Trypanocidal activity of arsonoliposomes: Effect of vesicle lipid composition

被引：9
作者：
Zagana, Paraskevi
KlepetsaniS, Pavlos
Loannou, Panayiotis V.
Loiseau, Philippe M.
Antimisiaris, S. G. [1 ]
机构：
[1] Univ Patras, Dept Pharm, Pharmaceut Technol Lab, Rion 26500, Greece
[2] Inst Chem Engn & High Temp Proc FORTH, GR-26500 Patras, Greece
[3] Univ Patras, Dept Chem, Rion 26500, Greece
[4] Univ Paris 11, CNRS, UMR Chimiotherapie Antiparasitaire 8076, F-92290 Chatenay Malabry, France
来源：
BIOMEDICINE & PHARMACOTHERAPY | 2007年 / 61卷 / 08期
关键词：
liposome; arsonolipid; arsenic; in vivo; trypanocidal activity; trypanosoma; toxicity; arsonoliposome;
D O I：
10.1016/j.biopha.2007.05.005
中图分类号：
R-3 [医学研究方法]; R3 [基础医学];
学科分类号：
1001 ;
摘要：
Sonicated arsonoliposomes were prepared using an arsonolipid with palmitic acid acyl chain (C16), mixed with phosphatidylcholine (PC-based) or 1,2-distearoyl-sn-glycero-3-phosphocholine (DSPC-based), and cholesterol (Chol) with a molar ratio C16 /PC or DSPC/ Chol 8:12:10. PEG-lipid (1,2-distearoyl-sn-glycero-3-phosphoethanolamine conjugated to polyethylenoglycol 2000) containing vesicles (pegylated-arsonoliposomes) were also prepared. The in vitro and in vivo trypanocidal activity of the various types of arsonoliposomes was evaluated. Although PC-based arsonoliposomes exhibited in vivo activity on an acute trypanosomiasis animal model, no evidence of activity was demonstrated for DSPC-based or pegylated-arsonoliposomes on a chronic model. Despite the fact that DSPC-based and pegylated-arsonoliposomes have better bioavailability compared to PC-based ones, their in vitro activity is lower than that of PC-based arsonoliposomes, indicating the importance of arsonoliposome lipid composition on their trypanocidal activity and suggesting that further arsonoliposome structure design is required to overcome these disadvantages. (c) 2007 Elsevier Masson SAS. All rights reserved.
引用
收藏
页码：499 / 504
页数：6
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