亲脂性
渗透
跨细胞
化学
地塞米松
上皮
磁导率
水解
色谱法
前药
角膜上皮
细胞通透性
体内
并行传输
药代动力学
药理学
生物物理学
生物化学
生物
内分泌学
病理
医学
膜
生物技术
作者
C. Civiale,Filippo Bucaria,Silvana Piazza,Ornella Peri,Fausto Miano,Vincenzo Enea
出处
期刊:Journal of Ocular Pharmacology and Therapeutics
[Mary Ann Liebert]
日期:2004-02-01
卷期号:20 (1): 75-84
被引量:20
标识
DOI:10.1089/108076804772745482
摘要
Dexamethasone transport across ocular epithelium was evaluated by means of permeability studies on a series of ester prodrugs with the aim of identifying the most promising candidates for the treatment of the ocular surface. Organotypic conjunctival bovine epithelial cell cultures were assumed representative of an average ocular epithelium and used to describe the mechanism of permeation. Permeability coefficients were also determined in excised rabbit corneas set up and in vivo pharmacokinetic experiments. All dexamethasone esters permeated through the transcellular route and their permeability coefficient rose with the increase of the molecules lipophilicity until a maximum was reached in correspondence of dexamethasone butyrate (Log P = 3.95). It was found that esters hydrolysis occurring in various extent along the transport process, affected the overall permeability rate. There was evidence that the permeation process can be confined at the ocular epithelium layer if the ester is highly hydrophobic and not susceptible of fast hydrolysis.
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