Studies On The Oxaliplatin Liposomes

ObjectiveTo prepare Oxaliplatin liposomes with high entrapment efficiency, appropriate drug loading and particle size that meet the requirements of liposomes. And then prepare the freeze-dried product of Oxaliplatin liposomes made above to enhance its stability. Finally, some experiments about the pharmacodynamic of Oxaliplatin liposomes will be done to examine the sustained release of the preparation.MethodsFirst, examined the nature of the drug Oxaliplatin before prescriptions, as well as established the method of determination of content and entrapment efficiency of Oxaliplatin liposomes by ultrafiltration-HPLC method, and thus laid the foundation for the subsequent process. Basing on the studies above, taking entrapment efficiency as the main indicators, investigated the formulation and process of preparation of oxaliplatin liposome, and then optimized the process. Furthermore, used the freeze-drying technology to improve the stability of Oxaliplatin liposomes. Finally, used the HPLC-MS method to determine the pharmacokinetic properties of the preparation. Results The results of method validation indicated that the HPLC method was fit for the determination of content and entrapment efficiency of Oxaliplatin liposomes. After the investigation and optimization of the formulation and process of preparation of Oxaliplatin liposome, and after the freeze-drying process, the encapsulation efficiency was83.20%, and the content was1.19mg·mL-1, and the average particle size was77.3nm, which achieved the desired objectives. The results of pharmacokinetic studies showed that the C0and AUC of Oxaliplatin liposome group were much bigger than that of normal Oxaliplatin injection group, and the CL of Oxaliplatin liposome group was much smaller than that of normal Oxaliplatin injection group.ConclusionAfter the studies of Oxaliplatin liposomes, we found a good way to prepare Oxaliplatin liposomes with high entrapment efficiency, appropriate drug loading and particle size that met the requirements of liposomes. After the studies of pharmacokinetic, we can find that Oxaliplatin liposomes preparation can prolong the residence time of Oxaliplatin in the body regarding to the normal Oxaliplatin injection preparation.