Guan Peipei, Lu Yi, Qi Jianping, Niu Mengmeng, Lian Ruyue, Wu Wei
School of Pharmacy, Fudan University, Shanghai 201203, PR China; College of Life and Health Sciences, Northeastern University, Shenyang 100819, PR China.
School of Pharmacy, Fudan University, Shanghai 201203, PR China.
Int J Pharm. 2015 Jan 30;478(2):655-64. doi: 10.1016/j.ijpharm.2014.12.016. Epub 2014 Dec 12.
The main purpose of this study was to investigate the effect of gelatin as interior support on the physical stability of freeze-dried liposomes. Anticancer agent paclitaxel (PTX) was selected as a model drug. Freeze-dried liposomes containing interior gelatin support (GLs) were prepared by thin-film dispersion/freeze-drying method. Several properties of the GLs, including entrapment efficiency, particle size and gelation temperature, were extensively characterized. Encapsulation efficiency of conventional liposomes (CLs) and liposomes containing lyoprotectants as interior support dropped to lower than 20% after reconstitution, while GLs still maintained an entrapment efficiency of over 84%. Scanning electron microscopy revealed well preserved liposomal structure of GLs after reconstitution. Meanwhile, the particle size and entrapment efficiency of GLs were also well preserved after reconstitution. In contrary, deformation of CLs and recrystallization of PTX were observed, as well as significant changes in particle size and entrapment efficiency. Taken together, interior gelatin support obviously enhanced the physical stability of liposomes against the lyophilization stress.
本研究的主要目的是研究明胶作为内部支撑对冻干脂质体物理稳定性的影响。选择抗癌药物紫杉醇（PTX）作为模型药物。采用薄膜分散/冷冻干燥法制备了含有内部明胶支撑的冻干脂质体（GLs）。对GLs的多种性质进行了广泛表征，包括包封率、粒径和凝胶化温度。常规脂质体（CLs）和含有冻干保护剂作为内部支撑的脂质体在重构后包封率降至20%以下，而GLs仍保持超过84%的包封率。扫描电子显微镜显示重构后GLs的脂质体结构保存良好。同时，GLs重构后的粒径和包封率也保存良好。相反，观察到CLs的变形和PTX的重结晶，以及粒径和包封率的显著变化。综上所述，内部明胶支撑明显增强了脂质体对冻干应力的物理稳定性。
