PREPARATION AND EVALUATION OF STERICALLY STABILIZED LIPOSOMES - COLLOIDAL STABILITY, SERUM STABILITY, MACROPHAGE UPTAKE, AND TOXICITY

被引:59
作者
KRONBERG, B
DAHLMAN, A
CARLFORS, J
KARLSSON, J
ARTURSSON, P
机构
[1] UNIV UPPSALA,DEPT PHARMACEUT,POB 580,S-75123 UPPSALA,SWEDEN
[2] INST SURFACE CHEM,S-11486 STOCKHOLM,SWEDEN
关键词
D O I
10.1002/jps.2600790803
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Sterically stabilized liposomes were produced by incorporating a nonionic surfactant, polysorbate 80 (Tween 80), into the lipid bilayer. The sterically stabilized liposomes exhibited a superior entrapment stability compared with surfactant‐free liposomes (i.e., liposomes prepared with lipids and cholesterol). The sterically stabilized liposomes were stable at high calcium ion concentrations, and liposome‐entrapped carboxyfluorescein was retained within the stabilized liposomes in the presence of serum for at least 5 h. The macrophage uptake of the sterically stabilized liposomes was comparable to that of liposomes containing lipids and cholesterol. The sterically stabilized liposomes were non‐toxic, in concentrations up to 3.0 mM, to macrophages. These results indicate that polysorbate 80 can be used to produce stable liposomes without changing the unique macrophage distribution of this drug delivery system. Copyright © 1990 Wiley‐Liss, Inc., A Wiley Company
引用
收藏
页码:667 / 671
页数:5
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