suggested that absorption enhancement by Sit-G NP may not be due to opening of a tight junction, but might be related to endocytosis via glucose residue of Sit-G.