Physical Characteristics of Sterically Stabilized Liposomes after Lyophilization and Rehydration

입체 구조적으로 안정화된 리포좀의 동결건조에 따른 물리적 특성

Sterically stabilized liposomes (SSL) have been introduced for longer circulation in blood than conventional liposomes (CL). However, there are a couple of problems in SSL preparation due to the instability of phospholipid and the degradation of drug in aqueous conditions. To solve these problems, it is necessary to go through lyophilization process. Therefore, in this study, effects of lyophilization on SSL were evaluated for physical characteristics changes upon rehydration of lyophilized SSL such as the particle size, efficiency of drug entrapment, turbidity and drug release. SSL containing streptozocin, a water-soluble anticancer drug as a model compound, were prepared with DSPC and DSPE-PEG 2000. The size was controlled to 100 nm by extrusion with polycarbonate membrane, and sucrose was used as a cryoprotectant for lyophilization at the 1:3 (lipid:sucrose) ratio. Upon rehydration of lyophilized SSL, the average size was in the range of $50{\sim}200\;nm$ which is adequate for longer circulation in blood, and the encapsulation efficiency was kept as its initial state. Rehydrated SSL were not adsorbed to rat plasma protein and revealed a similar drug release profile to that of fresh SSL before lyophilization. Therefore, lyophilization could be introduced efficiently to overcome aqueous instability problems of SSL.