Preparation and Evaluation of Oxaliplatin Long-circulating Liposomes

OBJECTIVE To prepare oxaliplatin long-circulating liposomes(LCL) and perform evaluations in vitro and in vivo. METHODS Oxaliplatin-loaded LCL were prepared by reverse phase evaporation method. Physicochemical properties of LCL were investigated, including particle size and encapsulation efficiency(EE). Pharmacokinetic study was conducted on rat model. RESULTS The average particle size of oxaliplatin LCL was (195.1±1.8) nm and the potential was (-29.53±0.57) mV. In addition, the encapsulation efficiency was 18% and the drug loading was 2.4%. Pharmacokinetic studies showed that the plasma clearance rate of oxaliplatin is 71-fold LCL, so LCL could significantly reduce the plasma clearance rate of oxaliplatin and prolong drug the residence time in vivo. The AUC of LCL was 70-fold of that for oxaliplatin solution which significantly improved the bioavailability. CONCLUSION This study select reverse phase evaporation method to prepare and obtain the optimal oxaliplatin LCL with suitable entrapment efficiency, low toxicity and high efficacy.