Pharmacokinetics research on paclitaxel nano-liposomes in rats
Zhang Yang-de
Abstract
Zhang Yang-de
Abstract
【Objectives】To study the pharmacokinetics parameters of paclitaxel nano-liposome in animals,to provide a basis for clinical medicine.【Methods】Establish HPLC method to determine the paclitaxel concentrations in plasma and measure the pharmacokinetic parameters in animals.【Results】The experiment with high-performance liquid method has higher specificity,with a satisfactory range of linearity in the plasma concentration(0.51~25.60) μg/mL and good correlation coefficient(r=0.9996),recovery(RSD9%).Paclitaxel and paclitaxel nano-liposomes were in line with three compartment model in rats.t 1/2α is(1.301±0.213) h and(0.516±0.228) h;t 1/2β is(34.361±5.981) h and(11.223±1.191) h,AUC 0→∞ is(735.201±168.260) mg/(h·L) and(269.298±35.435) mg/(h·L),respectively.【Conclusion】Paclitaxel and paclitaxel nano-liposomes were in line with two-compartment model,but paclitaxel nano-liposomes increased the area under the concentration-time curve and prolonged the effective time to enhance anti-tumor effect and reduce cardiac toxicity.
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【Objectives】To study the pharmacokinetics parameters of paclitaxel nano-liposome in animals,to provide a basis for clinical medicine.【Methods】Establish HPLC method to determine the paclitaxel concentrations in plasma and measure the pharmacokinetic parameters in animals.【Results】The experiment with high-performance liquid method has higher specificity,with a satisfactory range of linearity in the plasma concentration(0.51~25.60) μg/mL and good correlation coefficient(r=0.9996),recovery(RSD9%).Paclitaxel and paclitaxel nano-liposomes were in line with three compartment model in rats.t 1/2α is(1.301±0.213) h and(0.516±0.228) h;t 1/2β is(34.361±5.981) h and(11.223±1.191) h,AUC 0→∞ is(735.201±168.260) mg/(h·L) and(269.298±35.435) mg/(h·L),respectively.【Conclusion】Paclitaxel and paclitaxel nano-liposomes were in line with two-compartment model,but paclitaxel nano-liposomes increased the area under the concentration-time curve and prolonged the effective time to enhance anti-tumor effect and reduce cardiac toxicity.
Key concepts: Paclitaxel, Pharmacokinetics, Liposome, Pharmacology, Chemistry, High-performance liquid chromatography, Toxicity, Plasma concentration