Preparation And Pharmacokinetics Of Arsenic Trioxide Liposome

[Object] AS2O3- Liposome were prepared and the particle size, entrapment rate and morphology are determined. Also the in vitro release were studied.[Method]The calcium acetate gradient method was employed to prepare As2O3- Liposome. The morphology of liposome was screened by TEM. The particle size was measured by particle size and Zeta Potential Analyzer. Free AS2O3 was separated from nanoparticle with retrodialysis and choose atomic fluorescence method to measure the drug content and in vitro release of AS2O3. The pharmacokinetic parameters were calculated by DAS2.0 computer program.[Results]The liposome solution looks like transparent and weak blue in color, with a little opalescence. TEM gave the morphology of liposome is spherical. The mean diameter of nanoparticle is about 173 nm or so. The mean entrapment rate of As2O3-Liposome came to more than 80%. In vitro release test illuminated the drug release of liposome is slow. The cumulative percentage of drug is nearly to 45% after i.v. administration 24h and to 48% after 48 h. The pharmacokinetic parameters of As2O3-Liposome suggested that the metabolism speed of AS2O3-Liposome is slower than AS2O3 normal solution.[Conclusion] calcium acetate gradient method is a simple and feasible method. The As2O3-Liposome is in small and homogeneous size, good morphology and high entrapment rate. Drug released slowly and no burst release. As2O3-Liposome could prolong the elimination half-life time in rats markedly.