The enhancing effect of nasal absorption of FITC-dextran 4,400 by beta-sitosterol beta-D-glucoside in rabbits.
The effect and mechanism of action of beta-sitosterol beta-D-glucoside (Sit-G) on the in vitro and in vivo nasal absorption of FITC-dextran (molecular weight, 4400; FD-4) in rabbits were studied in comparison with beta-sitosterol (Sit). The FD-4 permeation in the powder dosage form was increased by Sit-G and Sit and related to the uptake of Sit-G and Sit with no changes in the amount of cholesterol in the excised nasal mucosa. The application of Sit and Sit-G increased FD-4 permeation with and without a decrease in transepithelial resistance (TEER), respectively. These results suggested that the mechanism of the enhancement by Sit-G was different from those of Sit and sodium caprate; Sit-G may exert its effects mainly via the transcellular pathway due to perturbation of the mucosal membrane.
Nakamura
K
K
Department of Pharmaceutics, Hoshi University, 2-4-41 Ebara, Shinagawa, 142-8501, Tokyo, Japan.
Maitani
Y
Y
Takayama
K
K
D000042:Absorption / Q000187:drug effects; D000277:Adjuvants, Pharmaceutic / Q000493:pharmacokinetics / Q000494:pharmacology*; D000281:Administration, Intranasal; D000818:Animals; D003911:Dextrans / Q000008:administration & dosage / Q000493:pharmacokinetics*; D004304:Dosage Forms; D004353:Drug Evaluation, Preclinical / Q000379:methods; D004357:Drug Synergism; D016650:Fluorescein-5-isothiocyanate / Q000008:administration & dosage / Q000031:analogs & derivatives / Q000493:pharmacokinetics*; D008297:Male; D009297:Nasal Mucosa / Q000187:drug effects / Q000378:metabolism*; D011817:Rabbits; D012855:Sitosterols / Q000008:administration & dosage / Q000493:pharmacokinetics / Q000494:pharmacology*
D000277:Adjuvants, Pharmaceutic; D003911:Dextrans; D004304:Dosage Forms; D012855:Sitosterols; C015219:fluorescein isothiocyanate dextran; D016650:Fluorescein-5-isothiocyanate; C011015:lyoniside