Preparation Of Vinorelbine Liposomes And Drug Concentration Detection Research For Nasopharyngeal Carcinoma HNE-1

Objective:Selecting vinorelbine as model drug,preparaing vinorelbine liposome,studying the technology of preparation and evaluating the drug concentration of the liposome in nasopharyngeal carcinoma HNE-1.Method:In this thesis,VLB liposome was prepared by pH gradient method.The stability of VLB liposome was valuated with the entrapment efficiency and preoxidation value in 4,25℃for 1 month.The concentration of VLB in HNE-1 was detected by HPLC.Result:Through orthogonal experimental design,one optimum recipes of VLB liposome was founded that it showed VLB /EPC 1:10,EPC/Ch 3:1,pH 6.8,incubation tempreture 60℃.Under the optimal formulation,VLB was encapsulated 84.42%.The observation of The liposome through transmission electron microscopy showed distribution of size uniformity,the average diameter was about 181.8nm.The results of liposome drug concentration for HNE-1 experiment at 3 time point showed that VLB-L was 1.81μg/mL at 1h,4.25μg/mL at 3h,4.62μg/mL at 6h,respectively and VLB was 0.43μg/mL at 1h,2.16μg/mL at 3h,2.86μg/mL at 6h,respectively.Conclusion:A method was developed for the determination of VLB concentration in liposome and encapsulation efficiency by HPLC,it was proved that this method was accurate,high sensitivity,specific and good enough to be used in concentration and encapsulation efficiency study of VLB.The stability result showed that the VLB liposome stored in 4℃would keep stable.The drug releasing experiment in vitro showed the liposome had more delayed release effect than free drug.VLB in liposome went into HEN-1 more easily than free drug and the time of entry was more quick and early,so it could get peak concentration quickly.VLB-L has better antitumor,and its toxicity is lower that free drug.