Abstract:
Intestinal lymphatic transport has been proved to have contribution to oral absorption of some highly
lipophilic drugs. T-OA, 3βhydroxyolea-12-en-28-oic acid-3,5,6-trimethylpyrazin-2-methylester, has been reported to
have anti-cancer activity. However, T-OA's poor solubility and difficulty to be absorbed cause low oral bioavailability.
This work aims to investigate the influence of T-OA liposomes on intestinal lymphatic transport with rat model. T-OA
liposomes were prepared by freeze-drying method, and particle size, zeta potential and entrapment efficiency of T-OA
liposomes were detected to evaluate liposomes. Conscious restrained rat model was selected to evaluate intestinal
lymphatic transport. The particle size, zeta potential and entrapment efficiency of T-OA liposomes were (184.05 ±
10.93) nm, (-21±0.85) mV and (93.24±2.25) %, respectively. The cumulative amounts in mesenteric lymph of T-OA
liposomes and T-OA suspension within 12 h were (921.39±19.73) µg and (332.31±21.39) µg (n=6), respectively.
Experimental results showed that T-OA liposomes could significantly promote T-OA’s intestinal lymphatic transport and
enhance its oral bioavailability