Cytotoxicity of potential ocular permeation enhancers evaluated on rabbit and human corneal epithelial cell lines

被引:82
作者
Burgalassi, S [1 ]
Chetoni, P [1 ]
Monti, D [1 ]
Saettone, MF [1 ]
机构
[1] Univ Pisa, Dept Bioorgan Chem & Biopharmaceut, I-56126 Pisa, Italy
关键词
ocular permeation enhancers; toxicity; human epithelial cells; rabbit epithelial cells; cell cultures;
D O I
10.1016/S0378-4274(01)00261-2
中图分类号
R99 [毒物学(毒理学)];
学科分类号
100405 ;
摘要
A series of prospective ocular permeation enhancers. benzalkonium chloride (BAC), cetylpyridinium chloride (CPC), ethylenediaminetrtraacetic acid (EDTA), polyoxyethylene (20) stearyl ether (PSE) and polyelhoxylated castor oil (PCO) were tested for cytotoxicity on cultures of rabbit (RCE) and human (HCE) corneal epithelial cells. The cells were treated for 5, 15 and 60 min with different concentrations of the test substances, in serum-free medium and in medium containing 15% foetal bovine serum (FBS). The cytotoxicity was evaluated by WST-1 test. The EC50 values For HCE, after 15 min exposure and in the presence of FBS, indicate the following order of cytotoxicity: PSE greater than or equal to BAC > CPC > EDTA > PCO. After 1 h exposure the order of decreasing cytotoxicity was PSE greater than or equal to BAC > CPC > PCO > EDTA. In all cases the presence of FBS appeared to exert a protective effect against the cytotoxic effect. (C) 2001 Elsevier Science Ireland Ltd. All rights reserved.
引用
收藏
页码:1 / 8
页数:8
相关论文
共 31 条
[1]  
ARAKISASAKI K, 1995, INVEST OPHTH VIS SCI, V36, P614
[2]   FORMULATION INFLUENCE ON CONJUNCTIVAL PENETRATION OF 4-BETA BLOCKERS IN THE PIGMENTED RABBIT - A COMPARISON WITH CORNEAL PENETRATION [J].
ASHTON, P ;
PODDER, SK ;
LEE, VHL .
PHARMACEUTICAL RESEARCH, 1991, 8 (09) :1166-1174
[3]  
Balls M, 1999, ATLA-ALTERN LAB ANIM, V27, P53
[4]  
CHIOU GCY, 1991, ANNU REV PHARMACOL, V31, P457
[5]   IMPROVEMENT OF SYSTEMIC ABSORPTION OF INSULIN THROUGH EYES WITH ABSORPTION ENHANCERS [J].
CHIOU, GCY ;
CHUANG, CY .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1989, 78 (10) :815-818
[6]  
Draize JH, 1944, J PHARMACOL EXP THER, V82, P377
[7]   FACTORS INFLUENCING CADMIUM UPTAKE AND CYTO-TOXICITY IN CULTURED-CELLS [J].
FISCHER, AB .
XENOBIOTICA, 1985, 15 (8-9) :751-757
[8]   INFLUENCE OF CETYLPYRIDINIUM CHLORIDE ON CORNEAL PERMEABILITY TO PENICILLIN [J].
GODBEY, REW ;
GREEN, K ;
HULL, DS .
JOURNAL OF PHARMACEUTICAL SCIENCES, 1979, 68 (09) :1176-1178
[9]   DOSE EFFECT RESPONSE OF THE RABBIT EYE TO CETYLPYRIDINIUM CHLORIDE [J].
GREEN, K ;
BOWMAN, KA ;
ELIJAH, RD ;
MERMELSTEIN, R ;
KILPPER, RW .
JOURNAL OF TOXICOLOGY-CUTANEOUS AND OCULAR TOXICOLOGY, 1985, 4 (01) :13-26
[10]   INFLUENCE OF VARIOUS AGENTS ON CORNEAL PERMEABILITY [J].
GREEN, K ;
TONJUM, A .
AMERICAN JOURNAL OF OPHTHALMOLOGY, 1971, 72 (05) :897-&