Cui JingXia, Li ChunLei, Deng YingJie, Wang YongLi, Wang Wei
School of Pharmacy, Hebei Medical University, No. 361, ZhongShan East Road, Shijiazhuang City, Hebei Province 050017, PR China.
Int J Pharm. 2006 Apr 7;312(1-2):131-6. doi: 10.1016/j.ijpharm.2006.01.004. Epub 2006 Feb 3.
The objective of this study was to obtain dehydrated liposomes using a novel procedure that involves freeze-drying (FD) of liposomes with TBA/water cosolvent systems. The effects of TBA on the integrity/stability of vesicles of HSPC (or SPC):Cholesterol (4:1) were investigated. TBA used as a cosolvent was detrimental to SPC liposomes, leading to increased particle size and leakage of trapped calcein. However, this was not the case for HSPC liposomes. The vesicle size and the retention of trapped calcein after lyophilization from cosolvents were similar to those after FD from water alone. Moreover, the addition of TBA can significantly enhance the sublimation of ice resulting in short FD cycles. The resulting lyophilized cake can form a loose powder upon agitation, which flowed well enough to be easily poured from the vial. Thus FD of HSPC liposomes using TBA/water cosolvent systems can provide sterile powder for specialized applications. In addition, in conjunction with a modified injection method, this FD technology might be used to produce dehydrated HSPC liposomes on a large scale.
本研究的目的是采用一种新方法获得脱水脂质体，该方法涉及用叔丁醇/水共溶剂体系对脂质体进行冷冻干燥（FD）。研究了叔丁醇对HSPC（或SPC）：胆固醇（4:1）囊泡完整性/稳定性的影响。用作共溶剂的叔丁醇对SPC脂质体有害，导致粒径增大和包封的钙黄绿素泄漏。然而，HSPC脂质体并非如此。从共溶剂冻干后囊泡大小和包封钙黄绿素的保留率与仅从水冻干后相似。此外，添加叔丁醇可显著增强冰的升华，从而缩短冷冻干燥周期。所得冻干饼搅拌后可形成疏松粉末，流动性良好，足以轻松从小瓶中倒出。因此，使用叔丁醇/水共溶剂体系对HSPC脂质体进行冷冻干燥可为特殊应用提供无菌粉末。此外，结合改进的注射方法，这种冷冻干燥技术可用于大规模生产脱水HSPC脂质体。
