Preparation of curcumin-loaded long-circulating liposomes and its pharmacokinetics in rats / 中国中药杂志

Curcumin has a wide spectrum of pharmaceutical properties such as antitumor, antioxidant, antiamyloid, and anti-inflammatory activity. However, poor aqueous solubility and low bioavailability of curcumin are major challenge in its development as a useful drug. To overcome many of these problems, curcumin-loaded long-circulating liposomes (Cur-LCL) were prepared by the ethanol injection method. Morphology of Cur-LCL was observed by transmission electron microscope, mean particle size and Zeta potential were detected by laser particle size analyzer, entrapment efficiency and drug loading were evaluated by ultracentrifugation. The drug release behavior in vitro and pharmacokinetic behavior in rats of Cur-LCL were investigated with curcumin (Cur) and curcumin liposomes (Cur-Lips) as control. The results showed that the mean diameter of Cur-LCL was 110 nm, the Zeta potential was -5.8 mV. The entrapment efficiency and drug loading of Cur-LCL was 80.25%, 2.06%, respectively. The release behavior in vitro studied by dialysis in PBS buffer showed significant sustained release profile that 48.95% Cur were released from Cur-LCL in 7 h, 88.92% in 24 h. The pharmacokinetic parameters showed that compared with Cur and Cur-Lips, the t(1/2beta) of Cur-LCL was extended to 13 and 1.8-fold, respectively. Besides, the AUC values was significantly increased (P < 0.01), and the clearance was evidently decreased (P < 0.01). These results from in vitro and in vivo indicated that Cur-LCL were able to realize controlled drug release and increase circulation time.

Studies on absorption kinetics characteristics of diterpenoid alkaloids in rats after oral administration of Sini Tang powder / 中国中药杂志

The purpose of this study was to investigate the absorption kinetics of aconitine, mesaconitine and hypaconitine in rats after oral administration of Sini Tang powder. With cannulate portal and jugular veins cannulated (double-cannulate), conscious moving rats were orally administered Sini Tang. Then samples of portal and systemic blood were collected at the designated periods of time and analyzed for aconitine, mesaconitine and hypaconitine by HPLC. Apparent absorption coefficient of aconitine, mesaconitine and hypaconitine was caculated respectively. The results indicated that the apparent absorption coefficient of aconitine, mesaconitine and hypaconitine come from Sini Tang were 0. 336, 0. 090, 0. 176, respectively, which had some differences among them. It was also suggested that double-cannulated rat was useful for estimating the absorption kinetics of aconitine, mesaconitine and hypaconitine after orally administered Sini Tang by determining the AUC values for drugs in portal and systemic blood samples. The three alkaloids could all be detected in blood, but the absorption differences were existed among the three alkaloids.