Pharmacokinetics and tissue distribution of paclitaxel submicro-emulsion injection in rats

Objective To study the pharmacokinetics and tissue distribution of paclitaxel submicro-emulsion injection (PSME) in rats. Methods High pressure homogenization method was used to prepare PSME. The commercial paclitaxel injection was used as a reference to evaluate the pharmacokinetics and tissue distribution of PSME. The 3p87 computer program was used to analyze the pharmacokinetic model, and the pharmacokinetic parameters were calculated using the statistical moment method. The relative tissue exposure values (re) were used to evaluate the tissue targeting of PSME. Results The mean particle size and Zeta potential of PSME were (135.5±47.7) nm and -39.10 mV , respectively. The pharmacokinetic data obtained with both preparations fitted a two-compartment model, and the main pharmacokinetic parameters exhibit no statistically significant difference (n=6, P 0.05). Compared to the commercial paclitaxel group, the re values of liver, spleen, lung, kidney in PSME group were 1.25, 1.28, 1.24 and 1.33 , respectively. Conclusions The PSME had a similar pharmacokinetic characteristics as the commercial paclitaxel injection. There is only a little accumulation of PSME in liver, spleen, lung and kidney without remarkable influence on the tissue distribution of paclitaxel in rats.