Casals Elisenda, Galán Ana María, Escolar Ginés, Gallardo Montserrat, Estelrich Joan
Departament de Físicoquímica, Facultat de Farmàcia, Universitat de Barcelona, Avda. Joan XXIII s/n, 08013, Barcelona, Catalonia, Spain.
Chem Phys Lipids. 2003 Oct;125(2):139-46. doi: 10.1016/s0009-3084(03)00086-0.
The physical stability of six liposome systems designed as platelet substitutes was determined on storage at 4 degrees C over a 3-month period under quiescent conditions. Liposomes used were large unilamellar vesicles. Correlation of the n-average mean diameter, polydispersity, zeta-potential and the presence of aminophospholipid on liposome surface (in those preparations which contain phosphatidylethanolamine (PE) and phosphatidylserine (PS)) led to the conclusion that liposomes that mimicked the composition of platelets were the most stable. When a net charge was present in the vesicles (liposomes with PS), the likelihood of aggregation was extremely low. In the period studied, a proportion of 25% of charged lipid (PS) conferred sufficient electrostatic stabilization to prevent vesicle fusion. An increase in this charge did not modify the stability characteristics. PE-containing liposomes behaved in a particular way: when PE content was 50%, the stability of the preparation was limited to 1 month; whereas if the content was 25%, the zeta-potential rose with time, as did the presence of PE in the liposome surface.
将设计用作血小板替代物的六种脂质体系统在4℃静态条件下储存3个月，测定其物理稳定性。所用脂质体为大单层囊泡。通过对数量平均直径、多分散性、ζ电位以及脂质体表面氨基磷脂的存在情况（在含有磷脂酰乙醇胺（PE）和磷脂酰丝氨酸（PS）的制剂中）进行相关性分析，得出结论：模拟血小板组成的脂质体最稳定。当囊泡中存在净电荷时（含PS的脂质体），聚集的可能性极低。在所研究的时间段内，25%的带电脂质（PS）比例赋予了足够的静电稳定性以防止囊泡融合。这种电荷的增加并未改变稳定性特征。含PE的脂质体表现出特殊的情况：当PE含量为50%时，制剂的稳定性仅限于1个月；而如果含量为25%，ζ电位随时间升高，脂质体表面的PE存在情况也是如此。
