Mills P C, Magnusson B M, Cross S E
School of Veterinary Science, University of Queensland Brisbane, Queensland 4072.
Aust Vet J. 2003 Dec;81(12):752-5. doi: 10.1111/j.1751-0813.2003.tb14608.x.
To investigate the effect of lipophilicity on the percutaneous penetration of a homologous series of alcohols through canine skin.
Skin harvested from Greyhound thorax was placed in Franz-type diffusion cells and the in vitro passage of radiolabelled (14C) alcohols (ethanol, butanol, hexanol and octanol (Log P 0.19-3.0)) through separate skin sections was measured in replicates of five. Permeability coefficient (kP, cm/h), maximum flux (Jmax, mol/cm2/h) and residue remaining within the skin were determined.
The kP increased with increasing lipophilicity (6.2 x 10(-4) +/- 1.6 x 10(-4) cm/h for ethanol to 1.8 x 10(-2) +/- 3.6 x 10(-3) cm/h for octanol). Alcohol residues remaining within each skin sample followed a similar pattern. An exponential decrease in Jmax with increasing lipophilicity was observed.
Changes in canine skin permeability occur with increasing alcohol lipophilicity. This finding has practical consequences for the design of topical formulations and optimisation of drug delivery through animal skin.
研究亲脂性对一系列同系醇类经犬皮肤渗透的影响。
从灵缇犬胸部采集的皮肤置于弗兰兹型扩散池中，对放射性标记的（14C）醇类（乙醇、丁醇、己醇和辛醇（Log P 0.19 - 3.0））通过不同皮肤切片的体外透过情况进行测量，每组重复五次。测定渗透系数（kP，cm/h）、最大通量（Jmax，mol/cm2/h）以及皮肤内残留量。
kP随亲脂性增加而升高（乙醇为6.2×10(-4)±1.6×10(-4) cm/h，辛醇为1.8×10(-2)±3.6×10(-3) cm/h）。每个皮肤样本中的醇类残留量呈现相似模式。观察到Jmax随亲脂性增加呈指数下降。
犬皮肤渗透性随醇类亲脂性增加而变化。这一发现对局部用制剂的设计以及优化药物经动物皮肤递送具有实际意义。
