A liposome permeability model for stratum corneum lipid bilayers based on commercial lipids.
A liposome permeability model for stratum corneum lipid bilayers based on commercial lipids.
复制标题
基于商业脂质的角质层脂质双层的脂质体渗透性模型。
DOI：
10.1002/jps.21306
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发表时间：
2008
影响因子：
3.8
通讯作者：
Herron,JamesN
中科院分区：
文献类型：
--
作者：
Suhonen,Marjukka;Li,SKevin;Higuchi,WilliamI;Herron,JamesN
目的是评估角质层脂质体（SCLL）制备的商业脂质作为一个方便的模型系统，用于研究化学渗透促进剂的机制。使用由提取的角质层脂质（ESCLL）制备的脂质体作为对照。通过超声处理或挤出从商业神经酰胺、胆固醇、游离脂肪酸和胆固醇3-硫酸酯（SCLL-I-III; 55/25/15/5重量比）的混合物制备三种不同类型的SCLL。SCLL中的甘露醇绝对渗透性比ESCLL低5- 20倍。1-烷基-2-吡咯烷酮增强剂对超声处理的SCLL（SCLL-I）中甘露醇流出产生与先前报道的ESCLL相同的增强因子。增强子诱导的变化在分级深度进一步监测SCLL-I囊泡使用荧光光谱与n-（9-anthrooxy）脂肪酸荧光探针。脂质包装顺序，从旋转相关时间来自稳态各向异性和寿命数据，被认为是较高的SCLL-I比ESCLLs。发现1-烷基-2-吡咯烷酮在中间深度（C6-C9）将双层的流动性增加到与先前报道的ESCLL大致相同的程度。本研究结果表明，超声SCLL模型可能是有用的，用于研究经皮渗透促进剂的作用机制。
The objective was to evaluate stratum corneum lipid liposomes (SCLLs) prepared from commercial lipids as a convenient model system for studying the mechanisms of chemical permeation enhancers. Liposomes prepared from extracted stratum corneum lipids (ESCLLs) were used as a control. Three different types of SCLLs were prepared by sonication or extrusion from mixtures of commercial ceramides, cholesterol, free fatty acids, and cholesterol 3-sulfate (SCLL-I–III; 55/25/15/5 weight ratio). Absolute mannitol permeabilities were 5- to 20-fold lower in SCLLs than in ESCLLs. 1-alkyl-2-pyrrolidone enhancers produced the same enhancement factor for mannitol efflux in sonicated SCLLs (SCLL-I) as reported previously for the ESCLLs. Enhancer-induced changes at graded depths were further monitored in SCLL-I vesicles using fluorescence spectroscopy withn-(9-anthroyloxy) fatty acid fluorescent probes. Lipid packing order, as determined from rotational correlation times derived from steady-state anisotropy and lifetime data, was found to be higher in SCLL-I than in ESCLLs. 1-alkyl-2-pyrrolidones were found to increase the fluidity of the bilayers to approximately the same extent at intermediate depths (C6–C9) as previously reported for the ESCLLs. The present results demonstrate that the sonicated SCLL model may be useful for studying the mechanisms of action of transdermal permeation enhancers.