Influence of route of administration on the absorption and disposition of α,- γ- and δ-tocotrienols in rats

AbstractA study was conducted to evaluate the bioavailability of α-, γ- and δ-tocotrienols administered via oral, intravenous, intramuscular and intraperitoneal routes in rats. Three separate experiments, each conducted according to a two-way crossover design, were carried out to compare intravenous and oral, intramuscular and oral, and intraperitoneal and oral administration. Oral absorption of all three tocotrienols was found to be incomplete. Of the three tocotrienols, α-tocotrienol had the highest oral bioavailability, at about 27.7 ± 9.2%, compared with γ- and δ-tocotrienols, which had values of 9.1 ± 2.4% and 8.5 ± 3.5%, respectively. Such biodiscrimination was also observed in their total clearance rates (estimated from the intravenous data). α-Tocotrienol showed the lowest clearance rate at about 0.16 L kg−1 h−1, whereas that of δ- and γ-tocotrienols was quite similar, with values of 0.24 and 0.23 L kg−1 h−1, respectively. Interestingly, all three tocotrienols were found to be negligibly absorbed when administered intraperitoneally and intramuscularly. Thus, these two routes of administration should be avoided when evaluating the biological activities of the tocotrienols in whole animal experiments.