| Objective:To reduce the toxicity of oxaliplatin and improve its biology ultilization,we compared four preparation methods of the long cycle oxaliplatin nanoliposomes, and optimized the design of their preparation technology in this article. This study may provide a solid foundation for the fellowing research of this kind of drug carry systems, and also for the ability to achieve their industrializations and clinical trial applications.Methods:In this experiments we compared four methods of liposomes preparation that were vacuum evaporation, thin film dispersion, ether injection and ethanol injection. The samples prepared by the four methods were observed by transmission electron microscopy. Furthermore, we analyzed and compared their particle size Zeta potential, drug encapsulation efficiency, rates of recovery and in vitro release. Finally, we detect their inhibition rate by cell MTT assay.Results:Comparison of biological characteristics of the samples revealed ethanol injection was a better method, the best prescription is oxaliplatin:soy lecithin:cholesterol:PEG 2000 by the ratio of 1:2:1:1,0.0lg oxaliplatin as a standard concentration control and mixing about 40 min. The long cycle nano liposome drug samples obtained by this method has a particle size 39.73 nm, Zeta potential -45.3mV, drug encapsulation efficiency 42.05%, recovery 100%,72h in vitro release rate of 36.6% for the Optimal. Cell MTT results showed that the inhibition rate of the sample groups with a drug concentration more than 100μg/ml reached above 90% after 72 hours,150μg/ml up to 97.2%.Conclusion:We prepared nano oxaliplatin long circulating liposomes successfully by the four preparation methods. The result revealed that the ethanol injection method were better than the other three drug sample preparation methods through sample biological characteristics comprehensive comparison. Drug samples prepared by this method steadily released within 72 hours, showing better control ability, stability and long-term sustainability than the positive groups. |